37776 acridine carboxamide An agent that inhibits Topoisomerase II and intercalates with a DNA hexanucleotide, causing DNA damage and inhibition of DNA replication, RNA and protein synthesis. C2203 37779 recombinant vaccinia-B7.1 vaccine A recombinant vaccinia virus encoding the T-cell co-stimulatory molecule B7-1. Co-administration of recombinant vaccinia-B7.1 and a tumor-associated antigen in a cancer vaccine may enhance tumor-associated antigen-specific T-cell responses. 37780 iodinated contrast dye A contrast agent containing an iodine-based dye used in many diagnostic imaging examinations, including computed tomography, angiography, and myelography. C28500 37783 alemtuzumab A recombinant DNA-derived humanized monoclonal antibody directed against the cell surface glycoprotein CD52. Alemtuzumab is an IgG1 kappa with human variable framework and constant regions, and complementarity-determining regions derived from a rat monoclonal antibody. This agent selectively binds to CD52, thereby triggering a host immune response that results in lysis of CD52 + cells. CD52 is a glycoprotein expressed on the surface of essentially all normal and malignant B and T cells, a majority of monocytes, macrophages and natural killer (NK) cells, a subpopulation of granulocytes, and tissues of the male reproductive system. 37792 L-377,202 A prodrug in which a peptide is covalently conjugated with the anthracycline antineoplastic antibiotic doxorubicin. This complex is hydrolyzed by the enzyme prostate-specific antigen (PSA), resulting in the formation of doxorubicin and leucine-doxorubicin. Selective targeting of these drugs to prostate tumor cells occurs because the hydrolyzing PSA enzyme is localized to the prostate gland. Doxorubicin and leucine-doxorubicin intercalate into DNA and interacts with topoisomerase II, thereby inhibiting DNA replication and repair and RNA and protein synthesis. These agents also produce toxic free-radical intermediates and interact with cell membrane lipids causing lipid peroxidation. C1853 37793 rosiglitazone maleate The maleate salt of rosiglitazone, an orally-active thiazolidinedione with antidiabetic properties and potential antineoplastic activity. Rosiglitazone activates peroxisome proliferator-activated receptor gamma (PPAR-gamma), a ligand-activated transcription factor, thereby inducing cell differentiation and inhibiting cell growth and angiogenesis. This agent also modulates the transcription of insulin-responsive genes, inhibits macrophage and monocyte activation, and stimulates adipocyte differentiation. C2583 37795 ISIS 2503 A synthetic oligodeoxynucleotide. Functioning as an anti-sense agent, it hybridizes to the translation initiation region of the human mRNA for the oncogene H-Ras. ISIS 2503 selectively inhibits the expression of H-Ras, and may inhibit the growth of some Ras-dependent tumor cells. 37796 liposomal daunorubicin citrate A liposome-encapsulated form of the citrate salt of the anthracycline antineoplastic antibiotic daunorubicin. Daunorubicin intercalates into DNA and interacts with topoisomerase II, thereby inhibiting DNA replication and repair and RNA and protein synthesis. Liposomal delivery of doxorubicin citrate improves drug penetration into tumors and decreases drug clearance, thereby increasing the duration of therapeutic drug effects. C2213 37797 monoclonal antibody 4B5 anti-idiotype vaccine A humanized anti-idiotypic (anti-Id) monoclonal antibody (MoAb) that mimics the disialoganglioside GD2 with potential immunostimulating and antineoplastic activities. Upon administration, monoclonal antibody 4B5 anti-idiotype vaccine may elicit both cellular and humoral immune responses against GD2- expressing tumor cells. GD2 is a glycosphingolipid (ceramide and oligosaccharide) that may be highly expressed by melanomas and other neuroectodermal tumors, while only minimally expressed by normal tissues. C2227 37800 salmonella VNP20009 A genetically stable Salmonella typhimurium strain, attenuated by chromosomal deletion of the purI and msbB genes, with tumor-targeting activity. In rodent models, salmonella VNP20009 has been shown to selectively accumulate and grow in a variety of tumor types, inhibiting the growth of primary and metastatic tumors. This agent may be genetically engineered to contain trangenes that express therapeutic agents or cell surface tumor-associated antigen-specific antibodies, such as CEA-specific antibodies, which may improve its tumor targeting and therapeutic potential. C2556 37807 pegfilgrastim A long-acting pegylated form of a recombinant therapeutic agent which is chemically identical to or similar to an endogenous human granulocyte colony-stimulating factor (G-CSF). Produced endogenously by monocytes, fibroblasts, and endothelial cells, G-CSF binds to and activates specific cell surface receptors, stimulating neutrophil progenitor proliferation and differentiation and selected neutrophil functions. Conjugation of the cytokine with a branched polyethylene glycol molecule (pegylation) significantly increases its therapeutic half-life. 37808 PSA RNA-pulsed dendritic cell vaccine An autologous dendritic cell vaccine with potential immunostimulatory activity. Dendritic cells harvested from a prostate cancer patient are transfected with the mRNA encoding for prostate specific antigen (PSA), a tumor marker secreted by prostatic epithelial and ductal cells. When reintroduced back to the patient, these PSA RNA pulsed autologous dendritic cells may elicit a cytotoxic T-cell (CTL) response against PSA-positive prostate cancer cells. C2236 37809 cefixime A broad-spectrum, third-generation cephalosporin antibiotic derived semisynthetically from the marine fungus Cephalosporium acremonium with antibacterial activity. As does penicillin, the beta-lactam antibiotic cefixime inhibits bacterial cell wall synthesis by disrupting peptidoglycan synthesis, resulting in a reduction in bacterial cell wall stability and bacterial cell lysis. Stable in the presence of a variety of beta-lactamases, this agent is more active against gram-negative bacteria and less active against gram-positive bacteria compared to second-generation cephalosporins. C1100 37812 rifabutin A semisynthetic ansamycin antibiotic with potent antimycobacterial properties. Rifabutin inhibits bacterial DNA-dependent RNA polymerase, thereby suppressing the initiation of RNA formation and leading to inhibition of RNA synthesis and transcription. 37814 didanosine A synthetic nucleoside analogue of deoxyadenosine in which the 3' hydroxyl on the ribose moiety is replaced by a hydrogen atom. In vivo, didanosine is converted to the active triphosphate form, which is incorporated into DNA. The absence of the 3' hydroxyl inhibits DNA elongation because phosphodiester bonds cannot be made with the substituted hydrogen. 37818 tositumomab A murine IgG2 monoclonal antibody directed against the CD20 antigen, found on the surface of B-cells. Tositumomab binds to the CD20 surface membrane antigen, resulting in apoptosis, and may stimulate antitumoral cell-mediated and/or antibody-dependent cytotoxicity. 37821 lerisetron The hydrochloride salt of a 2-piperazinylbenzimidazole-derivative serotonin type 3 (5-HT3) receptor antagonist with antiemetic activity. Lerisetron specifically binds to 5-HT3 receptors, located peripherally on vagus nerve terminals and centrally in the chemoreceptor trigger zone (CTZ) of the area postrema, which may result in suppression of chemotherapy-induced nausea and vomiting. C30143 37824 captopril A sulfhydryl-containing analog of proline with antihypertensive activity and potential antineoplastic activity. Captopril competitively inhibits angiotensin converting enzyme (ACE), thereby decreasing levels of angiotensin II, increasing plasma renin activity, and decreasing aldosterone secretion. This agent may also inhibit tumor angiogenesis by inhibiting endothelial cell matrix metalloproteinases (MMPs) and endothelial cell migration. Captopril may also exhibit antineoplastic activity independent of effects on tumor angiogenesis. 37825 tacedinaline An orally bioavailable substituted benzamide derivative with potential antineoplastic activity. Tacedinaline inhibits histone deacetylation, which may result in histone hyperacetylation, followed by the induction of differentiation, the inhibition of cell proliferation, and apoptosis in susceptible tumor cell populations. C2202 37828 pralatrexate A folate analogue inhibitor of dihydrofolate reductase (DHFR) exhibiting high affinity for reduced folate carrier-1 (RFC-1) with antineoplastic and immunosuppressive activities. Pralatrexate selectively enters cells expressing RFC-1; intracellularly, this agent is highly polyglutamylated and competes for the folate binding site of DHFR, blocking tetrahydrofolate synthesis, which may result in depletion of nucleotide precursors; inhibition of DNA, RNA and protein synthesis; and apoptotic tumor cell death. Efficient intracellular polyglutamylation of pralatrexate results in higher intracellular concentrations compared to non-polyglutamylated pralatrexate, which is more readily effuxed by the MRP (multidrug resistance protein) drug efflux pump. RFC-1, an oncofetal protein expressed at highest levels during embryonic development, may be overexpressed\non the cell surfaces of various cancer cell types. C2250 37830 triapine A synthetic heterocyclic carboxaldehyde thiosemicarbazone with potential antineoplastic activity. Triapine inhibits the enzyme ribonucleotide reductase, resulting in the inhibition of the conversion of ribonucleoside diphosphates to deoxyribonucleotides necessary for DNA synthesis. This agent has been shown to inhibit tumor growth in vitro. 37844 cilengitide A cyclic Arg-Gly-Asp peptide with potential antineoplastic activity. Cilengitide binds to and inhibits the activities of the alpha(v)beta(3) and alpha(v)beta(5) integrins, thereby inhibiting endothelial cell-cell interactions, endothelial cell-matrix interactions, and angiogenesis. 37852 BMS-214662 A nonsedating benzodiazepine derivative with potential antineoplastic activity. Farnesyltransferase inhibitor BMS-214662 inhibits the enzyme farnesyltransferase and the post-translational farnesylation of number of proteins involved in signal transduction, which may result in the inhibition of Ras function and apoptosis in susceptible tumor cells. This agent may reverse the malignant phenotype of H-Ras-transformed cells and has been shown to be active against tumor cells with and without Ras mutations. C1856 37856 thiamine A heat-labile and water-soluble essential vitamin, belonging to the vitamin B family, with antioxidant, erythropoietic, mood modulating, and glucose-regulating activities. Thiamine reacts with adenosine triphosphate (ATP) to form an active coenzyme, thiamine pyrophosphate. Thiamine pyrophosphate is necessary for the actions of pyruvate dehydrogenase and alpha-ketoglutarate in carbohydrate metabolism and for the actions of transketolase, an enzyme that plays an important role in the pentose phosphate pathway. Thiamine plays a key role in intracellular glucose metabolism and may inhibit the action of glucose and insulin on arterial smooth muscle cell proliferation. Thiamine may also protect against lead toxicity by inhibiting lead-induced lipid peroxidation. 37857 panitumumab A human monoclonal antibody produced in transgenic mice that attaches to the transmembrane epidermal growth factor (EGF) receptor. Panitumumab may inhibit autocrine EGF stimulation of tumor cells that express the EGF receptor, thereby inhibiting tumor cell proliferation. C1857 37860 ixabepilone An orally bioavailable semisynthetic analogue of epothilone B with antineoplastic activity. Ixabepilone binds to tubulin and promotes tubulin polymerization and microtubule stabilization, thereby arresting cells in the G2-M phase of the cell cycle and inducing tumor cell apoptosis. This agent demonstrates antineoplastic activity against taxane-resistant cell lines. 37862 imatinib mesylate The mesylate salt of imatinib, a tyrosine kinase inhibitor with antineoplastic activity. Imatinib binds to an intracellular pocket located within tyrosine kinases (TK), thereby inhibiting ATP binding and preventing phosphorylation and the subsequent activation of growth receptors and their downstream signal transduction pathways. This agent inhibits TK encoded by the bcr-abl oncogene as well as receptor TKs encoded by the c-kit and platelet-derived growth factor receptor (PDGFR) oncogenes. Inhibition of the bcr-abl TK results in decreased proliferation and enhanced apoptosis in malignant cells of Philadelphia-positive (Ph+) hematological malignancies such as CML and ALL; effects on c-kit TK activity inhibit mast-cell and cellular proliferation in those diseases overexpressing c-kit, such as mastocytosis and gastrointestinal stromal tumor (GIST). 37871 therapeutic allogeneic lymphocytes A population of lymphocytes therapeutically administered to a recipient individual who is genetically distinct from a donor of the same species. 37873 PR1 leukemia peptide vaccine A cancer vaccine containing PR1, a 9 amino-acid human leukocyte antigen (HLA)-A2 restricted peptide derived from proteinase 3, with potential immunotherapeutic activity. Vaccination with PR1 leukemia peptide vaccine may stimulate the host immune system to mount a cytotoxic T lymphocyte (CTL) response against tumor cells expressing proteinase 3, resulting in tumor cell lysis. Often overexpressed in leukemic cells, proteinase 3 is a serine proteinase that activates progelatinase A and is involved in angiogenesis and metastasis. C2235 37877 tariquidar An anthranilamide derivative with multidrug resistance properties. Tariquidar non-competitively binds to the p-glycoprotein transporter, thereby inhibiting transmembrane transport of anticancer drugs. Inhibition of transmembrane transport may result in increased intracellular concentrations of an anticancer drug, thereby augmenting its cytotoxicity. C2246 37878 Tc 99m sestamibi Sestamibi is a large synthetic molecule of the isonitrile family, which can be labeled with Tc99m. It passes through cells membranes passively, collecting in cells with large numbers of mitochondria. It is often used for imaging of the thyroid and parathyroid. C1419 37880 enoxaparin A low molecular weight, synthetic heparin. As an anticoagulant/antithrombotic agent, enoxaprin's mechanism of action is similar to that of heparin, although it exhibits a higher ratio of anti-Factor Xa to anti-Factor IIa activity. This agent also has anti-inflammatory properties, inhibiting monocyte adhesion to tumor necrosis factor alpha- or lipopolysaccharide-activated endothelial cells. Compared to unfractionated heparins, the use of enoxaparin is associated with lower incidences of osteoporosis and heparin-induced thrombocytopenia. 37882 Biomed 101 An agent binding to the leukotriene B4 receptor, leading to reduced interleukin-2 mediated hypoxia. Biomed 101 does not affect interleukin-2 antitumor activity. C2206 37922 adenovirus B7-1 A gene-viral vector complex comprised of an adenovirus vector and B7-1 gene targeting the CD80 antigen. Adenovirus B7-1 is used as a component in antineoplastic vaccines to elicit a cytotoxic T-cell response. C2204 37941 levofloxacin A broad-spectrum, third-generation fluoroquinolone antibiotic and optically active L-isomer of ofloxacin with antibacterial activity. Levofloxacin diffuses through the bacterial cell wall and acts by inhibiting DNA gyrase (bacterial topoisomerase II), an enzyme required for DNA replication, RNA transcription, and repair of bacterial DNA. Inhibition of DNA gyrase activity leads to blockage of bacterial cell growth. 37944 vorinostat A synthetic hydroxamic acid derivative with antineoplastic activity. Vorinostat, a second generation polar-planar compound, binds to the catalytic domain of the histone deacetylases (HDACs). This allows the hydroxamic moiety to chelate zinc ion located in the catalytic pockets of HDAC, thereby inhibiting deacetylation and leading to an accumulation of both hyperacetylated histones and transcription factors. Hyperacetylation of histone proteins results in the upregulation of the cyclin-dependant kinase p21, followed by G1 arrest. Hyperacetylation of non-histone proteins such as tumor suppressor p53, alpha tubulin, and heat-shock protein 90 produces additional anti-proliferative effects. This agent also induces apoptosis and sensitizes tumor cells to cell death processes. Vorinostat crosses the blood-brain barrier. C1796 37945 recombinant 70-kD heat-shock protein A recombinant peptide that is chemically identical to or similar to the endogenous 70-kD heat shock protein (HSP70). HSP70 is a molecular chaperone that prevents physiologic stress-induced cell death by inhibiting both caspase-dependent and caspase-independent apoptosis. Because this peptide is often overexpressed in tumor cells, autologous vaccination with HSP70 derived from tumor cells may stimulate the host immune system to mount a tumoricidal cytotoxic T lymphocyte (CTL) response. 37952 bispecific antibody MDX447 An antibody with potential antineoplastic activity. Specific for both the high-affinity immunoglobulin G (IgG) receptor CD64 and epidermal growth factor receptor (EGFR), bispecific antibody MDX447 may enhance cellular immune responses against EGFR positive cells, resulting in increased tumor cell lysis. 37968 progenipoietin A recombinant, chimeric, dual-receptor agonist fusion protein with immunohematopoietic activity. Progenipoietin (ProGP) consists of portions of the ligands for granulocyte colony-stimulating factor (G-CSF) and human fetal liver tyrosine kinase-3 (FLT3); variants progenipoietin-1, 2 and 3 differ in the orientation of the two receptor agonists. ProGP binds simultaneously to G-CSF and FLT3 receptors with receptor affinities approximately two- to three-fold higher than the respective native ligands. When administered in vivo, this agent may augment the number of circulating granulocytes and dendritic cells (DCs). ProGP may promote the proliferation of and prevent apoptosis in several human hematopoietic cell lineages, exhibiting the additive activities of a combination of C-GSF and FLT3. C2587 37976 lycopene A linear, unsaturated hydrocarbon carotenoid, the major red pigment in fruits such as tomatoes, pink grapefruit, apricots, red oranges, watermelon, rosehips, and guava. As a class, carotenoids are pigment compounds found in photosynthetic organisms (plants, algae, and some types of fungus), and are chemically characterized by a large polyene chain containing 35-40 carbon atoms; some carotenoid polyene chains are terminated by two 6-carbon rings. In animals, carotenoids such as lycopene may possess antioxidant properties which may retard ageing and many degenerative diseases. As an essential nutrient, lycopene is required in the animal diet. 37977 phenethyl isothiocyanate An isothiocyanate found in cruciferous vegetables with chemopreventive and potential antitumor activities. Although the mechanism of action is unclear, phenethyl Isothiocyanate (PEITC) was shown to induce apoptosis in tumor cells, possibly mediated through its metabolic intermediates, reactive oxygen species (ROS). PEITC also is able to activate ERK and JNK signal transduction, which in turn induces expression of stress-responsive genes. Specifically, this agent has been shown to reactivate gene expression of a detoxification enzyme, glutathione S-transferase that is silenced in prostate carcinoma. 37979 Technetium Tc 99m human serum albumin colloid A colloid formulation of human serum albumin (HSA) labeled with Technetium-99m (Tc-99m) with diagnostic imaging properties. This HSA radioconjugate contains the gamma-emitting Tc99m, a metastable nuclide of molybdenum-99. A potential advantage of the Tc-99m-HSA suspension is its smaller colloid particle size as compared to formulations containing either sulfur or tin, thereby allowing for enhanced imaging of the lymphatic draining pattern during lymphoscintigraphic or sentinel lymph node mapping procedures. C2557 37987 gadopentetate dimeglumine A gadolinium complex of diethylenetriamine pentaacetic acid with ionic paramagnetic properties. Gadopentetate dimeglumine may provide contrast enhancement during magnetic resonance imaging (MRI) of intracranial lesions with abnormal vascularity or of abnormalities in the blood-brain barrier (BBB). 37989 St. John's wort An herbal extract prepared from the plant Hypericum perforatum (St. John's wort) with photodynamic, antineoplastic, and antidepressant activities. Hypericin, one of the active compounds found in Hypericum perforatum, is a photosensitizer that, when exposed to a particular wavelength and intensity of light, may induce tumor cell apoptosis. Another compound, hyperforin, induces caspase-dependent apoptosis in certain tumor cell lines. Hypericum perforatum preparations may also stimulate the activity of cytochrome P450 enzymes and P-glycoprotein drug transporters, resulting in increased metabolism and decreased efficacy of various chemotherapeutic agents and other drugs. C2589 38001 anti-human chorionic gonadotropin vaccine A peptide vaccine consisting of the whole or partial beta subunit of human chorionic gonadotrophin hormone (hCG), linked to an adjuvant carrier of bacterial or viral origin, with anti-fertility activity. Anti-human chorionic gonadotropin vaccine blocks the activity of hCG which is naturally produced by the trophectoderm of the pre-implantation embryo within a few days of fertilization. hCG is required for the maintenance of the corpus luteum in the ovary thus ensuring its continued production of progesterone, which is required for the successful completion of implantation of the blastocyst. Without progesterone, the corpus luteum regresses, and menstruation is initiated. C28719 38004 monoclonal antibody HuM291 A humanized monoclonal antibody deficient in Fc receptor binding directed against CD3 on the surfaces of T cells. Monoclonal antibody HuM291 binds to the CD3 portion of the CD3:TCR (T-cell receptor) complex expressed on the surface of T cells, resulting in apoptosis of antigen-activated T cells., 38020 iobenguane I 131 An I 131 radioiodinated synthetic analogue of the neurotransmitter norepinephrine. Iobenguane localizes to adrenergic tissue and, in radioiodinated forms, may be used to image or eradicate tumor cells that take up and metabolize norepinephrine. 38031 monoclonal antibody Hu3S193 A humanized monoclonal antibody directed against the Lewis Y antigen, a tumor-associated epithelial antigen, with potential antineoplastic activity. Following binding, monoclonal antibody Hu3S193 triggers an antibody-dependent cell-mediated cytotoxicity in cells expressing Lewis Y antigen. C2547 38032 MUC1-KLH conjugate vaccine A peptide vaccine, containing human tumor-associated epithelial mucin (MUC1) conjugated with keyhole limpet hemocyanin (KLH), with potential antineoplastic activity. Vaccination with MUC1-KLH conjugate vaccine may stimulate humoral and cytotoxic T-lymphocyte (CTL) responses against tumor cells expressing the MUC1 antigen. In this vaccine, MUC1 antigen is conjugated with KLH, an immunostimulant and a hapten carrier, to enhance immune recognition. MUC1 antigen, a membrane-bound glycoprotein expressed by most glandular and ductal epithelial cells, is overexpressed in an aberrant or deglycosylated form in various cancers such as those of the breast, prostate, and ovary. C2232 38033 MUC1-KLH vaccine/QS21 A peptide vaccine containing the human tumor-associated antigen epithelial mucin (MUC1 antigen) conjugated with keyhole limpet hemocyanin (KLH) and combined with the nonspecific immunoadjuvant QS21 with potential antineoplastic activity. MUC1 antigen is linked with KLH, an immunostimulant and a hapten carrier, in order to enhance immune recognition; the co-administration of saponin-derived QS21 potentially amplifies the total immune response to the MUC1 antigen. Administration of MUC1-KLH vaccine/QS21 may result in both the production of antitumor antibodies and the stimulation of a cytotoxic T-lymphocyte (CTL) response against tumor cells expressing the MUC1 antigen. MUC1 antigen, a membrane-bound glycoprotein expressed by most glandular and ductal epithelial cells, is overexpressed as an aberrant or deglycosylated form in various cancers such as breast, prostate and ovarian cancers. C11845 38038 sipuleucel-T A cell-based vaccine composed of autologous antigen-presenting peripheral blood mononuclear cells (enriched for a dendritic cell fraction) that have been exposed to a recombinant protein consisting of granulocyte-macrophage colony-stimulating factor (GM-CSF) fused to prostatic-acid phosphatase (PAP), a protein expressed by prostate cancer cells. Upon administration, the vaccine may stimulate an antitumor T-cell response against tumor cells expressing PAP. C1985 38040 prostatic acid phosphatase-sargramostim fusion protein A genetically-engineered protein formed by the fusion of prostatic acid phosphatase (PAP) and sargramostim (GM-CSF). Vaccination with antigen-presenting cells (APC) loaded with prostatic acid phosphatase-sargramostim fusion protein may elicit a cytotoxic T-cell response against tumor cells that express PAP. C2548 38045 interleukin-2 gene The DNA sequence that encodes the protein cytokine interleukin-2 (IL-2). When introduced as the complementary DNA (cDNA) form into tumor cells by, for example, a genetically engineered adenovirus vector, the transfected IL-2 cDNA expresses IL-2 which may activate antitumoral natural killer cells and elicit an antitumoral cytotoxic T-cell response, resulting in an inhibition of tumor progression. C2549 38046 palladium Pd 103 A radioisotope of the metal palladium used in brachytherapy implants or 'seed'. With a half-life of 17 days, palladium 103 administered with brachytherapy allows continuous, tumor-site specific low-energy irradiation to the tumor cell population while sparing normal adjacent tissues from radiotoxicity. C2550 38047 HER-2/neu intracellular domain protein The cytoplasmic domain or intracellular domain (ICD) of the HER2/neu protein that exhibits tyrosine kinase activity. Based on sensitization theory, co-administration of trastuzumab (anti-HER-2/neu monoclonal antibody) and HER-2/neu intracellular domain protein may result in the potentiation of a HER2/neu-specific cytotoxic T lymphocyte (CTL) response against tumor cells overexpressing the HER2/neu protein. HER-2/neu protein, a glycoprotein cell surface receptor that is composed of an extracellular domain (ECD), a transmembrane domain, and an ICD, is overexpressed by many adenocarcinomas including breast adenocarcinoma. 38048 therapeutic autologous dendritic cells A population of a type of antigen-presenting cell (APC), the dendritic cell (DC), harvested from a patient and grown in vitro in the presence of tumor-associated antigens (TAAs) derived from the patient's tumor (a technique known as 'pulsing') and then injected back into the patient; autologous DCs so manipulated may stimulate a specific cell-mediated antitumoral cytotoxicity. DCs derived from a patient may also be fused with the patient's tumor cells in vitro to combine sustained tumor antigen expression with the antigen-presenting and immunostimulatory capacities of DCs; when injected back into the patient, these autologous DC-tumor cell hybrids (fusion cells) may stimulate an active antitumoral immune response. C2594 38051 CC-1088 An analog of thalidomide with potential antineoplastic activity that belongs to the functional class of agents called selective cytokine inhibitory drugs (SelCIDs). SelCIDs inhibit phosphodiesterase-4 (PDE 4), an enzyme involved in tumor necrosis factor alpha (TNF alpha) production. CC-1088 inhibits production of the cytokines vascular endothelial growth factor (VEGF) (a pro-angiogenic factor) and interleukin-6 (IL-6). 38058 indole-3-carbinol A naturally occurring, orally available cleavage product of the glucosinolate glucobrassicanin, a natural compound present in a wide variety of plant food substances including members of the family Cruciferae with antioxidant and potential chemopreventive properties. Indole-3-carbinol scavenges free radicals and induces various hepatic cytochrome P450 monooxygenases. Specifically, this agent induces the hepatic monooxygenase cytochrome P4501A1 (CYP1A1), resulting in increased 2-hydroxylation of estrogens and increased production of the chemoprotective estrogen 2-hydroxyestrone. 38088 rebimastat A sulfhydryl-based second-generation matrix metalloproteinase (MMP) inhibitor with potential antineoplastic activity. Rebimastat selectively inhibits several MMPs (MMP 1, 2, 8, 9, and 14), thereby inducing extracellular matrix degradation, and inhibiting angiogenesis, tumor growth and invasion, and metastasis. 38095 cintredekin besudotox A recombinant chimeric protein with potent antitumor activity. Cintredekin besudotox is composed of interleukin-13 (IL13), a pleiotropic immunoregulatory cytokine, linked to a mutated form of pseudomonas exotoxin A; this agent targets and kills tumor cells that express the IL13 receptor (IL13R).The IL13 moiety attaches to the IL13R on the tumor cell membrane, facilitating the entry of the exotoxin. The exotoxin moiety induces caspase-mediated apoptosis of tumor cells via a mechanism involving mitochondrial damage; it also catalyzes the transfer of ADP ribose from nicotinamide adenine dinucleotide (NAD) to elongation factor-2 in eukaryotic cells, thereby inactivating elongation factor 2 and inhibiting protein synthesis. 38097 yttrium Y 90 daclizumab A synthetic radioimmunoconjugate comprised of a humanized anti-interleukin-2 (IL-2) antibody linked to the radioisotope Yttrium 90 with potential antineoplastic activity. Daclizumab binds with high affinity to the Tac (also called CD25) subunit of the IL-2 receptor complex and inhibits the binding of IL-2, thereby blocking the IL-2-mediated activation of lymphocytes. As Yttrium Y 90 daclizumab, daclizumab delivers radiation specifically to lymphocytes that express the IL-2 receptor. C2600 38100 vincristine sulfate liposomes A sphingomyelin/cholesterol liposomal formulation of vincristine sulfate with potential antineoplastic activity. Vincristine, a vinca alkaloid isolated from the plant Vinca rosea, irreversibly binds to and stabilizes tubulin, thereby interrupting microtubule assembly/disassembly dynamics, thereby preventing the formation of the mitotic spindle and leading to cell cycle arrest in metaphase. Liposomal encapsulation prolongs bioavailability of vincristine, increases its delivery to tumor tissues and reduces its toxicity profile. Compared to standard liposomal delivery, sphingosomal drug delivery further increases circulation time of serum drug and enhances drug accumulation at tumor sites, thereby leading to a further increase in efficacy. 38102 yttrium Y 90-edotreotide A radioconjugate consisting of the octreotide derivative edotreotide labeled with yttrium 90 (Y-90) with potential radiotherapeutic uses. Similar to octreotide, yttrium Y 90-edotreotide binds to somatostatin receptors (SSTRs), especially type 2 receptors, present on the cell membranes of many types of neuroendocrine tumor cells, delivering tissue-specific, beta-emitting nuclide Y-90-mediated cytotoxicity to SSTR-positive cells. Yttrium Y 90-edotreotide is produced by substituting tyrosine for phenylalanine at the 3 position of the somatostatin analogue octreotide and chelating the substituted octreotide to Y-90 via dodecanetetraacetic acid (DOTA). 38109 donepezil hydrochloride The hydrochloride salt of a piperidine derivative with neurocognitive-enhancing activity. Donepezil reversibly inhibits acetylcholinesterase, thereby blocking the hydrolysis of the neurotransmitter acetylcholine and, consequently, increasing its activity. This agent may improve neurocognitive function in Alzheimer's disease, reduce sedation associated with opioid treatment of cancer pain, and improve neurocognitive function in patients who have received radiation therapy for primary brain tumors or brain metastases. 38135 monoclonal antibody 11D10 anti-idiotype vaccine A vaccine consisting of a monoclonal antibody (MoAB) directed against an idiotype that mimics a human milk fat globule (HMFG) membrane epitope. Vaccination with monoclonal antibody 11D10 anti-idiotype vaccine induces anti-anti-idiotype antibodies (Ab3) that may react with breast cancer cell lines expressing the HMFG membrane epitope. 38148 yttrium Y 90 monoclonal antibody BrE-3 A radioimmunotherapeutic agent consisting of a monoclonal antibody (BrE-3) directed against the tumor-associated antigen epithelial glycoprotein mucin chelated to the radioisotope yttrium-90. Yttrium Y 90 monoclonal antibody BrE-3 binds to tumor cells expressing epithelial glycoprotein mucin, selectively delivering a cytotoxic dose of beta radiation. C2607 38150 indium In 111 monoclonal antibody BrE-3 A humanized monoclonal antibody conjugated to the imaging radioisotope (indium-111). This radioimmunoconjugate binds to the breast epithelial mucin antigen, which is found primarily on breast cancer cells, permitting radioimmmuno-localization of mucin-positive tumor cells and an estimate of radiation dosimetry prior to administration of cytotoxic radiotherapy. 38156 SS1(dsFv)-PE38 immunotoxin A recombinant immunotoxin consisting of the single chain anti-mesothelin monoclonal antibody SS1(dsFv) linked to Pseudomonas exotoxin PE-38. The monoclonal antibody moiety of the agent binds to cells that express mesothelin, a cell surface glycoprotein which may be overexpressed in ovarian cancer, mesotheliomas, and some squamous cell carcinomas; after internalization, the exotoxin moiety inactivates eukaryotic translation elongation factor 2, thereby disrupting tumor cell protein synthesis. 38167 ceramide One of a number of a class of sphingolipids, N-acyl derivatives with long chains. Ceramide is the core molecule for the synthesis of sphingomyelin, an essential lipid for myelination and neurotransmission; it may function as a second messenger to stimulate differentiation, inhibit proliferation, and induce apoptosis. 38169 monoclonal antibody m170 A panadenocarcinoma murine monoclonal antibody with potential antineoplastic activity. Monoclonal antibody m170 may be conjugated with a radioactive element and used in radioimmunotherapy (RIT), a procedure that uses a tumor-specific monoclonal antibody to target radiation to cancer cells. C2610 38182 caspofungin acetate The acetate salt of an antimycotic echinocandin lipopeptide, semisynthetically derived from a fermentation product of the fungus Glarea lozoyensis. Caspofungin inhibits 1,3-beta-glucan synthase, resulting in decreased synthesis of beta(1,3)-D-glucan (an essential component of the fungal cell wall), weakening of the fungal cell wall, and fungal cell wall rupture. This agent is active against Aspergillus and Candida species. C1724 38188 yttrium Y 90 monoclonal antibody B3 A radioimmunoconjugate of monoclonal antibody (MoAb) B3 conjugated with isotope yttrium 90. MoAb B3 is a murine MoAb that recognizes a Lewis Y carbohydrate antigen present on the surface of many carcinomas. This radioimmunoconjugate emits beta particles that causes cytotoxicity in tumor cells and has both diagnostic and therapeutic uses. 38195 atamestane A synthetic steroidal substance with antineoplastic activity. Atamestane binds irreversibly to and inhibits the enzyme aromatase, thereby blocking the conversion of cholesterol to pregnenolone and the peripheral aromatization of androgenic precursors into estrogens. 38201 EGFR antisense DNA A synthetic sequence of DNA constructed in the antisense orientation to a sequence of DNA in epidermal growth factor receptor (EGFR), a member of the erbB gene family. EGFR antisense DNA suppresses the expression of EGFR by tumor cells, thereby inhibiting tumor cell proliferation and decreasing tumor growth. This agent also appears to reduce the invasiveness of certain breast cancer cells. Members of the erbB gene family are overexpressed in many cancers and play roles in carcinogenesis and the regulation of cell proliferation. C2617 38211 karenitecin A synthetic silicon-containing agent related to camptothecin with antineoplastic properties. Karenitecin stabilizes the cleavable complex between topoisomerase I and DNA, resulting in DNA breaks and consequently triggering apoptosis. Because it is lipophilic, karenitecin exhibits enhanced tissue penetration and bio-availability compared to water-soluble camptothecins. 38213 benzoylphenylurea A low molecular weight agent with antineoplastic activity. Benzoylphenylurea binds to the colchicine binding site on tubulin, thereby blocking tubulin polymerization and disrupting mitotic function. This agent also inhibits DNA polymerase, and has been shown to arrest leukemia cells in the G1-S transition phase of the cell cycle. 38215 recombinant vaccinia-CEA(6D)-TRICOM vaccine A vaccine consisting of recombinant vaccinia virus encoding the tumor-associated antigen carcinoembryonic antigen (CEA) and a TRIad of COstimulatory Molecules (B7-1, ICAM-1, and LFA-3; also called TRICOM). Vaccination with recombinant vaccinia-CEA(6D)-TRICOM vaccine stimulates the host immune system to mount a T-cell response against tumor cells expressing the CEA antigen. The use of TRICOM in the vaccine may elicit a greater antitumor cytotoxic T lymphocyte (CTL) immune response compared to the use of vaccinia-CEA alone. 38216 recombinant fowlpox-CEA(6D)/TRICOM vaccine A cancer vaccine comprised of a recombinant fowlpox virus vector encoding the carcinoembryonic antigen (CEA) and a TRIad of COstimulatory Molecules (B7-1, ICAM-1 and LFA-3) (TRICOM). This agent may enhance CEA presentation to antigen presenting cells (APC) and activate cytotoxic T-cells against CEA-expressing tumors. 38230 annamycin liposomal A liposome-encapsulated form of the semi-synthetic doxorubicin analogue annamycin with antineoplastic activity. Annamycin intercalates into DNA and inhibits topoisomerase II, resulting in the inhibition of DNA replication and repair and RNA and protein synthesis. This agent circumvents multidrug-resistance (MDR) transporters, including P-glycoprotein (P-gp). Liposomal annamycin is less toxic and shows improved antitumor activity compared to annamycin. 38236 carcinoembryonic antigen peptide 1-6D A 9-residue human leukocyte antigen (HLA)-restricted fragment of carcinoembryonic antigen (CEA). CEA:571-579 peptide, which has the amino acid sequence YLSGANLNL, may elicit a cytotoxic T lymphocyte (CTL) immune response against tumors expressing CEA. 38254 bispecific antibody 4G7xH22 A bispecific antibody containing a 4G7 hybridoma secreting IgG1 antibody specific for B-lymphocytes and a monoclonal antibody targeting Fc gamma RI-expressing cells. C2624 38264 plevitrexed An orally bioavailable, small molecule, non-polyglutamatable, antifolate quinazoline derivative thymidine synthetase inhibitor with potential antineoplastic activity. Plevitrexed is transported into the cell via the physiological reduced folate carrier (RFC) system. Intracellularly, this agent selectively binds to the folate binding site of thymidylate synthase and inhibits thymidine synthesis, which may result in DNA synthesis inhibition and apoptosis. C1629 38271 bismuth Bi213 monoclonal antibody M195 A radioimmunoconjugate consisting of murine monoclonal antibody (M195) and bismuth 213 (Bi213). Monoclonal antibody M195 binds to CD33, a surface antigen expressed by myelogenous leukemia cells. Bi213 is an isotope that emits short-ranged high-energy alpha particles. This radioimmunoconjugate selectively delivers alpha particle-mediated cytotoxicity to leukemic cells, thereby limiting the exposure of normal tissues to ionizing radiation. C28502 38278 GPI-0100 A semi-synthetic triterpene glycoside, derived from the naturally occurring saponins. GPI-0100 functions as an adjuvant when given as part of a vaccine preparation to improve the immunogenicity of antigens such as proteins, carbohydrates. GPI-0100 containing vaccines have been used with both viral and tumor antigens to elicit a Type 1 helper T cell response for those diseases in which a cytotoxic T lymphocyte (CTL) response is desired. C2627 38289 valganciclovir A synthetic prodrug of ganciclovir, a nucleoside analogue of 2'-deoxyguanosine, with antiviral activity. After phosphorylation, valganciclovir is incorporated into DNA, resulting in inhibition of viral DNA polymerase, viral DNA synthesis, and viral replication. 38293 Corynebacterium granulosum P40 An insoluble fraction isolated from the bacterium Corynebacterium granulosum with potential cancer immunotherapeutic activity. As a non-specific immunostimulant, Corynebacterium granulosum P40 activates the reticulo-endothelial system; induces the production of certain cytokines; enhances macrophage activity; and potentiates a delayed-type hypersensitivity response when co-administered with an antigen. 38294 entinostat A synthetic benzamide derivative with potential antineoplastic activity. Entinostat binds to and inhibits histone deacetylase, an enzyme that regulates chromatin structure and gene transcription. This agent appears to exert dose-dependent effects in human leukemia cells including cyclin-dependent kinase inhibitor 1A (p21/CIP1/WAF1)-dependent growth arrest and differentiation at low drug concentrations; a marked induction of reactive oxygen species (ROS); mitochondrial damage; caspase activation; and, at higher concentrations, apoptosis. In normal cells, cyclin-dependent kinase inhibitor 1A expression has been associated with cell-cycle exit and differentiation. 38315 cevimeline hydrochloride A cholinergic analogue with glandular secretion stimulatory activity. Cevimeline binds to and activates muscarinic receptors, thereby increasing the secretions in exocrine salivary and sweat glands. This cholinergic agonist also increases the tone of smooth muscle in the gastrointestinal and urinary tracts. Cevimeline is being studied as a treatment for dry mouth caused by radiation therapy to the head and neck. 38320 valdecoxib A sulfonamide derivative and non-steroidal anti-inflammatory drug (NSAID) with anti-inflammatory, analgesic, and antipyretic activities. Valdecoxib selectively binds to and inhibits cyclooxygenase (COX)-2, thereby preventing the conversion of arachidonic acid into prostaglandins, which are involved in the regulation of pain, inflammation, and fever. This NSAID does not inhibit COX-1 at therapeutic concentrations and therefore does not interfere with blood coagulation. 38321 vitamin E A natural fat-soluble antioxidant with potential chemopreventive activity. Vitamin E ameliorates free-radical damage to biological membranes, protecting polyunsaturated fatty acids (PUFA) within membrane phospholipids and within circulating lipoproteins. Peroxyl radicals react 1000-fold faster with vitamin E than with PUFA. In the case of oxygen free radical-mediated tumorigenesis, vitamin E may be chemopreventive. 38323 paclitaxel liposome A liposome-encapsulated formulation of paclitaxel, a taxoid compound extracted from the Pacific yew tree Taxus brevifolia, with antineoplastic property. Paclitaxel binds to tubulin and interferes with the assembly/disassembly dynamics of microtubules, thereby resulting in the inhibition of cell division. This agent also induces apoptosis via inactivation of the apoptosis inhibitor, B-cell Leukemia 2 (Bcl-2) protein. Paclitaxel liposome formulation potentially enhances delivery of higher doses of paclitaxel to the target tissues and exhibits lower systemic toxicity. C2631 38325 paclitaxel poliglumex The agent paclitaxel linked to a biodegradable, water-soluble polyglutamate polymer with antineoplastic properties. The polyglutamate residue increases the water solubility of paclitaxel and allows delivery of higher doses than those achievable with paclitaxel alone. Paclitaxel promotes microtubule assembly and prevents microtubule depolymerization, thus interfering with normal mitosis. 38329 pelitrexol A water soluble antifolate with anti-proliferative activity. Pelitrexol inhibits activity of glycinamide ribonucleotide formyltransferase (GARFT), the first folate-dependent enzyme of the de novo purine synthesis pathway essential for cell proliferation. Enzyme inhibition reduces the purine nucleotides pool required for DNA replication and RNA transcription. As a result, this agent causes cell cycle arrest in S-phase, and ultimately inhibits tumor cell proliferation. 38330 riboflavin An essential human nutrient that is a heat-stable and water-soluble flavin belonging to the vitamin B family. Riboflavin is a precursor of the coenzymes flavin mononucleotide (FMN) and flavin adenine dinucleotide (FAD). These coenzymes are of vital importance in normal tissue respiration, pyridoxine activation, tryptophan to niacin conversion, fat, carbohydrate, and protein metabolism, and glutathione reductase mediated detoxification. Riboflavin may also be involved in maintaining erythrocyte integrity. This vitamin is essential for healthy skin, nails, and hair. 38333 atrasentan hydrochloride The orally available hydrochloride salt of pyrrolidine-3-carboxylic acid with potential antineoplastic activity. As a selective antagonist of the endothelin-A (ETA) receptor, atrasentan binds selectively to the ETA receptor, which may result in inhibition of endothelin-induced angiogenesis and tumor cell proliferation. 38334 pirfenidone An orally active synthetic antifibrotic agent structurally similar to pyridine 2,4-dicarboxylate. Pirfenidone inhibits fibroblast, epidermal, platelet-derived, and transforming beta-1 growth factors, thereby slowing tumor cell proliferation. This agent also inhibits DNA synthesis and the production of mRNA for collagen types I and III, resulting in a reduction in radiation-induced fibrosis. 38335 HPPH A lipophilic, second-generation, chlorin-based photosensitizer. Upon intravenous administration, HPPH selectively accumulates in the cytoplasm of cancer or pre-cancerous cells. When laser light is applied, a photodynamic reaction between HPPH and oxygen occurs, resulting in the production of cytotoxic free radicals and singlet oxygen and free radical-mediated cell death. Compared to the first-generation photosensitizer porfimer sodium, HPPH shows improved pharmacokinetic properties and causes only mild skin photosensitivity which declines rapidly within a few days after administration. 38341 MOv-gamma chimeric receptor gene A recombinant engineered chimeric gene derived from the murine gene encoding the variable region of monoclonal antibody MOv18 against folate-binding protein, which is often overexpressed in human ovarian cancer cells, and the gene encoding the Fc receptor for the gamma subunit of human IgG and IgE. Peripheral blood lymphocytes expressing the MOv-gamma gene may be used in the immunotherapeutic treatment of ovarian cancer. 38350 cefepime hydrochloride The hydrochoride salt of a semi-synthetic, beta-lactamase-resistant, fourth-generation cephalosporin antibiotic derived from an Acremonium fungal species with broad-spectrum bactericidal activity. Administered parenterally, cefipime inhibits bacterial cell wall synthesis by binding to and inactivating penicillin-binding proteins (PBP) located on the inner membrane of the bacterial cell wall. Inactivation of PBPs interferes with the cross-linkage of peptidoglycan chains necessary for bacterial cell wall strength and rigidity, resulting in a reduction of bacterial cell wall stability and cell lysis. This agent is more active against a variety of Gram-positive pathogens compared to third-generation cephalosporins. C1041 38351 niacin A water-soluble vitamin belonging to the vitamin B family, which occurs in many animal and plant tissues, with antihyperlipidemic activity. Niacin is converted to its active form niacinamide, which is a component of the coenzymes nicotinamide adenine dinucleotide (NAD) and its phosphate form, NADP. These coenzymes play an important role in tissue respiration and in glycogen, lipid, amino acid, protein, and purine metabolism. Although the exact mechanism of action by which niacin lowers cholesterol is not fully understood, it may act by inhibiting the synthesis of very low density lipoproteins (VLDL), inhibiting the release of free fatty acids from adipose tissue, increasing lipoprotein lipase activity, and reducing the hepatic synthesis of VLDL-C and LDL-C. 38354 taurolidine A synthetic broad-spectrum antibiotic with antibacterial, anticoagulant and potential antiangiogenic activities. Taurolidine, derived from the amino acid taurine, binds to and neutralizes bacterial exotoxins and endotoxins, or lipopolysaccharides (LPS). Taurolidine binding to LPS prevents bacterial adherence to host epithelial cells, thereby prevents bacterial invasion of uninfected host cells. Although the mechanism underlying its antineoplastic activity has not been fully elucidated, it may be related to this agent's anti-adherence property. In addition, taurolidine also promotes apoptosis by inducing various apoptotic factors and suppresses the production of vascular endothelial growth factor (VEGF), a protein that plays an important role in angiogenesis. 38358 anti-FLT-1 ribozyme A nuclease-stabilized synthetic ribozyme with potential antineoplastic activity. Anti-Flt-1 ribozyme cleaves the mRNA encoding vascular endothelial growth factor 1 (VEGF-1, or Flt-1), thereby specifically inhibiting VEGF-stimulated angiogenesis, tumor growth, and metastasis. C1865 38362 telomerase: 540-548 peptide vaccine A recombinant peptide consisting of the amino acid residues 540 to 548 of the human telomerase reverse transcriptase (hTERT). Telomerase expression has been directly linked to tumor development; its catalytic subunit is expressed in the majority of human cancer cells, but infrequently in normal cells. Vaccination with telomerase:540-548 peptide may stimulate cytotoxic T cells to recognize and kill telomerase-expressing cells. 38367 canfosfamide hydrochloride The hydrochloride salt of a modified glutathione analogue with potential antineoplastic activity. Canfosfamide is selectively activated by glutathione S-transferase P1-1 into an alkylating metabolite that forms covalent linkages with nucleophilic centers in tumor cell DNA, which may induce a cellular stress response and cytotoxicity, and decrease tumor proliferation. S-transferase P1-1 is an enzyme that is overexpressed in many human malignancies. 38371 phenoxodiol A synthetic flavonoid derivative. Phenoxodiol activates the mitochondrial caspase system, inhibits X-linked inhibitor of apoptosis (XIAP), and disrupts FLICE inhibitory protein (FLIP) expression, resulting in tumor cell apoptosis. This agent also inhibits DNA topoisomerase II by stabilizing the cleavable complex, thereby preventing DNA replication and resulting in tumor cell death. 38385 trivalent influenza vaccine A synthetic vaccine consisting of three inactivated influenza viruses, two different influenza type A strains and one influenza type B strain. Trivalent influenza vaccine is formulated annually, based on influenza strains projected to be prevalent in the upcoming flu season. This agent may be formulated for injection or intranasal administration. 38388 doxorubicin-magnetic targeted carrier complex A formulation of the anthracycline antibiotic doxorubicin in which doxorubicin is bound to microscopic beads of activated carbon and iron as a magnetic-targeted carrier (MTC). Doxorubicin, an intercalator and a topoisomerase II inhibitor, prevents DNA replication and ultimately inhibits protein synthesis. This agent also generates oxygen free radicals, resulting in cytotoxic lipid peroxidation of cell membrane lipids. Guided by the placement of a magnet on the body surface overlying a tumor site, the doxorubicin-MTC complex delivers doxorubicin directly to the tumor site, thereby targeting and prolonging the duration of doxorubicin-mediated cytotoxicity to the tumor bed while minimizing systemic toxicity. C2644 38402 gabapentin A synthetic analogue of the neurotransmitter gamma-aminobutyric acid with anticonvulsant activity. Although its exact mechanism of action is unknown, gabapentin appears to inhibit excitatory neuron activity. This agent also exhibits analgesic properties. 38403 canertinib dihydrochloride The hydrochloride salt of an orally bio-available quinazoline with potential antineoplastic and radiosensitizing activities. Canertinib binds to the intracellular domains of epidermal growth factor receptor tyrosine kinases (ErbB family), irreversibly inhibiting their signal transduction functions and resulting in tumor cell apoptosis and suppression of tumor cell proliferation. This agent also acts as a radiosensitizing agent and displays synergistic activity with other chemotherapeutic agents. 38406 doxercalciferol A synthetic analog of vitamin D with potential antineoplastic activity. In the liver, doxercalciferol is converted to its biologically active vitamin D metabolites, which control the intestinal absorption of dietary calcium, the tubular reabsorption of calcium by the kidney and, in conjunction with parathyroid hormone (PTH), the mobilization of calcium from the skeleton. Through interaction with specific receptor proteins in target tissues, these vitamin D metabolites act directly on osteoblasts to stimulate skeletal growth, and on the parathyroid glands to suppress PTH synthesis and secretion. This agent has also been shown to inhibit the growth of retinoblastomas, and may exhibit some antiproliferative activity against prostate cancer cells. 38407 recombinant tyrosinase-related protein-2 A recombinant therapeutic agent which is chemically identical to or similar to an endogenous non-mutated melanocyte differentiation antigen expressed by both normal and malignant melanocytes. Vaccinations with recombinant tyrosinase-related protein-2 may elicit an antitumoral cytotoxic T-cell response against tumor cells and some normal cells that express tyrosinase-related protein-2. 38410 methyl-5-aminolevulinate hydrochloride cream A topical cream formulation containing the hydrochloride salt of methyl-5-aminolevulinate, a lipophilic methyl ester of 5-aminolevulinic acid, with photosensitizer prodrug activity. Upon topical administration, methyl-5-aminolevulinate in the cream is selectively absorbed by tumor cells where it is converted to the photosensitizer protoporphyrin IX (PpIX). Upon photoirradiation, PpIX is activated and transfers energy to oxygen, generating singlet oxygen and superoxide and hydroxyl radicals, which may result in free-radical-mediated DNA damage and cell death. C2647 38413 monoclonal antibody 105AD7 anti-idiotype vaccine A cancer vaccine consisting of a humanized monoclonal antibody that mimics a tumor-associated antigen 791Tgp72 (also known as CD55). Vaccination with this agent may stimulate a host cytotoxic T-cell response against tumor cells expressing CD55, resulting in tumor cell lysis. C2648 38414 DHA-paclitaxel A prodrug comprised of the naturally occurring omega-3 fatty acid docosahexaenoic acid (DHA) covalently conjugated to the anti-microtubule agent paclitaxel. Because tumor cells take up DHA, DHA-paclitaxel is delivered directly to tumor tissue, where the paclitaxel moiety binds to tubulin and inhibits the disassembly of microtubules, thereby resulting in the inhibition of cell division. Paclitaxel also induces apoptosis by binding to and blocking the function of the apoptosis inhibitor protein Bcl-2 (B-cell Leukemia 2). DHA-paclitaxel exhibits improved pharmacokinetic and toxicity profiles when compared to conventional paclitaxel and has demonstrated antineoplastic activity in animal models of cancer. 38421 SU6668 An orally bioavailable receptor tyrosine kinase inhibitor. SU6668 binds to and inhibits the autophosphorylation of vascular endothelial growth factor receptor 2 (VEGFR2), platelet-derived growth factor receptor (PDGFR), and fibroblast growth factor receptor (FGFR), thereby inhibiting angiogenesis and cell proliferation. SU6668 also inhibits the phosphorylation of the stem cell factor receptor tyrosine kinase c-kit, often expressed in acute myelogenous leukemia cells. 38423 silicon phthalocyanine 4 A synthetic photosensitizer agent containing a large macrocyclic ring chelated with silicon. Silicon phthalocyanine 4 localizes primarily in mitochondrial cytosolic membranes and, after photoexcitation, forms reactive oxygen species that induce apoptosis. 38428 erlotinib hydrochloride The hydrochloride salt of a quinazoline derivative with antineoplastic properties. Competing with adenosine triphosphate, erlotinib reversibly binds to the intracellular catalytic domain of epidermal growth factor receptor (EGFR) tyrosine kinase, thereby reversibly inhibiting EGFR phosphorylation and blocking the signal transduction events and tumorigenic effects associated with EGFR activation. 38431 teicoplanin A glycopeptide antibiotic complex isolated from the bacterium Actinoplanes teichomyceticus. Teicoplanin inhibits peptidoglycan polymerization, resulting in inhibition of bacterial cell wall synthesis and cell death. 38440 laromustine A sulfonyl hydrazine prodrug with antineoplastic activity. Laromustine releases the DNA chloroethylating agent 90CE after entering the blood stream; 90CE chloroethylates alkylates the 06 position of guanine, resulting in DNA crosslinking, strand breaks, chromosomal aberrations, and disruption of DNA synthesis. Intracellular metabolism of this agent also releases methyl isocyanate which inhibits 06-alkyl-guanine transferase, an enzyme involved with DNA repair. 38447 ipilimumab A monoclonal antibody directed against cytotoxic T-lymphocyte-associated antigen-4 (CTLA4), an antigen that is expressed on activated T-cells and exhibits affinity for B7 co-stimulatory molecules. By binding CTLA4, ipilimumab enhances T-cell activation and blocks B7-1 and B7-2 T-cell co-stimulatory pathways. 38451 apolizumab A humanized monoclonal antibody directed against 1D10, a polymorphic determinant on the HLA-DR beta chain that is expressed on normal and neoplastic B cells. Apolizumab induces complement-mediated cytotoxicity, antibody-dependent cell-mediated cytotoxicity, and apoptosis of 1D10 antigen-positive B cells in vitro. 38452 allopurinol A structural isomer of hypoxanthine. Allopurinol inhibits xanthine oxidase, an enzyme that converts oxypurines to uric acid. By blocking the production of uric acid, this agent decreases serum and urine concentrations of uric acid, thereby providing protection against uric acid-mediated end organ damage in conditions associated with excessive production of uric acid, i.e. the massive cell lysis associated with the treatment of some malignancies. 38456 monoclonal antibody CC49-delta CH2 A humanized CH2 domain-deleted second-generation monoclonal antibody based on the antibody B72.3 that is directed against tumor-associated glycoprotein 72 (TAG72). TAG72 is expressed by gastric, breast, pancreatic, colorectal, and ovarian carcinoma cells. 38472 2-methoxyestradiol An orally bioavailable estradiol metabolite with potential antineoplastic activity. 2-Methoxyestradiol inhibits angiogenesis by reducing endothelial cell proliferation and inducing endothelial cell apoptosis. This agent also inhibits tumor cell growth by binding to tubulin, resulting in antimitotic activity, and by inducing caspase activation, resulting in cell cycle arrest in the G2 phase, DNA fragmentation, and apoptosis. 38483 yttrium Y 90 ibritumomab tiuxetan A radioimmunotherapeutic agent consisting of a murine monoclonal anti-CD20 antibody (ibritumomab) linked by the chelator tiuxetan to the radioisotope yttrium-90 (Y 90). Yttrium Y 90 ibritumomab tiuxetan binds to and specifically delivers beta radiation to CD20-expressing tumor cells, thereby minimizing the systemic effects of radiation. 38485 halofuginone hydrobromide The hydrobromide salt of halofuginone, a semisynthetic quinazolinone alkaloid anticoccidial derived from the plant Dichroa febrifuga, with antifibrotic and potential antineoplastic activities. Halofuginone specifically inhibits collagen type I gene expression and matrix metalloproteinase 2 (MMP-2) gene expression, which may result in the suppression of angiogenesis, tumor stromal cell development, and tumor cell growth. These effects appear to be due to halofuginone-mediated inhibition of the collagen type I and MMP-2 promoters. Collagen type I and MMP-2 play important roles in fibro-proliferative diseases. 38491 etaracizumab A humanized monoclonal IgG1 antibody directed against the vitronectin receptor alpha v beta 3 integrin. Etaracizumab blocks the binding of ligands, such as vitronectin, to alpha v beta 3 integrin, resulting in inhibition of angiogenesis and metastasis. Alpha v beta 3 integrin is a cell adhesion and signaling receptor that is expressed on the surface of tumor vessel endothelial cells, some tumor cells, and a number of other cell types. C1800 38494 NY-ESO-1 peptide vaccine A cancer vaccine consisting of an immunogenic peptide derived from the cancer-testis antigen (NY-ESO-1), an antigen found in normal testis and various tumors. Vaccination with NY-ESO-1 peptide vaccine may stimulate the host immune system to mount a humoral and cytotoxic T lymphocyte (CTL) response to cells expressing NY-ESO-1 antigen, resulting in tumor cell lysis. 38497 iodine I 131 ethiodized oil A cytotoxic radioconjugate consisting of ethiodized oil, an iodinated ethyl ester derived from poppy seed oil, labeled with iodine 131 (I-131). Iodine I 131 ethiodized oil accumulates in hepatocellular carcinoma and hepatoblastoma tumor cells, resulting in targeted cytotoxicity to tumor cells while sparing surrounding normal cells and tissues. C2696 38498 ertumaxomab A murine monoclonal antibody with two antigen-recognition sites: one for CD3, an antigen expressed on mature T cells, and one for HER-2-neu, a tumor-associated antigen that promotes tumor growth. Ertumaxomab attaches to CD3-expressing T cells and HER-2-neu-expressing tumor cells, selectively cross-linking tumor and immunologic cells which results in the recruitment of cytotoxic T cells to the T cell/tumor cell aggregate. C2658 38505 monoclonal antibody CAL A humanized monoclonal antibody directed against parathyroid hormone-related protein (PTH-rP). As a poly-hormone with diverse biological roles, PTH-rP is expressed by normal tissues, acting in local tissue environments in a variety of ways; it is commonly overexpressed by breast, prostate, and other cancers, acting systemically by promoting bone resorption, inhibiting calcium excretion from the kidney, inducing hypercalcemia, and possibly playing a role in the formation of bony metastases. By blocking the effects of PTH-rP on calcium metabolism, monoclonal antibody CAL may inhibit cancer-related hypercalcemia. C2659 38508 tetanus toxoid A solution of formaldehyde-deactivated toxin isolated from the bacterium Clostridium tetani. Tetanus toxoid stimulates the production of antitoxin antibodies. This agent may be used as an adjuvant in cancer vaccines. C2660 38517 R(+)XK469 The R-isomer of a synthetic quinoxaline phenoxypropionic acid derivative with proapoptotic and antiproliferative activities. R(+)XK469 selectively inhibits topoisomerase II-beta, blocks activation of MEK/MAPK signaling kinases, stimulates caspases, and upregulates p53-dependent proteins, including cyclins A and B1, thereby arresting cancer cells in the G2/M phase of the cell cycle. Both R(+) and S(-) isomers of this agent are cytotoxic, although the R-isomer is more potent. C2662 38531 fibrin sealant A plasma-derived fibrin biomatrix preparation consisting of two separate solutions that are combined on application. The sealer protein solution contains clottable human fibrinogen and bovine aprotinin, a fibrinolysis inhibitor; the thrombin solution contains human thrombin and calcium chloride. When the solutions are combined, a clot is formed, reproducing the final stages of the coagulation cascade. C2664 38537 edotecarin A synthetic indolocarbazole with antineoplastic activity. Edotecarin inhibits the enzyme topoisomerase I through stabilization of the DNA-enzyme complex and enhanced single-strand DNA cleavage, resulting in inhibition of DNA replication and decreased tumor cell proliferation. 38542 recombinant fowlpox-B7.1 vaccine A cancer vaccine comprised of a recombinant fowlpox virus vector encoding the stimulatory molecule transgene B7-1. Recombinant fowlpox-B7.1 (rF-B7.1) vaccine may enhance antigen presentation and activate antitumoral cytotoxic T-cells. 38543 recombinant fowlpox-TRICOM vaccine A cancer vaccine comprised of a recombinant fowlpox virus vector encoding TRICOM. TRICOM is comprised of three co-stimulatory molecule transgenes (B7-1, ICAM-1 and LFA-3) that may enhance antigen presentation and activate cytotoxic T-cells. Fowlpox virus is an attractive vector because its genome is easy to manipulate and it is replication incompetent in mammalian cells. 38549 NB1011 A small molecule phosphoramidate derivative of (E)-5-(2-bromovinyl)-2'-deoxyuridine with potential antineoplastic activity. Selectively active against tumor cells expressing high levels of thymidylate synthase (TS), BVdU pronucleotide analogue NB1011 is converted intracellularly by TS to bromovinyldeoxyuridine monophosphate (BVdUMP) which competes with the natural substrate, deoxyuridine monophosphate, for binding to TS. Unlike TS inhibitors, this agent is a reversible substrate for TS catalysis. Thus, TS retains activity and converts BVdUMP into cytotoxic metabolites. As key enzyme in the de novo synthesis of dTMP, TS is an enzyme critical to DNA biosynthesis and is overexpressed in many solid tumors. 38552 Globo-H-GM2-Lewis-y-MUC1-32(aa)-sTn(c)-TF(c)-Tn(c)-KLH conjugate vaccine A heptavalent vaccine consisting of the tumor-associated carbohydrate antigens globohexaosylceramide (globo-H), GM2, Lewis-y, MUC1-32(aa), sTn(c), TF(c), and Tn(c) conjugated with keyhole limpet hemocyanin (KLH), an immunomodulator. This vaccine may induce the production of IgG and IgM antibodies and an antibody-dependent cell-mediated cytotoxicity (ADCC) against tumors expressing these antigens. C28551 38558 imiquimod A synthetic agent with immune response modifying activity. As an immune response modifier (IRM), imiquimod stimulates cytokine production, especially interferon production, and exhibits antitumor activity, particularly against cutaneous cancers. Imiquimod's proapoptotic activity appears to be related to Bcl-2 overexpression in susceptible tumor cells. 38564 lenalidomide A thalidomide analog with potential antineoplastic activity. Lenalidomide inhibits TNF-alpha production, stimulates T cells, reduces serum levels of the cytokines vascular endothelial growth factor (VEGF) and basic fibroblast growth factor (bFGF), and inhibits angiogenesis. This agent also promotes G1 cell cycle arrest and apoptosis of malignant cells. 38567 bupropion hydrochloride The hydrochloride salt of an aminoketone antidepressant. The molecular mechanism of the antidepressant effect of bupropion is unknown. This agent does not inhibit monoamine oxidase and, compared to classical tricyclic antidepressants, is a weak blocker of the neuronal uptake of serotonin and norepinephrine. Buproprion also weakly inhibits the neuronal re-uptake of dopamine. 38568 rofecoxib A synthetic, nonsteroidal derivative of phenyl-furanone with antiinflammatory, antipyretic and analgesic properties and potential antineoplastic properties. Rofecoxib binds to and inhibits the enzyme cyclooxygenase-2 (COX-2), resulting in an inhibition of the conversion of arachidonic acid to prostaglandins. COX-related metabolic pathways may represent key regulators of cell proliferation and neo-angiogenesis. Some epithelial tumor cell types overexpress pro-angiogenic COX-2. 38571 hydroxychloroquine A 4-aminoquinoline with immunosuppressive, antiautophagy, and antimalarial activities. Although the precise mechanism of action is unknown, hydroxychloroquine may suppress immune function by interfering with the processing and presentation of antigens and the production of cytokines. As a lysosomotropic agent, hydroxychloroquine raises intralysosomal pH, impairing autophagic protein degradation; hydroxychloroquine-mediated accumulation of ineffective autophagosomes may result in cell death in tumor cells reliant on autophagy for survival. In addition, this agent is highly active against the erythrocytic forms of P. vivax and malariae and most strains of P. falciparum but not the gametocytes of P. falciparum. 38589 monoclonal antibody Mik-beta-1 A murine monoclonal antibody directed against the beta subunit of the interleukin-2 receptor (IL-2R), expressed on resting T-lymphocytes, natural killer (NK) cells, and some leukemic cell types. Monoclonal antibody Mik-beta-1 prevents the binding of IL-2 to IL-2R beta, thereby inhibiting the IL-2-mediated proliferation and activation of T-cells. C2669 38596 S-3304 An orally-agent agent with potential antineoplastic activity. S-3304 inhibits matrix metalloproteinases (MMPs), thereby inducing extracellular matrix degradation, and inhibiting angiogenesis, tumor growth and invasion, and metastasis. 38604 epothilone D A natural polyketide compound isolated from the myxobacterium Sorangium cellulosum. Also known as desoxyepothilone B, epothilone D binds to tubulin and inhibits the disassembly of microtubules, resulting in the inhibition of mitosis, cellular proliferation, and cell motility. 38609 recombinant adenovirus-hIFN-beta A recombinant replication-defective adenovirus which encodes the gene for the cytokine human interferon-beta (IFN-beta). Once inserted into and replicating in host tumor cells, recombinant adenovirus-hIFN-beta expresses human IFN-beta, which may stimulate an antiproliferative natural killer (NK) cell response against tumor cells and induce caspase-mediated tumor cell apoptosis. 38611 clopidogrel bisulfate A thienopyridine with antiplatelet activity. Clopidogrel bisulfate irreversibly alters the platelet receptor for adenosine diphosphate (ADP), thereby blocking the binding of ADP to its receptor, inhibiting ADP-mediated activation of the glycoprotein complex GPIIb/IIIa, and inhibiting fibrinogen binding to platelets and platelet adhesion and aggregation. C2673 38629 recombinant fowlpox-prostate apecific antigen vaccine A cancer vaccine consisting of a recombinant fowlpox virus encoding human prostate-specific antigen (PSA). Administration of this agent may stimulate a cytotoxic T cell response against PSA-expressing tumor cells. Fowlpox virus is an attractive vector because its genome is easy to manipulate and it is replication incompetent in mammalian cells. 38634 G207 A neuroattenuated, replication-competent, recombinant herpes simplex virus-1 (HSV-1) with potential oncolytic activity. Upon intracerebral administration, oncolytic HSV-1 G207 preferentially replicates within glioma cells, which may elicit tumor-specific systemic immune and cytotoxic T\nlymphocyte (CTL) responses in addition to direct cytopathic effects. Derived from wild-type HSV-1 strain F, this agent has been neuroattenuated by deletions\nin both copies of the gamma34.5 gene, the major determinant of HSV\nneurovirulence. In addition, the HSV-1 gene UL39, encoding the viral ribonucleotide reductase large subunit infected cell protein 6 (ICP6), has been inactivated through the insertion of the Escherichia coli lacZ gene. By inactivating UL39, viral ribonucleotide reductase activity is disrupted, resulting in the inhibition of nucleotide metabolism\nand viral DNA synthesis in nondividing cells but not in\ndividing cells. C2676 38642 beta-glucan A polysaccharide isolated from the cell walls of bacteria, plants, and fungi with immunostimulant and antineoplastic activities. In a solubilized form, beta-glucan binds to a lectin site within complement receptor 3 (CR3) on leukocytes, priming the receptor to trigger cytotoxic degranulation of leukocytes when leukocyte CR3 binds to complement 3 (iC3b)-coated tumors. Thus, the attachment of beta-glucan to CR3 of circulating leukocytes simulates leukocytes to kill iC3b-coated tumor cells in the same way as they kill iC3b-coated yeast. C2678 38646 ABT-751 An orally bioavailable antimitotic sulfonamide. ABT-751 binds to the colchicine-binding site on beta-tubulin and inhibits the polymerization of microtubules, thereby preventing tumor cell replication. This agent also disrupts tumor neovascularization, reducing tumor blood flow and so inducing a cytotoxic effect. 38647 NA17-A antigen A specific melanoma antigen protein derived from a patient (NA17) with cutaneous melanoma metastases. When administered in a vaccine formulation, NA17-A antigen may stimulate a cytotoxic T lymphocyte (CTL) response against tumors that express this antigen, which may result in a reduction in tumor size. The NA17-A antigen is part of the enzyme N-acetyl glucosaminyl-transferase V (GnT-V). Approximately half of melanomas have been found to express significant levels of this atypical protein, which is not expressed by normal tissues. 38649 MAGE-10.A2 A synthetic nonapeptide derived from a melanoma-associated antigen. Vaccination with MAGE-10.A2 may stimulate a host cytotoxic T-cell response against tumor cells that express the melanoma-associated antigen, resulting in tumor cell lysis. C2681 38652 aflibercept A protein comprised of segments of the extracellular domains of human\nvascular endothelial growth factor receptors 1 (VEGFR1) and 2 (VEGFR2)\nfused to the constant region (Fc) of human IgG1 with potential\nantiangiogenic activity. Afilbercept, functioning as a soluble decoy\nreceptor, binds to pro-angiogenic vascular endothelial growth factors\n(VEGFs), thereby preventing VEGFs from binding to their cell receptors.\nDisruption of the binding of VEGFs to their cell receptors may result in\nthe inhibition of tumor angiogenesis, metastasis, and ultimately tumor\nregression. 38659 recombinant vaccinia-TRICOM vaccine A vaccine consisting of recombinant vaccinia virus encoding a triad of costimulatory molecules (B7-1, ICAM-1, and LFA-3; also called TRICOM). Vaccination with recombinant vaccinia-TRICOM vaccine stimulates the host immune system to mount a non-specific T-cell response. With the addition of a tumor-associated antigen peptide, this vaccine may enhance a tumor-specific immune response. 38660 agatolimod sodium The tricosasodium salt of a synthetic 24-mer oligonucleotide containing 3 CpG motifs with potential antineoplastic and immunostimulatory activity. Agatolimod selectively targets Toll-like receptor 9 (TLR9), thereby activating dendritic and B cells and stimulating cytotoxic T cell and antibody responses against tumor cells bearing tumor antigens. C28580 38672 yttrium Y 90 glass microspheres An injectable formulation of yttrium Y 90 consisting of glass microspheres containing the radioisotope yttrium Y 90. When injected into the tumor vascular bed, yttrium Y 90 glass microspheres occlude tumor blood vessels and deliver a cytotoxic dose of beta radiation to the tumor site, thereby reducing the tumor burden. C38679 38676 darbepoetin alfa A recombinant analog of the endogenous cytokine erythropoietin, an erythropoiesis-stimulating protein. Due to the addition of two carbohydrate chains, darbepoetin alfa exhibits a three-fold greater half-life than does erythropoietin. Similar to erythropoietin, darbopoietin alfa binds to and activates epoetin receptors, thereby inducing the differentiation and maturation of erythrocyte progenitors, stimulating endothelial cell proliferation, and stimulating B-cell proliferation and immunoglobulin production. 38680 recombinant fowlpox GM-CSF vaccine adjuvant A cancer vaccine adjuvant consisting of a recombinant fowlpox virus encoding human granulocyte-macrophage colony-stimulating factor (GM-CSF). GM-CSF binds to specific cell surface receptors on various immuno-hematopoietic cell types, enhancing their proliferation and differentiation and stimulating macrophage and dendritic cell functions in antigen presentation and antitumor cell-mediated immunity. Administration of recombinant fowlpox GM-CSF vaccine adjuvant may induce an immune response against tumor cells. Fowlpox virus is an attractive vector because its genome is easy to manipulate and it is replication incompetent in mammalian cells. 38685 visilizumab A humanized, non-Fc receptor (FcR)-binding IgG2 monoclonal antibody (MoAb) directed against CD3 with potential immunosuppressive activity. Visilizumab binds to invariant CD3 epsilon, one of the non-covalently-associated subunits of T-cell receptors (TCRs) on activated T-cells. Upon binding to the TCR/CD3 complex, visilizumab induces apoptosis, which may result in the selective clonal deletion of activated pathogenic T-cells. This MoAb is engineered with a substitution at amino acid residues 234 and 237 (Val3Ala) within the IgG2 Fc arm, rendering it unable to bind to type II FcRs; accordingly, this agent is less likely to activate type II FcR-expressing resting T-cells. C2687 38690 paclitaxel albumin-stabilized nanoparticle formulation A Cremophor ELP-free, albumin-stabilized nanoparticle formulation of the natural taxane paclitaxel with antineoplastic activity. Paclitaxel binds to and stabilizes microtubules, preventing their depolymerization and so inhibiting cellular motility, mitosis, and replication. This formulation solubilizes paclitaxel without the use of Cremophor ELP and permits the administration of larger doses of this agent, which would be toxic in a Cremophor ELP-containing formulation due to Cremophor ELP's toxicity profile. Cremophor ELP is a nonionic solubilizer made by reacting castor oil with ethylene oxide in a molar ratio of 1:35, followed by a purification step. 38698 infliximab A recombinant chimeric, mouse-human monoclonal antibody directed against tumor necrosis factor alpha (TNF-alpha), a protein involved in inflammation, cell survival, and apoptosis. Infliximab may be pro- apoptotic or anti-apoptotic, depending on cell type. 38702 epothilone B A compound isolated from the myxobacterium Sorangium cellulosum. Similar to paclitaxel, epothilone B induces microtubule polymerization and stabilizes microtubules against depolymerization conditions. In addition to promoting tubulin polymerization and stabilization of microtubules, this agent is cytotoxic for cells overexpressing P-glycoprotein, a characteristic that distinguishes it from the taxanes. Epothilone B may cause complete cell-cycle arrest. 38705 BAY 56-3722 A water-soluble camptothecin derivative conjugated to a carbohydrate moiety exhibiting antineoplastic activity. BAY 56-3722 stabilizes the topoisomerase I-DNA covalent complex and forms an enzyme-drug-DNA ternary complex. As a consequence of the formation of this complex, both the initial cleavage reaction and religation steps are inhibited and subsequent collision of the replication fork with the cleaved strand of DNA results in inhibition of DNA replication, double strand DNA breakage and triggering of apoptosis. The peptide carbohydrate moiety of this agent stabilizes the lactone form of camptothecin in blood. 38706 IH636 grape seed proanthocyanidin extract An oligomeric proanthocyanidin extracted from grape seeds. IH636 grape seed proanthocyanidin extract exhibits dose-dependent free-radical scavenging and antioxidant properties. C2689 38711 ginger extract An extract of the rhizome of the perennial plant Zingiber officinale with potential antineoplastic activity. Ginger extract contains a number of different phenolic compounds, some of which have displayed antineoplastic, anti-inflammatory, and antioxidant activities. This agent also exhibits antiemetic properties. C2691 38721 zinc sulfate A salt of the essential trace metal zinc. Zinc is involved in tissue repair and is an important constituent of some proteins, including those involved in taste and smell. Zinc sulfate supplementation may prevent radiation-induced aguesia. 38723 magnesium sulfate A small colorless crystal used as an anticonvulsant, a cathartic, and an electrolyte replenisher in the treatment of pre-eclampsia and eclampsia. It causes direct inhibition of action potentials in myometrial muscle cells. Excitation and contraction are uncoupled, which decreases the frequency and force of contractions. (From AMA Drug Evaluations Annual, 1992, p1083) (MSH2002_06_01). 38724 molybdenum An element with atomic symbol Mo, atomic number 42, and atomic weight 95.94. 38725 selenium A nonmetallic chemical element found in trace amounts in human body. Selenium primarily occurs in vivo as selenocompounds, mostly selenoproteins such as glutathione peroxidase and thioredoxin reductase (enzymes responsible for detoxification). Alone or in combination with Vitamin E, selenocompounds act as antioxidants. These agents scavenge free radicals; prevent blood clots by inhibiting platelet aggregation; strengthen the immune system; and have been shown, in some instances, to inhibit chromosomal damage and mutations. Exhibiting chemopreventive activity, selenocompounds also inhibit the induction of protein kinase C. 38775 pirarubicin An analogue of the anthracycline antineoplastic antibiotic doxorubicin. Pirarubicin intercalates into DNA and interacts with topoisomerase II, thereby inhibiting DNA replication and repair and RNA and protein synthesis. This agent is less cardiotoxic than doxorubicin and exhibits activity against some doxorubicin-resistant cell lines. 38852 ipomeanol A natural toxic furan isolated from a fungus-infected sweet potato (Ipomoea batatas) with potential antineoplastic activity. Ipomeanol is activated by mixed function oxidases in vivo to its epoxide form, an alkylating agent that covalently binds cell macromolecules. This agent causes cell death by a p53-independent mechanism. 38853 nimustine A nitrosourea with antineoplastic activity. Nimustine alkylates and crosslinks DNA, thereby causing DNA fragmentation, inhibition of protein synthesis, and cell death. C693 38860 doxorubicin hydrochloride The hydrochloride salt of doxorubicin, an anthracycline antibiotic with antineoplastic activity. Doxorubicin, isolated from the bacterium Streptomyces peucetius var. caesius, is the hydroxylated congener of daunorubicin. Doxorubicin intercalates between base pairs in the DNA helix, thereby preventing DNA replication and ultimately inhibiting protein synthesis. Additionally, doxorubicin inhibits topoisomerase II which results in an increased and stabilized cleavable enzyme-DNA linked complex during DNA replication and subsequently prevents the ligation of the nucleotide strand after double-strand breakage. Doxorubicin also forms oxygen free radicals resulting in cytotoxicity secondary to lipid peroxidation of cell membrane lipids; the formation of oxygen free radicals also contributes to the toxicity of the anthracycline antibiotics, namely the cardiac and cutaneous vascular effects. 38865 fotemustine A chloroethylating nitrosourea with antineoplastic activity. Fotemustine alkylates guanine by forming chloroethyl adducts at the 6 position of guanine, resulting in N1-guanine and N3-cytosine cross linkages, inhibition of DNA synthesis, cell cycle arrest, and finally apoptosis. This agent is lipophilic and crosses the blood-brain barrier. 38866 octreotide acetate The acetate salt of a synthetic long-acting cyclic octapeptide with pharmacologic properties mimicking those of the natural hormone somatostatin. Octreotide is a more potent inhibitor of growth hormone, glucagon, and insulin than somatostatin. Similar to somatostatin, this agent also suppresses the luteinizing hormone response to gonadotropin-releasing hormone, decreases splanchnic blood flow, and inhibits the release of serotonin, gastrin, vasoactive intestinal peptide (VIP), secretin, motilin, pancreatic polypeptide, and thyroid stimulating hormone. 38921 EPOCH regimen A chemotherapy regimen consisting of etoposide, prednisone, vincristine (Oncovin) and doxorubicin hydrochloride (hydroxydaunorubicin hycrochloride), which may be used in combination with rituximab (R-EPOCH) for the treatment of various aggressive B cell and T cell non-Hodgkin lymphomas. C63779 38943 asulacrine isethionate The isethionate salt of an amsacrine analogue with antineoplastic properties. Asulacrine inhibits the enzyme topoisomerase ll, thereby blocking DNA replication and RNA and protein synthesis. 38970 recombinant interleukin-3 A recombinant form of interleukin-3, a cytokine produced by activated T-cells and mast cells involved in intercellular communication, hematopoiesis, and inflammation. IL-3 binds and activates specific receptors on hematopoietic cells and in the nervous system, triggering expression of specific genes via the Ras signaling pathway and through Jak2 activation. This agent stimulates the proliferation of pluripotent hematopoietic progenitor cells. C588 39015 cytarabine An antimetabolite analogue of cytidine with a modified sugar moiety (arabinose instead of ribose). Cytarabine is converted to the triphosphate form within the cell and then competes with cytidine for incorporation into DNA. Because the arabinose sugar sterically hinders the rotation of the molecule within DNA, DNA replication ceases, specifically during the S phase of the cell cycle. This agent also inhibits DNA polymerase, resulting in a decrease in DNA replication and repair. 39022 quinidine An alkaloid extracted from the bark of the Cinchona tree with class 1A antiarrhythmic and antimalarial effects. Quinidine stabilizes the neuronal membrane by binding to and inhibiting voltage-gated sodium channels, thereby inhibiting the sodium influx required for the initiation and conduction of impulses resulting in an increase of the threshold for excitation and decreased depolarization during phase 0 of the action potential. In addition, the effective refractory period (ERP), action potential duration (APD), and ERP/APD ratios are increased, resulting in decreased conduction velocity of nerve impulses. Quinidine exerts its antimalarial activity by acting primarily as an intra-erythrocytic schizonticide through association with the heme polymer (hemazoin) in the acidic food vacuole of the parasite thereby preventing further polymerization by heme polymerase enzyme. This results in accumulation of toxic heme and death of the parasite. 39057 staphylococcus aureus protein A A protein that resides in the microbial wall of staphylococcus aureus and interferes with opsonization by binding to the Fc portion of immunoglobulin. The protein has a deleterious effect on the epithelial cells that line the respiratory tract, and plays a role in the induction of pneumonia. Protein A also initiates polymorphonuclear cell migration into airway passages via TNFR1 activation. 39058 levamisole hydrochloride The orally bioavailable hydrochloride salt of the synthetic imidazothiazole derivative levamisole with anthelminthic and immunostimulating activities. In immunosuppressed states, levamisole may restore immune function by: 1) stimulating antibody formation, 2) stimulating T-cell activation and proliferation, 3) potentiatiating monocyte and macrophage phagocytosis and chemotaxis and 4) increasing neutrophil mobility, adherence, and chemotaxis. C610 39059 therapeutic progesterone A synthetic form of the endogenous hormone progesterone. Progesterone binds to the progesterone receptor, resulting in dissociation of heat shock proteins, receptor phosphorylation, and transcription activation through direct or indirect interaction with transcription factors. This agent exerts inhibitory effects on estrogens by decreasing the number of estrogen receptors and increasing its metabolism to inactive metabolites. Progesterone induces secretory changes in the endometrium, decreases uterine contractility during pregnancy, and maintains pregnancy. 39060 CMF regimen A chemotherapy regimen consisting of cyclophosphamide, methotrexate, and fluorouracil, which may be used in the adjuvant setting for the treatment of nonmetastatic breast cancer or alone for the treatment of metastatic breast cancer. C63418 39061 atvogen A synthetic derivative of inosinic acid with antiretroviral and immunomodulatory activities. Atvogen acts through a number of pathways to stimulate the antiviral activity of the immune system. This agent stimulates interferon production; activates the oligoadenylate synthase-RNase L pathway; stimulates natural killer cell activity; and acts as a non-mitogenic stimulator of the immune system. Atvogen also inhibits replication of the human immunodeficiency virus (HIV) in vitro. C1001 39062 recombinant soluble human CD4 protein A recombinant human soluble CD4 with antiviral activity. Recombinant human soluble CD4 has the amino terminus but not the T-cell binding domain of the endogenous CD4 antigen. This soluble CD4 protein competitively binds to envelope glycoprotein (gp120) of human immunodeficiency virus (HIV) resulting in inhibition of interaction between gp120 and the endogenous CD4 antigen, thereby blocking viral recognition of CD4 and subsequent entry of HIV into CD4 bearing cells. C2342 39106 itraconazole A synthetic triazole agent with antimycotic properties. Formulated for both topical and systemic use, itraconazole preferentially inhibits fugal cytochrome P450 enzymes, resulting in a decrease in fungal ergosterol synthesis. Because of its low toxicity profile, this agent can be used for long-term maintenance treatment of chronic fungal infections. 39116 clotrimazole A synthetic, imidazole derivate with broad-spectrum, antifungal activity. Clotrimazole inhibits biosynthesis of sterols, particularly ergosterol, an essential component of the fungal cell membrane, thereby damaging and affecting the permeability of the cell membrane. This results in leakage and loss of essential intracellular compounds, and eventually causes cell lysis. 39117 levothyroxine sodium The sodium salt of levothyroxine, a synthetic levoisomer of thyroxine (T4) that is similar to the endogenous hormone produced by the thyroid gland. In peripheral tissues, levothyroxine is deiodinated by 5'-deiodinase to form triiodothyronine (T3). T3 enters the cell and binds to nuclear thyroid hormone receptors; the activated hormone-receptor complex in turn triggers gene expression and produces proteins required in the regulation of cellular respiration; thermogenesis; cellular growth and differentiation; and the metabolism of proteins, carbohydrates and lipids. T3 also exhibits cardiostimulatory effects. 39123 buthionine sulfoximine A synthetic amino acid. Buthionine sulfoximine irreversibly inhibits gamma-glutamylcysteine synthetase, thereby depleting cells of glutathione, a metabolite that plays a critical role in protecting cells against oxidative stress, and resulting in free radical-induced apoptosis. Elevated glutathione levels are associated with tumor cell resistance to alkylating agents and platinum compounds. By depleting cells of glutathione, this agent may enhance the in vitro and in vivo cytotoxicities of various chemotherapeutic agents in drug-resistant tumors. Buthionine sulfoximine may also exhibit antiangiogenesis activity. 39129 acetaminophen A p-aminophenol derivative with analgesic and antipyretic activities. Although the exact mechanism through which acetaminophen exert its effects has yet to be fully determined, acetaminophen may inhibit the nitric oxide (NO) pathway mediated by a variety of neurotransmitter receptors including N-methyl-D-aspartate (NMDA) and substance P, resulting in elevation of the pain threshold. The antipyretic activity may result from inhibition of prostaglandin synthesis and release in the central nervous system (CNS) and prostaglandin-mediated effects on the heat-regulating center in the anterior hypothalamus. C198 39130 acetylcysteine A synthetic N-acetyl derivative of the endogenous amino acid L-cysteine, a precursor of the antioxidant enzyme glutathione. Acetylcysteine regenerates liver stores of glutathione. This agent also reduces disulfide bonds in mucoproteins, resulting in liquification of mucus. Some evidence suggests that acetylcysteine may exert an anti-apoptotic effect due to its antioxidant activity, possibly preventing cancer cell development or growth. In addition, acetylcysteine has inhibited viral stimulation by reactive oxygen intermediates, thereby producing antiviral activity in HIV patients. 39131 aclarubicin An oligosaccharide anthracycline antineoplastic antibiotic isolated from the bacterium Streptomyces galilaeus. Aclarubicin intercalates into DNA and interacts with topoisomerases I and II, thereby inhibiting DNA replication and repair and RNA and protein synthesis. Aclarubicin is antagonistic to other agents that inhibit topoisomerase II, such as etoposide, teniposide and amsacrine. This agent is less cardiotoxic than doxorubicin and daunorubicin. 39132 acivicin A modified amino acid and structural analog of glutamine. Acivicin inhibits glutamine amidotransferases in the purine and pyrimidine biosynthetic pathways, thereby inhibiting tumor growth in cell lines dependent on glutamine metabolism. 39134 acyclovir A synthetic analog of the purine nucleoside, guanosine, with potent antiviral activity against herpes simplex viruses type 1 and 2, varicella-zoster virus and other viruses. After conversion in vivo to the active metabolite acyclovir triphosphate, acyclovir competitively inhibits viral DNA polymerase, incorporates into and terminates the growing viral DNA chain, and inactivates viral DNA polymerase. The greater antiviral activity of acyclovir against HSV compared to VZV is due to its more efficient phosphorylation by the thymidine kinase of HSV. 39135 valrubicin A semisynthetic derivative of the antineoplastic anthracycline antibiotic doxorubicin. With a mechanism of action that appears to differ from doxorubicin, valrubicin is converted intracytoplasmically into N-trifluoroacetyladriamycin, which interacts with topoisomerase II, stabilizing the complex between the enzyme and DNA; consequently, DNA replication and repair and RNA and protein synthesis are inhibited and the cell cycle is arrested in the G2 phase. In addition, this agent accumulates in the cell cytoplasm where it inhibits protein kinase C (PKC). Valrubicin is less cardiotoxic than doxorubicin when administered systemically; applied topically, this agent shows excellent tissue penetration. Structurally, the trifluoro-acetyl moiety on the amino group of the glycoside and the valerate moiety appear to result in a lipophilicity that is greater than of doxorubicin, resulting in increased intracytoplasmic concentrations. C1340 39136 bisantrene hydrochloride The hydrochloride salt of an anthracenyl bishydrazone with antineoplastic activity. Bisantrene intercalates with and disrupts the configuration of DNA, resulting in DNA single-strand breaks, DNA-protein crosslinking, and inhibition of DNA replication. This agent is similar to doxorubicin in activity, but unlike doxorubicin, does not exhibit cardiotoxicity. 39138 L-alanosine An amino acid analogue and antibiotic derived from the bacterium Streptomyces alanosinicus with antimetabolite and potential antineoplastic activities. L-alanosine inhibits adenylosuccinate synthetase, which converts inosine monophospate (IMP) into adenylosuccinate, an intermediate in purine metabolism. L-alanosine-induced disruption of de novo purine biosynthesis is potentiated by methylthioadenosine phosphorylase (MTAP) deficiency. The clinical use of this agent may be limited by its toxicity profile. MTAP is a key enzyme in the adenine and methionine salvage pathways. 39139 bleomycin sulfate A mixture of the sulfate salts of basic glycopeptide antineoplastic antibiotics isolated from Streptomyces verticillus. Bleomycin sulfate forms complexes with iron that reduce molecular oxygen to superoxide and hydroxyl radicals which cause single- and double-stranded breaks in DNA; these reactive oxygen species also induce lipid peroxidation, carbohydrate oxidation, and alterations in prostaglandin synthesis and degradation. C312 39141 aminopterin A synthetic derivative of pterins with antineoplastic and immunosuppressive properties. As a folate analogue, aminopterin competes for the folate binding site of the enzyme dihydrofolate reductase, thereby blocking tetrahydrofolate synthesis, and resulting in depletion of nucleotide precursors and inhibition of DNA, RNA and protein synthesis. 39142 amsacrine An aminoacridine derivative with potential antineoplastic activity. Although its mechanism of action is incompletely defined, amsacrine may intercalate into DNA and inhibit topoisomerase II, resulting in DNA double-strand breaks, arrest of the S/G2 phase of the cell cycle, and cell death. This agent's cytotoxicity is maximal during the S phase of the cell cycle when topoisomerase levels are greatest. In addition, amsacrine may induce transcription of tumor promoter p53 protein and block p53 ubiquitination and proteasomal degradation, resulting in p53-dependent tumor cell apoptosis. 39143 amphotericin B deoxycholate The deoxycholate salt of amphotericin B, a polyene antifungal antibiotic produced by Streptomyces nodosus, with antifungal activity. Amphotericin B binds to ergosterol, an essential component of the fungal cell membrane, resulting in depolarization of the membrane; alterations in cell membrane permeability and leakage of important intracellular components; and cell rupture. This agent may also induce oxidative damage in fungal cells and has been reported to stimulate host immune cells. C62201 39144 aminothiadiazole A synthetic derivative of nicotinamide adenine dinucleotide (NAD). Aminothiadiazole competitively inhibits inosine 5-monophosphate dehydrogenase, thereby disrupting the regulation of cell proliferation and differentiation in a number of cells. This agent is also a selective human adenosine A3 receptor antagonist. 39146 aniline mustard An alkylating mustard with antineoplastic activity. Aniline mustard forms covalent linkages with nucleophilic centers, resulting in depurination, base miscoding and strand scission, and crosslinking of DNA strands, all of which contribute to its cytotoxicity. 39148 anguidine A trichothecene mycotoxin and potent teratogen. Anguidine inhibits initiation of protein synthesis, resulting in the death of rapidly proliferating cells. Anguidine also has been shown to both potentiate and protect against the cytotoxic effects of other drugs. 39149 pamidronate disodium The disodium salt of the synthetic bisphosphonate pamidronate. Although its mechanism of action is not completely understood, pamidronate appears to adsorb to calcium phosphate crystals in bone, blocking their dissolution by inhibiting osteoclast-mediated bone resorption. This agent does not inhibit bone mineralization and formation. 39150 vidarabine A nucleoside antibiotic isolated from the bacterium Streptomyces antibioticus with antineoplastic activity. Vidarabine inhibits DNA polymerase, resulting in the inhibition of DNA replication in tumor cells. 39151 asaley An L-leucine derivative of melphalan with antineoplastic activity. Asaley alkylates and crosslinks DNA, resulting in disruption of DNA synthesis. 39152 acetylsalicylic acid An orally administered non-steroidal antiinflammatory agent. Acetylsalicylic acid binds to and acetylates serine residues in cyclooxygenases, resulting in decreased synthesis of prostaglandin, platelet aggregation, and inflammation. This agent exhibits analgesic, antipyretic, and anticoagulant properties. 39153 azacitidine A pyrimidine nucleoside analogue of cytidine with antineoplastic activity. Azacitidine is incorporated into DNA, where it reversibly inhibits DNA methyltransferase, thereby blocking DNA methylation. Hypomethylation of DNA by azacitidine may activate tumor suppressor genes silenced by hypermethylation, resulting in an antitumor effect. This agent is also incorporated into RNA, thereby disrupting normal RNA function and impairing tRNA cytosine-5-methyltransferase activity. 39154 azapicyl A hydrazine compound that has been investigated for antineoplastic activity. 39156 azaserine A naturally occurring serine derivative diazo compound with antineoplastic properties, Azaserine functions as a purine antagonist and glutamine analogue (glutamine amidotransferase inhibitor) that competitively inhibits pathways in which glutamine is metabolized. An antibiotic and antitumor agent, Azaserine is used in clinical studies as a potential antineoplastic agent. 39157 azathioprine sodium The sodium salt form of azathioprine, a pro-drug of purine analogue with immunosuppressive activity. Azathioprine is converted in vivo to its active metabolite 6-mercaptopurine (6-MP), which substitutes for the normal nucleoside and mistakenly gets incorporated into DNA sequences. This leads to inhibition of DNA, RNA, and protein synthesis. As a result, cell proliferation may be inhibited, particularly in lymphocytes and leukocytes. 39158 6-azauridine A synthetic triazine analogue of uridine with antimetabolite activity. 6-azauridine inhibits de novo pyrimidine synthesis and DNA synthesis and is converted intracellularly into mono, di-, and triphosphate derivatives, which incorporate into RNA and inhibit protein synthesis. C291 39161 diaziquone A synthetic bifunctional quinone derivative with potential antineoplastic activity. Diaziquone alkylates and cross-links DNA during all phases of the cell cycle, resulting in disruption of DNA function, cell cycle arrest, and apoptosis. This agent can also form free radicals, thereby initiating DNA damage via DNA strand breaks. Due to its lipophilicity, diaziquone readily crosses the blood brain barrier. 39162 triazinate A synthetic dihydrotriazine derivative with antineoplastic properties. As an antifolate agent related to methotrexate (MTX), triazinate inhibits the enzyme dihydrofolate reductase (DHFR), resulting in decreased tetrahydrofolate production and interference with thymidylate synthesis. Unlike MTX, this agent is not converted to polyglutamate forms. Triazinate also inhibits the transport of folates and may be selectively toxic to MTX-resistant tumor cells. 39163 diphenhydramine hydrochloride The hydrochloride salt form of diphenhydramine, an ethanolamine and first-generation histamine antagonist with anti-allergic activity. Diphenhydramine hydrochloride competitively blocks H1receptors, thereby preventing the actions of histamine on bronchial smooth muscle, capillaries, and gastrointestinal (GI) smooth muscle. This prevents histamine-induced bronchoconstriction, vasodilation, increased capillary permeability, and GI smooth muscle spasms. 39165 bromocriptine mesylate The mesylate salt of bromocriptine, a semisynthetic ergot alkaloid with dopaminergic, antidyskinetic, and antiprolactinemic activities. Bromocriptine selectively binds to and activates postsynaptic dopamine D2 receptors in the corpus striatum of the central nervous system (CNS). Activation of these D2 receptors activate inhibitory G-proteins, which inhibit adenylyl cyclase, preventing signal transduction mediated via cAMP and resulting in the inhibition of neurotransmission and an antidyskinetic effect. Ths agent also stimulates dopamine D2 receptors in the anterior pituitary gland, which results in the inhibition of prolactin secretion and lactation and may inhibit the proliferation of prolactin-dependent breast cancer cells. C317 39166 povidone-iodine An iodophor solution containing a water-soluble complex of iodine and polyvinylpyrrolidone (PVP) with broad microbicidal activity. Free iodine, slowly liberated from the polyvinylpyrrolidone iodine (PVPI) complex in solution, kills eukaryotic or prokaryotic cells through iodination of lipids and oxidation of cytoplasmic and membrane compounds. This agent exhibits a broad range of microbicidal activity against bacteria, fungi, protozoa, and viruses. Slow release of iodine from the PVPI complex in solution minimizes iodine toxicity towards mammalian cells. 39168 bromodeoxyuridine A halogenated thymidine analogue with potential antineoplastic and radiosensitizing activities. Bromodeoxyuridine competes with thymidine for incorporation into DNA, resulting in DNA mutation and the inhibition of cell proliferation. As a radiosensitizer, this agent is associated with the inhibition of repair of radiation-induced DNA double-strand breaks (DSBs). C318 39169 bruceantin A triterpene quassinoid antineoplastic antibiotic isolated from the plant Brucea antidysenterica. Bruceantin inhibits the peptidyl transferase elongation reaction, resulting in decreased protein and DNA synthesis. Bruceantin also has antiamoebic and antimalarial activity. 39170 buserelin A synthetic analog of gonadotropin-releasing hormone (GnRH). Buserelin binds to and activates pituitary gonadotropin releasing hormone (GnRH) receptors. Prolonged administration of buserelin results in sustained inhibition of gonadotropin production, suppression of testicular and ovarian steroidogenesis, and reduced levels of circulating gonadotropin and gonadal steroids. Buserelin is more potent that GnRH. 39172 calcium gluconate The gluconate salt of calcium. An element or mineral necessary for normal nerve, muscle, and cardiac function, calcium as the gluconate salt helps to maintain calcium balance and prevent bone loss when taken orally. This agent may also be chemopreventive for colon and other cancers. 39175 carubicin An anthracycline antineoplastic antibiotic isolated from the bacterium Actinomadura carminata. Carubicin intercalates into DNA and interacts with topoisomerase II, thereby inhibiting DNA replication and repair and RNA and protein synthesis. 39176 carboplatin A second-generation platinum compound with a broad spectrum of antineoplastic properties. Carboplatin contains a platinum atom complexed with two ammonia groups and a cyclobutane-dicarboxyl residue. This agent is activated intracellularly to form reactive platinum complexes that bind to nucleophilic groups such as GC-rich sites in DNA, thereby inducing intrastrand and interstrand DNA cross-links, as well as DNA-protein cross-links. These carboplatin-induced DNA and protein effects result in apoptosis and cell growth inhibition. This agent possesses tumoricidal activity similar to that of its parent compound, cisplatin, but is more stable and less toxic. 39177 cefotaxime A third generation semisynthetic cephalosporin antibiotic with bactericidal activity. Cefotaxime inhibits mucopeptide synthesis by binding to and inactivating penicillin binding proteins thereby interfering with the final transpeptidation step required for cross-linking of peptidoglycan units which are a component of bacterial cell walls. This results in a reduction of cell wall stability and causes cell lysis. 39179 ceftazidime sodium The sodium salt of ceftazidime, a third-generation cephalosporin antibiotic with bactericidal activity. Ceftazidime binds to and inactivates penicillin-binding proteins (PBPs), enzymes located on the inner membrane of the bacterial cell wall, resulting in the weakening of the bacterial cell wall and cell lysis. Compared to the second and first generation cephalosporins, ceftazidime is more active against gram-negative bacteria and less active against gram-positive bacteria. Ceftazidine also crosses the blood-brain barrier and reaches therapeutic concentrations in the central nervous system (CNS). PBPs participate in the terminal stages of assembling the bacterial cell wall, and in reshaping the cell wall during cell division. Inactivation of PBPs interferes with the cross-linkage of peptidoglycan chains necessary for bacterial cell wall strength and rigidity. C355 39182 chlorozotocin A glucose-linked chloroethylnitrosourea with potential antineoplastic activity. Chlorozotocin alkylates DNA and proteins, induces the formation of interstrand DNA and DNA-protein crosslinks, and causes DNA strand breakage, thereby damaging DNA and resulting in cell death. This agent has been shown to exhibit antitumor and immunomodulatory effects in cell lines and animal models. Chlorozotocin is a mutagen and is less myelotoxic than other nitrosoureas. 39183 iproplatin A synthetic second-generation platinum-containing compound related to cisplatin. Iproplatin binds to and forms DNA crosslinks and platinum-DNA adducts, resulting in DNA replication failure and cell death. Although less prone to glutathione inactivation compared to cisplatin, resistance to this agent has been observed in vitro due to repair of platination damage by tumor cells. 39184 chromomycin A3 A glycosidic antineoplastic antibiotic isolated from the bacterium Streptomyces griseus. Chromomycin A3 reversibly binds to guanine-cytosine (G-C) base pairs in the minor groove of DNA, thereby inhibiting RNA synthesis. This agent is used as a fluorescent chromosome dye. 39185 cimetidine A histamine H(2)-receptor antagonist. Enhancing anti-tumor cell-mediated responses, cimetidine blocks histamine's ability to stimulate suppressor T lymphocyte activity and to inhibit natural killer (NK) cell activity and interleukin-2 production. Cimetidine also may inhibit tumor growth by suppressing histamine's growth-factor activity and blocking histamine-induced stimulation of vascular endothelial growth factor (VEGF), a pro-angiogenic growth factor. 39187 coenzyme Q10 A naturally occurring benzoquinone important in electron transport in mitochondrial membranes. Coenzyme-Q functions as an endogenous antioxidant; deficiencies of this enzyme have been observed in patients with many different types of cancer and limited studies have suggested that coenzyme-Q may induce tumor regression in patients with breast cancer. This agent may have immunostimulatory effects. 39188 colchicine An alkaloid isolated from Colchicum autumnale with anti-gout and anti-inflammatory activities. The exact mechanism of action by which colchicine exerts its effect has not been completely established. Colchicine binds to tubulin, thereby interfering with the polymerization of tubulin, interrupting microtubule dynamics, and disrupting mitosis. This leads to an inhibition of migration of leukocytes and other inflammatory cells, thereby reducing the inflammatory response to deposited urate crystals. Colchicine may also interrupt the cycle of monosodium urate crystal deposition in joint tissues, thereby also preventing the resultant inflammatory response. Overall, colchicine decreases leukocyte chemotaxis/migration and phagocytosis to inflamed areas, and inhibits the formation and release of a chemotactic glycoprotein that is produced during phagocytosis of urate crystals. 39193 pibenzimol A fluorescent dye of benzimidazole derivative. Pibenzimol binds to AT-specific sites in the minor groove of duplex DNA and inhibits topoisomerase I, and DNA polymerase, thereby preventing DNA replication. This agent prolongs the G2 phase of the cell cycle and initiates apoptosis in tumor cells. 39194 anaxirone A synthetic triepoxide alkylating agent with potential antineoplastic activity. Anaxirone alkylates DNA via actual or derived epoxide groups, resulting in inhibition of DNA synthesis. This agent has been shown to exhibit a broad spectrum of antineoplastic activity against experimental tumors, including those resistant to other alkylating agents. C950 39199 ancitabine hydrochloride The hydrochloride salt of a cytarabine congener prodrug with antineoplastic activity. Upon administration, ancitabine is slowly hydrolyzed into cytarabine. Subsequently, cytarabine is converted to the triphosphate form within the cell and then competes with cytidine for incorporation into DNA. Because the arabinose sugar sterically hinders the rotation of the molecule within DNA, DNA replication ceases, specifically during the S phase of the cell cycle. Cytarabine agent also inhibits DNA polymerase, resulting in a decrease in DNA replication and repair. Compared to cytarabine, a more prolonged, consistent cytarabine-mediated therapeutic effect may be achieved with ancitabine because of the slow hydrolytic conversion of ancitabine to cytarabine. 39200 cycloleucine A non-metabolizable synthetic amino acid, formed through the cyclization of the amino acid leucine, with immunosuppressive, antineoplastic, and cytostatic activities. Cycloleucine competitively inhibits the enzyme methionine adenosyltransferase, resulting in the inhibition of S-adenosylmethionine (SAM) synthesis from methionine and ATP, and subsequent nucleic acid methylation and polyamine production; RNA, and perhaps to a lesser extent, DNA biosyntheses and cell cycle progression are finally disrupted. This agent is also a competitive inhibitor at the glycine modulatory site of the N-methyl-D-aspartate (NMDA) receptor. 39201 cyclosporine A natural cyclic polypeptide immunosuppressant isolated from the fungus Beauveria nivea. The exact mechanism of action of cyclosporine is not known but may involve binding to the cellular protein cytophilin, resulting in inhibition of the enzyme calcineurin. This agent appears to specifically and reversibly inhibit immunocompetent lymphocytes in the G0-or G1-phase of the cell cycle. T-lymphocytes are preferentially inhibited with T-helper cells as the primary target. Cyclosporine also inhibits lymphokine production and release. 39203 cyproterone acetate The acetate salt of a synthetic steroidal antiandrogen with weak progestational and antineoplastic activities. Cyproterone binds the androgen receptor (AR), thereby preventing androgen-induced receptor activation in target tissues and inhibiting the growth of testosterone-sensitive tumor cells. This agent also exerts progestational agonist properties at the level of the pituitary that reduce luteinizing hormone (LH), resulting in reductions in testicular androgen secretion and serum testosterone levels. Treatment with cyproterone alone results in incomplete suppression of serum testosterone levels. C1059 39204 danazol A synthetic androgen derived from ethinyl testosterone. Danazol indirectly reduces estrogen production by decreasing pituitary secretion of follicle-stimulating hormone and luteinizing hormone, and binds to sex hormone receptors in target tissues, thereby exhibiting antiestrogenic, anabolic and weakly androgenic effects. 39206 metoprine A diaminopyrimidine folate antagonist with potential antineoplastic activity. Metoprine inhibits dihydrofolate reductase, resulting in decreased cellular folate metabolism and cell growth; it also inhibits histamine-N-methyltransferase, resulting in decreased histamine catabolism. Lipid-soluble metoprine is capable of crossing the blood-brain barrier. 39207 etoposide A semisynthetic derivative of podophyllotoxin, a substance extracted from the mandrake root Podophyllum peltatum. Possessing potent antineoplastic properties, etoposide binds to and inhibits topoisomerase II and its function in ligating cleaved DNA molecules, resulting in the accumulation of single- or double-strand DNA breaks, the inhibition of DNA replication and transcription, and apoptotic cell death. Etoposide acts primarily in the G2 and S phases of the cell cycle. 39208 3-deazauridine A synthetic analogue of nucleoside uridine lacking a ring nitrogen in the 3-position. 3-deazauridine inhibits cytidine synthase, thereby reducing intracellular levels of cytidine and deoxycytidine and disrupting DNA and RNA synthesis. This agent may trigger apoptosis and enhance differentiation of neoplastic cells.. 39210 pentostatin A purine nucleotide analogue antibiotic isolated from the bacterium Streptomyces antibioticus. Also known as 2'-deoxycoformycin, pentostatin binds to and inhibits adenine deaminase (ADA), an enzyme essential to purine metabolism; ADA activity is greatest in cells of the lymphoid system with T-cells having higher activity than B-cells and T-cell malignancies higher ADA activity than B-cell malignancies. Pentostatin inhibition of ADA appears to result in elevated intracellular levels of dATP which may block DNA synthesis through the inhibition of ribonucleotide reductase. This agent may also inhibit RNA synthesis and may selectively deplete CD26+ lymphocytes. 39211 esorubicin A synthetic derivative of the anthracycline antineoplastic antibiotic doxorubicin with potential antineoplastic activity. Esorubicin intercalates into DNA and inhibits topoisomerase II, thereby inhibiting DNA replication and ultimately, interfering with RNA and protein synthesis. This agent exhibits less cardiotoxicity than the parent antibiotic doxorubicin, but may cause more severe myelosupression compared to other compounds within the anthracycline class. C972 39213 detorubicin A semi-synthetic derivative of the anthracycline antineoplastic antibiotic daunorubicin. Detorubicin intercalates into DNA and interacts with topoisomerase II, thereby inhibiting DNA replication and repair and RNA and protein synthesis. This agent also produces toxic free-radical intermediates and interacts with cell membrane lipids causing lipid peroxidation. Detorubicin is less toxic than daunorubicin. 39214 DHEA mustard A steroidal alkylating agent with potential antineoplastic activity. Alkylating agents exert cytotoxic and, in some cases, chemotherapeutic effects by transferring alkyl groups to DNA, thereby damaging DNA and interfering with DNA replication and cell division. 39215 dianhydrogalactitol A bifunctional hexitol derivative with potential antineoplastic activity. Dianhydrogalactitol alkylates and cross-links DNA via an epoxide group during all phases of the cell cycle, resulting in disruption of DNA function and cell cycle arrest. 39216 mitolactol A synthetic derivative of hexitol with antineoplastic and radiosensitizing properties. Mitolactol alkylates DNA via actual or derived epoxide groups, resulting in inhibition of DNA and RNA synthesis. 39217 dichloromethotrexate A chlorinated methotrexate derivative. Dichloromethotrexate inhibits the enzyme dihydrofolate reductase, thereby preventing the synthesis of purine nucleotides and thymidylates and inhibiting DNA and RNA synthesis. This agent is metabolized and excreted by the liver. 39218 inosine dialdehyde A toxic purine analogue. Inosine dialdehyde inhibits ribonucleotide reductase, resulting in decreased synthesis of DNA, RNA, and proteins, and G2/M-phase cell cycle arrest. This agent also forms stable covalent crosslinks in proteins, thereby inhibiting the activity of enzymes involved in nucleic acid synthesis. 39219 mitoxantrone hydrochloride The hydrochloride salt of an anthracenedione antibiotic with antineoplastic activity. Mitoxantrone intercalates into and crosslinks DNA, thereby disrupting DNA and RNA replication. This agent also binds to topoisomerase II, resulting in DNA strand breaks and inhibition of DNA repair. Mitoxantrone is less cardiotoxic compared to doxorubicin. 39220 dihydro-5-azacytidine A synthetic nucleoside analogue of deoxycytidine. Dihydro-5-azacytidine inhibits DNA methyltransferase, thereby interfering with abnormal DNA methylation patterns that are associated with genetic instability in some tumor cells. Inhibition of this enzyme may restore expression of tumor-suppressor genes and result in antitumor activity. 39221 dimethylbusulfan An aliphatic analogue of busulfan with potential antineoplastic activity. As an alkylating agent, dimethylbusulfan induces neutropenia and has been shown to exhibit antitumor effects in some animal models. Alkylating agents exert cytotoxic and chemotherapeutic effects by transferring alkyl groups to DNA, thereby damaging DNA and interfering with DNA synthesis and cell division. 39222 dimethyl sulfoxide A polar organic solvent. DMSO is a free radical scavenger that has been used to treat extravasation damage caused by anthracycline-based chemotherapy. 39224 diazooxonorleucine An L-glutamine diazo analogue amino acid antibiotic isolated from a species of the bacterial genus Streptomyces with potential antineoplastic activity. Diazooxonorleucine inhibits several glutamine-dependent biosynthetic pathways involved in the the syntheses of D-glucosamine phosphate, purines and pyrimidines. This agent inhibits phosphate-activated glutaminase, a key enzyme for the synthesis of releasable glutamine, depleting cells of this essential amino acid and reducing their capacity to proliferate. C427 39227 droperidol A butyrophenone with anti-emetic, sedative and anti-anxiety properties. Although the exact mechanism through which droperidol exerts its effects is unknown, droperidol may block dopamine receptors in the chemoreceptor trigger zone (CTZ), which may lead to its anti-emetic effect. This agent may also bind to postsynaptic gamma-aminobutyric acid (GABA) receptors in the central nervous system (CNS), which increases the inhibitory effect of GABA and leads to sedative and anti-anxiety activities. 39228 duborimycin An anthracycline antineoplastic antibiotic with therapeutic effects similar to those of doxorubicin. Duborimycin exhibits cytotoxic activity through topoisomerase-mediated interaction with DNA, thereby inhibiting DNA replication and repair and RNA and protein synthesis. 39229 dipyridamole A synthetic agent derivative of pyrimido-pyrimidine, with antiplatelet properties. Dipyridamole inhibits adenosine uptake by platelets and endothelial cells, triggering an accumulation of cyclic adenosine monophosphate (cAMP), and inhibiting the stimulation of platelet aggregation by agents such as platelet activating factor and collagen. 39231 elliptinium A derivative of the alkaloid ellipticine isolated from species of the plant family Apocynaceae, including Bleekeria vitensis, a plant with anti-cancer properties. As a topoisomerase II inhibitor and intercalating agent, elliptinium stabilizes the cleavable complex of topoisomerase II and induces DNA breakages, thereby inhibiting DNA replication and RNA and protein synthesis 39232 epirubicin hydrochloride The hydrochloride salt of the 4'-epi-isomer of the anthracycline antineoplastic antibiotic doxorubicin. Epirubicin intercalates into DNA and interacts with topoisomerase II, thereby inhibiting DNA replication and repair and RNA and protein synthesis. This agent also produces toxic free-radical intermediates and interacts with cell membrane lipids causing lipid peroxidation. 39234 erythromycin A broad-spectrum, topical macrolide antibiotic with antibacterial activity. Erythromycin diffuses through the bacterial cell membrane and reversibly binds to the 50S subunit of the bacterial ribosome. This prevents bacterial protein synthesis. Erythromycin may be bacteriostatic or bactericidal in action, depending on the concentration of the drug at the site of infection and the susceptibility of the organism involved. 39235 estramustine phosphate sodium The orally available disodium salt, monohydrate, of estramustine phosphate, a synthetic molecule that combines estradiol and nornitrogen mustard through a carbamate link. Estramustine and its major metabolite estramustine bind to microtubule-associated proteins (MAPs) and tubulin, thereby inhibiting microtubule dynamics and leading to anaphase arrest in a dose-dependent fashion. This agent also exhibits anti-androgenic effects. 39236 therapeutic estradiol A steroid sex hormone vital to the maintenance of fertility and secondary sexual characteristics in females. Typically esterified, estradiol derivatives are formulated for oral or parenteral administration. As the primary, most potent estrogen hormone produced by the ovaries, estradiol binds to and activates specific nuclear receptors. Estradiol exhibits mild anabolic and metabolic properties, and increases blood coagulability. 39237 conjugated estrogens Purified orally bioavailable female sex hormones isolated from pregnant mare urine or synthetically derived from plant materials and primarily conjugated as sulfate esters. Estrogen binds to and activates specific nuclear receptors, which, in turn, bind to estrogen response elements (EREs) in target genes, resulting in histone acetylation, alteration of chromatin conformation, and initiation of transcription. 39238 ethinyl estradiol A semisynthetic estrogen. Ethinyl estradiol binds to the estrogen receptor complex and enters the nucleus, activating DNA transcription of genes involved in estrogenic cellular responses. This agent also inhibits 5-alpha reductase in epididymal tissue, which lowers testosterone levels and may delay progression of prostatic cancer. In addition to its antineoplastic effects, ethinyl estradiol protects against osteoporosis. In animal models, short-term therapy with this agent has been shown to provide long-term protection against breast cancer, mimicking the antitumor effects of pregnancy. 39240 trifluridine A fluorinated thymidine analog with potential antineoplastic activity. Trifluridine is incorporated into DNA and inhibits thymidylate synthase, resulting in inhibition of DNA synthesis, inhibition of protein synthesis, and apoptosis. This agent also exhibits antiviral activity. 39241 fentanyl citrate The citrate salt of fentanyl, a synthetic opioid related to the phenylpiperidines with analgesic and anesthetic properties. Fentanyl exerts its analgesic effect by selectively binding to the mu-opioid receptor in the central nervous system (CNS), thereby mimicking the effects of endogenous opiates. Additional pharmacological effects of fentanyl include anxiolysis, euphoria, feelings of relaxation, respiratory depression, constipation, miosis, and cough suppression. C47994 39242 floxuridine A fluorinated pyrimidine monophosphate analogue of 5-fluoro-2'-deoxyuridine-5'-phosphate (FUDR-MP) with antineoplastic activity. As an antimetabolite, floxuridine inhibits thymidylate synthetase, resulting in disruption of DNA synthesis and cytotoxicity. This agent is also metabolized to fluorouracil and other metabolites that can be incorporated into RNA and inhibit the utilization of preformed uracil in RNA synthesis. 39243 fludrocortisone acetate The acetate salt of a synthetic fluorinated corticosteroid with antiinflammatory and antiallergic activities. As a glucocorticoid-receptor agonist, fludrocortisone binds to cytoplasmic receptors, translocates to the nucleus, and subsequently initiates the transcription of glucocorticoid-responsive genes such as lipocortins to inhibit phospholipase A2 (PLA2). Inhibition of PLA2 activity prevents the release of arachidonic acid, a precursor of eicosanoids such as prostaglandins and leukotrienes; eicosanoids are important mediators in the pro-inflammatory response mechanism. As a mineralocorticoid-receptor agonist, this agent stimulates Na+ reabsorption and water retention and K+ and H+ secretion in the distal tubules and collecting ducts of the kidney. C1103 39244 fludarabine phosphate The phosphate salt of a fluorinated nucleotide antimetabolite analog of the antiviral agent vidarabine (ara-A) with antineoplastic activity. Fludarabine phosphate is rapidly dephosphorylated to 2-fluoro-ara-A and then phosphorylated intracellularly by deoxycytidine kinase to the active triphosphate, 2-fluoro-ara-ATP. This metabolite may inhibit DNA polymerase alpha, ribonucleotide reductase and DNA primase, thereby interrupting DNA synthesis and inhibiting tumor cell growth. 39245 flurbiprofen A derivative of propionic acid, and a phenylalkanoic acid derivative of non-steroidal antiinflammatory drugs (NSAIDs) with analgesic, antiinflammatory and antipyretic effects. Flurbiprofen non-selectively binds to and inhibits cyclooxygenase (COX). This results in a reduction of arachidonic acid conversion into prostaglandins that are involved in the regulation of pain, inflammation and fever. This NSAID also inhibits carbonic anhydrase, thereby reducing the production of hydrogen and bicarbonate ions. Upon ocular administration, flurbiprofen may reduce bicarbonate ion concentrations leading to a decrease in the production of aqueous humor, thereby lowering intraocular pressure. 39247 furosemide An anthranilic derivative and loop diuretic with antihypertensive effect. Furosemide blocks the Na-K-Cl cotransporter (NKCC) in the luminal membrane of the thick ascending limb of the loop of Henle in the kidney, by binding to the Cl-binding site located in the cotransporter's transmembrane domain, thereby inhibiting reabsorption of sodium, chloride, potassium ions and water. This agent reduces plasma and extracellular fluid volume resulting in decreased blood pressure and cardiac output. 39248 tegafur A congener of the antimetabolite fluorouracil with antineoplastic activity. Tegafur is a prodrug that is gradually converted to fluorouracil in the liver by the cytochrome P-450 enzyme. Subsequently, 5-FU is metabolized to two active metabolites, 5-fluoro-2-deoxyuridine monophosphate (FdUMP) and 5-fluorouridine triphosphate (FUTP) by both tumor cells and normal cells. FdUMP inhibits DNA synthesis and cell division by inhibiting thymidylate synthase and reducing normal thymidine production, while FUTP inhibits RNA and protein synthesis by competing with uridine triphosphate. 39249 gallium nitrate A hydrated nitrate salt of the group IIIa element gallium with potential use in the treatment of malignancy-associated hypercalcemia. Gallium nitrate localizes preferentially to areas of bone resorption and remodeling and inhibits osteoclast-mediated resorption by enhancing hydroxyapatite crystallization and reduction of bone mineral solubility. This agent also increases calcium and phosphorous deposition into bone and may increase collagen synthesis. 39252 guanazole A cytostatic triazole derivative antimetabolite. Guanazole scavenges tyrosine free radicals, thereby inhibiting mammalian ribonucleotide reductase activity and DNA synthesis. 39254 norethindrone acetate The orally bioavailable acetate salt of norethindrone, a synthetic progestin with some anabolic, estrogenic, and androgenic activities. As do all progestins, norethindrone binds to and activates nuclear progesterone receptors (PRs) in target tissues such as the pituitary and reproductive system; ligand-receptor complexes are translocated to the nucleus where they bind to progesterone response elements (PREs) located on target genes, followed by various transcriptional events and histone acetylation. Physiological effects include the inhibition of luteinizing hormone (LH) release, an increase in the endometrial luteal-phase, and alterations in endocervical mucus secretion. C702 39270 estradiol valerate The parenterally-administered synthetic valerate ester of estradiol, a steroid sex hormone vital to the maintenance of fertility and secondary sexual characteristics in females. As the primary, most potent estrogen hormone produced by the ovaries, estradiol binds to and activates specific nuclear receptors. This agent exhibits mild anabolic and metabolic properties, and increases blood coagulability. 39272 beclomethasone dipropionate The dipropionate salt of a synthetic glucocorticoid with anti-inflammatory and immunomodulating properties. After cell surface receptor attachment and cell entry, beclomethasone enters the nucleus where it binds to and activates specific nuclear receptors, resulting in an altered gene expression and inhibition of proinflammatory cytokine production. 39273 betamethasone A synthetic glucocorticoid with metabolic, immunosuppressive and anti-inflammatory activities. Betamethasone binds to specific intracellular glucocorticoid receptors and subsequently binds to DNA to modify gene expression. The synthesis of certain anti-inflammatory proteins is induced while the synthesis of certain inflammatory mediators is inhibited. As a result, there is an overall reduction in chronic inflammation and autoimmune reactions. 39274 therapeutic hydrocortisone A synthetic or semisynthetic analog of natural hydrocortisone hormone produced by the adrenal glands with primary glucocorticoid and minor mineralocorticoid effects. As a glucocorticoid receptor agonist, hydrocortisone promotes protein catabolism, gluconeogenesis, capillary wall stability, renal excretion of calcium, and suppresses immune and inflammatory responses. 39275 triamcinolone A synthetic glucocorticoid with anti-inflammatory and immunomodulating properties. Upon cell entry, triamcinolone binds to and activates the glucocorticoid receptor, which leads to translocation of the ligand-receptor complex to the nucleus and induces expression of glucocorticoid-responsive genes such as lipocortins. Lipocortins inhibit phospholipase A2, thereby blocking the release of arachidonic acid from membrane phospholipids and preventing the synthesis of prostaglandins and leukotrienes, both mediators of inflammation. In addition, pro-inflammatory cytokine production, including interleukin (IL)-1and IL-6, and the activation of cytotoxic T-lymphocytes is also inhibited. T-cells are prevented from making IL-2 and proliferating. This agent also decreases the number of circulating lymphocytes, induces cell differentiation, and stimulates apoptosis through increasing Ikappa-B expression and curtailing activation of nuclear factor (NF)kappa-B. 39277 dinoprost tromethamine A synthetic analogue of the naturally occurring prostaglandin F2 alpha. Prostaglandin F2 alpha stimulates myometrial activity, relaxes the cervix, inhibits corpus luteal steroidogenesis, and induces luteolysis by direct action on the corpus luteum. 39278 meperidine hydrochloride The hydrochloride salt of a synthetic piperidine ester with opioid analgesic activity. Meperidine mimics the actions of endogenous neuropeptides via opioid receptors such as the mu-opiiod receptor, thereby producing characteristic morphine-like effects including analgesia, euphoria, sedation, respiratory depression, miosis, bradycardia and physical dependence. C635 39288 propylthiouracil A thiourea derivative with antithyroid property. Propylthiouracil (PTU) interferes with the oxidation of iodine possibly by interaction with peroxidase or a peroxidase-mediated complex reaction, thereby inhibiting synthesis of thyroid hormones tri-iodothyronine (T3) and thyroxine (T4). In addition, this agent inhibits the Type I 5'-deiodinase (D1), an enzyme involved in the peripheral conversion of thyroxine to tri-iodothyronine. This results in decreased plasma triodothyronine concentrations and decreased entrance of thyroxine into cells thereby reducing thyroid hormone activity. 39290 diazoxide A benzothiadiazine derivate with antihypertensive and hyperglycemic activities. Diazoxide increases membrane permeability to potassium ions in vascular smooth muscle, thereby stabilizing the membrane action potential and preventing vascular smooth muscle contraction; this results in peripheral vasodilatation and decreases in peripheral vascular resistance. This agent also inhibits insulin release by interacting with ATP-sensitive potassium channels of pancreatic islet beta-cells. C428 39299 decitabine A cytidine antimetabolite analogue with potential antineoplastic activity. Decitabine incorporates into DNA and inhibits DNA methyltransferase, resulting in hypomethylation of DNA and intra-S-phase arrest of DNA replication. 39307 enclomiphene citrate The orally bioavailable citrate salt of enclomiphene, the trans-isomer of the nonsteroidal triphenylethylene compound clomiphene, with tissue-selective estrogenic and antiestrogenic activities. As a selective estrogen receptor modulator (SERM), enclomiphene binds to hypothalamic estrogen receptors, blocking the negative feedback of endogenous estrogens and stimulating the release of gonadotropin-releasing hormone (GnRH) from the hypothalamus; released GnRH subsequently stimulates the release of follicle-stimulating hormone (FSH) and luteinizing hormone (LH) from the anterior pituitary, resulting in ovulation. In addition, this agent may bind to estrogen receptors on breast cancer cells, resulting in the inhibition of estrogen-stimulated proliferation in susceptible cell populations. 39309 nafoxidine hydrochloride The hydrochloride salt of the partial estrogen antagonist nafoxidine. Nafoxidine competes with endogenous estrogen for binding to specific estrogen receptors. This agent also inhibits angiogenesis in some tissues by blocking the effects of fibroblast growth factor (FGF) and vascular endothelial growth factor (VEGF); paradoxically, it may enhance angiogenesis in uterine tissue. Nafoxidine also induces oxidative stress, protein kinase C and calcium signaling. 39310 norgestrel A synthetic progestin commonly used alone or in combination with an estrogen for contraception. Norgestrel suppresses the secretion of luteinizing and follicle-stimulating hormones (LH and FSH), thickens cervical mucus, and slows the transit of ova through the fallopian tubes. This agent also exhibits antiproliferative activity in endometrial tissue and may exhibit chemopreventive and antineoplastic activities in endometrial carcinoma. 39324 recombinant interleukin-4 A recombinant therapeutic agent which is chemically identical to or similar to the endogenous cytokine interleukin-4 (IL-4). Produced primarily by activated T-cells, IL-4 binds to and activates its cell-surface receptor, stimulating the proliferation and differentiation of activated B-cells and enhancing their ability to present antigens to T-cells. As a potential immunotherapeutic agent, recombinant IL-4 also augments the effects of other cytokines on dendritic cells (DC), cytotoxic T lymphocytes (CTL), and tumor-infiltrating lymphocytes (TIL). 39337 anti-thymocyte globulin A purified gamma immunoglobulin (IgG) with immunosuppressive activity. Obtained from rabbits that have been immunized with human thymocytes, antithymocyte globulin specifically recognizes and destroys T lymphocytes. Although the exact mechanism of action is not completely understood, it appears to involve T lymphocyte clearance from the circulation and modulation of T lymphocyte activity. Administering antithymocyte globulin with chemotherapy prior to stem cell transplantation may reduce the risk of graft-versus-host disease. 39339 4-nitroestrone 3-methyl ether A synthetic derivative of estradiol. 4-nitroestrone 3-methyl ether inhibits estrogen sulfotransferase (EST), a progesterone-induced secretory endometrial enzyme which affects estrogen receptor levels. This agent has been shown to be an effective growth inhibitor of some chemically induced animal mammary tumors. 39352 edrecolomab A murine monoclonal IgG2a antibody to tumor-associated epithelial cell adhesion molecule (EpCAM, or 17-1A) antigen. Edrecolomab attaches to EpCAM, a human cell surface glycoprotein that is found on normal epithelial cells and some tumor cells, such as those of colon and breast carcinomas. Upon binding, this agent recruits the body's immune effector cells, which may exhibit antitumor cytotoxicity. 39362 monoclonal antibody R24 An IgG murine monoclonal antibody directed against the ganglioside GD3 glycolipid, located in the cell membranes of some tumor cells. Monoclonal antibody R24 binds to GD3-positive cells, thereby initiating antibody-dependent cytotoxicity against GD3-positive cells. 39364 ABVD regimen A chemotherapy regimen consisting of doxorubicin hydrochloride (Adriamycin), bleomycin, vinblastine and dacarbazine, used alone or in combination with radiation therapy, for the primary treatment of Hodgkin lymphoma. C63364 39410 amiodarone hydrochloride The hydrochloride salt of an iodine-rich benzofuran derivative with antiarrhythmic and vasodilatory activities. As a class III antiarrhythmic agent, amiodarone blocks the myocardial calcium, potassium and sodium channels in cardiac tissue, resulting in prolongation of the cardiac action potential and refractory period. In addition, this agent inhibits alpha- and beta-adrenergic receptors, resulting in a reduction in sympathetic stimulation of the heart, a negative chronotropic effect, and a decrease in myocardial oxygen demands. Amiodarone may cause vasodilation by stimulation of the release of nitric oxide and cyclooxygenase-dependent relaxing endothelial factors. C236 39411 teloxantrone hydrochoride The hydrochloride salt of an anthrapyrazole antineoplastic antibiotic. Teloxantrone intercalates into DNA and interacts with topoisomerase II, thereby inhibiting DNA replication and repair, as well as RNA and protein synthesis. C1520 39424 pegylated liposomal doxorubicin hydrochloride A liposome-encapsulated form of the hydrochloride salt of the anthracycline antineoplastic antibiotic doxorubicin. Doxorubicin intercalates between base pairs in the DNA helix, thereby preventing DNA replication and ultimately inhibiting protein synthesis. Additionally, doxorubicin inhibits topoisomerase II which results in an increased and stabilized cleavable enzyme-DNA linked complex during DNA replication and subsequently prevents the ligation of the nucleotide strand after double-strand breakage. Doxorubicin also forms oxygen free radicals resulting in cytotoxicity secondary to lipid peroxidation of cell membrane lipids. Liposomal delivery of doxorubicin HCL improves drug penetration into tumors and decreases drug clearance, thereby increasing the duration of therapeutic drug effects; a liposomal formulation of doxorubicin also modulates toxicity, specifically the cardiac effects commonly seen with anthracycline antitumor drugs. 39437 pyrazine diazohydroxide A congener of pyridine 2-diazohydroxide. Pyrazine diazohydroxide forms DNA adducts via the reactive pyrazine diazonium ion, thereby inhibiting DNA synthesis. 39441 spiromustine A bifunctional nitrogen alkylating agent with antineoplastic activity and lipophilic properties. Containing a lipophilic hydantoin group that serves as a carrier to cross the blood brain barrier, spiromustine forms covalent linkages with nucleophilic centers in DNA, causing depurination, base-pair miscoding, strand scission, and DNA-DNA cross-linking, which may result in cytotoxicity. 39444 spironolactone A synthetic 17-spironolactone corticosteroid with potassium-sparing diuretic, antihypertensive, and antiandrogen activities. Spironolactone competitively inhibits adrenocortical hormone aldosterone activity in the distal renal tubules, myocardium, and vasculature. This agent may inhibit the pathophysiologic effects of aldosterone produced in excess by various types of malignant and benign tumors. 39446 etanidazole A 2-nitroimidazole with radiosensitizing properties. Etanidazole depletes glutathione and inhibits glutathione transferase, thereby enhancing the cytotoxicity of ionizing radiation. This agent may also be useful as an imaging agent for identifying hypoxic, drug-resistant regions of primary tumors or metastases. C1092 39454 hepsulfam A bisulfamic ester which is similar in structure to busulfan and belongs to the family of drugs known as alkylsulfonate alkylating agents. Hepsulfam forms covalent linkages with nucleophilic centers in DNA, resulting in depurination, base miscoding, strand scission, DNA-DNA and DNA-protein cross-linking, and cytotoxicity. 39474 haloperidol A phenylbutylpiperadine derivative with antipsychotic, neuroleptic, and antiemetic activities. Haloperidol competitively blocks postsynaptic dopamine (D2) receptors in the mesolimbic system of the brain, thereby eliminating dopamine neurotransmission and leading to antidelusionary and antihallucinagenic effects. Antagonistic activity mediated through D2 dopamine receptors in the chemoreceptive trigger zone (CTZ) accounts for its antiemetic activity. 39475 altretamine A synthetic cytotoxic s-triazine derivative similar in structure to alkylating agent triethylenemelamin with antineoplastic activity. Although the precise mechanism by which altretamine exerts its cytotoxic effect is unknown, N-demethylation of altretamine may produce reactive intermediates which covalently bind to DNA, resulting in DNA damage. 39476 omacetaxine mepesuccinate A semisynthetic formulation of the cytotoxic plant alkaloid homoharringtonine isolated from the evergreen tree Cephalotaxus with potential antineoplastic activity. Omacetaxine mepesuccinate binds to the 80S ribosome in eukaryotic cells and inhibits protein synthesis by interfering with chain elongation. This agent also induces differentiation and apoptosis in some cancer cell types. 39477 hycanthone A thioxanthene derivative of lucanthone with anti-schistosomal activity and potential antineoplastic activity. Hycanthone interferes with parasite nerve function, resulting in parasite paralysis and death. This agent also intercalates into DNA and inhibits RNA synthesis in vitro. 39479 hyperbaric oxygen Oxygen that is administered at a higher pressure compared to standard (i.e. sea-level) atmospheric pressure. Administration of oxygen under hyperbaric conditions enhances the delivery of oxygen to hypoxic tumor cells, thereby increasing their sensitivity to radiation and chemotherapy. In addition, hyperbaric oxygen may improve the healing of radiation-induced injuries by improving oxygen delivery to damaged tissue. C2351 39480 razoxane An orally bioavailable bis-dioxopiperazine and a derivative of the chelating agent ethylenediaminetetraacetic acid (EDTA) with antineoplastic, antiangiogenic, and antimetastatic activities. Razoxane specifically inhibits the enzyme topoisomerase II without inducing DNA strand breaks, which may result in the inhibition of DNA synthesis and cell division in the premitotic and early mitotic phases of the cell cycle. This agent may also exhibit antiangiogenic and antimetastatic activities although the precise molecular mechanisms of these actions are unknown. 39481 idoxuridine An iodinated analogue of deoxyuridine. Idoxuridine incorporates into DNA during the S-phase of the cell cycle, sensitizing cells to ionizing radiation by increasing DNA strand breaks. When this agent contains a radioactive isomer of iodine, the radioactive idoxuridine kills cancer cells directly after preferential incorporation into the DNA of rapidly dividing tumor cells. 39482 indicine-N-oxide A natural pyrrolizidine alkaloid with antineoplastic properties. Indicine-N-oxide alkylates and crosslinks DNA. 39483 imidazole mustard A synthetic derivative of imidazole with potent antineoplastic properties. Imidazole mustard alkylates DNA, preferentially at guanine residues, resulting in DNA interstrand crosslinks and inhibition of DNA replication and RNA and protein synthesis. 39484 isoniazid A synthetic derivative of nicotinic acid with anti-mycobacterial properties. Although its mechanism of action is still unclear, isoniazid appears to block the synthesis of mycolic acids, major components of the mycobacterial cell wall. This agent is only active against actively growing mycobacteria because, as a pro-drug, it requires activation in susceptible mycobacterial species. Isoniazid also interferes with mycobacterial metabolism of vitamin B6. Resistance occurs due to decreased bacterial wall penetration. 39485 dexrazoxane hydrochloride The hydrochloride salt of a bisdioxopiperazine with iron-chelating, chemoprotective, cardioprotective, and antineoplastic activities. After hydrolysis to an active form that is similar to ethylenediaminetetraacetic acid (EDTA), dexrazoxane chelates iron, limiting the formation of free radical-generating anthracycline-iron complexes, which may minimize anthracycline-iron complex-mediated oxidative damage to cardiac and soft tissues. This agent also inhibits the catalytic activity of topoisomerase II, which may result in tumor cell growth inhibition. C66945 39488 ketoconazole A synthetic derivative of phenylpiperazine with broad antifungal properties and potential antineoplastic activity. Ketoconazole inhibits sterol 14-a-dimethylase, a microsomal cytochrome P450-dependent enzyme, thereby disrupting synthesis of ergosterol, an important component of the fungal cell wall. 39489 indomethacin A synthetic nonsteroidal indole derivative with anti-inflammatory activity and chemopreventive properties. As a nonsteroidal anti-inflammatory drug (NSAID), indomethacin inhibits the enzyme cyclooxygenase, thereby preventing cyclooxygenase-mediated DNA adduct formation by heterocyclic aromatic amines. This agent also may inhibit the expression of multidrug-resistant protein type 1, resulting in increased efficacies of some antineoplastic agents in treating multi-drug resistant tumors. In addition, indomethacin activates phosphatases that inhibit the migration and proliferation of cancer cells and downregulates survivin, which may result in tumor cell apoptosis. 39490 levonantradol A synthetic cannabinoid analogue of delta (9)-tetrahydrocannabinol (delta(9)-THC) with antiemetic and anti-analgesic properties. Although its precise mechanism of action is unknown, levonantradol appears to bind and activate the cannabinoid receptors CB1 and/or CB2. 39491 lithium carbonate The carbonate salt of lithium, a soft alkali metal, with antimanic and hematopoietic activities. Lithium interferes with transmembrane sodium exchange in nerve cells by affecting sodium, potassium-stimulated adenosine triphosphatase (Na+, K+-ATPase); alters the release of neurotransmitters; affects cyclic adenosine monophosphate (cAMP) concentrations; and blocks inositol metabolism resulting in depletion of cellular inositol and inhibition of phospholipase C-mediated signal transduction. The exact mechanism through which lithium exerts its mood-stabilizing effect has not been established. In addition, lithium stimulates granulocytopoiesis and appears to increase the level of pluripotent hematopoietic stem cells by stimulating the release of hematopoietic cytokines and/or directly acting on hematopoietic stem\ncells. C1318 39492 maytansine An ansamycin antibiotic originally isolated from the Ethiopian shrub Maytenus serrata. Maytansine binds to tubulin at the rhizoxin binding site, thereby inhibiting microtubule assembly, inducing microtubule disassembly, and disrupting mitosis. Maytansine exhibits cytotoxicity against many tumor cell lines and may inhibit tumor growth in vivo. 39493 mannitol A naturally occurring alcohol found in fruits and vegetables and used as an osmotic diuretic. Mannitol is freely filtered by the glomerulus and poorly reabsorbed from the renal tubule, thereby causing an increase in osmolarity of the glomerular filtrate. An increase in osmolarity limits tubular reabsorption of water and inhibits the renal tubular reabsorption of sodium, chloride, and other solutes, thereby promoting diuresis. In addition, mannitol elevates blood plasma osmolarity, resulting in enhanced flow of water from tissues into interstitial fluid and plasma. 39494 monobenzone A monobenzyl ether of hydroquinone with topical depigmentation activity. Although the exact mechanism of action of depigmentation is unknown, the metabolites of monobenzone appear to have a cytotoxic effect on melanocytes. Furthermore, the depigmentation effect might be mediated through the inhibition of tyrosinase, which is essential in the synthesis of melanin pigments, thereby causing permanent depigmentation of the skin. 39495 methanol extraction residue of BCG A cell wall fraction of bacillus Calmette-Guerin (BCG) obtained by menthol extraction with immunomodulating properties and potential use in cancer immunotherapy. 39497 methylmercaptopurine riboside A purine derivative with antineoplastic and anti-angiogenic properties. 6-methylmercaptopurine riboside (6-MMPR) inhibits amidophosphoribosyltransferase, the first committed step in de novo purine synthesis, and inhibits fibroblast growth factor-2 (FGF2)-induced cell proliferation. 39498 methadone hydrochloride The hydrochloride salt of methadone, a synthetic opioid with analgesic activity. Similar to morphine and other morphine-like agents, methadone mimics the actions of endogenous peptides at CNS opioid receptors, primarily the mu-receptor, resulting in characteristic morphine-like effects including analgesia, euphoria, sedation, respiratory depression, miosis, bradycardia and physical dependence. Because of the prolonged half-life of merthadone compared to other morphine-like agents such as heroin, the onset of opiate withdrawal symptoms is slower, the duration of opiate withdrawal is prolonged, and opiate wihdrawal symptoms are less severe. C638 39499 methoxsalen A naturally occurring substance isolated from the seeds of the plant Ammi majus with photoactivating properties. As a member of the family of compounds known as psoralens or furocoumarins, methoxsalen's exact mechanism of action is unknown; upon photoactivation, methoxsalen has been observed to bind covalently to and crosslink DNA. 39500 mitoguazone A guanylhydrazone with potential antineoplastic activity. Mitoguazone competitively inhibits S-adenosyl-L-methionine decarboxylase (SAMD), an enzyme involved in the synthesis of polyamines, resulting in decreased proliferation of tumor cells, antimitochondrial effects, and p53-independent apoptosis. Polyamines, specifically spermine and spermidine, are essential for thymidine kinase production, DNA synthesis, and cell proliferation. 39501 metyrosine A methylated tyrosine, a catecholamine synthesis antagonist with antihypertensive property. Metyrosine competitively inhibits tyrosine 3-monooxygenase, an enzyme that activates molecular oxygen to catalyze the hydroxylation of tyrosine to dihydroxyphenylalanine (Dopa), an intermediate to catecholamine (dopamine, norepinephrine, and epinephrine) production. This agent reduces the elevated levels of catecholamines associated with pheochromocytoma, thereby preventing hypertension. 39502 metoclopramide hydrochloride The hydrochloride salt of the substituted benzamide metoclopramide, a para-aminobenzoic acid (PABA) derivative that is structurally related to procainamide, with gastroprokinetic and antiemetic activities. Metoclopramide binds to dopamine 2 (D2) receptors in the peripheral nervous system (PNS), antagonizing dopamine-mediated relaxation of gastrointestinal smooth muscle and promoting gastroprokinesis; the pyloric sphincter and the duodenal bulb are relaxed, peristalsis of the duodenum and jejunum increase, and gastric emptying and intestinal transit accelerate. This agent may also increase the resting tone of the lower esophagus sphincter (LES), preventing acid reflux. In the central nervous system (CNS), metoclopramide antagonizes D2 dopamine receptors in the chemoreceptive trigger zone (CTZ) of the medulla, thereby preventing nausea and vomiting. C649 39503 metronidazole hydrochloride The hydrochloride salt of a synthetic nitroimidazole derivative with antiprotozoal and antibacterial activities. Although its mechanism of action is not fully elucidated, un-ionized metronidazole is readily taken up by obligate anaerobic organisms and is subsequently reduced by low-redox potential electron-transport proteins to an active, intermediate product. Reduced metronidazole causes DNA strand breaks, thereby inhibiting DNA synthesis and bacterial cell growth. C48005 39504 misonidazole A nitroimidazole with radiosensitizing and antineoplastic properties. Exhibiting high electron affinity, misonidazole induces the formation of free radicals and depletes radioprotective thiols, thereby sensitizing hypoxic cells to the cytotoxic effects of ionizing radiation. This single-strand breaks in DNA induced by this agent result in the inhibition of DNA synthesis. 39506 mitotane A synthetic derivative of the insecticide dichlorodiphenyl trichloroethane (DDT) with anti-adrenocorticoid properties. Following its metabolism in the adrenal cortex to a reactive acyl chloride intermediate, mitotane covalently binds to adrenal proteins, specifically inhibiting adrenal cortical hormone production. 39509 naloxone hydrochloride The hydrochloride salt of naloxone, a thebaine derivate with opioid antagonist activity. Naloxone binds to opioid receptors in the CNS in a competitive manner, reversing or inhibiting characteristic opioid effects, including analgesia, euphoria, sedation, respiratory depression, miosis, bradycardia, and physical dependence. This agent binds to mu-opioid receptors with a high affinity, and a lesser degree to kappa- and gamma-opioid receptors. C678 39510 zinostatin An enediyne antineoplastic antibiotic hybrid containing an aminoglycoside chromophore. Zinostatin is isolated from the bacterium Streptomyces carzinostaticus. The aminoglycoside component of zinostatin intercalates into DNA and the benzene diradical intermediate of the enediyne core binds to the minor groove of DNA, resulting in single- and double-strand breaks in DNA and apoptosis. 39511 N-methylformamide A water-soluble organic solvent. As an adjuvant antineoplastic agent, N-methylformamide depletes cellular glutathione, a key molecule involved in the antioxidation of reactive oxygen species (ROS) and other free radicals, thereby enhancing ionizing radiation-induced DNA cross-linking in and terminal differentiation of tumor cells. 39512 nystatin Macrolide antifungal antibiotic complex produced by Streptomyces noursei, S. aureus, and other Streptomyces species. The biologically active components of the complex are nystatin A1, A2, and A3. (MSH2002_06_01) 39515 cisplatin An inorganic platinum agent (cis-diamminedichloroplatinum) with antineoplastic activity. Cisplatin forms highly reactive, charged, platinum complexes which bind to nucleophilic groups such as GC-rich sites in DNA, inducing intrastrand and interstrand DNA cross-links, as well as DNA-protein cross-links. These cross-links result in apoptosis and cell growth inhibition. 39542 clomiphene citrate The citrate salt form of clomiphene, a triphenylethylene nonsteroidal ovulatory stimulant evaluated for antineoplastic activity against breast cancer. Clomiphene has both estrogenic and anti-estrogenic activities that compete with estrogen for binding at estrogen receptor sites in target tissues. This agent causes the release of the pituitary gonadotropins follicle stimulating hormone (FSH) and luteinizing hormone (LH), leading to ovulation. 39545 papaverine An opiate alkaloid isolated from the plant Papaver somniferum and produced synthetically. As a direct-acting smooth muscle relaxant, papaverine is not closely related to the other opium alkaloids in structure or pharmacological actions; its mechanism of action may involve the non-selective inhibition of phosphodiesterases and direct inhibition of calcium channels. This agent also exhibits antiviral activity against respiratory syncytial virus, cytomegalovirus, and HIV. 39547 N-phosphonacetyl-L-aspartate A stable transition state analogue for an aspartate transcarbamylase- cartalyzed reaction with antineoplastic activity. N-phosphonacetyl-L-aspartate (PALA) is a stable transition analogue of the activated complex for the reaction catalyzed by aspartate transcarbamylase, the first step in the pyrimidine biosynthetic pathway. This agent inhibits de novo pyrimidine biosynthesis and increases the extent to which fluorouracil metabolites are incorporated into RNA. C1398 39552 peplomycin A semisynthetic analog of Bleomycin, a mixture of several basic glycopeptide antineoplastic antibiotics isolated from the fungus Streptomyces verticillus. Peplomycin forms complexes with iron that reduce molecular oxygen to superoxide and hydroxyl radicals that cause single- and double-stranded breaks in DNA. This agent appears to show greater antitumor activity than bleomycin; its use is limited due to pulmonary toxicity. 39553 pentamethylmelamine A principal metabolite of hexamethylmelamine with antineoplastic activity. Pentamethylmelamine alkylates DNA and other macromolecules and forms DNA intrastrand and DNA-protein crosslinks, thereby preventing DNA replication. 39554 phosphorus P32 A radioactive isotope of phosphorus with beta particle-emitting radiocytotoxic activity. Emitted by phosphorus P32, beta particles directly damage cellular DNA and, by ionizing intracellular water to produce several types of cytotoxic free radicals and superoxides, indirectly damage intracellular biological macromolecules, resulting in tumor cell death. 39555 piperacillin sodium The sodium salt of piperacillin, a broad-spectrum semisynthetic, ampicillin-derived ureidopenicillin antibiotic with bactericidal activity. Piperacillin binds to and inactivates penicillin-binding proteins (PBPs), enzymes located on the inner membrane of the bacterial cell wall, resulting in the weakening of the bacterial cell wall and cell lysis. PBPs participate in the terminal stages of assembling the bacterial cell wall, and in reshaping the cell wall during cell division. Inactivation of PBPs interferes with the cross-linkage of peptidoglycan chains necessary for bacterial cell wall strength and rigidity. C749 39556 piperazinedione A crystalline antibiotic fermentation product isolated from the bacterium Streptomyces griseoluteus with antineoplastic activity. Piperazinedione alkylates DNA at the N-7 position of guanine, inhibiting DNA replication and inducing cell cycle arrest. 39557 poly AU A synthetic polyadenylic-polyuridylic acid double-stranded RNA. Poly AU may stimulate the release of cytotoxic cytokines and, by inducing the production of interferon, may increase the number and tumoricidal activities of various immunohematopoietic cells. 39558 poly IC A synthetic polyinosinic-polycytidylic acid double-stranded RNA. Poly IC may stimulate the release of cytotoxic cytokines and, by inducing interferon-gamma production, may increase the number and tumoricidal activities of various immunohematopoietic cells. 39559 poly ICLC A synthetic complex of carboxymethylcellulose, polyinosinic-polycytidylic acid, and poly-L-lysine double-stranded RNA. Poly ICLC may stimulate the release of cytotoxic cytokines and, by inducing interferon-gamma production, may increase the tumoricidal activities of various immunohematopoietic cells. 39564 prochlorperazine A synthetic propylpiperazine derivative of phenothiazine with antiemetic, antipsychotic, antihistaminic, and anticholinergic activities. Prochlorperazine antagonizes the dopamine D2-receptor in the chemoreceptor trigger zone (CTZ) of the brain and may prevent chemotherapy-induced emesis. 39567 promethazine hydrochloride The hydrochloride salt form of promethazine, a phenothiazine derivative with antihistaminic, sedative and antiemetic properties. Promethazine hydrochloride selectively blocks peripheral H1 receptors thereby diminishing the effects of histamine on effector cells. Promethazine hydrochloride also blocks the central histaminergic receptors, thereby depressing the reticular system causing sedative and hypnotic effects. In addition, promethazine hydrochloride also has centrally acting anticholinergic properties and probably mediates nausea and vomiting by acting on the medullary chemoreceptive trigger zone. 39571 aminobenzoate potassium The potassium salt form of aminobenzoate, with anti-inflammatory and antifibrotic activities. Aminobenzoate potassium increases oxygen uptake at the tissue level and may enhance monoamine oxidase (MAO) activity, which requires oxygen as a substrate. Enhanced MAO activity maybe accountable for the prevention or regression of fibrosis, which may occur due to too much serotonin or too little MAO activity. C1736 39574 polysaccharide-K A protein-bound polysaccharide derived from the mushroom Trametes versicolor (Turkey Tail) with immunoadjuvant and potential antitumor activities. Although its mechanism of action has yet to be fully elucidated, in vitro and in vivo studies indicate that polysaccharide-K induces peripheral blood monocyte secretion of IL-8 and TNF-alpha, induces T cell proliferation, and prevents cyclophosphamide-induced immunosuppression. This agent has also been reported to stimulate macrophages to produce reactive nitrogen intermediates and superoxide anions and to promote apoptosis in the promyelocytic leukemia cell line HL-60. 39575 pyrazofurin A nucleoside analog. Pyrazofurin potently inhibits orotidine 5'-monophosphate (OMP) decarboxylase, thereby interfering with de novo synthesis of uridine nucleotides and resulting in cytotoxicity. This agent also causes a rapid depletion of the pyrimidine deoxynucleotide pool, thereby inhibiting DNA synthesis and cell replication. 39577 PEG-interleukin-2 A complex of polyethylene glycol conjugated with human recombinant cytokine interleukin-2 (IL-2) with antineoplastic activity. PEG-interleukin-2 induces natural killer (NK) cell activity and the production of interferon-gamma (IFN-gamma), and enhances T cell-mediated cytotoxicity. Pegylation of IL-2 protects the cytokine from degradation. 39578 pyrimethamine A synthetic derivative of ethyl-pyrimidine with potent antimalarial properties. Pyrimethamine is a competitive inhibitor of dihydrofolate reductase (DHFR). DHFR is a key enzyme in the redox cycle for production of tetrahydrofolate, a cofactor that is required for the synthesis of DNA and proteins. This agent is often used in combination with other antimalarials for the treatment of uncomplicated falciparum malaria. 39580 muromonab-CD3 A murine IgG2a monoclonal antibody with immunosuppressive activity. Muromonab-CD3 binds to and inhibits CD3 on the surface of circulating T-lymphocytes; binding of muromonab-CD3 to CD3-positive T cells results in an early activation of this T cell subset, followed by cytokine release, and subsequently inhibition of T cell functions. This agent may cause the opsonization and elimination of CD3-positive T cells from the circulation by mononuclear phagocytes in the liver and spleen. CD3 is part of the functional T cell receptor (TCR) complex, which is necessary for antigen recognition by T cells, and is required for signal transduction. 39582 fenretinide An orally-active synthetic phenylretinamide analogue of retinol (vitamin A) with potential antineoplastic and chemopreventive activities. Fenretinide binds to and activates retinoic acid receptors (RARs), thereby inducing cell differentiation and apoptosis in some tumor cell types. This agent also inhibits tumor growth by modulating angiogenesis-associated growth factors and their receptors and exhibits retinoid receptor-independent apoptotic properties. 39587 echinomycin A polypeptide quinoxaline antineoplastic antibiotic isolated from the bacterium Streptomyces echinatus. Echinomycin intercalates into DNA at two locations simultaneously in a sequence-specific fashion, thereby inhibiting DNA replication and RNA synthesis. 39590 zorubicin A benzoyl-hydrazone derivative of the anthracycline antineoplastic antibiotic daunorubicin. Zorubicin intercalates into DNA and interacts with topoisomerase II, thereby inhibiting DNA replication and repair and RNA and protein synthesis. 39598 sodium fluoride An inorganic salt of fluoride used topically or in municipal water fluoridation systems to prevent dental caries. Fluoride appears to bind to calcium ions in the hydroxyapatite of surface tooth enamel, preventing corrosion of tooth enamel by acids. This agent may also inhibit acid production by commensal oral bacteria. 39600 magnesium hydroxide/aluminum hydroxide/simethicone suspension An oral suspension containing magnesium hydroxide, aluminum hydroxide and simethicone with antacid activity. Both magnesium hydroxide and aluminum hydroxide react with excess acid in the stomach thereby neutralizing gastric acid. Simethicone, a mixture of polydimethylsiloxane and silica gel, reduces the surface tension of gas bubbles, promoting gas bubble coalescence and so intestinal gas transit and evacuation. C78463 39602 sodium thiosulfate A water soluble salt and reducing agent that reacts with oxidizing agents. Although its exact mechanism of action is unknown, thiosulfate likely provides an exogenous source of sulfur, thereby hastening the detoxification of cyanide through the enzyme rhodanese (thiosulfate cyanide sulfurtransferase) which converts cyanide to the relatively nontoxic, excretable thiocyanate ion. In addition, this agent neutralizes the reactive alkylating species of nitrogen mustard, thereby decreasing skin toxicity related to nitrogen mustard extravasation. 39605 spirogermanium A synthetic organometallic compound containing the element germanium with possible antineoplastic activity. Spirogermanium exhibits significant toxicity, particularly neurotoxicity. 39607 lidocaine A synthetic aminoethylamide with local anesthetic and antiarrhythmic properties. Lidocaine stabilizes the neuronal membrane by binding to and inhibiting voltage-gated sodium channels, thereby inhibiting the ionic fluxes required for the initiation and conduction of impulses and effecting local anesthesia. 39610 porfiromycin An N-methyl derivative of the antineoplastic antibiotic mitomycin C isolated from the bacterium Streptomyces ardus and other Streptomyces bacterial species. Bioreduced porfiromycin generates oxygen radicals and alkylates DNA, producing interstrand cross-links and single-strand breaks, thereby inhibiting DNA synthesis. Porfiromycin is preferentially toxic to hypoxic cells. 39641 folic acid A collective term for pteroylglutamic acids and their oligoglutamic acid conjugates. As a natural water-soluble substance, folic acid is involved in carbon transfer reactions of amino acid metabolism, in addition to and purine and pyrimidine synthesis, and is essential for hematopoiesis and red blood cell production. C510 39659 alprazolam A triazolobenzodiazepine agent with anxiolytic, sedative-hypnotic and anticonvulsant activities. Alprazolam binds to a specific site distinct from the inhibitory neurotransmitter gamma-aminobutyric acid (GABA) binding site on the benzodiazepine-GABA-A-chloride ionophore receptor complex located in the limbic, thalamic and hypothalamic regions of the central nervous system (CNS). This binding causes an allosteric modification of the receptor and enhances the affinity of GABA to the receptor leading to an increase in the frequency of chloride-channel opening events. This leads to an increase in chloride ion conductance, neuronal hyperpolarization, inhibition of the action potential and leads to a decrease in neuronal excitability. 39675 dactinomycin A chromopeptide antineoplastic antibiotic isolated from the bacterium Streptomyces parvulus. Dactinomycin intercalates between adjacent guanine-cytosine base pairs, blocking the transcription of DNA by RNA polymerase; it also causes single-strand DNA breaks, possibly via a free-radical intermediate or an interaction with topoisomerase II. 39679 calcium carbonate The carbonic salt of calcium (CaCO3). Calcium carbonate is used therapeutically as a phosphate buffer in hemodialysis, as an antacid in gastric hyperacidity for temporary relief of indigestion and heartburn, and as a calcium supplement for preventing and treating osteoporosis. 39703 streptonigrin An aminoquinone antineoplastic antibiotic isolated from the bacterium Streptomyces flocculus. Streptonigrin complexes with DNA and topoisomerase II, resulting in DNA cleavage and inhibition of DNA replication and RNA synthesis. This agent also acts as a reverse transcriptase inhibitor and causes free radical-mediated cellular damage. 39707 dronabinol A synthetic form of delta-9-tetrahydrocannabinol, a psychoactive substance found in Cannabis sativa. Dronabinol acts directly on the appetite and vomiting control centers in the brain to stimulate appetite and prevent emesis. C867 39710 tetrahydrouridine A synthetic pyrimidine nucleoside analogue with biomodulating activity. Tetrahydrouridine increases the efficacy of the radiosensitizer cytochlor (5-chloro-2'-deoxycytidine) by inhibiting the enzyme deoxycytidine monophosphate (dCMP) deaminase and preventing the premature deamination of the cytochlor metabolite 5-chloro-2'-deoxycytidine monophosphate (CldCMP) to 5-chloro-2'-deoxyuridine monophosphate (CldUMP); in turn, this increases tumor concentrations of CldUMP which is then further anabolized and incorporated selectively into tumor DNA as CldU (5-chloro-2'-deoxyuridine). 39711 beta-thioguanine deoxyriboside A thiopurine nucleoside derivative with antineoplastic activity. After conversion to the triphosphate, beta-thioguanine deoxyriboside is incorporated into DNA, resulting in inhibition of DNA replication. This agent is cytotoxic against leukemia cell lines and has demonstrated some activity against leukemia cells in vivo. Beta-thioguanine deoxyriboside demonstrates antineoplastic activity against 6-thioguanine-resistant tumor cells. 39712 thalicarpine A natural aporphine benzylisoquinoline vinca alkaloid with antineoplastic activity. Thalicarpine binds to and inhibits p-glycoprotein, the multidrug resistance efflux pump. Thalicarpine also induces single-strand breaks in DNA and arrests cancer cells at the G2/M and G1 phase of the cell cycle. 39713 thiabendazole A benzimidazole derivative with anthelminthic property. Although the mechanism of action has not been fully elucidated, thiabendazole inhibits the helminth-specific mitochondrial enzyme fumarate reductase, thereby inhibiting the citric acid cycle, mitochondrial respiration and subsequent production of ATP, ultimately leading to helminth's death. In addition, it has been suggested that thiabendazole may lead to inhibition of microtubule polymerization by binding to beta-tubulin and has an overt ovicidal effect with regard to some trichostrongylids. 39714 timonacic A cyclic sulfur amino acid derivative with potential antineoplastic and antioxidant activities. Acting on cellular membranes of malignant cells through an unknown mechanism, timonacic may induce malignant cells to revert back to an untransformed state. This agent may also restore contact inhibition, a phenomenon characterized by the paracrine inhibition of mitosis following the formation of a critical cell mass, presumably the result of cell-to-cell signal transfer. Timonacic may also produce antioxidant effects secondary to its release of cysteine and restoration of glutathione concentrations. C2354 39715 thymidine A pyrimidine nucleoside that is composed of the pyrimidine base thymine attached to the sugar deoxyribose. As a constituent of DNA, thymidine pairs with adenine in the DNA double helix. 39716 thymosin A hormone secreted by the thymus gland and effects T-lymphocyte differentiation and activation. C2284 39717 tiazofurin A synthetic nucleoside analogue with antineoplastic activity. Tiazofurin (TR) is anabolized intracellularly to an analogue of NAD, tiazole-4-carboxamide adenine dinucleotide (TAD), a potent inhibitor of IMP dehydrogenase (IMPDH); IMPDH is the rate-limiting enzyme for de novo purine synthesis. Inhibition of IMPDH results in reduced levels of guanylates, resulting in the inhibition tumor cell growth in vitro and in vivo. 39719 trimethylcolchicinic acid A colchicine analog with potential antineoplastic activity. Trimethylcolchicinic acid binds to tubulin, inhibiting its polymerization into microtubules and preventing cell division. 39720 treosulfan The prodrug of a bifunctional sulfonate alkylating agent with myeloablative, immunosuppresive, and antineoplastic activities. Under physiological conditions, treosulfan converts nonenzymatically to L-diepoxybutane via a monoepoxide intermediate. The monoepoxide intermediate and L-diepoxybutane alkylate DNA at guanine residues and produce DNA interstrand crosslinks, resulting in DNA fragmentation and apoptosis. In escalated doses, this agent also exhbits myeloablative and immunosuppressive activities. 39722 teroxirone A triazene triepoxide with antineoplastic activity. Teroxine alkylates and cross-links DNA, thereby inhibiting DNA replication. 39723 triciribine phosphate The phosphate salt of the synthetic, cell-permeable tricyclic nucleoside triciribine with potential antineoplastic activity. Triciribine inhibits the phosphorylation, activation, and signalling of Akt-1, -2, and -3, which may result in the inhibition of Akt-expressing tumor cell proliferation. Akts are anti-apoptotic serine/theronine-specific protein kinases that phosphorylate and inactivate components of the apoptotic machinery, including Bcl-xL/Bcl-2-associated death promoter (BAD) and caspase 9. C1262 39724 trimethoprim-sulfamethoxazole A synthetic combination of two antibacterial agents, trimethoprim and sulfamethoxazole. This synergistic combination, also known as co-trimoxazole, inhibits two sequential steps in the bacterial metabolism of folic acid. Trimethoprim is a pyrimidine inhibitor of dihydrofolate reductase; sulfamethoxazole is a sulfamide inhibitor of bacterial dihydrofolate synthetase. 39725 trofosfamide An orally bioavailable oxazaphosphorine prodrug with antineoplastic activity. Trofosfamide (TFF) is metabolized predominantly to the cyclophosphamide analogue ifosfamide (IFO), which is then metabolized by liver cytochrome P450s to the active isophosphoramide mustard (IPM). IPM alkylates DNA to form DNA-DNA cross-links, which may result in inhibition of DNA, RNA and protein synthesis, and tumor cell apoptosis. C1268 39727 tobramycin sulfate The sulfate salt of tobramycin, an aminoglycoside antibiotic derived from the bacterium Streptomyces tenebrarius with bactericidal activity. Following active transport into the cell, tobramycin binds irreversibly to a specific aminoglycoside receptor on the bacterial 30S ribosomal subunit and fixes the 30 S-50 S ribosomal complex at the start codon (AUG), interfering with the initiation of protein synthesis. In addition, this agent induces misreading of the mRNA template, which results in 1) detachment of the ribosomal complex and inhibition of protein elongation or 2) incorporation of the incorrect amino acids into the growing polypeptide chain and the production of abnormal or nonfunctional proteins. Altogether, cell permeability is altered and cell death ensues. C893 39728 tubercidin An antibiotic and adenosine analog isolated from the bacterium Streptomyces tubercidicus with potential antineoplastic activity. Tubercidin is incorporated into DNA and inhibits polymerases, thereby inhibiting DNA replication and RNA and protein synthesis. This agent also exhibits antifungal and antiviral activities. 39730 verapamil A phenylalkylamine calcium channel blocking agent. Verapamil inhibits the transmembrane influx of extracellular calcium ions into myocardial and vascular smooth muscle cells, causing dilatation of the main coronary and systemic arteries and decreasing myocardial contractility. This agent also inhibits the drug efflux pump P-glycoprotein which is overexpressed in some multi-drug resistant tumors and may improve the efficacy of some antineoplastic agents. 39732 vindesine A synthetic derivative of vinblastine, a naturally occurring vinca alkaloid. Vindesine binds to and stabilizes tubulin, thereby interrupting tubulin polymerization and preventing the formation of the mitotic spindle and cell division; treated cells are unable to undergo mitosis and are arrested in metaphase. This agent also disrupts macromolecular synthesis. 39734 cholecalciferol A steroid hormone produced in the skin when exposed to ultraviolet light or obtained from dietary sources. The active form of cholecalciferol, 1,25-dihydroxycholecalciferol (calcitriol) plays an important role in maintaining blood calcium and phosphorus levels and mineralization of bone. The activated form of cholecalciferol binds to vitamin D receptors and modulates gene expression. This leads to an increase in serum calcium concentrations by increasing intestinal absorption of phosphorus and calcium, promoting distal renal tubular reabsorption of calcium and increasing osteoclastic resorption. 39735 vitamin A compound The fat soluble vitamin retinol. Vitamin A binds to and activates retinoid receptors (RARs), thereby inducing cell differentiation and apoptosis of some cancer cell types and inhibiting carcinogenesis. Vitamin A plays an essential role in many physiologic processes, including proper functioning of the retina, growth and differentiation of target tissues, proper functioning of the reproductive organs, and modulation of immune function. 39737 ascorbic acid A natural water-soluble vitamin (Vitamin C). Ascorbic acid is a potent reducing and antioxidant agent that functions in fighting bacterial infections, in detoxifying reactions, and in the formation of collagen in fibrous tissue, teeth, bones, connective tissue, skin, and capillaries. Found in citrus and other fruits, and in vegetables, vitamin C cannot be produced or stored by humans and must be obtained in the diet. 39739 yoshi-864 An alkylsulfonate. Yoshi-864 alkylates and crosslinks DNA, thereby inhibiting DNA replication. 39740 warfarin A synthetic anticoagulant. Warfarin appears to inhibit the regeneration of vitamin K1 epoxide and so the synthesis of vitamin K dependent clotting factors, which include Factors II, VII, IX and X, and the anticoagulant proteins C and S. This inhibition results in a sequential depression of Factors VII, IX, X and II activities. Vitamin K is an essential cofactor for the post ribosomal synthesis of the vitamin K dependent clotting factors. The vitamin promotes the biosynthesis of gamma-carboxyglutamic acid residues in these proteins which are essential for biological activity. 39741 amifostine trihydrate The trihydrate form of a phosphorylated aminosulfhydryl compound. After dephosphorylation of amifostine by alkaline phosphatase to an active free sulfhydryl (thiol) metabolite, the thiol metabolite binds to and detoxifies cytotoxic platinum-containing metabolites of cisplatin and scavenges free radicals induced by cisplatin and ionizing radiation. The elevated activity of this agent in normal tissues results from both the relative abundance of alkaline phosphatase in normal tissues and the greater vascularity of normal tissues compared to tumor tissues. 39748 cyclophosphamide A synthetic alkylating agent chemically related to the nitrogen mustards with antineoplastic and immunosuppressive activities. In the liver, cyclophosphamide is converted to the active metabolites aldophosphamide and phosphoramide mustard, which bind to DNA, thereby inhibiting DNA replication and initiating cell death. 39751 caracemide An agent derived from acetohydroxamic acid with potential antineoplastic activity. Caracemide inhibits ribonuclease reductase, resulting in decreased DNA synthesis and tumor growth; it also inhibits acetylcholinesterase. In vivo, caracemide contributes to the formation of the neurotoxin methyl isocyanate; this effect, along with the agent's acetylcholinesterase activity, may be responsible for the severe central nervous system toxicity observed in clinical trials. 39752 chlorpromazine A phenothiazine and traditional antipsychotic agent with anti-emetic activity. Chlorpromazine exerts its antipsychotic effect by blocking postsynaptic dopamine receptors in cortical and limbic areas of the brain, thereby preventing the excess of dopamine in the brain. This leads to a reduction in psychotic symptoms, such as hallucinations and delusions. Chlorpromazine appears to exert its anti-emetic activity by blocking the dopamine receptors in the chemical trigger zone (CTZ) in the brain, thereby relieving nausea and vomiting. 39753 idarubicin A semisynthetic 4-demethoxy analogue of the antineoplastic anthracycline antibiotic daunorubicin. Idarubicin intercalates into DNA and interferes with the activity of topoisomerase II, thereby inhibiting DNA replication, RNA transcription and protein synthesis. Due to its high lipophilicity, idarubicin penetrates cell membranes more efficiently than other anthracycline antibiotic compounds. 39754 eflornithine A difluoromethylated ornithine compound with antineoplastic activity. Eflornithine irreversibly inhibits ornithine decarboxylase, an enzyme required for polyamine biosynthesis, thereby inhibiting the formation and proliferation of tumor cells. Polyamines are involved in nucleosome oligomerization and DNA conformation, creating a chromatin environment that stimulates neoplastic transformation of cells. This agent has been shown to induce apoptosis in leiomyoma cells. 39756 aldesleukin A recombinant analog of the endogenous cytokine interleukin-2 (IL-2) with immunoregulatory and antineoplastic activities. Aldesleukin binds to and activates the IL-2 receptor, followed by heterodimerization of the cytoplasmic domains of the IL-2R beta and gamma(c) chains; activation of the tyrosine kinase Jak3; and phosphorylation of tyrosine residues on the IL-2R beta chain, resulting in an activated receptor complex. Various cytoplasmic signaling molecules are recruited to the activated receptor complex and become substrates for regulatory enzymes that are associated with the receptor complex. This agent enhances lymphocyte mitogenesis; stimulates long-term growth of human IL-2 dependent cell lines; enhances lymphocyte cytotoxicity; induces lymphokine-activated killer (LAK) cell and natural killer (NK) cell activities; and induces expression of interferon-gamma. Aldesleukin may induce T cell-mediated tumor regression in some tumor types. 39757 lorazepam A benzodiazepine with anxiolytic, anti-anxiety, anticonvulsant, anti-emetic and sedative properties. Lorazepam enhances the effect of the inhibitory neurotransmitter gamma-aminobutyric acid on the GABA receptors by binding to a site that is distinct from the GABA binding site in the central nervous system. This leads to an increase in chloride channel opening events, a facilitation of chloride ion conductance, membrane hyperpolarization, and eventually inhibition of the transmission of nerve signals, thereby decreasing nervous excitation. 39758 marcellomycin An antineoplastic oligosaccharide anthracycline antineoplastic antibiotic isolated from the bacterium Actinosporangium bohemicum. Marcellomycin intercalates into DNA and induces DNA crosslinks, thereby inhibiting DNA replication and repair and RNA and protein synthesis. This agent also induces differentiation in HL-60 promyelocytic leukemia cells by interfering with glycoprotein synthesis. 39759 mesna A sulfhydryl compound that is used to reduce the incidence of hemorrhagic cystitis associated with certain chemotherapeutic agents. Mesna is converted to a free thiol compound in the kidney, where it binds to and inactivates acrolein and other urotoxic metabolites of ifosfamide and cyclophosphamide, thereby reducing their toxic effects on the urinary tract during urinary excretion. 39760 nabilone A synthetic cannabinoid and dibenzopyrane derivative with anti-emetic activity. Although the mechanism of action has not been fully elucidated yet, it has been suggested that nabilone is a highly selective and strong agonist for the cannabinoid receptors CB1 and CB2, both of which are coupled to Gi/o proteins. The CB1 receptors are expressed predominantly in central and peripheral neurons and receptor stimulation has been implicated in the reduction of chemotherapy-induced nausea. 39761 piroxicam A nonsteroidal oxicam derivative with anti-inflammatory, antipyretic and analgesic properties. As a non-selective, nonsteroidal anti-inflammatory drug (NSAID), piroxicam binds and chelates both isoforms of cyclooxygenases (COX1 and COX2), thereby stalling phospholipase A2 activity and conversion of arachidonic acid into prostaglandin precursors at the rate limiting cyclooxygenase enzyme step. This results in inhibition of prostaglandin biosynthesis. As a second, independent effect, piroxicam inhibits the activation of neutrophils thereby contributing to its overall anti-inflammatory effects. 39762 paclitaxel A compound extracted from the Pacific yew tree Taxus brevifolia with antineoplastic activity. Paclitaxel binds to tubulin and inhibits the disassembly of microtubules, thereby resulting in the inhibition of cell division. This agent also induces apoptosis by binding to and blocking the function of the apoptosis inhibitor protein Bcl-2 (B-cell Leukemia 2). 39763 spiroplatin A synthetic derivative of cyclohexane sulfatoplatinum with antineoplastic properties. Spiroplatin induces DNA cross-links, thereby inhibiting DNA replication and RNA and protein synthesis. Similar to other platinum compounds, this agent has been shown to be mutagenic and carcinogenic. 39764 trimetrexate glucuronate A lipid soluble methotrexate derivative with potential antineoplastic activity. Trimetrexate glucuronate inhibits the enzyme dihydrofolate reductase, thereby preventing the synthesis of purine nucleotides and thymidylate, with subsequent inhibition of DNA and RNA synthesis. Trimetrexate glucuronate also exhibits antiviral activity. 39765 pyridoxine hydrochloride The hydrochloride salt of pyridoxine, a water-soluble B vitamin. Pyridoxine is converted in the liver into the metabolically active coenzyme form pyridoxal 5'-phosphate (P5P), an essential cofactor in many enzymatic reactions in amino acid metabolism, including transamination, deamination, and decarboxylation. P5P is required for glycogenolysis and the synthesis of sphingolipids and is essential to red blood cell, nervous system, and immune system functions. C48030 39768 dacarbazine A triazene derivative with antineoplastic activity. Dacarbazine alkylates and cross-links DNA during all phases of the cell cycle, resulting in disruption of DNA function, cell cycle arrest, and apoptosis. 39779 daunorubicin hydrochloride The hydrochloride salt of an anthracycline antineoplastic antibiotic with therapeutic effects similar to those of doxorubicin. Daunorubicin exhibits cytotoxic activity through topoisomerase-mediated interaction with DNA, thereby inhibiting DNA replication and repair and RNA and protein synthesis. 39786 acodazole A synthetic imidazoquinoline with antineoplastic activity. Acodazole intercalates into DNA, resulting in disruption of DNA replication. Use of this agent has been associated with significant cardiotoxicity. 39789 dexamethasone A synthetic adrenal corticosteroid with potent anti-inflammatory properties. In addition to binding to specific nuclear steroid receptors, dexamethasone also interferes with NF-kB activation and apoptotic pathways. This agent lacks the salt-retaining properties of other related adrenal hormones. 39811 flutamide A toluidine derivative and nonsteroidal antiandrogen that is structurally related to bicalutamide and nilutamide. Flutamide and its more potent active metabolite 2-hydroxyflutamide competitively block dihydrotestosterone binding at androgen receptors, forming inactive complexes which cannot translocate into the cell nucleus. Formation of inactive receptors inhibits androgen-dependent DNA and protein synthesis, resulting in tumor cell growth arrest or transient tumor regression. 39812 trilostane A synthetic derivative of androstane with adrenocortical suppressive properties. Trilostane reversibly inhibits 3 beta-hydroxysteroid dehydrogenase delta 5-4 isomerase in the adrenal cortex, resulting in the decreased synthesis of mineralocorticoids and glucocorticoids and the decreased conversion of pregnenolone to progesterone. 39813 medroxyprogesterone A synthetic derivative of progesterone administered as an acetate salt (medroxyprogesterone acetate) with antiestrogenic activity. As a do all progestins, medroxyprogesterone binds to and activates nuclear receptors which subsequently bind to and activate target genes for transcription. As an antiestrogen, this agent may inhibit the growth-stimulating effects of estrogen on estrogen-sensitive tumor cells. 39861 hydrocortisone sodium succinate The sodium salt of hydrocortisone succinate with glucocorticoid property. Hydrocortisone sodium succinate is chemically similar to the endogenous hormone that stimulates anti-inflammatory and immunosuppressive activities, in addition to exhibiting minor mineralocorticoid effects. This agent binds to intracellular glucocorticoid receptors and is translocated into the nucleus, where it initiates the transcription of glucocorticoid-responsive genes, such as various cytokines and lipocortins. Lipocortins inhibit phospholipase A2, thereby blocking the release of arachidonic acid from membrane phospholipids and preventing the synthesis of prostaglandins and leukotrienes, both potent mediators of inflammation. 39974 didemnin B A cyclic depsipeptide extracted from the Caribbean tunicate Trididemnum cyanophorum. Didemnin B activates caspase, thereby inducing apoptosis, and prevents eukaryotic elongation factor 2 (eEF-2)-dependent translocation, thereby inhibiting protein synthesis. This agent also has immunosuppressive and antiviral properties. 39990 hexamethylene bisacetamide A hybrid polar-planar compound with potential antineoplastic activity that induces terminal differentiation, inhibits cell growth, and causes apoptosis in several tumor cell lines. Its precise mechanism of action is unknown. 40024 ifosfamide A synthetic analogue of the nitrogen mustard cyclophosphamide with antineoplastic activity. Ifosfamide alkylates and forms DNA crosslinks, thereby preventing DNA strand separation and DNA replication. This agent is a prodrug that must be activated through hydroxylation by hepatic microsomal enzymes. 40052 suramin A polysulphonated naphthylurea with potential antineoplastic activity. Suramin blocks the binding of various growth factors, including insulin-like growth factor I (IGF-I), epidermal growth factor (EGF), platelet-derived growth factor (PDGF), and tumor growth factor-beta (TGF-beta), to their receptors, thereby inhibiting endothelial cell proliferation and migration. This agent also inhibits vascular endothelial growth factor (VEGF)- and basic fibroblast growth factor (bFGF)-induced angiogenesis; retroviral reverse transcriptase; uncoupling of G-proteins from receptors; topoisomerases; cellular folate transport; and steroidogenesis. 40058 leuprolide acetate The acetate salt of a synthetic nonapeptide analogue of gonadotropin-releasing hormone. Leuprolide binds to and activates gonadotropin-releasing hormone (GnRH) receptors. Continuous, prolonged administration of leuprolide in males results in pituitary GnRH receptor desensitization and inhibition of pituitary secretion of follicle stimulating hormone (FSH) and luteinizing hormone (LH), leading to a significant decline in testosterone production; in females, prolonged administration results in a decrease in estradiol production. This agent reduces testosterone production to castration levels and may inhibit androgen receptor-positive tumor progression. 40070 piritrexim A synthetic antifolate agent with antiparasitic, antipsoriatic and antitumor properties. Piritrexim inhibits the enzyme dihydrofolate reductase enzyme, thereby disrupting folate metabolism and DNA synthesis and cell division. 40107 dihydrolenperone A butyrophenone that has been investigated for antineoplastic activity. 40109 therapeutic immune globulin A preparation of plasma proteins derived from the pooled plasma of adult donors. Largely comprised of IgG antibodies, therapeutic immune globulin provides passive immunization by increasing the recipient's serum levels of circulating antibodies. IgG antibodies have multiple functions, including binding to and neutralizing bacterial toxins; opsonization of pathogens; activation of complement; and suppression of pathogenic cytokines and phagocytes through binding to CD5, interleukin-1a (IL-1a), interleukin 6 (IL-6), tumor necrosis factor-alpha (TNF-alpha), and T-cell receptors. Therapeutic immune globulin may diminish pathogenic mechanisms in some autoimmune diseases by binding to and inhibiting the activity of autoantibodies. 40121 zidovudine A synthetic dideoxynucleoside. After intracellular phosphorylation to its active metabolite, zidovudine inhibits DNA polymerase, resulting in the inhibition of DNA replication and cell death. This agent also decreases levels of available pyrimidines. 40122 diltiazem hydrochloride A benzothiazepine calcium channel blocking agent. Diltiazem hydrochloride inhibits the transmembrane influx of extracellular calcium ions into select myocardial and vascular smooth muscle cells, causing dilatation of coronary and systemic arteries and decreasing myocardial contractility. Because of its vasodilatory activity, this agent has been shown to improve the microcirculation in some tumors, thereby potentially improving the delivery of antineoplastic agents to tumor cells. 40141 hydrazine sulfate The synthetic sulfate salt of hydrazine, a derivative of ammonia. Hydrazine inhibits the enzyme phosphoenol pyruvate carboxykinase, thereby blocking gluconeogenesis. This agent has been reported to decrease the excessive energy needs and cachexia of cancer patients. Classified as a likely human carcinogen, hydrazine sulfate is also a weak inhibitor of mono-amine oxidase (MAO). 40152 flavone acetic acid A synthetic flavonoid with vascular targeting properties. Flavone acetic acid exhibits an antiproliferative effect on endothelial cells as a result of a superoxide-dependent mechanism, which induces changes in permeability of the vasculature of the tumor. This agent may stimulate tumor necrosis and promote shunting of blood flow to viable regions of the tumor, increasing their oxygenation and rendering them more susceptible to the antitumor effects of hyperthermia and ionizing radiation. 40153 menogaril A semisynthetic derivative of the anthracycline antineoplastic antibiotic nogalamycin. Menogaril intercalates into DNA and interacts with topoisomerase II, thereby inhibiting DNA replication and repair and RNA and protein synthesis. This agent is less cardiotoxic than doxorubicin. 40214 amonafide dihydrochloride The dihydrochloride salt of amonafide, an imide derivative of naphthalic acid. Amonafide intercalates into DNA and inhibits topoisomerase II, resulting in protein-associated strand breaks and impaired DNA and RNA synthesis. 40219 lymphokine-activated killer cells Killer cell lymphocytes activated in the presence of interleukin-2 (IL-2). Lymphokine-activated killer cells (LAKs) are cytotoxic effector cells with an exceptionally wide target cell spectrum including normal and malignant cells of different origins. LAK cells exhibit a profound heterogeneity with regard to phenotype surface marker expression; it remains to be determined if they represent a unique cell lineage. 40222 naproxen A propionic acid derivative and a non-steroidal anti-inflammatory drug (NSAID) with anti-inflammatory, antipyretic and analgesic activities. Naproxen inhibits the activity of the enzymes cyclo-oxygenase I and II, resulting in a decreased formation of precursors of prostaglandins and thromboxanes. The resulting decrease in prostaglandin synthesis is responsible for the therapeutic effects of naproxen. Naproxen also causes a decrease in the formation of thromboxane A2 synthesis, by thromboxane synthase, thereby inhibiting platelet aggregation. 40223 probenecid A benzoic acid derivative with antihyperuricemic property. Probenecid competitively inhibits the active reabsorption of urate at the proximal tubule in the kidney thereby increasing urinary excretion of uric acid and lowering serum urate concentrations. This prevents urate deposition and promotes resolution of existing urate deposits. In addition, probenecid modulates the transport of organic acids and acidic drugs at the proximal and distal renal tubule, thereby increasing the drug serum concentration. 40224 goserelin A synthetic decapeptide analog of luteinizing hormone-releasing hormone (LHRH) with antineoplastic activity. Goserelin binds to and activates pituitary gonadotropin releasing hormone (GnRH) receptors. Prolonged administration of goserelin inhibits the secretion of pituitary gonadotropin, thereby decreasing levels of testosterone (in males) and estradiol (in females). Administration of this agent in a depot formulation may result in the regression of sex hormone-sensitive tumors and a reduction in sex organ size and function. 40240 recombinant macrophage colony-stimulating factor A recombinant therapeutic agent which is chemically identical to or similar to the endogenous protein cytokine macrophage colony-stimulating factor (M-CSF). Synthesized endogenously by mesenchymal cells, M-CSF stimulates the survival, proliferation, and differentiation of hematopoietic cells of the monocyte-macrophage series and can reverse treatment-related neutropenias. Recombinant M-CSF may also enhance antigen presentation and activate antitumoral cytotoxic T-cells. C1290 40247 diethyldithiocarbamate A sulfhydryl-containing carbamate that is the primary in vivo metabolite of disulfiram. Diethyldithiocarbamate chelates zinc, thereby inhibiting metalloproteinases, thereby preventing the degradation of the extracellular matrix and inhibiting an initial step in cancer metastasis and angiogenesis. A known inhibitor of superoxide dismutase, this agent can either potentiate or protect against cell oxidative damage caused by ionizing radiation, depending on the time of administration. 40250 recombinant tumor necrosis factor family protein A recombinant therapeutic agent which is chemically identical to or similar to one of a number of endogenous tumor necrosis factor (TNF) proteins. TNF family cytokines bind to and activate specific cell-surface receptors, thereby mediating inflammatory processes, cell proliferation, immunity, angiogenesis, and tumor cell cytotoxicity. One primary antitumor effect of TNFs involves stimulation of T cell-mediated antitumor cytotoxicity. 40293 methylene dimethane sulfonate A member of the homologous series of dimethane sulphonic acid esters with alkylating properties. Methylene dimethane sulfonate alkylates DNA, resulting in interstrand DNA crosslinking, inhibition of DNA replication, disruption of the cell cycle, and cell death. C1162 40294 porfimer sodium The sodium salt of a mixture of oligomers formed by ether and ester linkages of up to eight porphyrin units with photodynamic activity. Absorbed selectively by tumor cells, porfimer produces oxygen radicals after activation by 630 nm wavelength laser light, resulting in tumor cell cytotoxicity. In addition, tumor cell death may occur due to ischemic necrosis secondary to vascular occlusion that appears to be partly mediated by the release of thromboxane A2. 40295 cyanocobalamin An essential nutrient and natural water-soluble vitamin of the B-complex family that must combine with an intrinsic factor for absorption by the intestine. Cyanocobalamin is necessary for hematopoiesis, neural metabolism, DNA and RNA production, and carbohydrate, fat, and protein metabolism. B12 improves iron functions in the metabolic cycle and assists folic acid in choline synthesis. B12 metabolism is interconnected with that of folic acid. Vitamin B12 deficiency causes pernicious anemia, megaloblastic anemia, and neurologic lesions. C64333 40312 pegaspargase A complex of polyethylene glycol conjugated with L-asparaginase. Asparaginase hydrolyzes L-asparagine to L-aspartic acid and ammonia, thereby depleting these cells of asparagine and blocking protein synthesis and tumor cell proliferation, especially in the G1 phase of the cell cycle. The agent also induces apoptosis in tumor cells. Pegylation decreases the enzyme's antigenicity. Asparagine is critical to protein synthesis in leukemic cells, which cannot synthesize this amino acid due to the absence of the enzyme asparagine synthase. 40313 retinyl acetate A naturally-occurring fatty acid ester form of retinol (vitamin A) with potential antineoplastic and chemopreventive activities. Retinyl acetate binds to and activates retinoid receptors, inducing cell differentiation and decreasing cell proliferation. This agent also inhibits carcinogen-induced neoplastic transformation in some cancer cell types and exhibits immunomodulatory properties. 40324 pentamidine A synthetic derivative of amidine with antiprotozoal and antifungal activities. Although the precise mode of action of pentamidine is unclear, it appears to interact directly with the pathogen genome by binding to AT-rich regions of duplex DNA and the minor groove of DNA, thereby interfering with DNA replication. 40325 ribavirin A synthetic nucleoside analogue of ribofuranosyl with antiviral activity. Ribavirin incorporates into viral nucleic acid, inhibits viral ribonucleic acid (RNA) synthesis, induces viral genome mutations, and inhibits normal viral replication. Ribavirin shows activity against a variety of RNA viruses, especially hepatitis C virus. 40346 AZP An aziridinyl-substituted cyclophosphazene and a putrescence derivative that may cause DNA cross-linkage. 40349 zalcitabine A synthetic dideoxynucleoside. After intracellular phosphorylation to its active metabolite, zalcitabine preferentially inhibits the gamma form of DNA polymerase present in tumor cell mitochondria, resulting in the inhibition of tumor cell mitochondrial DNA replication and tumor cell death. 40350 pentosan polysulfate sodium The sodium salt of a semisynthetic heparin-like glucosaminoglycan. Although its mechanism of action is unknown, pentosan polysulfate may act as a buffer to control cell permeability by preventing irritating solutes from reaching cells coated with it. Administered orally, excreted pentosan polysulfate adheres to the urinary bladder wall, preventing irritants from entering bladder cells and the development or progression of interstitial cystitis (IC), a complication of some chemotherapies. This agent also exhibits anticoagulant and fibrinolytic properties. 40369 gusperimus A derivative of the antitumor antibiotic spergualin with immunosuppressant activity. Gusperimus inhibits the interleukin-2-stimulated maturation of T cells to the S and G2/M phases and the polarization of the T cells into IFN-gamma-secreting Th1 effector T cells, resulting in the inhibition of growth of activated naive CD4 T cells; this agent may suppress growth of certain T-cell leukemia cell lines. 40446 trifluoperazine hydrochloride The hydrochloride salt of trifluoperazine, a phenothiazine derivative and a dopamine, alpha-adrenergic, and anticholinergic antagonist with antipsychotic, anxiolytic, and antiemetic activities. Trifluoperazine blocks central dopamine receptors, which may prevent or mitigate delusions and hallucinations caused by an excess of dopamine; dopamine blockade in the chemoreceptor trigger zone (CTZ) may result in an antiemetic effect. This agent binds to central adrenergic receptors, which may result in anxiolytic effects.Trifluoperazine also functions as a calmodulin inhibitor, elevating cytosolic calcium. C904 40449 vinorelbine ditartrate The ditartrate salt of a semisynthetic vinca alkaloid derived from the leaves of the periwinkle plant (Vinca rosea) with antineoplastic activity. Vinorelbine binds to tubulin, thereby inhibiting tubulin polymerization into microtubules and spindle formation and resulting in apoptosis of susceptible cancer cells. Inhibition of mitotic microtubules correlates with antitumor activity, whereas inhibition of axonal microtubules seems to correlate with vinorelbine's neurotoxicity. Compared to related vinca alkaloids, vinorelbine is more selective against mitotic than axonal microtubules in vitro, which may account for its decreased neurotoxicity. This agent is also a radiation-sensitizing agent. 40450 nilutamide A synthetic, nonsteroidal agent with antiandrogenic properties. Nilutamide preferentially binds to androgen receptors and blocks androgen receptor activation by testosterone and other androgens; this agent may inhibit androgen-dependent growth of normal and neoplastic prostate cells. 40462 polyethylene glycol Additional polymers of ethylene oxide and water and their ethers. They vary in consistency from liquid to solid, depending on the molecular weight, indicated by a number following the name. Used as surfactants in industry, including foods, cosmetics and pharmaceutics; in biomedicine, as dispersing agents, solvents, ointment and suppository bases, vehicles, tablet excipients. Some specific groups are lauromagrogols, nonoxynols, octoxynols and poloxamers. (MSH2002_06_01) 40467 recombinant interferon alfa A class of naturally-isolated or recombinant therapeutic peptides used as antiviral and anti-tumor agents. Alpha interferons are cytokines produced by nucleated cells (predominantly natural killer (NK) leukocytes) upon exposure to live or inactivated virus, double-stranded RNA or bacterial products. These agents bind to specific cell-surface receptors, resulting in the transcription and translation of genes containing an interferon-specific response element. The proteins so produced mediate many complex effects, including antiviral effects (viral protein synthesis); antiproliferative effects (cellular growth inhibition and alteration of cellular differentiation); anticancer effects (interference with oncogene expression); and immune-modulating effects (natural killer cell activation, alteration of cell surface antigen expression, and augmentation of lymphocyte and macrophage cytotoxicity). 40468 recombinant interferon beta A recombinant protein which is chemically identical to or similar to endogenous interferon beta with antiviral and anti-tumor activities. Endogenous interferons beta are cytokines produced by nucleated cells (predominantly natural killer cells) upon exposure to live or inactivated virus, double-stranded RNA or bacterial products. These agents bind to specific cell-surface receptors, resulting in the transcription and translation of genes with an interferon-specific response element. The proteins so produced mediate many complex effects, including antiviral (the most important being inhibition of viral protein synthesis), antiproliferative and immune modulating effects. The recombinant therapeutic forms of interferon beta are interferon beta 1-a and interferon beta 1-b. C495 40469 recombinant interferon gamma A recombinant therapeutic agent which is chemically identical to or similar to the endogenous lymphokine interferon gamma (IFN-gamma) with antineoplastic, immunoregulatory, and antiviral activities. Therapeutic IFN-gamma binds to and activates the cell-surface IFN-gamma receptor, stimulating antibody-dependent cytotoxicity and enhances natural killer cell attachment to tumor cells. This agent also activates caspases, thereby inducing apoptosis in malignant cells. 40474 perfosfamide The active metabolite of the nitrogen mustard cyclophosphamide with potent antineoplastic and immunosuppressive properties. Perfosfamide alkylates DNA, thereby inhibiting DNA replication and RNA and protein synthesis. 40475 ibuprofen A propionic acid derivate and nonsteroidal anti-inflammatory drug (NSAID) with anti-inflammatory, analgesic, and antipyretic effects. Ibuprofen inhibits the activity of cyclo-oxygenase I and II, resulting in a decreased formation of precursors of prostaglandins and thromboxanes. This leads to decreased prostaglandin synthesis, by prostaglandin synthase, the main physiologic effect of ibuprofen. Ibuprofen also causes a decrease in the formation of thromboxane A2 synthesis, by thromboxane synthase, thereby inhibiting platelet aggregation. 40490 L-leucovorin The active l-isomer of the racemic mixture of the 5-formyl derivative of tetrahydrofolic acid. Metabolically active, l-leucovorin, also known levoleucovorin, does not require bioactivation by dihydrofolate reductase, an enzyme inhibited by folic acid antagonists. This agent may enhance the effects of fluoropyrimidines by stabilizing their binding to the enzyme thymidylate synthase. 40563 codeine phosphate The phosphate salt of codeine, a naturally occurring phenanthrene alkaloid and opioid agonist with analgesic, antidiarrheal and antitussive activities. Codeine mimics the actions of endogenous opioids by binding to the opioid receptors at many sites within the central nervous system (CNS). Stimulation of mu-subtype opioid receptors results in a decrease in the release of nociceptive neurotransmitters such as substance P, GABA, dopamine, acetylcholine and noradrenaline; in addition, the codeine metabolite morphine induces opening of G-protein-coupled inwardly rectifying potassium (GIRK) channels and blocks the opening of N-type voltage-gated calcium channels, resulting in hyperpolarization and reduced neuronal excitability. Stimulation of gut mu-subtype opioid receptors results in a reduction in intestinal motility and delayed intestinal transit times. Antitussive activity is mediated through codeine’s action on the cough center in the medulla. C74548 40564 fazarabine An orally-active pyrimidine analogue of an aza-substituted cytidine in which the ribose moiety is replaced by an arabinose sugar. Similar in action to cytarabine, fazarabine is phosphorylated by deoxycytidine kinase to a triphosphate form which competes with thymidine for incorporation into DNA; its incorporation into DNA inhibits DNA synthesis, resulting in tumor cell death and tumor necrosis. The presence of deoxycytidine kinase in a tumor is a determinant of tumor sensitivity to this drug. 40565 ganciclovir A synthetic guanine derivative with antiviral activity. As the active metabolite of ganciclovir, ganciclovir-5-triphosphate (ganciclovir-TP) appears to inhibit viral DNA synthesis by competitive inhibition of viral DNA polymerases and incorporation into viral DNA, resulting in eventual termination of viral DNA elongation. 40566 sargramostim A recombinant therapeutic agent which is chemically identical to or similar to endogenous human GM-CSF. Binding to specific cell surface receptors, sargramostim modulates the proliferation and differentiation of a variety of hematopoietic progenitor cells with some specificity towards stimulation of leukocyte production and may reverse treatment-induced neutropenias. This agent also promotes antigen presentation, up-regulates antibody-dependent cellular cytotoxicity (ADCC), and increases interleukin-2-mediated lymphokine-activated killer cell function; it may also augment host antitumoral immunity. 40569 ketorolac A synthetic pyrrolizine carboxylic acid derivative with anti-inflammatory, analgesic, and antipyretic activities. Ketorolac non-selective inhibits the enzymes cyclooxygenase 1 (COX-1) and COX-2. The inhibition of COX-2, up-regulated at sites of inflammation, prevents conversion of arachidonic acid to pro-inflammatory prostaglandins. The inhibition of COX-1 by this agent prevents the normal steady-state production of prostaglandins that play housekeeping roles in the protection of the gastrointestinal tract, the regulation of renal blood flow, and platelet aggregation. As a result, the inhibition of COX-1 may be associated with gastrointestinal toxicity, nephrotoxicity, and the inhibition of platelet aggregation. 40650 recombinant human chorionic gonadotropin A recombinant therapeutic agent which is chemically identical to or similar to the endogenous glycoprotein hormone human chorionic gonadotropin (HCG). HCG binds to cells of the corpus luteum, thereby stimulating progesterone production and helping to maintain a secretory endometrium. C528 40685 hydroxyurea A monohydroxyl-substituted urea (hydroxycarbamate) antimetabolite. Hydroxyurea selectively inhibits ribonucleoside diphosphate reductase, an enzyme required to convert ribonucleoside diphosphates into deoxyribonucleoside diphosphates, thereby preventing cells from leaving the G1/S phase of the cell cycle. This agent also exhibits radiosensitizing activity by maintaining cells in the radiation-sensitive G1 phase and interfering with DNA repair. 40693 ondansetron A carbazole derivative with antiemetic activity. As a selective serotonin receptor antagonist, ondansetron competitively blocks the action of serotonin at 5HT3 receptors, resulting in suppression of chemotherapy- and radiotherapy-induced nausea and vomiting. 40783 amoxicillin-clavulanate potassium A combination of the semisynthetic broad-spectrum antibiotic amoxicillin and the beta-lactamase enzyme inhibitor clavulanate potassium. Clavulanate potassium increases the serum half-life of amoxicillin by inhibiting beta-lactamase-mediated metabolism of amoxicillin. Amoxicillin inhibits bacterial cell wall synthesis by binding to penicillin binding proteins and inhibiting peptidoglycan synthesis, a critical component of bacterial cell walls. C1023 40784 ciprofloxacin A synthetic broad spectrum fluoroquinolone antibiotic. Ciprofloxacin binds to and inhibits bacterial DNA gyrase, an enzyme essential for DNA replication. This agent is more active against Gram-negative bacteria than Gram-positive bacteria. 40791 piroxantrone An anthrapyrazole antineoplastic antibiotic. Piroxantrone intercalates into DNA and interacts with topoisomerase II, thereby inhibiting DNA replication and repair and RNA and protein synthesis. Although less cardiotoxic than doxorubicin, this agent exhibits a narrow spectrum of antineoplastic activity. 40793 recombinant interleukin-1-beta A recombinant therapeutic agent which is chemically identical to or similar to the endogenous protein cytokine interleukin 1 (IL-1)-beta. Produced by monocytes and activated macrophages, endogenous mature IL-1 is generated through proteolytic cleavage by proteases such as IL-1-beta converting enzyme (ICE). This agent promotes angiogenesis, fibroblast proliferation, and neutrophil chemotaxis; it also regulates the functions of lymphocytes and epithelial cells and is involved in the 'acute phase response' to infection. 40795 penicillin V potassium The potassium salt of penicillin V, a member of the penicillin antibiotic family with broad-spectrum bactericidal activity. Penicillin V binds to and inactivates penicillin-binding proteins (PBPs), enzymes located on the inner membrane of the bacterial cell wall, resulting in the weakening of the bacterial cell wall and cell lysis. PBPs participate in the terminal stages of assembling the bacterial cell wall, and in reshaping the cell wall during cell division. Inactivation of PBPs interferes with the cross-linkage of peptidoglycan chains necessary for bacterial cell wall strength and rigidity. C730 40799 dideoxyadenosine A synthetic nucleoside analogue of deoxyadenosine and a prodrug of didanosine in which the 3' hydroxyl group on the ribose moiety is replaced by a hydrogen atom. Dideoxyadenosine competitively inhibits adenylyl cyclase, thereby reducing levels of cyclic adenosine monophosphate (cAMP). By inhibiting cAMP-mediated gene activation in tumor cells, this agent may retard tumor cell proliferation. 40800 uridine A nucleoside consisting of uracil and D-ribose and a component of RNA. Uridine has been studied as a rescue agent to reduce the toxicities associated with 5-fluorouracil (5-FU), thereby allowing the administration of higher doses of 5-FU in chemotherapy regimens. 40810 foscarnet sodium The trisodium salt of a synthetic organic analogue of inorganic pyrophosphate with antiviral activity. Foscarnet selectively blocks the pyrophosphate binding site of herpesvirus-specific DNA polymerases at concentrations that do not affect cellular DNA polymerases. This agent does not require phosphorylation by thymidine kinase (TK) or other kinases and therefore is active in vitro against herpes simplex virus (HSV) TK deficient mutants and cytomegalovirus (CMV) UL97 mutants. Because foscarnet crosses the blood brain barrier, it may be used in the treatment of viral infections of the CNS. C1193 40817 caffeine A naturally occurring xanthine derivative with central nervous system (CNS) stimulating activity. Due to the structural similarity to adenosine, caffeine binds to and blocks adenosine receptors, thereby preventing the inhibitory effects of adenosine on nerve cells. This leads to stimulation of medullary, vagal, vasomotor, and respiratory centers in the brain; and the release of epinephrine. Physiologic responses can include bradycardia, tachycardia, vasoconstriction, CNS excitablility, increased respiratory rate, increased blood pressure, increased blood flow to muscles, decreased blood flow to skin and inner organs, and release of glucose by the liver. Due to the interaction between adenosine A2A and dopamine D2 receptors, caffeine can also indirectly increase the levels of dopamine in the brain. 40818 naltrexone hydrochloride The hydrochloride salt of naltrexone, a noroxymorphone derivative with competitive opioid antagonistic activity. Naltrexone and its metabolite 6-beta-naltrexol reverse the effects of opioids by binding to various opioid receptors in the central nervous system CNS), including the mu-, kappa- and gamma-opioid receptors; opioid effects of analgesia, euphoria, sedation, respiratory depression, miosis, bradycardia, and physical dependence are inhibited. Naltrexone is longer-acting and more potent compared to naloxone. C679 40842 fluconazole A synthetic triazole with antifungal activity. Fluconazole preferentially inhibits fungal cytochrome P-450 sterol C-14 alpha-demethylation, resulting in the accumulation of fungal 14 alpha-methyl sterols, the loss of normal fungal sterols, and fungistatic activity. Mammalian cell demethylation is much less sensitive to fluconazole inhibition. 40848 heparin A sulfur-rich glycosaminoglycan with anticoagulant property. Heparin binds to antithrombin III to form a heparin-antithrombin III complex. The complex binds to and irreversibly inactivates thrombin and other activated clotting factors, such as factors IX, X, XI, and XII, thereby preventing the polymerization of fibrinogen to fibrin and the subsequent formation of clots. C539 40848 heparin A sulfur-rich glycosaminoglycan with anticoagulant property. Heparin binds to antithrombin III to form a heparin-antithrombin III complex. The complex binds to and irreversibly inactivates thrombin and other activated clotting factors, such as factors IX, X, XI, and XII, thereby preventing the polymerization of fibrinogen to fibrin and the subsequent formation of clots. C539 40860 m-azidopyrimethamine An antifolate derived from diaminopyrimidine with cytotoxic properties. With a mechanism of action similar to that of methotrexate (MTX), m-azidopyrimethamine blocks tetrahydrofolate synthesis, resulting in depletion of nucleotide precursors and inhibition of DNA, RNA and protein synthesis. This agent is more lipophilic but less potent than MTX. 40863 recombinant interferon One of a group of recombinant therapeutic glycoprotein cytokines with antiviral, anti-proliferative, and immunomodulating activities. Interferons bind to specific cell-surface receptors, leading to the transcription and translation of genes with interferon-specific response elements (ISREs). The resultant proteins mediate many complex effects, ultimately leading to inhibition of viral protein synthesis and cellular growth, alteration of cellular differentiation, interference with oncogene expression, activation of natural killer cells, alteration of cell surface antigen expression, and augmentation of lymphocyte and macrophage cytotoxicity. The production of endogenous interferons is induced in response to foreign agents such as bacteria, viruses and parasites and to tumor cells. C584 40886 brequinar A synthetic quinolinecarboxylic acid analogue with antineoplastic properties. Brequinar inhibits the enzyme dihydroorotate dehydrogenase, thereby blocking de novo pyrimidine biosynthesis. This agent may also enhance the in vivo antitumor effect of antineoplastic agents such as 5-FU. 40887 edatrexate A polyglutamatable folate antagonist analogue of methotrexate with antineoplastic activity. Edatrexate inhibits dihydrofolate reductase, thereby increasing cellular levels of polyglutamates, inhibiting thymidylate synthase and glycinamide ribonucleotide formyl transferase, impairing synthesis of purine nucleotides and amino acids, and resulting in tumor cell death. Edatrexate may overcome tumor resistance to methotrexate, which loses its activity after it is polyglutamated. 40888 mifepristone A derivative of the synthetic progestin norethindrone with antiprogesterone activity. Mifepristone competitively binds to the progesterone receptor, resulting in inhibition of the effects of endogenous or exogenous progesterone. This agent also exhibits antiglucocorticoid and weak antiandrogenic activities. 40931 CHOP regimen A chemotherapy regimen consisting of cyclophosphamide, hydroxydaunorubicin hydrochloride (doxorubicin hydrochloride), vincristine and prednisone used to treat both indolent and aggressive forms of non-Hodgkin lymphoma. C63450 40973 CAF regimen A chemotherapy regimen consisting of cyclophosphamide, doxorubicin hydrochloride (Adriamycin), and fluorouracil, which may be used in the adjuvant setting for the treatment of nonmetastatic breast cancer or alone for the treatment of metastatic breast cancer. C63417 40992 beta carotene A naturally-occurring retinol (vitamin A) precursor obtained from certain fruits and vegetables with potential antineoplastic and chemopreventive activities. As an anti-oxidant, beta carotene inhibits free-radical damage to DNA. This agent also induces cell differentiation and apoptosis of some tumor cell types, particularly in early stages of tumorigenesis, and enhances immune system activity by stimulating the release of natural killer cells, lymphocytes, and monocytes. 41004 therapeutic tumor infiltrating lymphocytes A preparation of cells, consisting of autologous tumor infiltrating lymphocytes, that are manipulated in vitro and, upon administration in vivo, re-infiltrate the tumor to initiate tumor cell lysis. In vitro, therapeutic tumor-infiltrating lymphocytes (TILs) are isolated from tumor tissue and cultured with lymphokines such as interleukin-2; the therapeutic TILs are then infused into the patient, where, after re-infiltration of the tumor, they may induce lysis of tumor cells and tumor regression. The use of therapeutic TILs is considered a form of adoptive immunotherapy. C28699 41023 flucytosine A pyrimidine compound and a fluorinated cytosine analog exhibiting antifungal activity. After penetration into the fungal cells, flucytosine is deaminated to its active metabolite 5-fluorouracil. 5-fluorouracil replaces uracil during fungal RNA synthesis, thereby inhibiting fungal protein synthesis. In addition, fluorouracil is further metabolized to 5-fluorodeoxyuridylic acid monophosphate, which inhibits thymidylate synthetase, thereby interrupting nucleotide metabolism, DNA synthesis and ultimately protein synthesis. 41025 fadrozole hydrochloride The hydrochloride salt of the nonsteroidal aromatase inhibitor fadrozole with potential antineoplastic activity. Fadrozole specifically inhibits aromatase, blocking the aromatization of androstenedione and testosterone into estrone and estradiol, respectively, the final step in estrogen biosynthesis; the reduction in estrogen levels may inhibit growth in estrogen-dependent cancers. Aromatase, a member of the cytochrome P-450 superfamily, is found in many tissues; overexpression has been linked to the development of preneoplastic and neoplastic changes in breast tissue. C1044 41055 chloroquinoxaline sulfonamide A chlorinated heterocyclic sulfanilamide with potential antineoplastic activity and potential immunosuppressive activity. Chloroquinoxaline sulfonamide poisons topoisomerase II alpha and topoisomerase II beta, thereby causing double-stranded breaks in DNA, accumulation of unrepaired DNA, and apoptosis. This agent also exhibits lymphotoxicity by inhibiting lymphocyte activation in a cell cycle-specific manner. 41056 midazolam hydrochloride The hydrochloride salt of a short-acting benzodiazepine derivative with an imidazole structure and anxiolytic, amnestic, hypnotic, anticonvulsant and sedative properties. Midazolam binds to the benzodiazepine receptor at the gamma-aminobutyric acid (GABA) receptor-chloride ionophore complex in the central nervous system (CNS), resulting in increases in the opening of chloride channels, membrane hyperpolarization, and the inhibitory effect of GABA. This agent may also interfere with the reuptake of GABA, thereby causing accumulation of GABA in the synaptic cleft. C654 41057 filgrastim A recombinant therapeutic agent which is chemically identical to or similar to the endogenous cytokine human granulocyte colony-stimulating factor (G-CSF). Produced endogenously by monocytes, fibroblasts, and endothelial cells, G-CSF binds to and activates specific cell surface receptors, stimulating neutrophil progenitor proliferation and differentiation and selected neutrophil functions. 41064 stavudine A synthetic nucleoside, analog of didehydro-3-deoxythymidine with potent antiretroviral activity. In vivo, stavudine is phosphorylated by cellular kinases to the active metabolite stavudine triphosphate; this metabolite inhibits the activity of HIV reverse transcriptase both by competing with the natural substrate deoxythymidine triphosphate and by incorporation into viral DNA causing a termination of DNA chain elongation (due to the lack the essential 3'-OH group). 41096 finasteride A synthetic 4-azasteroid compound. Finasteride competitively binds to and inhibits steroid type II 5-alpha-reductase in the prostate gland, liver, and skin, thereby interfering with the enzymatic conversion of testosterone to 5-dihydrotestosterone (DHT) and reducing serum DHT levels. The reduction in serum DHT levels results in diminished stimulation of androgen receptors in the nuclei of prostate cells and, so, diminished prostate cell proliferation. C1099 41102 epoetin alfa A recombinant therapeutic agent which is chemically identical to or similar to the endogenous cytokine human erythropoietin (EPO). Produced primarily by cells of the peritubular capillary endothelium of the kidney in response to hypoxia, circulating EPO binds to EPO receptors on the surface of committed erythroid progenitors in the bone marrow resulting in their replication and maturation into functional erythrocytes. 41103 toremifene A nonsteroidal triphenylethylene antiestrogen. Chemically related to tamoxifen, toremifene is a selective estrogen receptor modulator (SERM). This agent binds competitively to estrogen receptors, thereby interfering with estrogen activity. Toremifene also has intrinsic estrogenic properties, which are manifested according to tissue type or species. 41122 sulofenur A diarylsulfonylurea with potential antineoplastic activity. Sulofenur's antineoplastic mechanism of action is unknown. 41124 tryptophanase Encoded by human TDO2 Gene, 406-aa 48-kDa Tryptophanase is a homotetramer that may bind protoheme IV involved in tryptophan catabolism with broad specificity towards tryptamine and derivatives including tryptophan, 5-hydroxytryptophan, and serotonin. 41126 monoclonal antibody Lym-1 A murine IgG2a monoclonal antibody directed against the HLA-Dr10 protein, a cell surface marker present on over eighty percent of lymphoma cells. When conjugated with a radioactive isotope, Lym-1 monoclonal antibody selectively transports the cytotoxic radioisotope to HLA-Dr10-expressing tumor cells, thereby sparing healthy B-cells and normal tissues. This agent also mediates antibody-dependent cytotoxicity thereby promoting Raji B-lymphoid cell lysis by human neutrophils. 41146 asparaginase An enzyme isolated from the bacterium Escherichia coli or the bacterium Erwinia carotovora with antileukemic activity. Asparaginase hydrolyzes L-asparagine to L-aspartic acid and ammonia in leukemic cells, resulting in the depletion of asparagine, inhibition of protein synthesis, cell cycle arrest in the G1 phase, and apoptosis in susceptible leukemic cell populations. Asparagine is critical to protein synthesis in leukemic cells; some leukemic cells cannot synthesize this amino acid de novo due to the absent or deficient expression of the enzyme asparagine synthase. The E. carotovora-derived form of asparaginase is typically reserved for cases of asparaginase hypersensitivity. 41153 fosquidone A water-soluble pentacyclic pyrolloquinone analogue of mitoquidone with potential antineoplastic activity. Currently, the mechansim of action of fosquidone is unknown. In vitro studies indicate that this agent does not bind to DNA or inhibit topoisomerases. C1371 41154 CB10-277 A synthetic derivative of dimethylphenyl-triazene related to dacarbazine, with antineoplastic properties. Related to the agent dacarbazine, CB10-277 is converted in vivo to a monomethyl triazene form that alkylates DNA, resulting in inhibition of DNA replication and repair; in addition, this agent may act as a purine analogue, resulting in inhibition of DNA synthesis, and may interact with protein sulfhydryl groups. 41162 4'-iodo-4'-deoxydoxorubicin An iodinated doxorubicin analogue with antiamyloid activity. 4'-Iodo-4'-deoxydoxorubicin (IDOX) binds with high affinity to five types of natural amyloid fibrils including immunoglobulin light chains, amyloid A, transthyretin (methionine-30 variant), ß-protein (Alzheimer), and ß2-microglobulin. This agent may inhibit fibril growth, increasing the solubility of amyloid tissue deposits and facilitating their clearance. IDOX has also been shown to insulin amyloid fibrillogenesis in vitro. C971 41163 ethacrynic acid An aryloxy-acetic acid derivative belonging to the class of loop diuretics. Ethacrynic acid interferes with the chloride binding site of the Na+, K+, Cl- cotransporter system in the thick ascending loop of Henle, thereby inhibiting the reabsorption of sodium, potassium, and chloride ions. This leads to an increase in the excretion of sodium, potassium, chloride, calcium, and water. 41184 cladribine A purine nucleoside antimetabolite analogue. Cladribine triphosphate, a phosphorylated metabolite of cladribine, incorporates into DNA, resulting in single-strand breaks in DNA, depletion of nicotinamide adenine dinucleotide (NAD) and adenosine triphosphate (ATP), and apoptosis. Because this agent is resistant to adenosine deaminase, an enzyme that inactivates some antineoplastic agents, it is selectively toxic to lymphocytes and monocytes which exhibit little deoxynucleotide deaminase activity. 41185 topotecan hydrochloride The hydrochloride salt of a semisynthetic derivative of camptothecin with antineoplastic activity. During the S phase of the cell cycle, topotecan selectively stabilizes topoisomerase I-DNA covalent complexes, inhibiting religation of topoisomerase I-mediated single-strand DNA breaks and producing potentially lethal double-strand DNA breaks when complexes are encountered by the DNA replication machinery. Camptothecin is a cytotoxic quinoline-based alkaloid extracted from the Asian tree Camptotheca acuminata. 41205 Re-186 hydroxyethylidene diphosphonate An synthetic compound containing the organic phosphonate hydroxyethylidene diphosphonate (HEDP) labeled with the radioisotope rhenium Re 186. Re-186 hydroxyethylidene diphosphonate binds to hydroxyapatitie in bone, delivering a cytotoxic dose of beta radiation to primary and metastatic bone tumors. Re-186 is a beta emitter with a short half-life, a radioisotope profile that provides localized antitumor radiocytotoxicity while sparing extramedullary bone marrow tissues. C1562 41210 nimodipine A dihydropyridine derivative and an analogue of the calcium channel blocker nifedipine, with antihypertensive activity. Nimodipine inhibits the transmembrane influx of calcium ions in response to depolarization in smooth muscle cells, thereby inhibiting vascular smooth muscle contraction and inducing vasodilatation. Nimodipine has a greater effect on cerebral arteries than on peripheral smooth muscle cells and myocardial cells, probably because this agent can cross the blood brain barrier due to its lipophilic nature. Furthermore, this agent also inhibits the drug efflux pump P-glycoprotein, which is overexpressed in some multi-drug resistant tumors, and may improve the efficacy of some antineoplastic agents. 41211 ormaplatin A platinum(IV) analogue with antineoplastic activity. Ormaplatin alkylates DNA, forming both inter- and intra-strand platinum-DNA crosslinks, which result in inhibition of DNA replication and transcription and cell-cycle nonspecific cytotoxicity. C1250 41212 miltefosine An orally- and topically-active alkyl-phosphocholine compound with potential antineoplastic activity. Miltefosine targets cellular membranes, modulating cell membrane permeability, membrane lipid composition, phospholipid metabolism, and mitogenic signal transduction, resulting in cell differentiation and inhibition of cell growth. This agent also inhibits the anti-apoptotic mitogen-activated protein kinase (MAPK) pathway and modulates the balance between the MAPK and pro-apoptotic stress-activated protein kinase (SAPK/JNK) pathways, thereby inducing apoptosis. As an immunomodulator, miltefosine stimulates T-cells, macrophages and the expression of interleukin 3 (IL-3), granulocyte-macrophage colony stimulating factor (GM-CSF), and interferon gamma (INF-gamma). 41213 gemcitabine hydrochloride The hydrochloride salt of an analogue of the antimetabolite nucleoside deoxycytidine with antineoplastic activity. Gemcitabine is converted intracellularly to the active metabolites difluorodeoxycytidine di- and triphosphate (dFdCDP, dFdCTP). dFdCDP inhibits ribonucleotide reductase, thereby decreasing the deoxynucleotide pool available for DNA synthesis; dFdCTP is incorporated into DNA, resulting in DNA strand termination and apoptosis. 41225 methylphenidate hydrochloride The hydrochloride salt of the synthetic central nervous system stimulant methylphenidate. Methylphenidate appears to activate the brain stem arousal system and cortex to produce its stimulant effect and, in some clinical settings, may improve cognitive function. 41244 monoclonal antibody 14G2A A murine monoclonal antibody directed against the ganglioside GD2 with potential antineoplastic activity. Monoclonal antibody 14G2A binds to the ganglioside GD2 and induces antibody-dependent cell mediated cytotoxicity and complement-dependent cytotoxicity against GD2-expressing tumor cells. GD2 is overexpressed in malignant melanoma, neuroblastoma, osteosarcoma, and small cell carcinoma of the lung. 41252 liarozole fumarate The orally active fumarate salt of the benzimidazole derivative liarozole with potential antineoplastic activity. As a retinoic acid metabolism blocking agent (RAMBA), liarozole inhibits cytochrome P450-dependent all-trans-retinoic acid (ATRA)-4-hydroxylase, resulting in an increase in endogenous ATRA production, inhibition of cell proliferation, and induction of cell differentiation. This agent also inhibits aromatase, the enzyme that catalyzes the final, rate-limiting step in estrogen biosynthesis. C1524 41253 quinine A quinidine alkaloid isolated from the bark of the cinchona tree. Quinine has many mechanisms of action, including reduction of oxygen intake and carbohydrate metabolism; disruption of DNA replication and transcription via DNA intercalation; and reduction of the excitability of muscle fibers via alteration of calcium distribution. This agent also inhibits the drug efflux pump P-glycoprotein which is overexpressed in multi-drug resistant tumors and may improve the efficacy of some antineoplastic agents. 41254 mafosfamide A synthetic oxazaphosphorine derivative with antineoplastic properties. Mafosfamide alkylates DNA, forming DNA cross-links and inhibiting DNA synthesis. Although closely related to cyclophosphamide, mafosfamide, unlike cyclophosphamide, does not require hepatic activation to generate its active metabolite 4-hydroxy-cyclophosphamide; accordingly, mafosfamide is potentially useful in the intrathecal treatment of neoplastic meningitis. 41258 tretinoin A naturally-occurring acid of retinol. Tretinoin binds to and activates retinoic acid receptors (RARs), thereby inducing changes in gene expression that lead to cell differentiation, decreased cell proliferation, and inhibition of tumorigenesis. This agent also inhibits telomerase, resulting in telomere shortening and eventual apoptosis of some tumor cell types. The oral form of tretinoin has teratogenic and embryotoxic properties. 41259 monoclonal antibody 3F8 A murine monoclonal antibody directed against the cell-surface, tumor-associated antigen ganglioside GD2. Vaccination with monoclonal antibody 3F8 may stimulate a host cytotoxic immune response against tumors that express ganglioside GD2. 41269 dexverapamil The R-enantiomer of the calcium channel blocker verapamil. Dexverapamil competitively inhibits the multidrug resistance efflux pump P-glycoprotein (MDR-1), thereby potentially increasing the effectiveness of a wide range of antineoplastic drugs which are inactivated by MDR-1 mechanisms. This agent exhibits decreased calcium antagonistic activity and toxicity compared to racemic verapamil. 41298 bicalutamide A synthetic, nonsteroidal antiandrogen. Bicalutamide competitively binds to cytosolic androgen receptors in target tissues, thereby inhibiting the receptor binding of androgens. This agent does not bind to most mutated forms of androgen receptors. 41299 alendronate sodium The sodium salt of alendronate, a second generation bisphosphonate and synthetic analog of pyrophosphate with bone anti-resorption activity. Alendronate sodium binds to and inhibits the activity of geranyltranstransferase (farnesyl pyrophosphate synthetase), an enzyme involved in terpenoid biosynthesis. Inhibition of this enzyme prevents the biosynthesis of isoprenoid lipids (FPP and GGPP) that are donor substrates of farnesylation and geranylgeranylation during the post-translational modification of small GTPase signalling proteins, which is important in the process of osteoclast turnover. As a result, osteoclast activity is inhibited and bone resorption and turnover are reduced. 41305 ranpirnase A natural homologue of ribonuclease A isolated from the eggs of the frog Rana pipiens. Ranpirnase primarily degrades cellular transfer RNA with a substrate specificity for uridine-guanidine base-pair sequences, resulting in inhibition of protein synthesis and cytotoxicity. This agent also activates caspase-9 in mitochondria, resulting in tumor cell apoptosis. 41339 albuterol sulfate The sulfate salt of the short-acting sympathomimetic agent albuterol, a 1:1 racemic mixture of (R)-albuterol and (S)-albuterol with bronchodilator activity. Albuterol stimulates beta2-adrenergic receptors in the lungs, thereby activating the enzyme adenylate cyclase that catalyzes the conversion of ATP to cyclic-3',5'-adenosine monophosphate (cAMP). Increased cAMP concentrations relax bronchial smooth muscle, relieve bronchospasms, and reduce inflammatory cell mediator release, especially from mast cells. To a lesser extent albuterol stimulates beta1-adrenergic receptors, thereby increasing the force and rate of myocardial contraction. 41340 theophylline A natural alkaloid derivative of xanthine isolated from the plants Camellia sinensis and Coffea arabica. Theophylline appears to inhibit phosphodiesterase and prostaglandin production, regulate calcium flux and intracellular calcium distribution, and antagonize adenosine. Physiologically, this agent relaxes bronchial smooth muscle, produces vasodilation (except in cerebral vessels), stimulates the CNS, stimulates cardiac muscle, induces diuresis, and increases gastric acid secretion; it may also suppress inflammation and improve contractility of the diaphragm. 41347 glycine A non-essential, non-polar, non-optical, glucogenic amino acid. Glycine, an inhibitory neurotransmitter in the CNS, triggers chloride ion influx via ionotropic receptors, thereby creating an inhibitory post-synaptic potential. In contrast, this agent also acts as a co-agonist, along with glutamate, facilitating an excitatory potential at the glutaminergic N-methyl-D-aspartic acid (NMDA) receptors. Glycine is an important component and precursor for many macromolecules in the cells. 41351 terephthalamidine A derivative of the phthalanilide compounds. Terephthalamidine belongs to a family of compounds which appear to reversibly bind to the minor groove of the DNA double helix but not intercalate DNA. This agent also has been suggested to form ionic complexes with many biological components in vitro, including nucleic acids, proteins and lipids. 41354 dolasetron mesylate An indole derivative with antiemetic activity. As a selective serotonin receptor antagonist, dolasetron mesylate competitively blocks the action of serotonin at 5HT3 receptors, resulting in suppression of chemotherapy- and radiotherapy-induced nausea and vomiting. 41375 Detox-B adjuvant A cancer vaccine adjuvant that consists of an oil droplet emulsion of monophosphoryl lipid A and mycobacterial cell wall skeleton. Detox-B adjuvant is a non-specific immunostimulant that may enhance the host immune response to certain cancer vaccines. Detox-B differs from Detox adjuvant in that Detox-B contains lecithin. 41409 elsamitrucin A heterocyclic antineoplastic antibiotic isolated from the bacterium Actinomycete strain J907-21. Elsamitrucin intercalates into DNA at guanine-cytosine (G-C)-rich sequences and inhibits topoisomerase I and II, resulting in single-strand breaks and inhibition of DNA replication. C1080 41410 roquinimex A quinoline-3-carboxamide with potential antineoplastic activity. Roquinimex inhibits endothelial cell proliferation, migration, and basement membrane invasion; reduces the secretion of the angiogenic factor tumor necrosis factor alpha by tumor-associated macrophages (TAMs); and inhibits angiogenesis. This agent is also an immune modulator that appears to alter cytokine profiles and enhance the activity of T cells, natural killer cells, and macrophages. 41418 pyrazoloacridine A 9-methoxy acridine compound containing a reducible 5-nitro substituent. Pyrazoloacridine appears to intercalate into DNA and inhibit RNA synthesis, DNA synthesis, and the activities of topoisomerases I and II, thereby causing cytotoxicity. 41432 pentoxifylline A methylxanthine derivative with hemorrheologic and immunomodulating properties. Pentoxifylline inhibits phosphodiesterase, resulting in increased levels of cyclic adenosine monophosphate (cAMP) in erythrocytes, endothelium, and the surrounding tissues. This leads to vasodilation, improves erythrocyte flexibility, and enhances blood flow. In addition, the increased level of cAMP in platelets inhibits platelet aggregation, which may contribute to a reduction in blood viscosity. This agent also inhibits production of tumor necrosis factor-alpha and interferon-gamma, while it induces Th2-like (T-helper 2) cytokine production, thereby inhibiting Th1-mediated (T-helper 1) inflammatory and autoimmune responses. 41433 cyclopentenyl cytosine A pro-drug carbocyclic analogue of cytidine with antineoplastic and antiviral activities. Cyclopentenyl cytosine (CPEC) is converted to the active metabolite cyclopentenyl cytosine 5'-triphosphate (CPEC-TP); CPEC-TP competitively inhibits cytidine triphosphate (CTP) synthase, thereby depleting intracellular cytidine pools and inhibiting DNA and RNA synthesis. This agent may also induce differentiation of some tumor cell types. The antiviral activity of this agent is broad-spectrum. C1359 41472 monoclonal antibody L6 A murine IgG2a monoclonal antibody with potential antineoplastic activity. Monoclonal antibody L6 binds to the L6 antigen, a cell surface glycoprotein overexpressed in many carcinomas, and induces antibody-dependent cell-mediated cytotoxicity and complement-dependent cytotoxicity against L6-expressing tumor cells. This agent may be conjugated with various toxins in order to target their cytotoxic activity to tumor cells expressing the L6 antigen. 41474 recombinant interleukin-6 A recombinant therapeutic agent which is chemically identical to or similar to the endogenous cytokine interleukin-6 (IL-6) with antiapoptotic, proinflammatory, antiinflammatory, proproliferative and proangiogenic activities. IL-6 binds to its receptor (IL-6R), activating a receptor-CD130 receptor complex; the CD130 portion of the complex is a signal transduction protein that activates JAK kinases and ras-mediated signaling pathways, which in turn activate downstream signaling pathways, resulting in the activation of various transcription factors (STAT, ELK-1, NF-IL-6, etc.) and gene transcription. The physiological effects of IL-6 are complex and varied and include hematopoietic, pyrogenic and thermogenic, proinflammatory, antiinflammatory, proproliferative (anti-apoptotic), and angiogenic effects. C591 41486 interleukin-2 liposome A formulation in which liposomes are loaded with the cytokine interleukin-2 (IL-2). By activating cytotoxic T-lymphocytes, such as lymphokine-activated killer cells, and increasing levels of the cytotoxic cytokines interferon-gamma (IFN-gamma) and transforming growth factor-beta (TGF-beta), IL-2 may exhibit antitumoral activity. Liposomal formulations of IL-2 may promote entry of the cytokine into target tumor cells and may be used as an immunoadjuvant in cancer vaccine therapy. 41528 methylprednisolone A synthetic corticosteroid with anti-inflammatory and immunomodulating properties. Methylprednisolone binds to and activates specific nuclear receptors, resulting in altered gene expression and inhibition of proinflammatory cytokine production. This agent also decreases the number of circulating lymphocytes, induces cell differentiation, and stimulates apoptosis in sensitive tumor cell populations. 41538 sulindac A sulfinylindene derivative prodrug with potential antineoplastic activity. Converted in vivo to an active metabolite, sulindac, a nonsteroidal anti-inflammatory drug (NSAID), blocks cyclic guanosine monophosphate-phosphodiesterase (cGMP-PDE), an enzyme that inhibits the normal apoptosis signal pathway; this inhibition permits the apoptotic signal pathway to proceed unopposed, resulting in apoptotic cell death. 41541 mifamurtide A liposomal formulation containing a muramyl dipeptide (MDP) analogue with potential immunomodulatory and antineoplastic activities.. Muramyl tripeptide phosphatidylethanolamine (MTP-PE), a derivative of the mycobacterial cell wall component MDP, activates both monocytes and macrophages. Activated macrophages secrete cytokines and induce the recruitment and activation of other immune cells, which may result in indirect tumoricidal effects. Liposomal encapsulation of MTP-PE prolongs its half-life and enhances tissue targeting. C1394 41544 chlorhexidine A biguanide compound used as an antiseptic agent with topical antibacterial activity. Chlorhexidine is positively charged and reacts with the negatively charged microbial cell surface, thereby destroying the integrity of the cell membrane. Subsequently, chlorhexidine penetrates into the cell and causes leakage of intracellular components leading to cell death. Since gram positive bacteria are more negatively charged, they are more sensitive to this agent. 41546 aloe vera gel A preparation of leaf pulp from the parenchymal tissue of the plant Aloe vera (Liliaceae). Aloe vera gel contains carbohydrate polymers, such as glucomannans or pectic acid, and various vitamins and essential amino acids, as well as other organic and inorganic compounds. This agent has been used internally or externally for sunburn, skin problems, insect bites, ulcers, arthritis, constipation, and as an immune system enhancer. C1565 41579 QS21 A purified, natural saponin isolated from the soapbark tree Quillaja saponaria Molina with potential immunoadjuvant activity. When co-administered with vaccine peptides, QS21 may increase total antitumoral vaccine-specific antibody responses and cytotoxic T-cell responses. 41589 GM2-KLH vaccine A cancer vaccine consisting of GM2 ganglioside, a melanoma-specific antigen, conjugated with the immunostimulant keyhole limpet hemocyanin. Vaccination with GM2-KLH vaccine may stimulate the host immune system to mount a cytotoxic T lymphocyte (CTL) response against GM2 ganglioside-expressing melanoma cells, resulting in tumor growth inhibition. 41607 procarbazine hydrochloride The hydrochloride salt of a methylhydrazine derivative with antineoplastic and mutagenic activities. Although the exact mode of cytotoxicity has not been elucidated, procarbazine, after metabolic activation, appears to inhibit the trans-methylation of methionine into transfer RNA (t-RNA), thereby preventing protein synthesis and consequently DNA and RNA synthesis. This agent may also undergo auto-oxidation, resulting in the formation of cytotoxic free radicals which damage DNA through an alkylation reaction. 41613 carboxyamidotriazole An orally-active agent with potential antineoplastic activity. Carboxyamidotriazole binds to and inhibits non-voltage-operated Ca2+ channels, blocking both Ca2+ influx into cells and Ca2+ release from intracellular stores and resulting in the disruption of calcium channel-mediated signal transduction and inhibition of vascular endothelial growth factor (VEGF) signaling, endothelial proliferation, and angiogenesis. This agent may also inhibit tumor cell growth, invasion and metastasis. 41614 chamomile The flower-heads of either the plant Anthemis nobilis or the plant Matricaria chamomilla. Chamomile has a warm aromatic odour and a very bitter taste and contains volatile oils which are a mixture of butyl and amyl angelates and valerates. Due to its coumarin constituents, large doses may interfere with coagulation. 41615 milodistim A recombinant fusion protein derived from the coding sequences of two growth factors, interleukin-3 (IL-3) and granulocyte-macrophage colony-stimulating factor (GM-CSF). Milodistim exhibits greater receptor binding affinity and colony stimulating activity than its parent cytokines. This agent stimulates proliferation of immature hematopoietic cells and allows the stimulation and expansion of multi-lineage hematopoiesis from immature bone marrow progenitor cells. 41645 L-leucyl-L-leucine methyl ester A 2-amino acid compound with immunomodulatory activity. L-leucyl-L-leucine methyl ester (LLME) is a lysosomotropic agent entering cells via receptor-mediated endocytosis. LLME undergoes a condensation process catalyzed by dipeptidyl peptidase I (DPPI) in lysosomes. Condensation of LLME leads to lysosomal rupture and DNA fragmentation in DPPI-expressing immune cells such as cytotoxic T-cells and natural killer cells. Therefore, this agent may be able to decrease the incidence of graft versus host disease (GVHD) via cytotoxic T-cell depletion. Furthermore, LLME has the potential for augmenting antibody production when used in pretreatment of peripheral blood mononuclear cells (PBMCs), possibly by interfering with gene expression of inflammatory factors. C2377 41653 Stanford V regimen A chemotherapy regimen consisting of mechlorethamine, doxorubicin hydrochloride, vinblastine, vincristine, bleomycin, etoposide and prednisone, administered on a compressed schedule and used in the treatment of Hodgkin lymphoma; it may be followed by consolidative radiation therapy. C63369 41655 thymopentin A synthetic pentapeptide which is the active site of the naturally occurring hormone thymopoietin with immunomodulating properties. Thymopentin enhances the production of thymic T cells and may help restore immunocompetence in immunosuppressed subjects. This agent also augments the effects of ionizing radiation by arresting cancer cells in the G2/M phase of the cell cycle. 41656 mivobulin isethionate The isethionate salt of mivobulin, a synthetic colchicine analogue with potential antineoplastic activity. Mivobulin isethionate binds to tubulin, thereby inhibiting microtubule polymerization and mitosis. C1357 41657 docetaxel A semi-synthetic, second-generation taxane derived from a compound found in the European yew tree Taxus baccata. Docetaxel displays potent and broad antineoplastic properties; it binds to and stabilizes tubulin, thereby inhibiting microtubule disassembly which results in cell- cycle arrest at the G2/M phase and cell death. This agent also inhibits pro-angiogenic factors such as vascular endothelial growth factor (VEGF) and displays immunomodulatory and pro-inflammatory properties by inducing various mediators of the inflammatory response. Docetaxel has been studied for use as a radiation-sensitizing agent. 41658 lovastatin A lactone metabolite isolated from the fungus Aspergillus terreus with cholesterol-lowering and potential antineoplastic activities. Lovastatin is hydrolyzed to the active beta-hydroxyacid form, which competitively inhibits 3-hydroxyl-3-methylgutarylcoenzyme A (HMG-CoA) reductase, an enzyme involved in cholesterol biosynthesis. In addition, this agent may induce tumor cell apoptosis and inhibit tumor cell invasiveness, possibly by inhibiting protein farnesylation and protein geranylgeranylation, and may arrest cells in the G1 phase of the cell cycle. The latter effect sensitizes tumor cells to the cytotoxic effects of ionizing radiation. 41665 glucarpidase A zinc-dependent enzyme isolated from a strain of the bacterium Pseudomonas. Because glucarpidase rapidly hydrolyzes methotrexate into inactive metabolites, it may be useful as a rescue agent for methotrexate-induced nephrotoxicity. In antibody-directed enzyme prodrug therapy (ADEPT), this agent is conjugated with an antibody that binds to a specific tumor cell type, allowing for glucarpidase-catalyzed activation of a co-administered prodrug at the site of the tumor. 41670 lometrexol A folate analog antimetabolite with antineoplastic activity. As the 6R diastereomer of 5,10-dideazatetrahydrofolate, lometrexol inhibits glycinamide ribonucleotide formyltransferase (GARFT), the enzyme that catalyzes the first step in the de novo purine biosynthetic pathway, thereby inhibiting DNA synthesis, arresting cells in the S phase of the cell cycle, and inhibiting tumor cell proliferation. The agent has been shown to be active against tumors that are resistant to the folate antagonist methotrexate. 41671 temozolomide A triazene analog of dacarbazine with antineoplastic activity. As a cytotoxic alkylating agent, temozolomide is converted at physiologic pH to the short-lived active compound, monomethyl triazeno imidazole carboxamide (MTIC). The cytotoxicity of MTIC is due primarily to methylation of DNA at the O6 and N7 positions of guanine, resulting in inhibition of DNA replication. Unlike dacarbazine, which is metabolized to MITC only in the liver, temozolomide is metabolized to MITC at all sites. Temozolomide is administered orally and penetrates well into the central nervous system. 41690 omega-3 fatty acid Any fatty acid that contains an unsaturated bond originating from the 3rd carbon from the methyl end. Omega-3 fatty acids do not occur naturally with chain lengths shorter than 16 carbon units. C493 41696 deferoxamine mesylate The mesylate salt of an iron-chelating agent that binds free iron in a stable complex, preventing it from engaging in chemical reactions. Deferoxamine chelates iron from intra-lysosomal ferritin and ferrioxamine, a water-soluble complex excreted by the kidneys and in the feces via the bile. This agent does not readily chelate iron bound to transferrin, hemoglobin, myoglobin or cytochrome. 41703 fostriecin An anti-tumor antibiotic isolated from the bacterium Streptomyces pulveraceus. Fostriecin inhibits topoisomerase II catalytic activity, resulting in protein-associated strand breaks and impaired DNA and RNA synthesis in various malignant cell types. This agent also inhibits serine/threonine protein phosphatase type 2A in some tumor cell types, thereby interfering with cellular proliferation and differentiation. 41710 calusterone A 17-alkylated orally active androgenic steroid. Calusterone may alter the metabolism of estradiol and reduce estrogen production. 41714 irinotecan hydrochloride The hydrochloride salt of a semisynthetic derivative of camptothecin, a cytotoxic, quinoline-based alkaloid extracted from the Asian tree Camptotheca acuminata. Irinotecan, a prodrug, is converted to a biologically active metabolite 7-ethyl-10-hydroxy-camptothecin (SN-38) by a carboxylesterase-converting enzyme. One thousand-fold more potent than its parent compound irinotecan, SN-38 inhibits topoisomerase I activity by stabilizing the cleavable complex between topoisomerase I and DNA, resulting in DNA breaks that inhibit DNA replication and trigger apoptotic cell death. Because ongoing DNA synthesis is necessary for irinotecan to exert its cytotoxic effects, it is classified as an S-phase-specific agent. 41718 rhizoxin A macrocyclic lactone. Rhizoxin binds to tubulin and inhibits microtubule assembly, thereby inducing cytotoxicity. This agent also may inhibit endothelial cell-induced angiogenic activity, which may result in decreased tumor cell proliferation. 41719 methotrexate An antimetabolite and antifolate agent with antineoplastic and immunosuppressant activities. Methotrexate binds to and inhibits the enzyme dihydrofolate reductase, resulting in inhibition of purine nucleotide and thymidylate synthesis and, subsequently, inhibition of DNA and RNA syntheses. Methotrexate also exhibits potent immunosuppressant activity although the mechanism(s) of actions is unclear. 41724 mistletoe extract An extract of the whole plant Viscum album (mistletoe) with potential biological response modifier (BRM) activity. Mistletoe extract may both stimulate the antitumoral functions of the immune system and have a direct toxic effect on tumor cells. 41725 TNP-470 A synthetic analog of fumagillin, an antibiotic isolated from the fungus Aspergillus fumigatus fresenius with antineoplastic activity. TNP-470 binds to and irreversibly inactivates methionine animopeptidase-2 (MetAP2), resulting in endothelial cell cycle arrest late in the G1 phase and inhibition of tumor angiogenesis. This agent may also induce the p53 pathway, thereby stimulating the production of cyclin-dependent kinase inhibitor p21 and inhibiting angiogenesis. 41738 plicamycin An antibiotic isolated from the bacterium Streptomyces plicatus with antineoplastic activity. Plicamycin, also known as mithramycin, binds to the minor groove of DNA at GC-rich sites, resulting in inhibition of RNA synthesis; this agent also inhibits mRNA expression, resulting in a reduction in protein synthesis. In addition, plicamycin may inhibit bone resorption by down regulating transcription of c-src, an oncogene involved in bone metabolism and resorption. 41750 valspodar An analogue of cyclosporin-A. Valspodar inhibits p-glycoprotein, the multidrug resistance efflux pump, thereby restoring the retention and activity of some drugs in some drug-resistant tumor cells. This agent also induces caspase-mediated apoptosis. 41760 monoclonal antibody CC49 A second-generation murine monoclonal antibody based on the antibody B72.3 that is directed against tumor-associated glycoprotein 72 (TAG72). TAG72 is expressed by gastric, breast, pancreatic, colorectal, and ovarian carcinoma cells. 41766 formestane A synthetic steroidal substance with antineoplastic activity. Formestane binds irreversibly to and inhibits the enzyme aromatase, thereby blocking the conversion of cholesterol to pregnenolone and the peripheral aromatization of androgenic precursors into estrogens. 41767 triacetyluridine A synthetic uridine pro-drug that is converted to uridine in vivo. Uridine, a pyrimidine nucleotide, has been used in a variety of diseases including depressive disorders and inherited myopathies. 41779 MOPP regimen A chemotherapy regimen consisting of mechlorethamine, vincristine (Oncovin), procarbazine and prednisone, used alone or in combination with radiation therapy for the treatment of stage I-IV Hodgkin lymphoma. Due to the increased risk of gonadal toxicity, this regimen has been widely replaced by the ABVD regimen. C63365 41780 methylene blue A synthetic basic dye. Methylene blue stains to negatively charged cell components like nucleic acids; when administered in the lymphatic bed of a tumor during oncologic surgery, methylene blue may stain lymph nodes draining from the tumor, thereby aiding in the visual localization of tumor sentinel lymph nodes. When administered intravenously in low doses, this agent may convert methemoglobin to hemoglobin. 41792 aminocamptothecin A water-insoluble camptothecin derivative. Aminocamptothecin binds to the nuclear enzyme topoisomerase I, thereby inhibiting repair of single-strand DNA breakages. Because the terminal lactone ring of aminocamptothecin required for the agent's antitumor activity spontaneously opens under physiological conditions to an inactive carboxy form, the drug must be administered over an extended period of time to achieve effective cytotoxicity. 41803 calcium glucarate The orally bioavailable calcium salt of glucaric acid, a natural substance found in many fruits and vegetables, with potential chemopreventive activity. After absorption, glucaric acid is converted to d-glucaro-1,4-lactone which inhibits beta-glucuronidase, an enzyme found in certain bacteria that reside in the human gut. The detoxification of various toxin and sex hormone metabolites depends upon their conjugation to glucuronic acid in the liver and subsequent excretion of glucuronic acid conjugated metabolites in the bile. Bacterial beta-glucuronidase may catalyze the deconjugation of glucuronic acid conjugated metabolites of toxins and sex hormones, thus prolonging exposure to unconjugated and unexcreted toxin and sex hormone metabolites. Accordingly, calcium glucarate supplementation may indirectly inhibit sex hormone-mediated and toxin-mediated tumorigenesis by inhibiting bacterial beta-glucuronidase activity. Elevated bacterial beta-glucuronidase activity may be associated with an increased risk for sex hormone-mediated and toxin-mediated cancers such as breast, prostate, and colon cancers. 41804 morphine sulfate The sulfate salt of morphine, an opiate alkaloid isolated from the plant Papaver somniferum and produced synthetically. Morphine binds to and activates specific opiate receptors (delta, mu and kappa), each of which are involved in controlling different brain functions. In the central nervous and gastrointestinal systems, this agent has widespread effects including analgesia, anxiolysis, euphoria, sedation, respiratory depression, and gastrointestinal system smooth muscle contraction. C669 41810 strontium chloride Sr 89 The chloride salt of a radioactive isotope of strontium. Strontium chloride Sr 89 is taken up and incorporated preferentially in metastatic lesions in bone where it emits cytotoxic beta radiation, resulting in an inhibition and/or reduction of tumor growth and so tumor-related bone pain. 41817 calcium citrate The citrate salt of calcium. An element necessary for normal nerve, muscle, and cardiac function, calcium as the citrate salt helps to maintain calcium balance and prevent bone loss when taken orally. This agent may also be chemopreventive for colon and other cancers. 41827 oral sodium phenylbutyrate An orally active derivative of the short-chain fatty acid butyrate with potential antineoplastic activity. 4-Phenylbutyrate inhibits histone deacetylase, resulting in cell cycle gene expression modulation, reduced cell proliferation, increased cell differentiation, and apoptosis. This agent also initiates fragmentation of genomic DNA, resulting in decreased DNA synthesis and the inhibition of tumor cell migration and invasion. C67083 41835 hydralazine hydrochloride The hydrochloride salt of hydralazine, a phthalazine derivative with antihypertensive and potential antineoplastic activities. Hydralazine alters intracellular calcium release and interferes with smooth muscle cell calcium influx, resulting in arterial vasodilatation. This agent also inhibits the phosphorylation of myosin protein and chelation of trace metals required for smooth muscle contraction, resulting in an increase in heart rate, stroke volume and cardiac output. In addition to its cardiovascular effects, hydralazine inhibits DNA methyltransferase, which may result in inhibition of DNA methylation in tumor cells. C551 41836 keyhole limpet hemocyanin A natural protein isolated from the marine mollusc keyhole limpet. Keyhole limpet hemocyanin is an immunogenic carrier protein that, in vivo, increases antigenic immune responses to haptens and other weak antigens such as idiotype proteins. 41848 anti-B4 blocked ricin immunotoxin An immunotoxin comprised of an anti-B4 (anti-CD19) murine monoclonal antibody linked to the modified plant-derived toxin blocked ricin. The antibody moiety of anti-B4 blocked ricin immunotoxin binds to B lymphocytes that express B4; after internalization of the immunotoxin by the B4-expressing B cell, the ricin moiety cleaves the N-glycosidic bond between the ribose and adenine base at position 4324 in the B lymphocyte 28S ribosomal RNA, resulting in ribosome inactivation, inhibition of protein synthesis, and cell death. "Blocked" ricin is ricin which has been chemically modified such that the lectin binding sites of the B chain (galactose-binding sites) have been blocked by covalent attachment of affinity ligands, leaving the ribosome-inactivating activity of the ricin A chain intact. C2380 41857 therapeutic epinephrine The synthetic form of the naturally occurring sympathomimetic amine with vasoconstricting, intraocular pressure-reducing, and bronchodilating activities. By stimulating vascular alpha-adrenergic receptors, epinephrine causes vasoconstriction, thereby increasing vascular resistance and blood pressure. When administered in the conjunctiva, this agent binds to alpha-adrenergic receptors in the iris sphincter muscle, resulting in vasoconstriction, a decrease in the production of aqueous humor, and a lowering of intraocular pressure. Through its beta1 receptor-stimulating actions, epinephrine increases the force and rate of myocardial contraction and relaxes bronchial smooth muscle, resulting in bronchodilation. C473 41858 methotrexate-e therapeutic implant An injectable collagen matrix gel containing the antimetabolite methotrexate and the sympathicomimetic agent epinephrine with potential antineoplastic activity. After intratumoral injection, methotrexate binds to and inhibits the enzyme dihydrofolate reductase, resulting in inhibition of purine nucleotide and thymidylate synthesis and, subsequently, inhibition of DNA and RNA syntheses. Epinephrine, a potent vasoconstrictor, is added to the gel to enhance penetration of methotrexate into the tumor tissue and reduce dispersion to the surrounding tissues thereby enhancing the local concentration of methotrexate and increasing its anti-tumor activity. Intratumoral injection of methotrexate combined with epinephrine may potentially increase chemotherapeutic efficacy compared to systemic administration and reduce systemic toxicity and side effects. 41859 fluorouracil-e therapeutic implant An injectable collagen matrix gel containing the antimetabolite fluorouracil and the sympathicomimetic agent epinephrine with potential antineoplastic activity. After intratumoral injection, fluorouracil is converted into the active metabolite 5-fluoroxyuridine monophosphate that competes with uracil during RNA synthesis while another active metabolite, 5-5-fluoro-2'-deoxyuridine-5'-O-monophosphate, inhibits thymidylate synthase and, so, DNA synthesis. Epinephrine, a potent vasoconstrictor, is added to the gel to enhance penetration of fluorouracil into tumor tissue and reduce dispersion to surrounding tissues, thus enhancing the local concentration of fluorouracil. Compared to systemic administration, the intratumoral injection of fluorouracil combined with epinephrine may increase fluorouracil's chemotherapeutic efficacy while minimizing systemic toxicity. 41862 clodronate disodium The disodium salt of a nitrogen-free bisphosphonate analog of naturally occurring pyrophosphate. Clodronate binds to calcium and inhibits osteoclastic bone resorption and hydroxyapatite crystal formation and dissolution, resulting in a reduction of bone turnover. This agent may control malignancy-associated hypercalcemia, inhibit osteolytic bone metastasis and decrease pain. 41899 meropenem A broad-spectrum carbapenem with antibacterial properties, synthetic Meropenem inhibits cell wall synthesis in gram-positive and gram-negative bacteria. It penetrates cell walls and binds to penicillin-binding protein targets. Meropenem acts against aerobes and anaerobes including Klebsiella, E. coli, Enterococcus, Clostridium sp.. 41910 safingol A saturated derivative of sphingosine. As an inhibitor of protein kinase C (PKC), safingol competitively binds to the regulatory phorbol-binding domain of PKC, a kinase involved in tumorigenesis. This agent has been shown to act synergistically with other chemotherapeutic agents and may potentiate chemotherapy drug-induced apoptosis in vitro and in vivo. C1568 41911 loperamide hydrochloride The hydrochloride salt form of loperamide, a synthetic, piperidine derivative and opioid agonist with antidiarrheal activity. Loperamide acts on the mu-receptors in the intestinal mucosa. This leads to a decrease in gastrointestinal motility by decreasing the circular and longitudinal smooth muscle activity of the intestinal wall. This slows intestinal transit and allows for more water and electrolyte absorption from the intestines. Loperamide is not significantly absorbed from the gut and does not cross the blood-brain barrier. Therefore it has no central nervous system effects. 41915 adozelesin An alkylating agent that bind to the DNA minor groove in a sequence-specific manner and form covalent adducts with adenines, resulting in the inhibition of DNA replication and induction of apoptosis. 41919 calcitriol A synthetic physiologically-active analog of vitamin D, specifically the vitamin D3 form. Calcitriol regulates calcium in vivo by promoting absorption in the intestine, reabsorption in the kidneys, and, along with parathyroid hormone, regulation of bone growth. A calcitriol receptor-binding protein appears to exist in the mucosa of human intestine. Calcitriol also induces cell cycle arrest at G0/G1 phase of the cell cycle, cell differentiation, and apoptosis, resulting in inhibition of proliferation of some tumor cell types. This agent may be chemopreventive for colon and prostate cancers. 41929 recombinant human stem cell factor A therapeutic glycoprotein cytokine chemically identical to or similar to endogenous human stem cell factor with hematopoietic activity. Recombinant human stem cell factor (rhSCF) binds to the receptor tyrosine kinase c-kit, which may stimulate the growth of peripheral blood progenitor cells (PBPCs). This agent works synergistically with other hematopoietic growth factors. rhSCF may promote bone marrow recovery after myeloablative therapies and procedures. C1410 41938 ammonium trichlorotellurate A synthetic non-toxic tellurium derivative, structurally similar to cisplatin, with immuno-modulating, antiviral, and hair growth-promoting activities. Ammonium trichlorotellurate may inhibit the inflammatory cytokine interleukin-10 (IL-10) and may induce hematopoietic cells to express interleukin-2 (IL-2), IL-2 receptors, granulocyte-macrophage colony-stimulating factor (GM-CSF), IL-3, tumor necrosis factor (TNF) and interferons (INFs). This agent is also a potent inducer of IL-1 and IL-6. Accordingly, ammonium trichlorotellurate may protect against chemotherapy-induced myelosuppression. In addition, this agent exhibits hair growth-promoting activity by inducing anagen production and inhibiting catagen production, resulting in the promotion of follicular keratinocyte proliferation and interference with follicular keratinocyte terminal differentiation, respectively. Accordingly, ammonium trichlorotellurate may protect against chemotherapy-induced alopecia. 41947 busulfan A synthetic derivative of dimethane-sulfonate with antineoplastic and cytotoxic properties. Although its mechanism of action is not fully understood, busulfan appears to act through the alkylation of DNA. Following systemic absorption of busulfan, carbonium ions are formed, resulting in DNA alkylation and DNA breaks and inhibition of DNA replication and RNA transcription. 41959 bryostatin 1 A macrocyclic lactone isolated from the bryozoan Bugula neritina with antineoplastic activity. Bryostatin-1 binds to and inhibits the cell-signaling enzyme protein kinase C, resulting in the inhibition of tumor cell proliferation, the promotion of tumor cell differentiation, and the induction of tumor cell apoptosis. This agent may act synergistically with other chemotherapeutic agents. 41963 perflubron A synthetic radiopaque liquid form of perfluorooctyl bromide. Used as a contrast agent for magnetic resonance imaging (MRI), perflubron is also used as a liquid ventilation agent to improve pulmonary gas exchange and lung compliance and may be used in surgery to reduce or eliminate the need for a donor blood. Ventilation with perfluorocarbon fluid improves lung function in conditions involving surfactant deficiency and dysfunction, including respiratory distress syndrome and adult respiratory distress syndrome. 41973 penclomedine A synthetic derivative of pyrimidine with antineoplastic activity. Penclomedine alkylates and crosslinks DNA, resulting in DNA strand breaks and inhibition of DNA and RNA synthesis. This agent is more active against tumor cells that are defective in p53 function. 41984 antineoplaston A10 A piperidinedione antineoplaston with potential antineoplastic activity. Antineoplaston A10 was originally isolated from human urine but is now synthetically derived. This agent intercalates into DNA, resulting in cell cycle arrest in G1 phase, reduction of mitosis, and decreased protein synthesis. Antineoplaston A10 may also inhibit ras-oncogene expression and activate tumor suppressor gene p53, leading to cell differentiation and apoptosis. 41985 antineoplaston AS2-1 A 4:1 mixture of phenylacetate and phenylacetylgluatmine, degradation products of the antineoplaston agent A10. Antineoplaston AS2-1 inhibits the incorporation of L-glutamine into tumor-cell proteins, leading to cell cycle arrest in the G1 phase and inhibition of mitosis. This agent may also inhibit RAS oncogene expression and activate tumor suppressor gene p53, resulting in cell differentiation and apoptosis. 41990 FOLFIRI regimen A chemotherapy regimen consisting of leucovorin calcium (calcium folinate), 5-fluorouracil, and irinotecan used in the treatment of advanced-stage and metastatic colorectal cancer. C63593 42000 alum adjuvant An aluminum compound with immune adjuvant activity. This agent adsorbs and preciptates protein antigens in solution; the resulting precipitate improves vaccine immunogenicity by faclitating the slow release of antigen from the vaccine depot formed at the site of inoculation. 42006 daclizumab A recombinant monoclonal antibody interleukin-2 receptor antagonist. Daclizumab binds specifically to the alpha subunit of the human interleukin-2 (IL-2) receptor expressed on the surface of activated lymphocytes in vivo, thereby inhibiting IL-2 binding and IL-2-mediated lymphocyte activation, a critical cellular immune response pathway. 42009 tacrolimus A macrolide isolated from the fungus Streptomyces tsukubaensis. Tacrolimus binds to the FKBP-12 protein and forms a complex with calcium-dependent proteins, thereby inhibiting calcineurin phosphatase activity and resulting in decreased cytokine production. This agent exhibits potent immunosuppressive activity in vivo and prevents the activation of T-lymphocytes in response to antigenic or mitogenic stimulation. Tacrolimus possesses similar immunosuppressive properties to cyclosporine, but is more potent. 42021 shark cartilage extract AE-941 A multifunctional antiangiogenic agent derived from shark cartilage with potential antineoplastic activity. Shark cartilage extract AE-941 competitively inhibits the binding of pro-angiogenic vascular endothelial growth factor (VEGF) to its cell receptor, thereby inhibiting endothelial cell proliferation. This agent also inhibits matrix metalloproteinases (MMPs), stimulates tissue plasminogen activator (tPA), and activates caspase-mediated apoptotic pathways in endothelial cells. 42024 recombinant transforming growth factor-beta-2 A recombinant polypeptide chemically identical to or similar to the endogenous cytokine transforming growth factor-beta-2 (TGF-beta-2). TGF-beta-2 modulates cell growth and immune function and may promote or inhibit tumor growth, depending on the tumor cell type. TGF-beta-2 may also suppress host immune system recognition of and/or response to tumor cells. C1286 42032 DAB389 epidermal growth factor A recombinant fusion protein composed of the diphtheria toxin with the receptor-binding domain replaced by human epidermal growth factor (EGF). When administered, EGF binds to the endothelial cell growth factor receptor, EGFR, which is upregulated in many solid tumors. After binding to the EGF receptor, the agent is internalized by the cell, where the diphtheria toxin moiety exerts its cytotoxic effect, inhibiting protein synthesis through ADP-ribosylation of elongation factor 2. C2383 42033 recombinant tissue plasminogen activator A recombinant therapeutic agent which is chemically identical to or similar to endogenous tissue plasminogen activator (tPA). tPA is a serine protease which converts plasminogen to plasmin, a fibrinolytic enzyme. Upon administration, recombinant tPA increases plasmin enzymatic activity, resulting in hyperfibrinolysis and potential dissolution of a thrombus or embolism. C39607 42042 monoclonal antibody Ch14.18 A chimeric mouse/human monoclonal antibody with potential antineoplastic activity. Monoclonal antibody Ch14.18 binds to the ganglioside GD2 and induces antibody-dependent cell-mediated cytotoxicity and complement-dependent cytotoxicity against GD2-expressing tumor cells. GD2 is overexpressed in malignant melanoma, neuroblastoma, osteosarcoma, and small cell carcinoma of the lung. 42043 carbogen An inhalant consisting of hyperoxic gas (95%-98% oxygen and 2%-5% carbon dioxide) with radiosensitizing properties. Inhaled carbogen reduces diffusion-limited tumor hypoxia, increasing tumor radiosensitivity due to the increased availability of molecular oxygen for cytotoxic radiation-induced oxygen free radical production. 42044 niacinamide The active form of vitamin B3 and a component of the coenzyme nicotinamide adenine dinucleotide (NAD). Niacinamide acts as a chemo- and radio-sensitizing agent by enhancing tumor blood flow, thereby reducing tumor hypoxia. This agent also inhibits poly(ADP-ribose) polymerases, enzymes involved in the rejoining of DNA strand breaks induced by radiation or chemotherapy. 42049 lintuzumab A humanized recombinant monoclonal antibody directed against CD33, a cell surface antigen found on myeloid leukemia blasts and early hematopoietic progenitor cells. Lintuzumab stimulates antibody-dependent cell-mediated cytotoxicity (ADCC) against tumor cells expressing CD33, resulting in a decrease in tumor burden. The humanized version of this monoclonal antibody exhibits less immunogenicity and improved binding affinity compared to its murine counterpart. 42068 alvocidib A synthetic N-methylpiperidinyl chlorophenyl flavone compound. As an inhibitor of cyclin-dependent kinase, alvocidib induces cell cycle arrest by preventing phosphorylation of cyclin-dependent kinases (CDKs) and by down-regulating cyclin D1 and D3 expression, resulting in G1 cell cycle arrest and apoptosis. This agent is also a competitive inhibitor of adenosine triphosphate activity. 42086 letrozole A nonsteroidal inhibitor of estrogen synthesis with antineoplastic activity. As a third-generation aromatase inhibitor, letrozole selectively and reversibly inhibits aromatase, which may result in growth inhibition of estrogen-dependent breast cancer cells. Aromatase, a cytochrome P-450 enzyme localized to the endoplasmic reticulum of the cell and found in many tissues including those of the premenopausal ovary, liver, and breast, catalyzes the aromatization of androstenedione and testosterone into estrone and estradiol, the final step in estrogen biosynthesis. 42095 apaziquone An indolequinone bioreductive prodrug and analog of mitomycin C with potential antineoplastic and radiosensitization activities. Apaziquone is converted to active metabolites in hypoxic cells by intracellular reductases, which are present in greater amounts in hypoxic tumor cells. The active metabolites alkylate DNA, resulting in apoptotic cell death. This agent displays activity towards both hypoxic solid tumors, which exhibits higher expression of cytochrome P450 reductase, and well-oxygenated malignant cells that overexpress the bioreductive enzyme NQO1 (NAD(P)H: quinone oxidoreductase). Apaziquone may selectively sensitize hypoxic tumor cells to radiocytotoxicity. 42108 clofibrate An aryloxyisobutyric acid derivate with antihyperlipidemic activity. Although the exact mechanism of action has not been fully characterized, clofibrate may enhance the conversion of very-low-density lipoprotein (VLDL) to low-density lipoprotein (LDL), decreasing the production of hepatic VLDL, inhibiting cholesterol production, and increasing fecal excretion of neutral sterols. 42113 O6-benzylguanine A guanine analogue with antineoplastic activity. O(6)-benzylguanine binds the DNA repair enzyme O(6)-alkylguanine DNA alkyltransferase (AGT), transferring the benzyl moiety to the active-site cysteine and resulting in inhibition of AGT-mediated DNA repair. Co-administration of this agent potentiates the effects of other chemotherapeutic agents that damage DNA. 42116 imipenem A broad-spectrum, semi-synthetic beta-lactam carbapenem derived from thienamycin, produced by Streptomyces cattleya. Imipenem binds to and inactivates penicillin-binding proteins (PBPs) located on the inner membrane of the bacterial cell wall. PBPs are enzymes that are involved in the last stages of assembling the bacterial cell wall and in reshaping the cell wall during growth and division. This inactivation results in the weakening of the bacterial cell wall and eventually causes cell lysis. Imipenem has the greatest affinity for PBP 1A, 1B, and 2, and its lethal effect is related to binding to PBP 2 and 1B. This antibiotic is active against a wide range of gram-positive and gram-negative organisms and is stable in the presence of beta-lactamases. 42117 bexarotene A synthetic retinoic acid agent with potential antineoplastic, chemopreventive, teratogenic and embryotoxic properties. Bexarotene selectively binds to and activates retinoid X receptors (RXRs), thereby inducing changes in gene expression that lead to cell differentiation, decreased cell proliferation, apoptosis of some cancer cell types, and tumor regression. 42120 incomplete Freund's adjuvant A water-in-oil emulsion that stimulates the T-cell immune response to antigens and may be used in various types of cancer vaccines. 42130 verteporfin A synthetic light-activated agent with photodynamic activity. Upon systemic administration, verteporfin accumulates in neovessels in the eye and, once stimulated by nonthermal red light in the presence of oxygen, produces highly reactive short-lived singlet oxygen and other reactive oxygen radicals, resulting in local damage to neovascular endothelium and blood vessel occlusion. 42140 acarbose A complex oligosaccharide used as a hypoglycemic agent in diabetes management. Acarbose inhibits enzymes required in catabolism of carbohydrates, specifically pancreatic alpha-amylase, which hydrolyzes complex starches to oligosaccharides in the lumen of the small intestine, and the membrane-bound intestinal alpha-glucosidases, which hydrolyze oligosaccharides, trisaccharides, and disaccharides to glucose and other monosaccharides in the small intestine. When acarbose is orally administered, less digestion of complex carbohydrates occur and less glucose is absorbed in the small intestine, thereby producing a smaller rise in postprandial blood glucose levels after a carbohydrate load. 42141 satraplatin An orally administered third generation platinum compound with potential antineoplastic activity. Satraplatin forms highly reactive, charged, platinum complexes which bind to nucleophilic groups in DNA, inducing intrastrand and interstrand DNA cross-links, as well as DNA-protein cross-links. These cross-links result in cell growth inhibition and apoptosis. C1493 42147 alitretinoin An orally- and topically-active naturally-occurring retinoic acid with antineoplastic, chemopreventive, teratogenic, and embryotoxic activities. Alitretinoin binds to and activates nuclear retinoic acid receptors (RAR) and retinoid X receptors (RXR); these activated receptors act as transcription factors, regulating gene expression that results in the inhibition of cell proliferation, induction of cell differentiation, and apoptosis of both normal cells and tumor cells. 42149 tecogalan sodium A sulfated polysaccharide isolated from various Arthrobacter bacterial species. Possessing potential antiangiogenic and antineoplastic properties, tecogalan binds to basic fibroblast growth factor (bFGF), thereby preventing bFGF from binding to its receptors. Disruption of this receptor binding results in the inhibition of bFGF-stimulated endothelial cell growth, proliferation, and migration. 42152 disaccharide tripeptide glycerol dipalmitoyl A lipophilic disaccharide tripeptide derivative of muramyl dipeptide (MDP) with immunomodulatory activity. Disaccharide tripeptide glycerol dipalmitoyl (DTP-GDP)stimulates macrophage activity and increases serum levels of tumor necrosis factor alpha (TNF alpha), neopterin, interleukin (IL)-1 alpha, IL-1 beta, IL-6, IL-8, and IL-12, which may activate host immune system antitumor functions. DTP-GDP may be packaged in liposomes for improved delivery. The immunomodulatory effects of this agent may be superior to those of MDP. C1575 42153 recombinant interleukin-12 A recombinant form of the endogenous heterodimeric cytokine interleukin-12 with potential antineoplastic activity. Recombinant interleukin-12 binds to and activates its cell-surface receptor, stimulating the production of interferon-gamma (IFN) which, in turn, induces IFN-gamma-inducible protein-10 (IP-10) and so inhibits tumor angiogenesis. 42158 tirapazamine A benzotriazine di-N-oxide with potential antineoplastic activity. Tirapazamine is selectively activated by multiple reductases to form free radicals in hypoxic cells, thereby inducing single-and double-strand breaks in DNA, base damage, and cell death. This agent also sensitizes hypoxic cells to ionizing radiation and inhibits the repair of radiation-induced DNA strand breaks via inhibition of topoisomerase II. 42168 talc Finely-powdered native hydrous magnesium silicate. When administered into the pleural space, talc initiates an inflammatory reaction, resulting in adhesion of the visceral pleura to the parietal pleura and fibrosis, thereby effectively closing the pleural space and preventing further accumulation of fluid. This agent exhibits no intrinsic antineoplastic activity. 42183 iron An element with atomic symbol Fe, atomic number 26, and atomic weight 55.85. 42205 MART-1 antigen A tumor-associated melanocytic differentiation antigen. Vaccination with MART-1 antigen may stimulate a host cytotoxic T-cell response against tumor cells expressing the melanocytic differentiation antigen, resulting in tumor cell lysis. 42211 gp100 antigen A melanoma-associated antigen. When administered in a vaccine formulation, gp100 antigen may stimulate a cytotoxic T cell HLA-A2.1-restricted immune response against tumors that express this antigen, which may result in a reduction in tumor size. 42217 sedoxantrone trihydrochloride The trihydrochloride salt of the anthrapyrazole antineoplastic antibiotic sedoxantrone with potential antineoplastic activity. Sedoxantrone intercalates into DNA and interacts with topoisomerase II, thereby inhibiting DNA replication and repair and RNA and protein synthesis. C1576 42223 nolatrexed dihydrochloride The dihydrochloride salt of nolatrexed, a water-soluble lipophilic quinazoline folate analog with antineoplastic activity. Nolatrexed occupies the folate binding site of thymidylate synthase, resulting in inhibition of thymidylate synthase activity and thymine nucleotide synthesis with subsequent inhibition of DNA replication, DNA damage, S-phase cell cycle arrest, and caspase-dependent apoptosis. This agent also exhibits radiosensitizing activity. 42227 bispecific antibody MDX-H210 A humanized bivalent antibody directed against both cytotoxic effector cells expressing Fc gamma receptor type I (Fc gammaRI, or CD64) and HER2/neu-overexpressing tumor cells with potential antineoplastic activity. Bispecific antibody MDX-H210 was constructed by chemically linking Fab' fragments of the anti-HER2/neu-specific monoclonal antibody 520C9 and the Fab' fragments of the anti-Fc gammaRI-specific monoclonal antibody H22. This agent selectively binds to both HER2/neu-expressing tumor cells and Fc gammaRI-expressing cytotoxic effector cells, which may trigger antibody-dependent cell-mediated cytotoxicity (ADCC) and cell lysis of HER2/neu-expressing tumor cells. While HER2/neu is overexpressed in a variety of epithelial malignancies, expression of Fc gammaRI is primarily found in cytotoxic immune cells, including monocytes, macrophages, and cytokine-activated polymorphonuclear (PMN) cells. C1578 42234 epratuzumab A recombinant, humanized monoclonal antibody directed against CD22, a cell surface glycoprotein present on mature B-cells and on many types of malignant B-cells. After binding to CD22, epratuzumab's predominant antitumor activity appears to be mediated through antibody-dependent cellular cytotoxicity (ADCC). 42236 granisetron hydrochloride The hydrochloride salt of an indazole derivative with antiemetic properties. As a selective serotonin receptor antagonist, granisetron competitively blocks the action of serotonin at 5-hydroxytryptamine3 (5-HT3) receptors, resulting in the suppression of chemotherapy- and radiotherapy-induced nausea and vomiting. 42243 nicotine A plant alkaloid, found in the tobacco plant, and addictive central nervous system (CNS) stimulant that causes either ganglionic stimulation in low doses or ganglionic blockage in high doses. Nicotine acts as an agonist at the nicotinic cholinergic receptors in the autonomic ganglia, at neuromuscular junctions, and in the adrenal medulla and the brain. Nicotine's CNS-stimulating activities may be mediated through the release of several neurotransmitters, including acetylcholine, beta-endorphin, dopamine, norepinephrine, serotonin, and ACTH. As a result, peripheral vasoconstriction, tachycardia, and elevated blood pressure may be observed with nicotine intake. This agent may also stimulate the chemoreceptor trigger zone, thereby inducing nausea and vomiting. 42245 samarium Sm 153 lexidronam pentasodium The pentasodium salt of samarium Sm 135 lexidronam, a therapeutic agent consisting of a medium energy beta- and gamma-emitting radioisotope, samarium Sm 135, and a teraphosphonate chelator, ethylenediaminetetramethylene phosphonic acid (EDTMP). The chelator moiety of samarium Sm 153 lexidronam associates with hydroxyapatite crystals concentrated in areas of bone turnover, thereby selectively delivering samarium Sm 153-mediated cytotoxic radiation to osteoblastic bone metastases. C1220 42251 vincristine sulfate The sulfate salt of a natural alkaloid isolated from the plant Vinca rosea Linn with antimitotic and antineoplastic activities. Vincristine binds irreversibly to microtubules and spindle proteins in S phase of the cell cycle and interferes with the formation of the mitotic spindle, thereby arresting tumor cells in metaphase. This agent also depolymerizes microtubules and may also interfere with amino acid, cyclic AMP, and glutathione metabolism; calmodulin-dependent Ca++ -transport ATPase activity; cellular respiration; and nucleic acid and lipid biosynthesis. 42253 leflunomide A derivative of isoxazole used for its immunosuppressive and anti-inflammatory properties. As a prodrug, leflunomide is converted to an active metabolite, A77 1726, which blocks dihydroorotate dehydrogenase, a key enzyme of de novo pyrimidine synthesis, thereby preventing the expansion of activated T lymphocytes. This agent also inhibits various protein tyrosine kinases, such as protein kinase C (PKC), thereby inhibiting cell proliferation. 42257 becatecarin A synthetic diethylaminoethyl analogue of the indolocarbazole glycoside antineoplastic antibiotic rebeccamycin. Becatecarin intercalates into DNA and stabilizes the DNA-topoisomerase I complex, thereby interfering with the topoisomerase I-catalyzed DNA breakage-reunion reaction and initiating DNA cleavage and apoptosis. 42258 NG-monomethyl-L-arginine An amino acid derivative with potential antineoplastic activity. NG-monomethyl-L-arginine inhibits the enzyme nitric oxide synthase, resulting in a diminution of nitrous oxide production. This agent may inhibit tumor angiogenesis. 42260 liposomal cytarabine A liposomal intrathecal formulation of the antimetabolite cytarabine. As an S-phase-specific antimetabolite, cytarabine is phosphorylated by deoxycytidine kinase to a triphosphate form which competes with thymidine for incorporation into DNA; the incorporation of cytarabine triphosphate into DNA appears to inhibit DNA polymerase and so DNA synthesis, resulting in cell death. 42265 trastuzumab A recombinant humanized monoclonal antibody directed against the human epidermal growth factor receptor 2 (HER2). After binding to HER2 on the tumor cell surface, trastuzumab induces an antibody-dependent cell-mediated cytotoxicity against tumor cells that overexpress HER2. HER2 is overexpressed by many adenocarcinomas, particularly breast adenocarcinomas. 42270 PADRE 965.10 Pan-DR epitope (PADRE) 965.10 is a helper peptide. PADRE peptides have been shown the capacity to deliver help for antibody responses in vivo. They were also found to be able to provide significant helper T-cell activity in vivo. Acts as an adjuvant. 42271 recombinant MAGE-3.1 antigen A recombinant tumor-specific melanoma antigen. Vaccination with recombinant MAGE-3.1 antigen may induce a host immune response against MAGE-expressing cells, resulting in antitumoral T cell-mediated cytotoxicity. MAGE-expressing cells are found in melanoma, non-small-cell lung carcinoma (NSCLC), head and neck squamous cell carcinoma, transitional cell carcinoma of the bladder, and esophageal carcinoma. 42274 synthetic human papillomavirus 16 E6 peptide A synthetic peptide sequence of human papillomavirus (HPV) type 16 oncoprotein E6. The E6 oncoprotein is implicated in the tumorigenesis of cervical carcinoma. Vaccination with HPV 16 E6 peptide may stimulate the host immune system to mount a cytotoxic T lymphocyte (CTL) response against cells expressing the E6 oncoprotein, resulting in tumor cell lysis. C38726 42275 human papillomavirus 16 E7 peptide A synthetic peptide sequence of human papillomavirus (HPV) E7 nuclear protein which is used to produce vaccines against HPV infection and HPV-related neoplasms. HPV E7 oncogenic protein binds the retinoblastoma tumor suppressor protein, pRB, as well as a number of other cellular proteins, and serves as a transcriptional activator. This protein is important in the induction and maintenance of cellular transformation and is co-expressed in the majority of HPV-containing carcinomas. 42285 tretinoin liposome An intravenous formulation of tretinoin (vitamin A acid or all-trans retinoic acid) encased in liposomes. Tretinoin is a naturally occurring retinoic acid agent that binds to and activates retinoic acid receptors (RAR), effecting changes in gene expression that lead to cell differentiation, decreased cell proliferation, and inhibition of carcinogenesis. This agent also inhibits telomerase, leading to telomere shortening and eventual apoptosis of certain tumor cell types. Liposome encapsulation extends the half-life of intravenously administered tretinoin. 42286 bispecific antibody 2B1 A monoclonal antibody with potential antineoplastic activity. Specific for both the immunoglobulin G (IgG) receptor CD16 and c-erbB-2, bispecific antibody 2B1 may enhance cellular immune responses against c-erbB-2-positive cells, resulting in increased tumor cell lysis. 42290 tributyrin A triglyceride prodrug of butyric acid with potential antineoplastic activity. Butyrate, the active metabolite of tributyrin, inhibits histone deacetylase, resulting in increased differentiation, decreased proliferation, cell cycle arrest, and apoptosis in some tumor cell lines. 42291 disulfiram A carbamoyl derivate used in the treatment of alcoholism. Disulfiram irreversibly inhibits acetaldehyde dehydrogenase that oxidizes the ethanol metabolite acetaldehyde into acetic acid. This leads to an accumulation of acetaldehyde that produces a variety of very unpleasant symptoms referred to as the disulfiram-alcohol reaction. This reaction includes , but is not limited to, flushing, headache, respiratory difficulty, nausea,vomiting, sweating, thirst, chest pain, tachycardia, blurred vision and hypotension. 42297 exemestane A synthetic androgen analogue. Exemestane binds irreversibly to and inhibits the enzyme aromatase, thereby blocking the conversion of cholesterol to pregnenolone and the peripheral aromatization of androgenic precursors into estrogens. 42298 glutamine A nonessential amino acid. Glutamine can donate the ammonia on its side chain to the formation of urea (for eventual excretion by the kidneys) and to purines (necessary for the synthesis of nucleic acids). Glutamic acid-to-glutamine conversion, in which an ammonia group is added to glutamic acid (catalyzed by glutamine synthase), is of central importance in the regulation of toxic levels of ammonia in the body. This agent is a substrate for the production of both excitatory and inhibitory neurotransmitters (glutamate and GABA) and is also an important source of energy for the nervous system. Glutamine may become a conditionally essential amino acid during certain catabolic states. 42305 7-hydroxystaurosporine A synthetic derivative of staurosporine with antineoplastic activity. 7-hydroxystaurosporine inhibits many phosphokinases, including the serine/threonine kinase AKT, calcium-dependent protein kinase C, and cyclin-dependent kinases. This agent arrests tumor cells in the G1/S of the cell cycle and prevents nucleotide excision repair by inhibiting the G2 checkpoint kinase chk1, resulting in apoptosis. 42307 tetracycline hydrochloride The hydrochloride salt of tetracycline, a broad-spectrum naphthacene antibiotic produced semisynthetically from chlortetracycline, an antibiotic isolated from the bacterium Streptomyces aureofaciens. In bacteria, tetracycline blocks binding of aminoacyl-tRNA to the mRNA-ribosome complex, thereby inhibiting protein synthesis and bacterial cell growth. Because naturally fluorescing tetracycline binds to newly formed bone at the bone/osteoid interface, tetracycline-labeling of bone and fluorescence microscopy may be used to perform bone histomorphometry. C48020 42308 clarithromycin A semisynthetic 14-membered ring macrolide antibiotic. Clarithromycin binds to the 50S ribosomal subunit and inhibits RNA-dependent protein synthesis in susceptible organisms. Clarithromycin has been shown to eradicate gastric MALT (mucosa-associated lymphoid tissue) lymphomas, presumably due to the eradication of tumorigenic Helicobacter pylori infection. This agent also acts as a biological response modulator, possibly inhibiting angiogenesis and tumor growth through alterations in growth factor expression. 42309 omeprazole A benzimidazole with selective and irreversible proton pump inhibition activity. Omeprazole forms a stable disulfide bond with the sulfhydryl group of the hydrogen-potassium (H+ - K+) ATPase found on the secretory surface of parietal cells, thereby inhibiting the final transport of hydrogen ions (via exchange with potassium ions) into the gastric lumen and suppressing gastric acid secretion. This agent exhibits no anticholinergic activities and does not antagonize histamine H2 receptors. 42310 amoxicillin A broad-spectrum, semisynthetic aminopenicillin antibiotic with bactericidal activity. Amoxicillin binds to and inactivates penicillin-binding protein (PBP) 1A located on the inner membrane of the bacterial cell wall. Inactivation of PBPs interferes with the cross-linkage of peptidoglycan chains necessary for bacterial cell wall strength and rigidity. This interrupts bacterial cell wall synthesis and results in the weakening of the bacterial cell wall and causes cell lysis. 42311 bismuth subsalicylate A bismuth salt of salicylic acid. Little absorbed from the gastrointestinal tract, bismuth subsalicylate exerts a local effect on the gastric mucosa, coating it and protecting it from the corrosive effects of acid and pepsin. This agent also has local antimicrobial properties. 42316 dolastatin 10 A pentapeptide originally isolated from the marine mollusk Dolabella auricularia with potential antineoplastic activity. Binding to tubulin, dolastatin 10 inhibits microtubule assembly, resulting in the formation of tubulin aggregates and inhibition of mitosis. This agent also induces tumor cell apoptosis through a mechanism involving bcl-2, an oncoprotein that is overexpressed in some cancers. 42317 recombinant platelet factor 4 A recombinant form of the endogenous chemokine platelet factor 4 with potential antiangiogenesis and antineoplastic activities. As a heparin-binding tetramer, recombinant platelet factor 4 inhibits growth factor-stimulated endothelial cell proliferation, migration, and angiogenesis; it has been shown that this agent inhibits fibroblast growth factor 2 (FGF2) angiogenic activity downstream from the FGF2 receptor. Its activity is antagonized by heparin. Recombinant platelet factor 4 may also directly inhibit the proliferation of some tumor cell types. C2251 42325 denileukin diftitox A cytotoxic recombinant protein consisting of interleukin-2 (IL-2) protein sequences fused to diphtheria toxin. The IL-2 protein sequence moiety of denileukin difitox directs the cytocidal action of diphtheria toxin to cells that express IL-2 receptors. After the toxin moiety is internalized into target IL-2 receptor-expressing cells, its catalytic domain catalyzes the transfer of the ADP-ribose moiety of NAD to a posttranslationally modified histidine residue of elongation factor 2 (EF-2), called diphthamine. This covalent modification inactivates EF-2 and disrupts polypeptide chain elongation, resulting in cell death. 42328 pemetrexed disodium The disodium salt of a synthetic pyrimidine-based antifolate. Pemetrexed binds to and inhibits the enzyme thymidylate synthase (TS) which catalyses the methylation of 2'-deoxyuridine-5'-monophosphate (dUMP) to 2'-deoxythymidine-5'-monophosphate (dTMP), an essential precursor in DNA synthesis. 42331 lurtotecan A semisynthetic analogue of camptothecin with antineoplastic activity. Lurtotecan selectively stabilizes the topoisomerase I-DNA covalent complex and forms an enzyme-drug-DNA ternary complex. As a consequence of the formation of this complex, both the initial cleavage reaction and religation steps are inhibited and subsequent collision of the replication fork with the cleaved strand of DNA results in inhibition of DNA replication, double strand DNA breakage and triggering of apoptosis. Independent from DNA replication inhibition, lurtotecan also inhibits RNA synthesis, multi-ubiquitination and degradation of topoisomerase I and chromatin reorganization. 42332 thalidomide A synthetic derivative of glutamic acid (alpha-phthalimido-glutarimide) with teratogenic, immunomodulatory, anti-inflammatory and anti-angiogenic properties. Thalidomide acts primarily by inhibiting both the production of tumor necrosis factor alpha (TNF-alpha) in stimulated peripheral monocytes and the activities of interleukins and interferons. This agent also inhibits polymorphonuclear chemotaxis and monocyte phagocytosis. In addition, thalidomide inhibits pro-angiogenic factors such as vascular endothelial growth factor (VEGF) and basic fibroblast growth factor (bFGF), thereby inhibiting angiogenesis. 42334 perillyl alcohol A naturally occurring monoterpene related to limonene with antineoplastic activity. Perillyl alcohol inhibits farnesyl transferase and geranylgeranyl transferase, thereby preventing post-translational protein farnesylation and isoprenylation and activation of oncoproteins such as p21-ras, and arresting tumor cells in the G1 phase of the cell cycle. 42338 tyrosinase peptide One of a number of recombinant peptides consisting of amino acid residues of the enzyme tyrosinase, a protein frequently expressed by melanoma cells. Vaccination with tyrosinase peptide may stimulate cytotoxic T lymphocyte response against tyrosinase-expressing tumor cells, resulting in decreased tumor growth. 42346 therapeutic melatonin A therapeutic chemically synthesized form of the pineal indole melatonin with antioxidant properties. The pineal synthesis and secretion of melatonin, a serotonin-derived neurohormone, is dependent on beta-adrenergic receptor function. Melatonin is involved in numerous biological functions including circadian rhythm, sleep, the stress response, aging, and immunity. 42352 lobradimil A synthetic analog of bradykinin. Lobradimil is a potent, specific bradykinin B-2 receptor agonist that stimulates B-2 receptors expressed on the surface of brain capillary endothelial cells, thereby reversibly increasing the permeability of the blood-brain barrier (BBB). Compared to bradykinin, this agent possesses enhanced receptor selectivity, greater plasma stability, and a longer half-life. 42358 octreotide pamoate A synthetic long-acting octapeptide analogue of endogenous somatostatin. Octreotide pamoate binds to somatostatin receptors expressed by some neuroendocrine and non-neuroendocrine tumor cells, thereby initiating somatostatin receptor-mediated apoptosis. Other possible antineoplastic activities of this agent include suppression of tumor angiogenesis and tumor growth-promoting insulin-like growth factor 1 (IGF-1). 42365 recombinant interleukin-11 A recombinant therapeutic agent which is chemically identical to or similar to the endogenous cytokine interleukin 11 (IL-11). Secreted by bone marrow stromal cells and a number of mesenchymal cells, IL-11 binds to and activates its cell-surface receptor, promoting primary and secondary immune responses, modulating antigen-specific antibody reactions, and preventing apoptotic cell death. This agent also stimulates the T-cell-dependent development of IgG-secreting B-cells in spleen cell cultures and may be an important regulator of megakaryocytopoiesis. 42374 oxaliplatin An organoplatinum complex in which the platinum atom is complexed with 1,2-diaminocyclohexane (DACH) and with an oxalate ligand as a 'leaving group.' A 'leaving group' is an atom or a group of atoms that is displaced as a stable species taking with it the bonding electrons. After displacement of the labile oxalate ligand leaving group, active oxaliplatin derivatives, such as monoaquo and diaquo DACH platinum, alkylate macromolecules, forming both inter- and intra-strand platinum-DNA crosslinks, which result in inhibition of DNA replication and transcription and cell-cycle nonspecific cytotoxicity. The DACH side chain appears to inhibit alkylating-agent resistance. 42384 cetuximab A recombinant, chimeric monoclonal antibody directed against the epidermal growth factor (EGFR) with antineoplastic activity. Cetuximab binds to the extracellular domain of the EGFR, thereby preventing the activation and subsequent dimerization of the receptor; the decrease in receptor activation and dimerization may result in an inhibition in signal transduction and anti-proliferative effects. This agent may inhibit EGFR-dependent primary tumor growth and metastasis. EGFR is overexpressed on the cell surfaces of various solid tumors. 42391 motexafin gadolinium A synthetic metallotexaphyrin with radiosensitizing and chemosensitizing properties. Motexafin gadolinium accumulates in tumor cells preferentially due to their increased rates of metabolism, generating reactive oxygen species (ROS) intracellularly and lowering the tumor cell apoptotic threshold to ionizing radiation and chemotherapy. 42402 motexafin lutetium A pentadentate aromatic metallotexaphyrin with photosensitizing properties. Motexafin lutetium preferentially accumulates in tumor cells due to their increased rates of metabolism and absorbs light, forming an extended high energy conformational state that produces high quantum yields of singlet oxygen, resulting in local cytotoxic effects. 42404 boronophenylalanine-fructose complex A boronated phenylalanine complexed with fructose to increase its solubility. When exposed to neutron irradiation, boronophenylalanine absorbs neutrons and self-destructs releasing short-range alpha radiation and 'recoil' lithium in tumor cells, resulting in alpha radiation-induced tumor cell death. This highly selective, localized radiotargeting of tumor cells, known as boron neutron capture therapy (BNCT), spares adjacent normal tissues. 42405 phenobarbital A long-acting barbituric acid derivative with antipsychotic property. Phenobarbital binds to and activates the gamma-aminobutyric acid (GABA)-A receptor, thereby mimicking the inhibitory actions of GABA in the brain. The activation effects of the phenobarbital-receptor-ionophore complex include increased frequency of chloride channel openings, membrane hyperpolarization and ultimately synaptic inhibition and decreased neuronal excitability. In addition, this agent inhibits glutamate induced depolarization. 42418 carbamazepine A tricyclic compound chemically related to tricyclic antidepressants (TCA) with anticonvulsant and analgesic properties. Carbamazepine exerts its anticonvulsant activity by reducing polysynaptic responses and blocking post-tetanic potentiation. Its analgesic activity is not understood; however, carbamazepine is commonly used to treat pain associated with trigeminal neuralgia. 42419 therapeutic dehydroepiandrosterone A synthetic form of dehydroepiandrosterone with potential chemopreventive activity. Produced endogenously, dehydroepiandrosterone (DHEA) is an intermediate in the conversion of cholesterol to androgens and estrogens. Although the mechanisms of action of exogenously administered DHEA have not been fully illuminated, they may result in both direct and indirect physiologic effects. Direct effects include GABA-a receptor complex and NMDA receptor modulation, and enhanced pancreatic beta cell insulin secretion and antiglucocorticoid activities. 42429 KW 2189 A semisynthetic water-soluble derivative of the antineoplastic antibiotic duocarmycin B2. Activated by carboxyl esterase, KW 2189 alkylates DNA by binding to adenine-thymine (A-T)-rich sequences in the minor groove of DNA, thereby inhibiting DNA replication and inducing apoptosis. 42443 marimastat An orally-active synthetic hydroxamate with potential antineoplastic activity. Marimastat covalently binds to the zinc(II) ion in the active site of matrix metalloproteinases (MMPs), thereby inhibiting the action of MMPs, inducing extracellular matrix degradation, and inhibiting angiogenesis, tumor growth and invasion, and metastasis. This agent may also inhibit tumor necrosis factor-alpha converting enzyme (TACE), an enzyme involved in tumor necrosis factor alpha (TNF-alpha) production that may play a role in some malignancies as well as in the development of arthritis and sepsis. 42444 7-cyanoquinocarcinol A semisynthetic analogue of the Streptomyces melanovinaceus-derived tetracyclic antitumor antibiotic quinocarmycin with potential antineoplastic activity. Quinocarmycin belongs to the naphthyridinomycin/saframycin class of antitumor antibiotics. These antibiotics appear to act through DNA alkylation. C1611 42454 MUC-1 antigen MUC-1 antigen is a mammary-type apomucin, a high molecular weight transmembrane glycoprotein, of which the extracellular domain is formed by a repeating 20 amino acid sequence (in tandem) with a high content of serine and threonine on which are O-linked carbohydrate chains. MUC-1 synthesis and secretion are features of glandular epithelial tissues; MUC-1 is overexpressed in lactating breast and in breast, ovary, lung, and prostate malignancies. 42455 biricodar dicitrate The dicitrate salt of a synthetic pipecolinate derivative with potential chemosensitizing activity. Biricodar binds directly to the plasma membrane drug-efflux pumps P-glycoprotein (Pgp) and multidrug resistance protein 1 (MRP-1) and inhibits their activities, which may result in increased intracellular accumulation and retention of cytotoxic agents. C1653 42482 T4N5 liposomal lotion A topical lotion that contains the enzyme T4-bacteriophage endonuclease V encapsulated within liposomes. With topical liposomal delivery, the DNA repair enzyme T4-bacteriophage endonuclease V is transported into skin cells, where the enzyme enters cell nuclei and binds to and incises pyrimidine dimers, thereby catalyzing the first reaction step of the cellular excision repair pathway for removing DNA replication-inhibiting pyrimidine dimers produced within duplex DNA through exposure to ultraviolet (UV) irradiation. In vitro and in vivo studies indicate that T4N5 liposomes increases repair of DNA damage caused by UV irradiation. C2408 42487 prednisone A synthetic glucocorticoid with anti-inflammatory and immunomodulating properties. After cell surface receptor attachment and cell entry, prednisone enters the nucleus where it binds to and activates specific nuclear receptors, resulting in an altered gene expression and inhibition of proinflammatory cytokine production. This agent also decreases the number of circulating lymphocytes, induces cell differentiation, and stimulates apoptosis in sensitive tumor cells populations. 42490 dextromethorphan hydrobromide The hydrobromide salt form of dextromethorphan, a synthetic, methylated dextrorotary analogue of levorphanol, a substance related to codeine and a non-opioid derivate of morphine. Dextromethorphan exhibits antitussive activity and is devoid of analgesic or addictive property. This agent crosses the blood-brain-barrier and activates sigma opioid receptors on the cough center in the central nervous system, thereby suppressing the cough reflex. C423 42491 coumarin O hydroxycinnamic acid. Pleasant smelling compound found in many plants and released on wilting. Has anticoagulant activity by competing with Vitamin K. 42492 arginine butyrate The butyric acid salt of the amino acid arginine. In EBV-related lymphomas, arginine butyrate induces EBV thymidine kinase transcription and may act synergistically with the antiviral agent ganciclovir to inhibit cell proliferation and decrease cell viability. In addition, the butyrate moiety inhibits histone deacetylase, which results in hyperacetylation of histones H3 and H4. Acetylated histones have a reduced affinity for chromatin; this reduced histone-chromatin affinity may allow chromosomal unfolding, potentially enhancing the expression of genes related to tumor cell growth arrest and apoptosis. 42493 soy protein isolate A dietary protein isolated from soybeans that contains isoflavone phytoestrogens. Soy protein isolate has been shown to reduce tumor incidence and growth in some animal studies, possibly by modulating estrogen metabolism, reducing tumor cell proliferation, and inducing tumor cell apoptosis. Soy protein isolate may also inhibit endothelial cell proliferation. Isoflavone phytoestrogens display mild estrogen-like activities which may regulate hormone balance and reduce the risks of breast cancer, heart disease, and osteoporosis. 42494 doxycycline A synthetic, broad-spectrum tetracycline with antimicrobial activity. Doxycycline binds reversibly to the 30S ribosomal subunit and possibly to the 50S ribosomal subunit, blocking the binding of aminoacyl-tRNA to the mRNA-ribosome complex, which results in an inhibition of bacterial protein synthesis. In addition, this agent may inhibit collagenase activity. 42507 zoledronic acid A synthetic imidazole bisphosphonate analog of pyrophosphate with anti-bone-resorption activity. A third-generation bisphosphonate, zoledronic acid binds to hydroxyapatite crystals in the bone matrix, slowing their dissolution and inhibiting the formation and aggregation of these crystals. This agent also inhibits farnesyl pyrophosphate synthase, an enzyme involved in terpenoid biosynthesis. Inhibition of this enzyme prevents the biosynthesis of isoprenoid lipids, donor substrates of farnesylation and geranylgeranylation during the post-translational modification of small GTPase signalling proteins, which are important in the process of osteoclast turnover. Decreased bone turnover and stabilization of the bone matrix contribute to the analgesic effect of zoledronic acid with respect to painful osteoblastic lesions. The agent also reduces serum calcium concentrations associated with hypercalcemia. 42512 FOLFOX regimen One of several chemotherapy regimens that include leucovorin calcium (calcium folinate), 5-fluorouracil and oxaliplatin and which may be used in the treatment of advanced-stage and metastatic colorectal cancer. FOLFOX regimens differ in agent dosing and administration schedule and include FOLFOX 4, FOLFOX 6, modified FOLFOX 6 (mFOLFOX 6) and FOLFOX 7. C11197 42523 monoclonal antibody Me1-14 F(ab')2 The F(ab)2 fragment of Me1-14, a murine IgG2a monoclonal antibody directed against proteoglycan chondroitin sulfate-associated protein expressed by gliomas and melanomas. By binding to proteoglycan chondroitin sulfate-associated protein, monoclonal antibody Me1-14 F(ab')2 conjugated to a radioisotope may localize gliomas and melanomas when used as a tracer in radioimaging applications; in radioimmunotherapeutic applications, this agent conjugated to a radioisotope may be used to deliver targeted radiotoxicity to these tumors. C2409 42527 monoclonal antibody A33 A humanized monoclonal antibody directed against the human A33 antigen. Monoclonal antibody A33 recognizes the human A33 antigen, a 43 KDa transmembrane glycoprotein of the immunoglobulin superfamily, which is highly and homogenously expressed in 95% of colorectal cancer metastases with only restricted expression in normal colonic mucosa. 42528 rubitecan A semisynthetic agent related to camptothecin with potent antitumor and antiviral properties. Rubitecan binds to and inhibits the enzyme topoisomerase I and induces protein-linked DNA single-strand breaks, thereby blocking DNA and RNA synthesis in dividing cells; this agent also prevents repair of reversible single-strand DNA breaks. 42540 anastrozole A nonsteroidal inhibitor of estrogen synthesis that resembles paclitaxel in chemical structure. As a third-generation aromatase inhibitor, anastrozole selectively binds to and reversibly inhibits aromatase, a cytochrome P-450 enzyme complex found in many tissues including those of the premenopausal ovary, liver, and breast; aromatase catalyzes the aromatization of androstenedione and testosterone into estrone and estradiol, the final step in estrogen biosynthesis. In estrogen-dependent breast cancers, anastrozole may inhibit tumor growth. 42544 enalapril maleate The maleate salt form of enalapril, a dicarbocyl-containing peptide and angiotensin-converting enzyme (ACE) inhibitor with antihypertensive activity. As a prodrug, enalapril is converted by de-esterification into its active form enalaprilat. Enalaprilat competitively binds to and inhibits ACE, thereby blocking the conversion of angiotensin I to angiotensin II. This prevents the potent vasoconstrictive actions of angiotensin II and results in vasodilation. Enalapril also decreases angiotensin II-induced aldosterone secretion by the adrenal cortex, which leads to an increase in sodium excretion and subsequently increases water outflow. C468 42545 cidofovir A synthetic, acyclic, monophosphate nucleotide analog of deoxycytidine with antiviral activity, and mostly used against cytomegalovirus (CMV). After incorporation into the host cell, cidofovir is phosphorylated by pyruvate kinases to its active metabolite cidofovir diphosphate. Cidofovir diphosphate, bearing structural similarity to nucleotides, competes with deoxycytosine-5-triphosphate (dCTP) for viral DNA polymerase and gets incorporated into the growing viral DNA strands. As a result, it prevents further DNA polymerization and disrupts DNA replication of viruses. 42546 penicillamine A beta dimethyl analog of the amino acid cysteine. As a degradation product of penicillin antibiotics, penicillamine chelates with heavy metals and increases their urinary excretion. Possessing antineoplastic properties, penicillamine induces apoptosis by a p53-mediated mechanism and inhibits angiogenesis by chelating with copper, a cofactor for angiogenesis. 42554 larotaxel A semi-synthetic derivative of the taxane 10-deacetylbaccatin III with potential antineoplastic activities. Larotaxel binds to tubulin, promoting microtubule assembly and stabilization and preventing microtubule depolymerization, thereby inhibiting cell proliferation. As it represents poor substrate for P-glycoprotein-related drug resistance mechanisms, this agent may be useful for treating multi-drug resistant tumors. Larotaxel penetrates the blood brain barrier. C48427 42555 sirolimus A natural macrocyclic lactone produced by the bacterium Streptomyces hygroscopicus, with immunosuppressant properties. In cells, sirolimus binds to the immunophilin FK Binding Protein-12 (FKBP-12) to generate an immunosuppressive complex that binds to and inhibits the activation of the mammalian Target Of Rapamycin (mTOR), a key regulatory kinase. This results in inhibition of T lymphocyte activation and proliferation that occurs in response to antigenic and cytokine (IL-2, IL-4, and IL-15) stimulation and inhibition of antibody production. 42559 carboxyphenyl retinamide A synthetic phenylretinamide analogue of retinol (vitamin A) with potential antineoplastic and chemopreventive activities. Carboxyphenyl retinamide induces cell differentiation and inhibits tumor cell growth and carcinogenesis. This agent may also induce cell cycle arrest in the G1 phase in some cancer cell types. 42562 pentetic acid calcium The calcium salt of pentetic acid, a synthetic chelating agent related to the chelating agent ethylenediaminetetraacetic acid (EDTA). Pentetic acid chelates with the metallic radioisotopic moieties of unbound, extracellular radioimmunotherapeutic agents, resulting in higher specific tumor cell binding of radioimmunotherpeutic agents; this results in improved tumor cell radiocytotoxicity and the sparing of normal cells and tissues from the radiocytotoxic effects of these agents. 42572 KW-2149 A semisynthetic water-soluble disulfide derivative of the antineoplastic antibiotic mitomycin C. Activated by serum and glutathione, KW-2149 causes interstrand DNA cross-links and DNA-protein cross-links, resulting in single-strand DNA breaks and inhibition of DNA synthesis. 42577 trabectedin A tetrahydroisoquinoline alkaloid isolated from the marine tunicate Ecteinascidia turbinate with potential antineoplastic activity. Binding to the minor groove of DNA, trabectedin inteferes with the transcription-coupled nucleotide excision repair machinery to induce lethal DNA strand breaks.and blocks the cell cycle in the G2 phase. 42581 KRN5500 A semisynthetic derivative of the nucleoside-like antineoplastic antibiotic spicamycin, originally isolated from the bacterium Streptomyces alanosinicus. KRN 5500 inhibits protein synthesis by interfering with endoplasmic reticulum and Golgi apparatus functions. This agent also induces cell differentiation and caspase-dependent apoptosis. 42584 leucovorin calcium An active metabolite of folic acid (also called folinic acid and citrovorum factor), which does not require metabolism by dihydrofolate reductase, the molecular target of folate antagonist-type chemotherapeutic drugs. Leucovorin calcium counteracts the toxic effects of these medications, 'rescuing' the patient while permitting the antitumor activity of the folate antagonist. This agent also potentiates the effects of fluorouracil and its derivatives by stabilizing the binding of the drug's metabolite to its target enzyme, thus prolonging drug activity. 42585 carcinoembryonic antigen peptide 1 A nine amino acid peptide fragment of carcinoembryonic antigen (CEA), a protein that is overexpressed in several cancer cell types, including gastrointestinal, breast, and non-small cell lung. Autologous vaccination with activated autologous dendritic cells (DC) or peripheral blood mononuclear cells (PBMC) which have been exposed to CEA peptide 1 in vitro may stimulate the host immune system to mount a cytotoxic T lymphocyte (CTL) response against tumor cells expressing CEA, thereby inhibiting tumor growth. 42587 gimeracil A pyridine derivative with antitumor activity. Gimeracil enhances the antitumor activity of fluoropyrimidines by competitively and reversibly inhibiting the enzyme dihydropyrimidine dehydrogenase causing decreased degradation of the fluoropyrimidines. 42593 lamivudine A synthetic nucleoside analogue with activity against hepatitis B virus (HBV) and HIV. Intracellularly, lamivudine is phosphorylated to its active metabolites, lamiduvine triphosphate (L-TP) and lamiduvine monophosphate (L-MP). In HIV, L-TP inhibits HIV-1 reverse transcriptase (RT) via DNA chain termination after incorporation of the nucleoside analogue into viral DNA. In HBV, incorporation of L-MP into viral DNA by HBV polymerase results in DNA chain termination. L-TP is a weak inhibitor of mammalian DNA polymerases alpha and beta, and mitochondrial DNA polymerase. 42594 indinavir sulfate A synthetic antiviral agent. Indinavir selectively binds to the active site of human immunodeficiency virus (HIV) protease and inhibits its activity, preventing the protease-mediated cleavage of gag-pol viral polyproteins; as a result immature, noninfectious virions are produced. C1662 42600 romidepsin A bicyclic depsipeptide antibiotic isolated from the bacterium Chromobacterium violaceum with antineoplastic activity. After intracellular activation, romidepsin binds to and inhibits histone deacetylase (HDAC), resulting in alterations in gene expression and the induction of cell differentiation, cell cycle arrest, and apoptosis. This agent also inhibits hypoxia-induced angiogenesis and depletes several heat shock protein 90 (Hsp90)-dependent oncoproteins. 42606 tin ethyl etiopurpurin A synthetic purpurin with photosensitizing activity. Tin ethyl etiopurpurin preferentially accumulates in tumor cells due to an increased rate of metabolism. Upon exposure to a light source, this agent absorbs light, forming an extended high energy conformational state that produces high quantum yields of singlet oxygen with local cytotoxic effects. 42609 fludeoxyglucose F 18 A positron-emitting radiopharmaceutical containing radioactive 2-deoxy-2-[18F] fluoro-D-glucose. With similar cell uptake as glucose (high in tumor cells), fludeoxyglucose F 18 is not dephosphorylated and further metabolized. 42612 arcitumomab A murine IgG monoclonal Fab fragment antibody labeled with technetium-99m directed against carcinoembryonic antigen (CEA), a protein that is overexpressed by many tumor cell types. For tumors that overexpress CEA, arcitumomab may be used as an adjunct diagnostic imaging tool to obtain prognostic information following resection and to monitor for recurrent disease. 42613 rituximab A recombinant chimeric murine/human antibody directed against the CD20 antigen, a hydrophobic transmembrane protein located on normal pre-B and mature B lymphocytes. Following binding, rituximab triggers a host cytotoxic immune response against CD20-positive cells. 42622 levodopa An amino acid precursor of dopamine with antiparkinsonian properties. Levodopa is a prodrug that is converted to dopamine by DOPA decarboxylase and can cross the blood-brain barrier. When in the brain, levodopa is decarboxylated to dopamine and stimulates the dopaminergic receptors, thereby compensating for the depleted supply of endogenous dopamine seen in Parkinson's disease. To assure that adequate concentrations of levodopa reach the central nervous system, it is administered with carbidopa, a decarboxylase inhibitor that does not cross the blood-brain barrier, thereby diminishing the decarboxylation and inactivation of levodopa in peripheral tissues and increasing the delivery of dopamine to the CNS. 42624 efaproxiral A synthetic small molecule with radiosensitizing activity. Efaproxiral increases oxygen levels in hypoxic tumor tissues by binding non-covalently to the hemoglobin tetramer and decreasing hemoglobin-oxygen binding affinity. Increasing tumor oxygenation reduces tumor radioresistance. C37453 42625 raltitrexed A quinazoline folate analogue with antineoplastic activity. After transport into cells via the reduced folate carrier, raltitrexed undergoes intracellular polyglutamation and blocks the folate-binding site of thymidylate synthase, thereby inhibiting tetrahydrofolate activity and DNA replication and repair and resulting in cytotoxicity. 42626 tipifarnib A nonpeptidomimetic quinolinone with potential antineoplastic activity. Tipifarnib binds to and inhibits the enzyme farnesyl protein transferase, an enzyme involved in protein processing (farnesylation) for signal transduction. By inhibiting the farnesylation of proteins, this agent prevents the activation of Ras oncogenes, inhibits cell growth, induces apoptosis, and inhibits angiogenesis. 42628 gonadotrophin releasing hormone Specifically expressed in hypothalamic neurons as a preproprotein, Gonadotropin Releasing Hormones (GnRH Family) are secreted into the median eminence capillary plexus, bind to receptors on anterior pituitary gonadotrophs, and stimulate release of LHRH and FSH gonadotropins to control female reproduction. 42631 recombinant adenovirus-p53 SCH-58500 A genetically-engineered adenovirus that contains the gene that encodes the human tumor-suppressor protein p53 with potential antineoplastic activity. Recombinant adenovirus-p53 SCH-58500 delivers p53 into tumor cells, which may result in p53-mediated cell cycle arrest and apoptosis. 42639 isosulfan blue A synthetic visual lymphatic imaging agent. Injected into the periphery of the tumor site, isosulfan blue localizes to the lymphatic system and aids in the surgical identification of tumor sentinel nodes which stain blue. 42648 aminolevulinic acid A topically administered metabolic precursor of protoporphyrin IX. After topical administration, aminolevulinic acid (ALA) is converted to protoporphyrin IX (PpIX) which is a photosensitizer. When the proper wavelength of light activates protoporphyrin IX, singlet oxygen is produced, resulting in a local cytotoxic effect. 42650 methionine C 11 A synthetic amino acid radiolabeled with carbon-11. Acting as a methyl donor, methionine C 11 is incorporated into macromolecules, where it serves as a positron emission tomography (PET) imaging agent for detecting tumors with high rates of protein synthesis. C1534 42652 monoclonal antibody 3H1 anti-idiotype vaccine A recombinant monoclonal antibody in which the heavy and light chain variable domains mimic a specific epitope of the tumor-associated protein carcinoembryonic antigen (CEA). This agent is used as a cancer vaccine against tumors that express CEA. 42653 DetoxPC A detoxified, nonspecific immunostimulant consisting of a combination of the active monophosphoryl lipid A component of lipopolysaccharide (LPS) isolated from the bacterium Salmonella minnesota combined with a residue of the cell wall of the bacterium Mycobacterium phlei. Detox-PC differs from Detox adjuvant and Detox-B in that Detox-PC contains egg phosphatidylcholine and alpha-tocopherol. 42657 isotretinoin A naturally-occurring retinoic acid with potential antineoplastic activity. Isotretinoin binds to and activates nuclear retinoic acid receptors (RARs); activated RARs serve as transcription factors that promote cell differentiation and apoptosis. This agent also exhibits immunomodulatory and anti-inflammatory responses and inhibits ornithine decarboxylase, thereby decreasing polyamine synthesis and keratinization. 42662 HER-2/neu peptide vaccine A cancer vaccine comprised of peptides derived from the extracellular domain of the tumor-associated antigen Her-2/neu with potential antineoplastic activity. HER-2/neu peptide vaccine may induce antibodies with anti-tumor activity and may also elicit a specific CD8 T-cell response against specific tumor cell types. C2537 42663 dendritic cell-MART-1 peptide vaccine A cancer vaccine consisting of dendritic cells harvested from a patient with cancer and pulsed or transduced with a peptide fragment of MART-1 (melanoma antigen recognized by T-cells), an antigen expressed by melanoma cells. When the altered dendritic cells are returned to the patient, they stimulate the host immune system to mount a cytotoxic T-lymphocyte immune response against tumor cells expressing MART-1. 42665 ritonavir A synthetic aromatic derivative with antiviral properties. Ritonavir is a peptidomimetic agent that inhibits both HIV-1 and HIV-2 proteases, thereby preventing the cleavage of Gag-Pol polyproteins and resulting in the production of noninfectious viral particles. This agent is more active against HIV-1. Because ritonavir targets the HIV replication cycle after translation and before assembly, it is active in chronically infected cells that generally are not affected by nucleoside reverse transcriptase inhibitors. 42667 cordycepin A purine nucleoside antimetabolite and antibiotic isolated from the fungus Cordyceps militaris with potential antineoplastic activity. Cordycepin is an adenosine analogue, which is readily phosphorylated to its mono-, di-, and triphosphate intracellularly. Triphosphate cordycepin can be incorporated into RNA, and inhibits transcription elongation and RNA synthesis due to the absence of a hydroxyl moiety at the 3' position. Because it can be converted to an inactive metabolite by adenosine deaminase, this agent must be administered with an adenosine deaminase inhibitor in order to be effective. Cordycepin has displayed cytotoxicity against some leukemic cell lines in vitro. 42670 tocladesine An antimetabolite and a chlorine derivative of the intracellular secondary messenger, cyclic adenosine 3,5-monophosphate (cAMP), with potential antineoplastic activity. Tocladesine appears to be converted to 8-chloro-adenosine by phosphodiesterases and subsequently phosphorylated to 8-chloro-ATP, which functions as a purine analogue and competes with ATP in transcription. In addition, generation of 8-chloro-ATP depletes endogenous ATP pool that is essential for many biological reactions in intracellular energy transfer. As a result, this agent causes RNA synthesis inhibition, blocks cellular proliferation, and induces apoptosis. 42672 benzydamine hydrochloride An indazole non-steroidal anti-inflammatory drug (NSAID) with analgesic, antipyretic, and anti-edema properties. Unlike other NSAIDs, benzydamine hydrochloride does not inhibit cyclooxygenases (COX) but stabilizes membranes, resulting in local anesthesia; inhibits the production of pro-inflammatory cytokines; inhibits the generation of reactive oxygen species by neutrophils; inhibits leukocyte aggregation and adhesion; and exhibits antimicrobial properties. 42674 mitomycin C A methylazirinopyrroloindoledione antineoplastic antibiotic isolated from the bacterium Streptomyces caespitosus and other Streptomyces bacterial species. Bioreduced mitomycin C generates oxygen radicals, alkylates DNA, and produces interstrand DNA cross-links, thereby inhibiting DNA synthesis. Preferentially toxic to hypoxic cells, mitomycin C also inhibits RNA and protein synthesis at high concentrations. C1820 42675 tanomastat A biphenyl matrix metalloproteinase (MMP) inhibitor (MMPI) with potential antineoplastic activity. Tanomastat inhibits MMP-2, MMP-3, and MMP-9, inhibiting extracellular matrix degradation and potentially inhibiting angiogenesis, tumor growth and invasion, and metastasis. MMPs consist of at least 18 zinc-containing endo-proteinases that are capable of degrading collagen and proteoglycan. C1705 42677 nandrolone decanoate The decanoate salt form of nandrolone, an anabolic steroid analog of testosterone with androgenic, anabolic, and erythropoietin stimulating effects. Nandrolone enters the cell and binds to and activates specific nuclear androgen receptors in responsive tissue, including the prostate, seminal vesicles, scrotum, penis, larynx, hair follicles, muscle, and bone. The resulting activated hormone receptor complex translocates into the nucleus and binds to androgen response elements (ARE) in the promoter region of targeted genes, where the complex promotes gene expression necessary for maintaining male sex characteristics. Mimicking the negative feedback mechanism of testosterone, nandrolone decanoate also suppresses the secretion of luteinizing hormone (LH). Furthermore, this agent also stimulates erythropoietin production by enhancing the production of erythropoietic stimulating factors. 42679 sargramostim plasmid DNA melanoma vaccine adjuvant A vaccine adjuvant consisting of a plasmid DNA encoding sargramostim (a granulocyte macrophage-colony stimulating factor). Upon administration, expressed sargramostim may stimulate a cytotoxic T cell response enhancing the host immune response to a concomitantly administered melanoma vaccine. C2430 42680 iodine I 131 monoclonal antibody 3F8 A radioimmunoconjugate consisting of 3F8, a murine anti-GD2 ganglioside monoclonal antibody labeled with iodine 131 (I-131), with radioimaging and radioimmunotherapeutic properties. Using monoclonal antibody 3F8 as a carrier for I-131 results in the targeted imaging and/or destruction of cells expressing GD2. GD2 is a ganglioside which is overexpressed in malignant melanoma, neuroblastoma, and small cell carcinoma of the lung. 42681 autologous Epstein-Barr virus-specific cytotoxic T lymphocytes A preparation of lymphocytes harvested from a patient with an Epstein-Barr virus (EBV)-positive tumor. Ex vivo, the lymphocytes are activated against EBV-specific antigens and then returned to the patient, where they mount a specific immune response against EBV-positive tumor cells. 42682 vitespen An autologous cancer vaccine derived from tumor-specific gp96 heat shock proteins. Heat shock proteins chaperone peptides through the endoplasmic reticulum, are key regulators of dendritic cell maturation, migration and antigen processing, and are involved in T-cell activation. 42683 LMB-7 immunotoxin A single chain chimeric protein consisting of a monoclonal antibody fragment attached to a portion of the Pseudomonas exotoxin A. LMB-7 immunotoxin attaches to B3, a Lewis Y-related carbohydrate epitope on some solid tumor cells. The antibody attaches to the cell and the exotoxin inhibits protein synthesis by inactivating elongation factor 2. 42684 sabarubicin A disaccharide analogue of the anthracycline antineoplastic antibiotic doxorubicin. Sabarubicin intercalates into DNA and interacts with topoisomerase II, thereby inhibiting DNA replication and repair and RNA and protein synthesis. This agent also induces apoptosis through a p53-independent mechanism. Sabarubicin is less cardiotoxic than doxorubicin. C1706 42688 bizelesin A synthetic cyclopropylpyrroloindole antineoplastic antibiotic. Bizelesin binds to the minor groove of DNA and induces interstrand cross-linking of DNA, thereby inhibiting DNA replication and RNA synthesis. Bizelesin also enhances p53 and p21 induction and triggers G2/M cell-cycle arrest, resulting in cell senescence without apoptosis. 42690 voriconazole A synthetic triazole with antifungal activity. Voriconazole selectively inhibits 14-alpha-lanosterol demethylation in fungi, preventing the production of ergosterol, an essential constituent of the fungal cell membrane, and resulting in fungal cell lysis. C1707 42691 recombinant vaccinia prostate-specific antigen vaccine A vaccine consisting of recombinant vaccinia virus encoding prostate specific antigen (PSA). Vaccination with recombinant vaccinia prostate-specific antigen vaccine stimulates the host immune system to mount a cytotoxic T-cell response against tumor cells expressing PSA. 42692 ethynyluracil An orally-active fluoropyrimidine analogue. Ethynyluracil inhibits dihydropyrimidine dehydrogenase, the rate-limiting enzyme that catabolizes and inactivates 5-fluorouracil (5-FU) in the liver. Co-administration of ethynyluracil permits the oral administration of 5-FU. 42693 saquinavir mesylate The mesylate salt form of saquinavir, a synthetic peptidomimetic substrate with antiviral property. Saquinavir selectively binds to and inhibits human immunodeficiency virus type 1 (HIV-1) protease, an aspartic protease that cleaves viral gag and gag-pol polyprotein (precursors for viral proteases, reverse transcriptase, and integrase). Inhibition of HIV-1 protease prevents functional viral proteins to be cleaved from the viral polyprotein precursor and results in the release of immature, noninfectious virions. 42694 nelfinavir mesylate The mesylate salt form of the antiviral agent nelfinavir. Nelfinavir selectively inhibits human immunodeficiency virus (HIV) protease, thereby preventing cleavage of the gag-pol viral polyprotein and resulting in the release of immature, noninfectious virions. In vivo, this agent exhibits broad tissue distribution compared to related agents. 42697 cisplatin-e therapeutic implant An injectable collagen matrix gel containing the inorganic platinum agent cisplatin and the sympathicomimetic agent epinephrine with potential antineoplastic activity. After intratumoral injection, cisplatin alkylates guanine nucleosides in DNA, and causes DNA-DNA or DNA-protein cross-linkages, thereby preventing DNA replication and resulting in tumor cell growth inhibition and apoptosis. Epinephrine, a potent vasoconstrictor, is added to the gel to enhance penetration of cisplatin into tumor tissue and reduce dispersion into the surrounding tissues. Intratumoral injection of cisplatin-E therapeutic implant may increase local chemotherapeutic efficacy compared to the systemic administration of these agents while reducing systemic toxicity. C17879 42699 IL-2 plasmid DNA/lipid complex An immunotherapeutic agent consisting of a plasmid DNA encoding human Interleukin-2 (IL-2) complexed with a cationic lipid, 1,2-dimyristyloxypropyl-3-dimethyl-hydroxyethyl ammonium bromide/dioleyl-phosphatidyl-ethanolamine (DMRIE/DOPE), in a 5:1 ratio. Due to the lipophilic nature of this cation liposome complex, this gene transfer system may improve the efficiency of introducing the IL-2 gene into the cells, thereby increasing the production of IL-2 and inducing an immune response. 42702 ras peptide cancer vaccine A cancer vaccine containing a RAS oncogene-encoded peptide with potential antineoplastic activity. RAS peptide cancer vaccine may stimulate a RAS peptide-specific antitumoral T-cell cytotoxic immune response, resulting in an inhibition of tumor cell proliferation and tumor cell death. C2438 42704 carcinoembryonic antigen RNA-pulsed DC cancer vaccine A vaccine comprising autologous dendritic cells pulsed with mRNA-encoded Carcinoembryonic Antigen (CEA) that targets tumor cells expressing CEA. 42706 troglitazone An orally-active thiazolidinedione with antidiabetic and hepatotoxic properties and potential antineoplastic activity. Troglitazone activates peroxisome proliferator-activated receptor gamma (PPAR-gamma), a ligand-activated transcription factor, thereby inducing cell differentiation and inhibiting cell growth and angiogenesis. This agent also modulates the transcription of insulin-responsive genes, inhibits macrophage and monocyte activation, and stimulates adipocyte differentiation. 42707 iodine I 124 monoclonal antibody A33 A radioimmunoconjugate of a humanized monoclonal antibody (MoAb) A33 labelled with Iodine 124 (I-124). MoAb A33 recognizes A33 antigen, a 43 KDa transmembrane glycoprotein of the immunoglobulin superfamily, highly and homogenously expressed in 95% of colorectal cancer metastases, with only restricted expression in normal colonic mucosa. I-124 MoAb A33 delivers beta particle emitting I-124 nuclide directly to metastatic colorectal tissues, thereby this agent could be used in kinetics studies or radioimmunotherapy. C2440 42766 canarypox-hIL-12 melanoma vaccine A vaccine consisting of a replication-defective recombinant canarypox virus (ALVAC) that encodes the gene for human interleukin-12 (hIL-12). Produced mainly by B-cells, IL-12 is an endogenous cytokine that activates natural killer (NK) cells, promotes cytotoxic T lymphocyte (CTL) responses, induces the release of interferon-gamma (IFN-gamma), and may exhibit antitumor and anti-angiogenic effects. Vaccination with canarypox-hIL-12 melanoma vaccine may stimulate the host immune system to mount an immune response against tumor cells, thereby inhibiting tumor growth and/or metastasis. 42783 alfentanil hydrochloride The hydrochloride salt form of alfentanil, an ultra short-acting, synthetic, opioid agonist with analgesic and local anesthesia enhancing activity. Alfentanil hydrochloride primarily binds to and stimulates the opiate receptors in the central nervous system (CNS), thereby mimicking the actions of endogenous opioids. Stimulation of the mu-subtype opioid receptor stimulates the exchange of GTP for GDP on the G-protein complex and subsequently inhibits adenylate cyclase. This results in a decrease in intracellular cAMP and leads to a reduction in the release of various neurotransmitters. The analgesic effect of alfentanil is likely due to the actions of its metabolite morphine, which induces opening of G-protein-coupled inwardly rectifying potassium (GIRK) channels and blocks the opening of N-type voltage-gated calcium channels, thereby resulting in hyperpolarization and reduced neuronal excitability. 42793 paroxetine hydrochloride The hydrochloride salt form of paroxetine, a phenylpiperidine derivative and a selective serotonin reuptake inhibitor (SSRI) with antidepressant and anxiolytic properties. Paroxetine binds to the pre-synaptic serotonin transporter complex resulting in negative allosteric modulation of the complex thereby blocking reuptake of serotonin by the pre-synaptic transporter. Inhibition of serotonin recycling enhances serotonergic function through serotonin accumulation in the synaptic cleft, resulting in long-term desensitization and downregulation of 5HT1 (serotonin) receptors and leading to symptomatic relief of depressive illness. 42797 mycophenolate mofetil The morpholinoethyl ester of mycophenolic acid (MPA) with potent immunosuppressive properties. Mycophenolate stops T-cell and B-cell proliferation through selective inhibition of the de novo pathway of purine biosynthesis. In vivo, the active metabolite, MPA, reversibly inhibits inosine 5'-monophosphate dehydrogenase, an enzyme involved in the de novo synthesis of guanine nucleotides. MPA displays high lymphocyte specificity and cytotoxicity due to the higher dependence of activated lymphocytes on both salvage and de novo synthesis of guanine nucleotides relative to other cell types. 42801 etoposide phosphate A phosphate salt of a semisynthetic derivative of podophyllotoxin. Etoposide binds to the enzyme topoisomerase II, inducing double-strand DNA breaks, inhibiting DNA repair, and resulting in decreased DNA synthesis and tumor cell proliferation. Cells in the S and G2 phases of the cell cycle are most sensitive to this agent. 42806 iodine I 131 tositumomab A monoclonal antibody directed against the CD20 protein expressed on the surface of B-lymphocytes and radiolabeled with the radioisotope iodine I 131 with potential antineoplastic activity. Iodine I 131 tositumomab binds to and selectively delivers cyctotoxic radiation to CD20-expressing B-lymphocytes, thereby minimizing systemic radiotoxicity. 42810 sargramostim plasmid DNA pancreatic tumor cell vaccine A whole cell vaccine comprised of irradiated allogenic pancreatic tumor cells transfected with a plasmid DNA encoding human sargramostim (GM-CSF). Vaccination results in expression of GM-CSF, which induces proliferation and differentiation hematopoietic lineage cells as well as stimulating macrophage and dendritic cell functions in antigen presentation and antitumor cell-mediated immunity. Furthermore, administration of this pancreatic tumor cell vaccine may elicit a cytotoxic T lymphocyte (CTL) response against similar host tumor cells, resulting in decreased tumor growth. C2445 42818 technetium Tc 99m sulfur colloid A gamma-emitting colloid used in scintillation scanning of the reticuloendothelial system (RES). After intravenous administration, technetium Tc 99m sulfur colloid is phagocytized by the reticuloendothelial system and concentrated in the liver, spleen, and bone marrow; detection/localization of phagocytized gamma ray-emitting colloid is performed with a gamma-ray scintillation camera. Scintillation scanning using technetium Tc 99m colloid sulfur helps determine the distribution and function of the RES and the extent to which tumor involves the RES. The RES includes cells types that can phagocytize and sequester inert particles and vital dyes; RES cell types include macrophages or macrophage precursors, specialized endothelial cells lining the sinusoids of the liver, spleen, and bone marrow, and reticular cells of lymphatic tissue and of bone marrow. 42831 streptozocin A methylnitrosourea antineoplastic antibiotic isolated from the bacterium Streptomyces achromogenes. Streptozocin alkylates DNA, forming inter-strand DNA cross-links and inhibiting DNA synthesis. Due to its glucose moiety, this agent is readily taken up by pancreatic beta cells, inducing diabetes mellitus at high concentrations. Unlike other nitrosoureas, streptozocin causes little myelosuppression. 42834 monoclonal antibody A27.15 A murine IgG1 monoclonal antibody directed against the human transferrin (Tf) receptor. Monoclonal antibody A27.15 binds to the Tf receptor, blocking the binding of transferrin to the receptor and resulting in decreased tumor cell growth. 42835 monoclonal antibody E2.3 A murine IgG1 monoclonal antibody directed against the human transferrin (Tf) receptor. Monoclonal antibody E2.3 binds to the Tf receptor, blocking the binding of transferrin to the receptor and resulting in decreased tumor cell growth. 42852 capecitabine A fluoropyrimidine carbamate belonging to the class of antineoplastic agents called antimetabolites. As a prodrug, capecitabine is selectively activated by tumor cells to its cytotoxic moiety, 5-fluorouracil (5-FU); subsequently, 5-FU is metabolized to two active metabolites, 5-fluoro-2-deoxyuridine monophosphate (FdUMP) and 5-fluorouridine triphosphate (FUTP) by both tumor cells and normal cells. FdUMP inhibits DNA synthesis and cell division by reducing normal thymidine production, while FUTP inhibits RNA and protein synthesis by competing with uridine triphosphate for incorporation into the RNA strand. 42854 iodine I 131 chimeric monoclonal antibody G-250 A radioimmunoconjugate comprised of the chimeric monoclonal antibody G-250 conjugated with iodine I 131 with potential antineoplastic activity. The antibody moiety of iodine I 131 chimeric monoclonal antibody G-250 binds to G-250, a renal-cell carcinoma-associated antigen, delivering cytotoxic iodine I 131 specifically to renal cell carcinoma cells that express G-250. C2449 42856 arzoxifene hydrochloride The hydrochloride salt of arzoxifene, a synthetic aromatic derivative with anti-estrogenic properties. Arzoxifene binds to estrogen receptors as a mixed estrogen agonist/antagonist. In comparison to other selective estrogen receptor modulators (SERMs), arzoxifene exhibits greater bioavailability and higher anti-estrogenic potency in the breast than raloxifene; it exhibits reduced estrogenicity in the uterus compared with either tamoxifen or raloxifene. This agent may have beneficial effects on bone and the cardiovascular system. 42860 ALVAC-hB7.1 A vaccine comprise of a canarypox viral vector that carries the gene for human B7.1 (CD80 antigen) with potential use as an autologous therapeutic cancer vaccine. Tumor cells harvested from a patient are infected with ALVAC-hB7 1, thereby producing an autologous cell line that exhibits increased expression of HLA class I and class II, CD54 (ICAM), and CD80. Increased expression of these proteins by this autologous cell line may activate an antitumor T-cell response when the modified cells are administered to the patient. 42865 ofloxacin A fluoroquinolone antibacterial antibiotic. Ofloxacin binds to and inhibits bacterial topoisomerase II (DNA gyrase) and topoisomerase IV, enzymes involved in DNA replication and repair, resulting in cell death in sensitive bacterial species. 42866 ziconotide A synthetic, nonopiod, twenty-five amino acid polybasic peptide analogue of an omega-conotoxin derived from the marine snail Conus magus with analgesic activity. Ziconotide appears to block neuronal N-type voltage-sensitive calcium channels (NCCB), inhibiting transmission from pain-sensing primary nociceptors. This agent may exhibit significant analgesic activity in refractory pain. C1475 42868 gemtuzumab ozogamicin A recombinant, humanized anti-CD33 monoclonal antibody attached to the cytotoxic antitumor antibiotic calicheamicin. In this conjugate, the antibody binds to and is internalized by tumor cells expressing CD33 antigen (a sialic acid-dependent glycoprotein commonly found on the surface of leukemic blasts), thereby delivering the attached calicheamicin to CD33-expressing tumor cells. Calicheamicin binds to the minor groove of DNA, causing double strand DNA breaks and resulting in inhibition of DNA synthesis. 42870 interferon alfacon-1 An analogue of consensus interferon which contains an additional methionyl amino acid residue. Consensus interferon (also known as interferon alfacon-1, rCon-IFN, and CIFN) is a genetically engineered synthetic interferon created from the most common amino acid sequences from the naturally occurring alpha interferons. Alpha interferons bind to specific cell-surface receptors, resulting in the transcription and translation of genes whose protein products have antiviral, antiproliferative, anticancer, and immune-modulating effects. 42870 interferon alfacon-1 An analogue of consensus interferon which contains an additional methionyl amino acid residue. Consensus interferon (also known as interferon alfacon-1, rCon-IFN, and CIFN) is a genetically engineered synthetic interferon created from the most common amino acid sequences from the naturally occurring alpha interferons. Alpha interferons bind to specific cell-surface receptors, resulting in the transcription and translation of genes whose protein products have antiviral, antiproliferative, anticancer, and immune-modulating effects. 42875 erb-38 immunotoxin A bivalent fusion protein consisting of disulfide-stabilized Fv fragments of an anti-HER2 (erbB2) monoclonal antibody (e23) and a truncated version of the M(r) 38 fragment of Pseudomonas exotoxin that lacks the toxin's cell binding domain. ERB-38 immunotoxin binds specifically to cells that overexpress HER2, the antigenic target of the monoclonal antibody; the exotoxin portion of the immunotoxin then lyses the cells bound by the antibody portion. 42876 pilocarpine hydrochloride The hydrochloride salt of a natural alkaloid extracted from plants of the genus Pilocarpus with cholinergic agonist activity. As a cholinergic parasympathomimetic agent, pilocarpine predominantly binds to muscarinic receptors, thereby inducing exocrine gland secretion and stimulating smooth muscle in the bronchi, urinary tract, biliary tract, and intestinal tract. When applied topically to the eye, this agent stimulates the sphincter pupillae to contract, resulting in miosis; stimulates the ciliary muscle to contract, resulting in spasm of accomodation; and may cause a transitory rise in intraocular pressure followed by a more persistent fall due to opening of the trabecular meshwork and an increase in the outflow of aqueous humor. 42884 incyclinide A chemically-modified tetracycline with potential antineoplastic activity. Incyclinide inhibits matrix metalloproteinases (MMPs), thereby inducing extracellular matrix degradation, and inhibiting angiogenesis, tumor growth and invasion, and metastasis. This agent also causes mitochondrial depolarization in tumor cells and induces both cellular apoptosis and tissue necrosis. 42885 pneumococcal polyvalent vaccine An polyvalent vaccine used to prevent infection by the bacterium Streptococcus pneumoniae. Pneumococcal polyvalent vaccine contains higly purified capsular antigens from the 23 most prevalent or invasive pneumococcal types of Streptococcus pneumoniae to ensure cross-protection. Following vaccination, protective capsular type-specific\nantibody levels typically develop by the third week; serotype-specific antibody levels generally decline after 5-10 years. C1643 42886 Haemophilus influenzae b vaccine A vaccine against serotype b of the Gram-negative bacterium H. influenzae (Hib). Hib vaccines contain polysaccharide-protein conjugate antigens that produce greater host immune responses than first-generation purified polysaccharide vaccine. These vaccines may differ with regard to use of protein carriers, polysaccharides, diluents, and preservatives. 42901 tamoxifen citrate The citrate salt of an antineoplastic nonsteroidal selective estrogen receptor modulator (SERM). Tamoxifen competitively inhibits the binding of estradiol to estrogen receptors, thereby preventing the receptor from binding to the estrogen-response element on DNA. The result is a reduction in DNA synthesis and cellular response to estrogen. In addition, tamoxifen up-regulates the production of transforming growth factor B (TGFb), a factor that inhibits tumor cell growth, and down-regulates insulin-like growth factor 1 (IGF-1), a factor that stimulates breast cancer cell growth. Tamoxifen also down-regulates protein kinase C (PKC) expression in a dose-dependant manner, inhibiting signal transduction and producing an antiproliferative effect in tumors such as malignant glioma and other cancers that overexpress PKC. 42904 doxorubicin-HPMA conjugate A copolymer conjugate of the antineoplastic anthracycline doxorubicin and the water-soluble polymer N-(2-hydroxypropyl) methacrylamide (HPMA). Doxorubicin, an intercalator and a topoisomerase II inhibitor, prevents DNA replication and ultimately inhibits protein synthesis. This agent also generates oxygen free radicals, resulting in cytotoxic lipid peroxidation of cell membrane lipid. HPMA conjugation enhances the permeability and retention of this agent within the tumor vasculature. Poorly cleared by the lymphatic system, this formulation undergoes increased cleavage by tumor cell lysosomal proteinases, resulting in increased, sustained intracellular concentrations of free doxorubicin. Compared to other doxorubicin-containing formulations, this formulation may exhibit an improved toxicity profile due to the lower concentrations of free doxorubicin to which non-malignant tissues are exposed. 42905 palifermin A recombinant form of the endogenous human keratinocyte growth factor. Palifermin binds to epithelial cell surface receptors in the lining of the mouth and gastrointestinal tract, resulting in stimulation of epithelial cell proliferation, differentiation and upregulation of cytoprotective mechanisms. C2455 42916 testolactone A progesterone derivative with antineoplastic activity. Testolactone inhibits steroid aromatase, thereby preventing the formation of estrogen from adrenal androstenedione and reducing endogenous estrogen levels. 42926 therapeutic testosterone A synthetic form of the endogenous androgenic steroid testosterone. In vivo, testosterone is irreversibly converted to dihydrotestosterone (DHT) in target tissues by the enzyme 5-alpha reductase. Testosterone or DHT ligand-androgen receptor complexes act as transcription factor complexes, stimulating the expression of various responsive genes. DHT binds with higher affinity to androgen receptors than testosterone, activating gene expression more efficiently. In addition, testosterone is irreversibly converted to estradiol by the enzyme complex aromatase, particularly in the liver and adipose tissue. Testosterone and DHT promote the development and maintenance of male sex characteristics related to the internal and external genitalia, skeletal muscle, and hair follicles; estradiol promotes epiphyseal maturation and bone mineralization. Due to rapid metabolism by the liver, therapeutic testosterone is generally administered as an ester derivative. 42928 recombinant flt3 ligand A recombinant therapeutic agent which is chemically identical to or similar to the endogenous cytokine Flt3. Flt3 ligand binds to the Flt3 tyrosine kinase receptor and, synergistically with other growth factors, stimulates the proliferation and mobilization of certain bone marrow precursor cells, including CD34+ cells, and dendritic cells. When proteolytically cleaved, the transmembrane isoform of Flt3 ligand generates the soluble form soluble Flt3 ligand , which is also biologically active. C1714 42933 thiotepa A synthetic alkylating agent. Related to nitrogen mustard, thiotepa alkylates and crosslinks DNA, resulting in the inhibition of DNA replication. 42934 therapeutic autologous lymphocytes A population of lymphocytes isolated from an individual, altered in vitro, and returned to the same individual for therapeutic purposes. 42935 oblimersen sodium The sodium salt of a phosphorothioate antisense oligonucleotide targeted to the initiation codon region of mRNA for the anti-apoptotic gene Bcl-2. Oblimersen inhibits Bcl-2 mRNA translation, which may result in decreased expression of the Bcl-2 protein and tumor cell apoptosis. This agent may enhance the efficacy of standard cytotoxic chemotherapy. The anti-apoptotic bcl-2 protein is an integral outer mitochondrial membrane protein (OMMP) that is overexpressed in some cancer cell types and is linked to tumor drug resistance. C66722 42944 triptorelin A synthetic decapeptide agonist analog of luteinizing hormone releasing hormone (LHRH). Possessing greater potency than endogenous LHRH, triptorelin reversibly represses gonadotropin secretion. After chronic, continuous administration, this agent effects sustained decreases in LH and FSH production and testicular and ovarian steroidogenesis. Serum testosterone concentrations may fall to levels typically observed in surgically castrated men. 42951 vinblastine A natural alkaloid isolated from the plant Vinca rosea Linn. Vinblastine binds to tubulin and inhibits microtubule formation, resulting in disruption of mitotic spindle assembly and arrest of tumor cells in the M phase of the cell cycle. This agent may also interfere with amino acid, cyclic AMP, and glutathione metabolism; calmodulin-dependent Ca++ -transport ATPase activity; cellular respiration; and nucleic acid and lipid biosynthesis. 42952 streptavidin An extracellular protein that has four high affinity binding sites for biotin. Streptavidin is widely utilized in fluorescence microscopy applications due to the ease with which a conjugate fluorescent moiety can be coupled to the protein. C17334 42953 ISIS 3521 A synthetic phosphorothioate oligodeoxynucleotide. As an antisense molecule, ISIS 3521 hybridizes to the 3-untranslated region of the human protein kinase C (PKC-alpha) mRNA, thereby inhibiting PKC-alpha expression and growth of PKC-alpha-dependent tumor cells. 42958 green tea extract A defined, decaffeinated green tea polyphenol mixture isolated from Camellia sinensis, a plant native to Asia, with antiviral and antioxidant activities and potential chemopreventive activity. Green tea extract contains antioxidant compounds, including flavonoids, vitamins and polyphenols such as epigallocatechin-3-gallate (EGCG), which may have antineoplastic properties. Consumption of green tea extract may confer chemopreventive protection against various cancers including those of the prostate, stomach, and esophagus. 42973 melphalan An orally available phenylalanine derivative of nitrogen mustard with antineoplastic activity. Melphalan alkylates DNA at the N7 position of guanine and induces DNA inter-strand cross-linkages, resulting in the inhibition of DNA and RNA synthesis and cytotoxicity against both dividing and non-dividing tumor cells. 42978 tetanus peptide melanoma vaccine A vaccine consisting of peptides derived from melanoma-associated antigens and a modified T-cell epitope derived from tetanus toxoid. Vaccination with this agent may stimulate a host cytotoxic and helper T-cell response against tumor cells expressing melanoma-associated antigens, resulting in decreased tumor growth. C2468 42994 ISIS 5132 A synthetic, 20-base antisense oligodeoxynucleotide that hybridizes to c-raf kinase messenger RNA. ISIS 5132 has been shown to specifically suppress Raf-1 expression both in vitro and in vivo. Raf-1 serine/threonine kinase functions as a critical effector of Ras-mediated signal transduction; constitutive activation of this pathway directly contributes to malignant transformation. 43007 anakinra A recombinant human nonglycosylated interleukin-1 (IL-1) receptor antagonist with potential antineoplastic activity. Anakinra binds to the IL-1 receptor, thereby blocking the binding of the IL-1 to and activation of its receptor. Blockade of IL-1 activity may inhibit the cascade of downstream pro-angiogenic factors such as vascular endothelial cell growth factor, tumor necrosis factor-alpha, and IL-6, resulting in inhibition of tumor angiogenesis. 43010 liposomal NDDP A synthetic liposomal formulation of bis-neodecanoate diaminocyclohexane platinum (NDDP), a third-generation platinum complex analogue of cisplatin, with potential antineoplastic activity. After displacement of the 2 long-chain aliphatic leaving groups (neodecanoic acid), platinum diaminocyclohexane (DACH) complexes become highly reactive and alkylate macromolecules, forming both inter- and intra-strand DNA crosslinks and inhibiting DNA synthesis, which results in tumor cell cytotoxicity. Because DNA mismatch-repair (MMR) complexes do not recognize DACH–platinum adducts, DNA repair mechanisms are inhibited, overcoming limitations observed with other platinum-based agents. In addition, the liposomal encapsulation improves the bioavailability of NDDP and reduces its toxicity profile. C1383 43016 Ad5CMV-p53 gene A replication-defective adenoviral-CMV vector that encodes a wild-type p53 gene. Ad5CMV-p53 induces tumor cells that have been transfected with the vector to produce wild-type p53, a tumor suppressor gene that is deleted or mutated in a significant number of cancers. In transfected tumor cells, the wild-type p-53 gene product exerts an antitumor effect by blocking cell cycle progression at the G1/S regulation point, activating DNA repair proteins in the presence of DNA damage, and initiating apoptosis when DNA damage is irreparable. 43018 LMB-9 immunotoxin A recombinant disulfide stabilized anti-Lewis Y IgG immunotoxin containing a 38 KD toxic element derived from the Pseudomonas aeruginosa exotoxin A and a monoclonal antibody fragment, designed to target adenocarcinomas expressing Lewis Y. LMB-9 immunotoxin attaches to tumor cells, facilitating he entry of the exotoxin. The exotoxin moiety induces caspase-mediated apoptosis of tumor cells via a mechanism involving mitochondrial damage; it also catalyzes the transfer of ADP ribose from nicotinamide adenine dinucleotide (NAD) to elongation factor-2 in eukaryotic cells, thereby inactivating elongation factor 2 and inhibiting protein synthesis. 43023 celecoxib A nonsteroidal anti-inflammatory drug (NSAID) with a diaryl-substituted pyrazole structure. Celecoxib selectively inhibits cyclo-oxygenase-2 activity (COX-2); COX-2 inhibition may result in apoptosis and a reduction in tumor angiogenesis and metastasis. 43025 EF5 A fluorinated derivative of the 2-nitroimidazole etanidazole. EF5 is effective in accessing oxygen levels in tumor tissue through its adduct formation to intracellular macromolecules in the absence of oxygen. Reduction of this agent is carried out by a diverse group of enzymes in the cytoplasm, microsomes and mitochondria. Tissue hypoxia detection via EF5 has been reported in several cancers, including squamous cell carcinoma of the cervix and the head and neck, and in sarcoma. C45873 43027 carmustine An antineoplastic nitrosourea. Carmustine alkylates and cross-links DNA during all phases of the cell cycle, resulting in disruption of DNA function, cell cycle arrest, and apoptosis. This agent also carbamoylates proteins, including DNA repair enzymes, resulting in an enhanced cytotoxic effect. Carmustine is highly lipophilic and crosses the blood-brain barrier readily. 43028 BCG vaccine A vaccine containing bacillus Calmette-Guerin (BCG), an attenuated strain of Mycobacterium bovis, with non-specific immunoadjuvant and immunotherapeutic activities. Although the mechanism of its anti-tumor activity is unclear, immunization with BCG vaccine likely activates a Th1 cytokine response that includes the induction of interferon. Vaccination with BCG vaccine may be immunoprotective against infection with Mycobacterium tuberculosis. C298 43029 adenovirus vector One of a number of genetically-engineered adenoviruses designed to insert a gene of interest into a eukaryotic cell where the gene of interest is subsequently expressed. Unlike most other vectors, adenovirus vectors have the ability to infect post-mitotic cells. Thus, these agents are especially useful for gene transfer into neuronal cells. 43031 dendritic cell-CEA peptide vaccine A cancer vaccine consisting of dendritic cells harvested from a patient with cancer and pulsed or transduced with a peptide fragment of carcinoembryonic antigen (CEA), a tumor-associated antigen expressed by a wide range of cancers. When the altered dendritic cells are returned to the patient, they may stimulate the host immune system to mount a cytotoxic T-lymphocyte immune response against tumor cells expressing CEA. 43035 ONYX-015 An E1B-55kDa-deleted adenovirus that is able to selectively replicate in and lyse TP53-deficient human tumor cells. After tumor cell lysis, released viruses infect neighboring tumor cells, tripping a chain of ONYX-015-mediated tumor cell cytotoxicity. 43048 liposomal amphotericin B A liposome-encapsulated formulation of the polyene antifungal antibiotic amphotericin B produced by the bacterium Streptomyces nodosus with antifungal activity. Amphotericin B binds to ergosterol, an essential component of the fungal cell membrane, and alters cell membrane integrity, resulting in leakage of intracellular components and cell rupture. This agent may also induce oxidative damage in fungal cells and has been reported to stimulate host immune cells. Compared to amphotericin B alone, liposomal delivery of amphotericin B allows for a greater drug concentration in target tissues while decreasing systemic side effects. C1566 43053 fulvestrant A synthetic estrogen receptor antagonist. Unlike tamoxifen (which has partial agonist effects) and the aromatase inhibitors (which reduce the estrogen available to tumor cells), fulvestrant binds competitively to estrogen receptors in breast cancer cells, resulting in estrogen receptor deformation and decreased estrogen binding. In vitro studies indicate that fulvestrant reversibly inhibits the growth of tamoxifen-resistant, estrogen-sensitive, human breast cancer cell lines. 43057 exisulind An inactive metabolite of the nonsteroidal, anti-inflammatory agent sulindac. After oral administration, sulindac undergoes extensive biotransformation including irreversible oxidation to sulindac sulfone. Approximately, one half of an administered dose of sulindac is eliminated through the urine, mostly as the conjugated sulfone metabolite. 43058 prinomastat A synthetic hydroxamic acid derivative with potential antineoplastic activity. Prinomastat inhibits matrix metalloproteinases (MMPs) (specifically, MMP-2, 9, 13, and 14), thereby inducing extracellular matrix degradation, and inhibiting angiogenesis, tumor growth and invasion, and metastasis. As a lipophilic agent, prinomastat crosses the blood-brain barrier. 43065 lomustine A nitrosourea with antineoplastic activity. Lomustine alkylates and crosslinks DNA, thereby inhibiting DNA and RNA synthesis. This agent also carbamoylates DNA and proteins, resulting in inhibition of DNA and RNA synthesis and disruption of RNA processing. Lomustine is lipophilic and crosses the blood-brain barrier. 43067 arsenic trioxide A small-molecule arsenic compound with antineoplastic activity. The mechanism of action of arsenic trioxide is not completely understood. This agent causes damage to or degradation of the promyelocytic leukemia protein/retinoic acid receptor-alpha (PML/RARa) fusion protein; induces apoptosis in acute promyelocytic leukemia (APL) cells and in many other tumor cell types; promotes cell differentiation and suppresses cell proliferation in many different tumor cell types; and is pro-angiogenic. 43080 ibritumomab tiuxetan An immunoconjugate of the monoclonal antibody ibritumomab conjugated with the linker-chelator tiuxetan, a high affinity, conformationally restricted chelation site for radioisotopes. When bound to indium In 111 or yttrium Y 90, ibritumomab tiuxetan, targeting the CD20 antigen on B cell surfaces, specifically delivers a potentially cytotoxic dose of radiation to B lymphocytes. Ibritumomab is a murine IgG1 kappa monoclonal antibody directed against the CD20 antigen, which is found on the surface of normal and malignant B lymphocytes. C29981 43081 diethylstilbestrol DES; the acronym for diethylstilbestrol, a synthetic, nonsteroidal form of estrogen. A well-known teratogen and carcinogen, DES inhibits the hypothalamic-pituitary-gonadal axis, thereby blocking the testicular synthesis of testosterone, lowering plasma testosterone, and inducing a chemical castration. 43094 sodium salicylate The sodium salt of salicylic acid. As a nonsteroidal anti-inflammatory drug (NSAID), sodium salicylate irreversibly acetylates cyclooxygenases I and II, thereby inhibiting prostaglandin synthesis and associated inflammation and pain. This agent may also activate mitogen-activated protein kinase (p38MAPK), thereby inducing apoptosis in cancer cells. 43097 irofulven A semisynthetic sesquiterpene derivative of illudin S, a natural toxin isolated from the fungus Omphalotus illudens. Irofulven alkylates DNA and protein macromolecules, forms adducts, and arrests cells in the S-phase of the cell cycle. This agent requires NADPH-dependent metabolism by alkenal/one oxidoreductase for activity. Irofulven is more active in vitro against tumor cells of epithelial origin and is more resistant to deactivation by p53 loss and MDR1 than other alkylating agents. 43103 dinitrophenyl A small molecule containing 2 phenol rings, characterized as a hapten for use in vaccine preparation. Dinitrophenyl by itself will not elicit any immune response nor bind to antigen. Dinitrophenyl compound is commonly used to couple with peptides in vaccine preparation to enhance the immunogenicity of otherwise weak immunogenic antigens. C2478 43107 T138067 sodium A synthetic pentafluorophenylsulfonamide with potential antineoplastic activity. T138067 covalently binds to and selectively modifies the beta 1, beta 2, beta 3, and beta 4 isotypes of beta tubulin at a conserved cysteine residue, resulting in disruption of microtubule polymerization, collapse of the cytoskeleton, an increase in chromosomal ploidy, cell cycle arrest, and tumor cell apoptosis. 43109 raloxifene A selective benzothiophene estrogen receptor modulator (SERM). Raloxifene binds to estrogen receptors (ER) as a mixed estrogen agonist/antagonist; it displays both an ER-alpha-selective partial agonist/antagonist effect and a pure ER-beta-selective antagonist effect. This agent functions as an estrogen agonist in some tissues (bones, lipid metabolism) and as an estrogen antagonist in others (endometrium and breasts), with the potential for producing some of estrogen's beneficial effects without producing its adverse effects. 43113 chlorambucil An orally-active antineoplastic aromatic nitrogen mustard. Chlorambucil alkylates and cross-links DNA during all phases of the cell cycle, resulting in disruption of DNA function, cell cycle arrest, and apoptosis. 43115 curcumin A phytopolylphenol pigment isolated from the plant Curcuma longa, commonly known as turmeric, with a variety of pharmacologic properties. Curcumin blocks the formation of reactive-oxygen species, possesses anti-inflammatory properties as a result of inhibition of cyclooxygenases (COX) and other enzymes involved in inflammation; and disrupts cell signal transduction by various mechanisms including inhibition of protein kinase C. These effects may play a role in the agent's observed antineoplastic properties, which include inhibition of tumor cell proliferation and suppression of chemically induced carcinogenesis and tumor growth in animal models of cancer. 43130 fluorouracil An antimetabolite fluoropyrimidine analog of the nucleoside pyrimidine with antineoplastic activity. Fluorouracil and its metabolites possess a number of different mechanisms of action. In vivo, fluoruracil is converted to the active metabolite 5-fluoroxyuridine monophosphate (F-UMP); replacing uracil, F-UMP incorporates into RNA and inhibits RNA processing, thereby inhibiting cell growth. Another active metabolite, 5-5-fluoro-2'-deoxyuridine-5'-O-monophosphate (F-dUMP), inhibits thymidylate synthase, resulting in the depletion of thymidine triphosphate (TTP), one of the four nucleotide triphosphates used in the in vivo synthesis of DNA. Other fluorouracil metabolites incorporate into both RNA and DNA; incorporation into RNA results in major effects on both RNA processing and functions. 43142 polifeprosan 20 with carmustine implant A synthetic, biodegradable wafer containing the agent carmustine with antineoplastic activity. Used to deliver drug directly into a brain tumor site and typically implanted post-surgically, the wafer is made of a biodegradable poly-anhydride copolymer and contains the nitrosourea carmustine. As an antineoplastic nitrosourea, carmustine alkylates and cross-links DNA during all phases of the cell cycle, resulting in disruption of DNA function, cell cycle arrest, and apoptosis. Carmustine also carbamoylates proteins, including DNA repair enzymes, resulting in an enhanced cytotoxic effect. Carmustine is highly lipophilic and crosses the blood-brain barrier readily. 43146 iodine I 131 monoclonal antibody 81C6 A radioimmunoconjugate consisting of 81C6, a murine IgG2 anti-tenascin monoclonal antibody labeled with iodine 131 (I-131), with radioimaging and radioimmunotherapeutic activities. Using monoclonal antibody 81C6 as a carrier for I-131 results in the targeted imaging and/or destruction of cells expressing tenascin. Tenascin is an extracellular matrix protein which is overexpressed in gliomas and other cancers. 43151 pegylated interferon alfa A covalent conjugate of recombinant interferon alpha and polyethylene glycol (PEG), used as an antiviral and antineoplastic agent. The biological activity of this agent is derived from its interferon alpha protein moiety. Interferons alfa bind to specific cell-surface receptors, leading to the transcription and translation of genes whose protein products mediate antiviral, antiproliferative, anticancer, and immune-modulating effects. The PEG moiety lowers the clearance of interferon alpha, thereby extending the duration of its therapeutic effects, but may also reduce interferon-mediated stimulation of an immune response. 43154 von Hippel-Lindau peptide vaccine A cancer vaccine composed of peptides derived from a tumor-associated protein encoded by a mutated Von Hippel-Lindau (VHL) oncogene. VHL peptide vaccine may stimulate a cytotoxic T cell response against tumor cells expressing the VHL tumor-associated protein. 43214 genistein A soy-derived isoflavone and phytoestrogen with antineoplastic activity. Genistein binds to and inhibits protein-tyrosine kinase, thereby disrupting signal transduction and inducing cell differentiation. This agent also inhibits topoisomerase-II, leading to DNA fragmentation and apoptosis, and induces G2/M cell cycle arrest. Genistein exhibits antioxidant, antiangiogenic, and immunosuppressive activities. 43222 GPX-100 An analogue of the anthracycline antineoplastic antibiotic doxorubicin. GPX-100 intercalates DNA and interacts with topoisomerase II, thereby inhibiting DNA replication and repair and RNA and protein synthesis. GPX-100 was designed to be a non-cardiotoxic anthracycline antibiotic. 43234 bevacizumab A recombinant humanized monoclonal antibody directed against the vascular endothelial growth factor (VEGF), a pro-angiogenic cytokine. Bevacizumab binds to VEGF and inhibits VEGF receptor binding, thereby preventing the growth and maintenance of tumor blood vessels. 43236 dimesna A synthetic derivative of dithio-ethane sulfonate with uroprotective properties. In the kidney, dimesna undergoes reduction to the free thiol compound, mesna, which reacts chemically with the urotoxic ifosfamide metabolites acrolein and 4-hydroxy-ifosfamide, resulting in their detoxification. This agent also inhibits cyclophosphamide-induced hemorrhagic cystitis. 43238 venlafaxine A synthetic phenethylamine bicyclic derivative with antidepressant activity. Venlafaxine and its active metabolite, O-desmethylvenlafaxine (ODV), are potent inhibitors of neuronal serotonin and norepinephrine reuptake and weak dopamine reuptake inhibitors. This agent may reduce hormone-related vasomotor symptoms. 43241 iodine I 125 A radioactive isotope of iodine, a nonmetallic element of the halogen group. With a half-life of 60 days, iodine 125 occurs naturally and can be produced artificially. This agent has both therapeutic and diagnostic uses, particularly in thyroid disease. 43244 acitretin An orally-active metabolite of the synthetic aromatic retinoic acid agent etretinate with potential antineoplastic, chemopreventive, anti-psoratic, and embryotoxic properties. Acitretin activates nuclear retinoic acid receptors (RAR), resulting in induction of cell differentiation, inhibition of cell proliferation, and inhibition of tissue infiltration by inflammatory cells. This agent may also inhibit tumor angiogenesis. 43250 PSA prostate cancer vaccine A peptide vaccine containing the prostate specific antigen (PSA) with potential antineoplastic activity. PSA, a glycoprotein secreted by prostatic epithelial and ductal cells, is overexpressed in prostate cancer cells and is used as a tumor marker for both diagnosis and treatment evaluation. Vaccination with PSA peptide vaccine may produce anti-PSA antibodies as well as elicit a cytotoxic T-cell (CTL) response against prostate cancer cells expressing this antigen, thereby decreasing tumor cell growth. 43251 oregovomab A murine monoclonal antibody that attaches to the tumor-associated antigen CA125. Vaccination with monoclonal antibody B43.13 may stimulate a host cytotoxic immune response against tumor cells that express CA125. 43255 multivitamin A dietary supplement containing all or most of the vitamins that may not be readily available in the diet. Vitamins may be classified according to their solubility either in lipids (vitamins A, D, E, K, F) or in water (vitamins C, B-complex). Present in minute amounts in various foods, vitamins are essential to maintaining normal metabolism and biochemical functions. C1654 43260 nelarabine An arabinonucleoside antimetabolite with antineoplastic activity. Nelarabine is demethoxylated by adenosine deaminase to become biologically active 9-beta-D-arabinosylguanine (ara-G); ara-G incorporates into DNA, thereby inhibiting DNA synthesis and inducing an S phase-dependent apoptosis of tumor cells. 43265 LMB-1 immunotoxin A chimeric protein consisting of the Fv portion of a monoclonal antibody attached to a fragment of Pseudomonas exotoxin A without its cell-binding region. LMB-1 immunotoxin targets B3, a Lewis Y-related carbohydrate epitope found on some solid tumors. The antibody attaches to the tumor cell and the exotoxin stops protein synthesis by inactivating elongation factor 2. 43266 B43-PAP immunotoxin A mouse-derived anti-human CD19 monoclonal antibody linked to pokeweed (Phytolacca americana) antiviral protein (PAP) with antileukemic activity. The monoclonal antibody portion specifically binds to the CD19 antigen, a cell surface molecule normally expressed only by B lymphocytes and follicular dendritic cells and over-expressed in B-lineage lymphocytic leukemia cells. Following internalization, PAP, a plant hemitoxin and a ribosome-inactivating protein, is cleaved from the immunoconjugate and released into the cytoplasm where it enzymatically removes a single adenine base from a conserved, surface exposed loop sequence of rRNA leading to inhibition of protein synthesis and cell growth, but not necessarily cell death. 43288 tinidazole A 5-nitroimidazole derivative with antiprotozoal property. Although the mechanism of action has not been fully elucidated, it has been suggested that tinidazole is metabolized and yields nitrite anions and metronidazole. Metronidazole's nitro group in turn is reduced via the parasite ferredoxin, thereby generating a series of free nitro radicals including nitro anions. Toxicity is achieved via depletion of sulfhydryl groups and DNA strand breaks with multiple hits having an additive effect and ultimately leading to cell death. 43290 dalteparin A low molecular weight, synthetic heparin. As an anticoagulant/antithrombotic agent, dalteparin binds to antithrombin and enhances the inhibition of Factor Xa. Compared to unfractionated heparins, the use of dalteparin is associated with lower incidences of osteoporosis and heparin-induced thrombocytopenia. 43292 cisplatin liposomal A synthetic formulation in which the antineoplastic agent cisplatin is encapsulated in lipids. Cisplatin liposomal consists of small aggregates of cisplatin covered by a single lipid bilayer. Encasement in liposomes improves cisplatin's tumor bioavailability and toxicity profile. Liposomal encapsulation does not affect the pharmacological properties of cisplatin directly. Cisplatin forms highly reactive, charged, platinum complexes which bind to nucleophilic groups such as GC-rich sites in DNA, inducing intrastrand and interstrand DNA cross-links, as well as DNA-protein cross-links. These cross-links result in apoptosis and cell growth inhibition. 43296 prednisolone A synthetic glucocorticoid with anti-inflammatory and immunomodulating properties. After cell surface receptor attachment and cell entry, prednisolone enters the nucleus where it binds to and activates specific nuclear receptors, resulting in an altered gene expression and inhibition of proinflammatory cytokine production. This agent also decreases the number of circulating lymphocytes, induces cell differentiation, and stimulates apoptosis in sensitive tumor cells populations. 43301 polyvalent melanoma vaccine A cancer vaccine consisting of whole irradiated heterologous melanoma cells which express multiple melanoma-related antigens. Polyvalent melanoma vaccine may stimulate an antitumoral cytotoxic T-cell immune response in the host, resulting in inhibition of tumor cell proliferation and tumor cell death. 43310 semaxanib A quinolone derivative with potential antineoplastic activity. Semaxanib reversibly inhibits ATP binding to the tyrosine kinase domain of vascular endothelial growth factor receptor 2 (VEGFR2), which may inhibit VEGF-stimulated endothelial cell migration and proliferation and reduce the tumor microvasculature. This agent also inhibits the phosphorylation of the stem cell factor receptor tyrosine kinase c-kit, often expressed in acute myelogenous leukemia cells. C1831 43316 fosbretabulin disodium The disodium salt of a water-soluble phosphate derivative of a natural stilbenoid phenol derived from the African bush willow (Combretum caffrum) with potential vascular disrupting and antineoplastic activities. Upon administration, the prodrug fosbretabulin is dephosphorylated to its active metabolite, the microtubule-depolymerizing agent combretastatin A4, which binds to tubulin dimers and prevents microtubule polymerization, resulting in mitotic arrest and apoptosis in endothelial cells. In addition, this agent disrupts the engagement of the endothelial cell–specific junctional molecule vascular endothelial-cadherin (VE-cadherin) and so the activity of the VE-cadherin/β-catenin/Akt signaling pathway, which may result in the inhibition of endothelial cell migration and capillary tube formation. As a result of fosbretabulin's dual mechanism of action, the tumor vasculature collapses, resulting in reduced tumor blood flow and ischemic necrosis of tumor tissue. 43320 dimethylxanthenone acetic acid A fused tricyclic analogue of flavone acetic acid with potential antineoplastic activity. Dimethylxanthenone acetic acid induces the cytokines tumor necrosis alpha (TNF-alpha), serotonin and nitric oxide, resulting in hemorrhagic necrosis and a decrease in angiogenesis. This agent also stimulates the anti-tumor activity of tumor-associated macrophages. 43322 BL22 immunotoxin A recombinant immunotoxin consisting of the Fv portion of the anti-CD22 antibody RFB4 fused to a fragment of Pseudomonas exotoxin-A with potential antineoplastic activity. BL22 immunotoxin binds to CD22, an antigen expressed in B-cell malignancies, thereby delivering its toxin directly to tumor cells. The toxin moiety induces caspase-mediated apoptosis of tumor cells via a mechanism involving mitochondrial damage; it also blocks translational elongation via binding to elongation factor-2 in eukaryotic cells. 43325 SarCNU An alkylating chloroethylnitrosourea with antineoplastic activity. Selectively accumulating in some tumor cells, SarCNU forms covalent linkages with nucleophilic centers in DNA, causing depurination, base pair miscoding, strand scission, and DNA-DNA cross-linking, which may result in cytotoxicity. C963 43332 monoclonal antibody HeFi-1 A murine monoclonal antibody with potential antineoplastic activity. Monoclonal antibody HeFi-1 binds to CD30, a cell surface antigen found on mitogen-activated B-cells and T-cells, and Reed-Sternberg cells. Monoclonal antibody HeFi-1 has been shown to arrest tumor growth and prevent metastasis in animal models. 43345 therapeutic insulin A synthetic or animal-derived form of insulin used in the treatment of diabetes mellitus. Therapeutic insulin is formulated to be short-, intermediate- and long-acting in order to individualize an insulin regimen according to individual differences in glucose and insulin metabolism. Therapeutic insulin may be derived from porcine, bovine or recombinant sources. Endogenous human insulin, a pancreatic hormone composed of two polypeptide chains, is important for the normal metabolism of carbohydrates, proteins and fats and has anabolic effects on many types of tissues. C581 43349 hu14.18-IL2 fusion protein A recombinant protein consisting of the hu14.18 monoclonal antibody fused to the cytokine interleukin-2 (IL2) with potential antineoplastic activity. The monoclonal antibody portion of the hu14.18-IL2 fusion protein binds to tumor cells expressing the GD2 antigen (melanoma, neuroblastoma and certain other tumors); the Fc component of the fusion protein antibody moiety and natural killer (NK) cells mediate antibody-dependent cell-mediated cytotoxicity (ADCC) and complement-dependent cellular cytotoxicity (CDCC) towards GD2-expressing tumor cells. The localized IL2 moiety of the fusion protein stimulates NK and T-cell antitumor cellular immune responses. 43356 lepirudin A yeast cell-derived recombinant polypeptide related to the naturally occurring, leech-derived anticoagulant hirudin. Lepirudin directly binds to and inactivates thrombin, producing dose-dependent increases in the activated partial thromboplastin time (aPTT) and prothrombin time (PT). The mechanism of action of this agent is independent of antithrombin III and is not inhibited by platelet factor 4. Natural hirudin, a family of highly homologous isopolypeptides, is produced in trace amounts by the leech Hirudo medicinalis. 43364 indium In 111 ibritumomab tiuxetan A targeted radioimmunoconjugate composed of a murine monoclonal anti-CD20 antibody (ibritumomab) linked by a chelator (tiuxetan) to the imaging radioisotope indium-111. This radioimmunoconjugate binds to CD20-positive cells, permitting radioimmuno-localization of CD20-positive cell biodistribution. 43366 AFP gene hepatocellular carcinoma vaccine A cancer vaccine composed of naked plasmid DNA of the gene for the tumor-associated antigen alpha-fetoprotein (AFP), a macromolecule that acts as a specific immunologic target for hepatocellular carcinoma. This agent exerts an antitumor effect by inducing cytotoxic T-lymphocytes to attack AFP-expressing tumor cells. C2512 43369 temsirolimus An ester analog of rapamycin. Temsirolimus binds to and inhibits the mammalian target of rapamycin (mTOR), resulting in decreased expression of mRNAs necessary for cell cycle progression and arresting cells in the G1 phase of the cell cycle. mTOR is a serine/threonine kinase which plays a role in the PI3K/AKT pathway that is upregulated in some tumors. 43371 flu matrix peptide p58-66 A short chain synthetic antigenic peptide (GILGFVFTL) derived from the influenza virus A matrix protein and presented by HLA-A2 major histocompatibility complex (MHC) class I molecules. Flu matrix peptide p58-66 stimulates the lytic functions of cytotoxic T lymphocytes (CTLs), which may result in the eradication of virus-infected or malignant tumor cells. C39677 43377 LMB-2 immunotoxin A fusion protein consisting of the Fv portion of a monoclonal antibody attached to a 38-kDa fragment of the Pseudomonas exotoxin A (with amino acids 365-380 deleted). LMB-2 immunotoxin targets the interleukin 2 receptor (also known as IL-2R or CD25) which is expressed on activated normal T and B cells and macrophages and on the cells of various hematologic malignancies. The antibody attaches to the IL-2R on the cell membrane, facilitating the entry of the exotoxin. The exotoxin moiety induces caspase-mediated apoptosis of tumor cells via a mechanism involving mitochondrial damage; it also catalyzes the transfer of ADP ribose from nicotinamide adenine dinucleotide (NAD) to elongation factor-2 in eukaryotic cells, thereby inactivating elongation factor 2 and inhibiting protein synthesis. 43386 exatecan mesylate A semisynthetic, water-soluble derivative of camptothecin with antineoplastic activity. Exatecan mesylate inhibits topoisomerase I activity by stabilizing the cleavable complex between topoisomerase I and DNA and inhibiting religation of DNA breaks, thereby inhibiting DNA replication and triggering apoptotic cell death. This agent does not require enzymatic activation and exhibits greater potency than camptothecin and other camptothecin analogues. 43387 oglufanide disodium The disodium salt of a synthetic form of a naturally-occurring dipeptide consisting of L-glutamic acid and L-tryptophan with potential antiangiogenic and potential immunomodulating activities. Oglufanide inhibits vascular endothelial growth factor (VEGF), which may inhibit angiogenesis. This agent has also been reported to stimulate the immune response to hepatitic C virus and intracellular bacterial infections. C2558 43388 c-myb antisense oligonucleotide G4460 A 24-base phosphorothiolate antisense oligodeoxynucleotide (ODN) for the proto-oncogene c-myb with potential antineoplastic activity. C-myb antisense oligonucleotide G4460 binds to codon sequences 2 to 9 of c-myb mRNA, inhibiting translation of the transcript. Suppression of c-myb expression with this agent may result in the restoration of normal differentiation pathways, increased antiproliferative effects, and the induction of apoptosis in early progenitor hematopoietic cells and in tumor cells that overexpress c-myb. Tumor-cell overexpression of c-myb blocks differentiation, promotes proliferation, and inhibits apoptosis. C1541 43407 PEG-interferon alfa-2b A covalent conjugate of recombinant interferon alpha, subtype 2b, and polyethylene glycol (PEG), used as an antiviral and antineoplastic agent. The biological activity of this agent is derived from its interferon alpha-2b protein moiety. Interferons alfa bind to specific cell-surface receptors, leading to the transcription and translation of genes whose protein products mediate antiviral, antiproliferative, anticancer, and immune-modulating effects. The PEG moiety lowers the clearance of interferon alpha-2b, thereby extending the duration of its therapeutic effects, but may also reduce the interferon-mediated stimulation of an immune response. 43408 perifosine An orally active alkyl-phosphocholine compound with potential antineoplastic activity. Targeting cellular membranes, perifosine modulates membrane permeability, membrane lipid composition, phospholipid metabolism, and mitogenic signal transduction, resulting in cell differentiation and inhibition of cell growth. This agent also inhibits the anti-apoptotic mitogen-activated protein kinase (MAPK) pathway and modulates the balance between the MAPK and pro-apoptotic stress-activated protein kinase (SAPK/JNK) pathways, thereby inducing apoptosis. Perifosine has a lower gastrointestinal toxicity profile than the related agent miltefosine. 43417 cephalexin A beta-lactam, first-generation cephalosporin antibiotic with bactericidal activity. Cephalexin binds to and inactivates penicillin-binding proteins (PBP) located on the inner membrane of the bacterial cell wall. Inactivation of PBPs interferes with the cross-linking of peptidoglycan chains necessary for bacterial cell wall strength and rigidity. This results in the weakening of the bacterial cell wall and causes cell lysis. Compared to second and third generation cephalosporins, cephalexin is more active against gram-positive and less active against gram-negative organisms. 43434 mechlorethamine hydrochloride The hydrochloride salt of mechlorethamine, a nitrogen mustard and an analogue of sulfur mustard, with antineoplastic and immunosuppressive activities. Mechlorethamine is metabolized to an unstable, highly reactive ethyleniminium intemediate that alkylates DNA, particularly the 7 nitrogen of guanine residues, resulting in DNA base pair mismatching, DNA interstrand crosslinking, the inhibition of DNA repair and synthesis, cell-cycle arrest, and apoptosis. This agent also exhibits lympholytic properties. 43435 megestrol acetate The acetate salt of megestrol, a synthetic derivative of the naturally occurring female sex hormone progesterone, with progestogenic, antiestrogenic, and antineoplastic activities. Mimicking the action of progesterone, megestrol binds to and activates nuclear progesterone receptors (PRs) in the reproductive system and pituitary; ligand-receptor complexes are translocated to the nucleus where they bind to progesterone response elements (PREs) located on target genes. Megestrol’s antineoplastic activity against estrogen-responsive tumors may be due, in part, to the suppression of pituitary gonadotrophin production and the resultant decrease in ovarian estrogen secretion; interference with the estrogen receptor complex in its interaction with genes and; as part of the progesterone receptor complex, direct interaction with the genome and downregulation of specific estrogen-responsive genes. This agent may also directly kill tumor cells. 43436 mercaptopurine A thiopurine-derivative antimetabolite with antineoplastic and immunosuppressive activities. Produced through the metabolism of mercaptopurine by hypoxanthine-guanine phosphoribosyltransferase (HGPRT), mercaptopurine metabolites 6-thioguanosine-5'-phosphate (6-thioGMP) and 6-thioinosine (T-IMP) inhibit nucleotide interconversions and de novo purine synthesis, thereby blocking the formation of purine nucleotides and inhibiting DNA synthesis. This agent is also incorporated into DNA in the form of deoxythioguanosine, which results in the disruption of DNA replication. In addition, mercaptopurine is converted to 6-methylmercaptopurine ribonucleoside (MMPR) by 6-thiopurine methyltransferase; MMPRs are also potent inhibitors of de novo purine synthesis. 43444 fowlpox virus vaccine vector A recombinant fowlpox virus-based vaccine vector designed to express various tumor-associated peptide antigens. Strong CD8 cytotoxic T cell responses may be induced after prolonged immunization with fowlpox virus vaccines and have been associated with tumor regression. Fowlpox virus is an attractive vector because its genome is easy to manipulate and it does not multiply in human tissues. C48390 43463 iodine I 131 monoclonal antibody BC8 A radioimmunoconjugate consisting of BC8, a murine IgG1 anti-CD45 monoclonal antibody labeled with iodine 131 (I-131), with radioimmunotherapeutic properties. Using monoclonal antibody BC8 as a carrier for I-131 results in the targeted destruction of cells expressing CD45. CD45 is tyrosine phosphatase expressed on virtually all leukocytes, including myeloid and lymphoid precursors in bone marrow and mature lymphocytes in lymph nodes; it is also expressed on most myeloid and lymphoid leukemic cells, but not on mature erythrocytes or platelets. 43469 placebo An inactive substance, treatment or procedure that is intended to provide baseline measurements for the experimental protocol of a clinical trial. C753 43475 MG 98 A second-generation, mixed-backbone, phosphorothioate antisense oligonucleotide (ODN) with potential antitumor activity. MG 98 is a highly specific inhibitor of translation of the mRNA for human DNA (cytosine-5-)-methyltransferase 1 (DNMT1), hybridizing to the 3' un-translated region of DNMT1 mRNA. The silencing of DNMT1 translation by MG 98 may result in the prevention or reversal of abnormal methylation of tumor suppressor genes and ultimately in tumor growth inhibition or tumor regression. C2530 43477 leridistim A recombinant chimeric dual G-CSF and IL-3 receptor agonist. Leridistim binds with high affinity to both the interleukin-3 (IL-3) and granulocyte colony-stimulating factor (G-CSF) receptors, thereby stimulating the production and maturation of neutrophils, platelets, and lymphocytes after chemotherapy. 43488 vaccinia-tyrosinase vaccine A vaccine consisting of recombinant vaccinia virus, based on the modified vaccinia virus Ankara (MVA), that encodes the melanoma-associated antigen tyrosinase. Vaccination with vaccinia-tyrosinase may stimulate the host immune system to mount a cytotoxic T-cell response against tumor cells expressing tyrosinase. Tyrosinase is a melanoma-specific differentiation agent that catalyzes the synthesis of the melanin precursor L-3,4-dihydroxyphenylalanine (L-DOPA). 43492 proteolytic enzymes Enzymes produced and secreted by the pancreas which aid in the proteolysis of proteins in the digestive tract. Pancreatic proteolytic enzymes include trypsin, chymotrypsin and carboxypeptidase; these enzymes are secreted as zymogens, inactive precursors of the enzymes, and are activated in the lumen of the digestive canal. Another proteolytic enzyme, enteropeptidase, is associated with the brush border of enterocytes; this enzyme catalyses the conversion of trypsinogen into trypsin which, in turn, can activate a number of other pancreatic zymogens. C38728 43503 lonafarnib A synthetic tricyclic derivative of carboxamide with antineoplastic properties. Lonarfanib binds to and inhibits farnesyl transferase, an enzyme involved in the post-translational modification and activation of Ras proteins. Ras proteins participate in numerous signalling pathways (proliferation, cytoskeletal organization), and play an important role in oncogenesis. Mutated ras proteins have been found in a wide range of human cancers. 43507 tropisetron An indole derivative with antiemetic activity. As a selective serotonin receptor antagonist, tropisetron competitively blocks the action of serotonin at 5HT3 receptors, resulting in suppression of chemotherapy-and radiotherapy-induced nausea and vomiting. 43511 yttrium Y 90 monoclonal antibody MN-14 A radioimmunotherapeutic monoclonal antibody (MN-14) directed against tumor-associated carcinoembryonic antigen (CEA) and chelated to the radioisotope yttrium-90 (Y 90). Y 90 monoclonal antibody MN-14 binds to tumor cell expressing CEA, delivering a cytotoxic dose of beta radiation. 43522 defibrotide A polydeoxyribonucleotide with antithrombotic, thrombolytic, and fibrinolytic properties. Defibrotide induces the release of prostaglandin 12 and reduces the expression of adhesion molecules on endothelial cells, thereby interfering with platelet and leukocyte adhesion to the endothelium. 43525 lung tumor associated antigen A tumor associated antigen derived from the cell surface antigen of lung cancer cells. Lung tumor associated antigen could be used as a diagnostic marker or as a form of immunotherapy targeted against lung cancer cells. C2224 43530 vatalanib An orally bioavailable anilinophthalazine with potential antineoplastic activity. Vatalanib binds to and inhibits the protein kinase domain of vascular endothelial growth factor receptors 1 and 2; both receptor tyrosine kinases are involved in angiogenesis. This agent also binds to and inhibits related receptor tyrosine kinases, including platelet-derived growth factor (PDGF) receptor, c-Kit, and c-Fms. 43534 RevM10 gene RevM10 is a dominant-negative mutant of HIV-1 Rev gene, which encodes a RNA-binding protein involving in nuclear trafficking of unspliced viral mRNAs. Due to the fact that Rev is essential for HIV-1 replication makes it an attractive target for antiviral approaches. Based on the notion of intracellular immunization, in vitro studies that introducing RevM10 gene into stem cells have demonstrated its ability to combat HIV-1 infection in human hematopoietic cells. C18318 43548 S-1 An orally bioavailable fluoropyrimidine antagonist composed of tegafur combined with two modulators of 5-flurouracil (5-FU) activity, 5-chloro-2,4-dihydroxypyridine (CDHP) and potassium oxonate, in a molar ratio of 1:0.4:1. Tegafur is a prodrug of 5-fluorouracil, an antimetabolite that inhibits thymidylate synthase, DNA synthesis and cell division, and competes with uridine triphosphate, thus inhibiting RNA and protein synthesis. CDHP is a reversible inhibitor of dihydropyrimidine dehydrogenase (DPD), the liver enzyme responsible for rapid catabolism of 5-FU into inactive metabolites. Potassium oxonate preferentially localizes in the gut and inhibits the enzyme orotate phosphoribosyl-transferase (OPRT), thereby decreasing activation of 5-FU in the gut and activated 5-FU-related gastrointestinal toxicity. C1833 43549 dendritic cell-gp100-MART-1 antigen vaccine An autologous dendritic cell vaccine with antineoplastic property. Dendritic cells harvested from cancer patients are pulsed with human gp100 melanoma antigen and MART-1 antigen (a melanoma antigen recognized by T-cells); both antigens are up-regulated in melanomas. Vaccination with this vaccine may elicit the host immune response against MART-1 or gp100 expressing cells. C2214 43554 autologous tumor cell vaccine A therapeutic agent produced by isolating tumor cells from an individual and processing these tumor cells into a vaccine formulation in vitro; the vaccine is then administered to the individual from whom the tumor cells were isolated. Typically combined with an adjuvant immunostimulant, an autologous cell vaccine may elicit a cytotoxic T-lymphocytic immune response to cell surface-expressed tumor-associated antigens (TAAs), resulting in tumor cell death. 43560 bortezomib A dipeptide boronic acid analogue with antineoplastic activity. Bortezomib reversibly inhibits the 26S proteasome, a large protease complex that degrades ubiquinated proteins. By blocking the targeted proteolysis normally performed by the proteasome, bortezomib disrupts various cell signaling pathways, leading to cell cycle arrest, apoptosis, and inhibition of angiogenesis. Specifically, the agent inhibits nuclear factor (NF)-kappaB, a protein that is constitutively activated in some cancers, thereby interfering with NF-kappaB-mediated cell survival, tumor growth, and angiogenesis. In vivo, bortezomib delays tumor growth and enhances the cytotoxic effects of radiation and chemotherapy. 43561 iodine I 131 monoclonal antibody TNT-1/B An iodine 131 labeled radioimmunoconjugate of monoclonal antibody (MOAB) TNT-1/B with radioimaging and antineoplastic properties. MOAB TNT-1/B was developed for radioimmunotherapy of solid tumors, designated as Tumor Necrosis Treatment (TNT). TNT exploits the presence of degenerating and necrotic cells within tumors by utilizing MOAbs directed against universal, intracellular nucleosomal determinants consisting of histone H1 and DNA. This MOAB was conjugated with biotin (B) molecules, which increase pharmacokinetic performance of the monoclonal antibody. MOAB TNT-1/B delivers I 131 to tumor cells and results in the targeted imaging and/or destruction of cells with exposed necrotic antigens. 43568 BIBX 1382 A pyrimido-pyrimidine with antitumor activity. BIBX 1382 inhibits the intracellular tyrosine kinase domain of the Epidermal Growth Factor Receptor (EGFR) thus specifically reversing the aberrant enzymatic activity from overexpressed and constitutively activated EGFR, and subsequently inhibiting cell proliferation and inducing cell differentiation. 43584 mureletecan A water-soluble prodrug, consisting of camptothecin covalently linked to polymeric backbone methacryloylglycynamide, with potential antineoplastic activity. After entering tumor cells, the active moiety camptothecin is slowly released from mureletecan via hydrolysis of the ester linkage. Camptothecin, an alkaloid isolated from the Chinese tree Camptotheca acuminata, binds to and stabilizes the topoisomerase I-DNA covalent complex. This inhibits the religation of topoisomerase I-mediated single-stranded DNA breaks and produces potentially lethal double-stranded DNA breaks when encountered by the DNA replication machinery, resulting in the inhibition of DNA replication and apoptosis. Compared to camtpothecin, this prodrug formulation increases camptothecin drug delivery to the tumor site while reducing systemic toxicity. C2234 43586 mutant p53 peptide pulsed dendritic cell vaccine A cancer vaccine consisting of autologous dendritic cells which have been pulsed with a mutant p53 peptide. Vaccination with mutant p53 peptide pulsed dendritic cells may stimulate the host immune system to mount a cytotoxic T lymphocyte (CTL) response against tumor cells expressing mutant p53, resulting in tumor cell lysis. Many tumor cells overexpress mutant p53 proteins, resulting in the loss of apoptosis regulation and abnormal cell proliferation. C2540 43623 bcr-abl peptide vaccine A multivalent antineoplastic vaccine comprised of the bcr-abl oncogene breakpoint fusion peptide that elicits a bcr-abl specific T-cell immune response. 43625 HPV 16 E7:86-93 peptide vaccine A synthetic peptide vaccine consisting of amino acids 86 through 93 (TLGIVCPI) of the viral oncoprotein human papillomavirus (HPV) 16 E7. Vaccination with HPV-16 E7:86-93 peptide, which binds to HLA-A* 0201 molecule, may stimulate the host immune system to mount a cytotoxic T-lymphocyte (CTL) response against tumor cells positive for HPV-16 E7. C38761 43629 liothyronine sodium The sodium salt form of liothyronine, a synthetic form of the levorotatory isomer of the naturally occurring thyroid hormone triiodothyronine (T3). Liothyronine sodium binds to nuclear thyroid receptors which then bind to thyroid hormone response elements of target genes. As a result, liothyronine sodium induces gene expression that is required for normal growth and development. Liothyronine sodium is more potent and has a more rapid action than thyroxine (T4). C2581 43630 iodine I 131 A radioactive isotope of iodine with an atomic mass of 131, a half life of eight days, and potential antineoplastic activity. Selectively accumulating in the thyroid gland, iodine I 131 emits beta and gamma particles, thereby killing thyroid cells and decreasing thyroid hormone production. C1639 43632 interleukin-12 gene The DNA sequence that encodes the protein cytokine interleukin-12 (IL-12). When introduced as the complementary DNA (cDNA) form into tumor cells by, for example, a genetically engineered adenovirus vector, the transfected IL-12 cDNA expresses IL-12 which activates antitumoral natural killer (NK) cells and CD8+ T-cells and stimulates the secretion of interferon-gamma (IFN-gamma), potentially inhibiting tumor cell metastasis. This gene therapy may also result in IL-12-mediated inhibition of vascular endothelial growth factor (VEGF) and enhancement of matrix metalloproteinases (MMPs). C2222 43633 p53 peptide vaccine A peptide-based cancer vaccine composed of amino acids 264 to 272 of the wild-type protein encoded by the P53 gene. p53 peptide vaccine may elicit an HLA-A2.1-restricted cytotoxic T lymphocyte immune response against tumor cells that overexpress p53 protein. 43635 tanespimycin A benzoquinone antineoplastic antibiotic derived from the antineoplastic antibiotic geldanamycin. Tanespimycin binds to and inhibits the cytosolic chaperone functions of heat shock protein 90 (HSP90). HSP90 maintains the stability and functional shape of many oncogenic signaling proteins; the inhibition of HSP90 promotes the proteasomal degradation of oncogenic signaling proteins that may be overexpressed by tumor cells. 43639 recombinant CD40-ligand A recombinant therapeutic agent which is chemically identical to or similar to CD40-ligand. CD40-ligand, also known as CD40L/TRAP and CD154, is a type II membrane protein which binds to CD40, a cell surface receptor that belongs to the tumor necrosis factor receptor family; CD40 is expressed on B lymphocytes, monocytes, dendritic cells (DC), hematopoietic progenitors, endothelial cells and epithelial cells. Recombinant CD40-ligand may be used to activate DC ex vivo via CD40 binding; CD40-ligand-activated DC may provide or augment a protective antitumor immunity when administered in dendritic cell cancer vaccines. 43646 troxacitabine A dioxolane derivative and a novel L-configuration deoxycytidine analogue with potent antineoplastic activity. When incorporated into growing chain during DNA replication, troxacitabine stops DNA polymerization due to its unnatural L-configuration, in contrast to the normal nucleotides with D-configuration. As a result, this agent terminates DNA synthesis upon incorporated into DNA molecules, and consequently interrupts tumor cell proliferation. 43648 yttrium Y 90 epratuzumab A radioimmunoconjugate consisting of the anti-CD22 monoclonal antibody epratuzumab chelated to the radioisotope yttrium-90 (Y 90). Yttrium Y 90 epratuzumab binds to tumor cells expressing CD22, delivering a cytotoxic dose of beta radiation. Epratuzumab is a humanized version of the murine monoclonal antibody LL2; CD22 is a B cell-restricted antigen present on the surfaces of mature B cells. 43649 gefitinib An anilinoquinazoline with antineoplastic activity. Gefitinib inhibits the catalytic activity of numerous tyrosine kinases including the epidermal growth factor receptor (EGFR), which may result in inhibition of tyrosine kinase-dependent tumor growth. Specifically, this agent competes with the binding of ATP to the tyrosine kinase domain of EGFR, thereby inhibiting receptor autophosphorylation and resulting in inhibition of signal transduction. Gefitinib may also induce cell cycle arrest and inhibit angiogenesis. 43655 vaccine-sensitized draining lymph node cells Cells isolated from lymph nodes from patients, and activated in vitro to generate tumor-specific effector T cells. Lymph nodes in the lymphatics draining tumors often contain T cells that are immunologically sensitized but functionally deficient. Vaccine-sensitized draining lymph node cells are prepared by isolating these lymphocytes in vitro and stimulating them with cytokines to differentiate into mature effector cells. Vaccine-draining lymph node cells may also be produced by pharmacological activation of lymph node-derived lymphocytes with drugs such as ionomycin or with bacterial toxin; these activated lymphocytes may be expanded in culture with cytokines such as interleukin-2 prior to infusion into the patient. C2542 43659 zosuquidar trihydrochloride A difluorocyclopropyl quinoline. Zosuquidar trihydrochloride binds with high affinity to P-glycoprotein and inhibits P-glycoprotein-mediated multidrug resistance (MDR). P-glycoprotein, encoded by the MDR-1 gene, is a member of the ATP-binding cassette superfamily of transmembrane transporters and prevents the intracellular accumulation of many natural product-derived cytotoxic agents. 43661 tetradecanoylphorbol acetate A phorbol ester with potential antineoplastic effects. Tetradecanoylphorbol acetate (TPA) induces maturation and differentiation of hematopoietic cell lines, including leukemic cells. This agent may induce gene expression and protein kinase C (PKC) activity. In addition to potential antineoplastic effects, TPA may exhibit tumor promoting activity. 43669 thioguanine A synthetic guanosine analogue antimetabolite. Phosphorylated by hypoxanthine-guanine phosphoribosyltransferase, thioguanine incorporates into DNA and RNA, resulting in inhibition of DNA and RNA syntheses and cell death. This agent also inhibits glutamine-5-phosphoribosylpyrophosphate amidotransferase, thereby inhibiting purine synthesis. 43671 teniposide A semisynthetic derivative of podophyllotoxin with antineoplastic activity. Teniposide forms a ternary complex with the enzyme topoisomerase II and DNA, resulting in dose-dependent single- and double-stranded breaks in DNA, DNA: protein cross-links, inhibition of DNA strand religation, and cytotoxicity. This agent acts in the late S or early G phase of the cell cycle. 43727 semustine A methylated derivative of carmustine with antineoplastic activity. As an alkylating agent, semustine forms covalent linkages with nucleophilic centers in DNA, causing depurination, base-pair miscoding, strand scission, and DNA-DNA cross-linking, which may result in cytotoxicity. C827 256405 pyroxamide A synthetic derivative of hydroxamic acid with antineoplastic properties, Pyroxamide inhibits histone deacetylases involved in transcription; induces hyperacetylation of core histones, modulating chromatin structure and affecting transcription of some genes that inhibit tumor growth; and induces growth arrest and apoptosis. Pyroxamide is used in clinical studies for cancer chemotherapy. 256422 D1/3-MAGE-3-His fusion protein A recombinant fusion protein derived from the melanoma antigen MAGE-3 with potential immunostimulating and antineoplastic activities. Recognized by specific cytotoxic T lymphocytes, D1/3-MAGE-3-His fusion protein may boost antitumoral immune responses when used in a vaccine formulation. This recombinant chimeric protein is produced by fusing MAGE-3 with a lipidated protein D derived from H. influenzae at its N-terminus and a sequence of several histidine residues at its C-terminus. 256423 SB-AS02B adjuvant A proprietary oil-in-water emulsion specifically designed for combining protein preparations used in vaccines. SB-AS02B adjuvant contains monophosphoryl lipid A and QS21, a saponin extracted from the South American tree Quillaja saponaria Molina. This agent may be used for formulating cancer-specific vaccine preparations such as those containing MAGE-3 melanoma protein. 256445 risedronate sodium The hemipentahydrate monosodium salt of risedronic acid, a synthetic pyridinyl bisphosphonate. Risedronic acid binds to hydroxyapatite crystals in bone and inhibits osteoclast-dependent bone resorption. 256449 modafinil A synthetic central nervous system stimulant with wakefulness-promoting activity. Modafinil appears to inhibit dopamine reuptake, resulting in an increase in extracellular dopamine. This agent exhibits pronounced wakefulness-promoting activity (without sympathomimetic activity) and may improve cognitive function in certain clinical settings. C26661 256453 dendritic cell-autologous lung tumor vaccine A cancer vaccine consisting of lymphocytes harvested from a patient with lung cancer and induced to become antigen-presenting cells (APCs) known as dendritic cells. The dendritic cells are transduced with the gene encoding an antigen specific to the patient's cancer and then returned to the patient. In the host, the altered cells stimulate the immune system to mount a primary T cell response against lung tumor cells expressing the target antigen. Dendritic cell-autologous lung tumor vaccines have been investigated for use in cancer immunotherapy. C26446 257154 R-flurbiprofen An orally active synthetic enantiomer of flurbiprofen. R-flurbiprofen activates c-Jun N terminal kinase, increases AP-1 binding to DNA, and downregulates cyclin D1 expression, resulting in arrest of tumor cells in the G1 phase of the cell cycle and apoptosis. This agent also affects the expression of nuclear factor kappa B, a rapid response transcription factor that stimulates the immune response to tumor cells. R-flurbiprofen does not inhibit the enzyme cyclo-oxygenase. 257159 Virulizin A natural biological response modifier (BRM) isolated from bovine reticuloendothelial tissue. Viruzlin may enhance cell-mediated immune response to tumor cells by direct macrophage activation. 257174 monoclonal antibody GD2 anti-idiotype vaccine A class of vaccines that consist of anti-idiotype monoclonal antibodies against the tumor-associated antigen disialoganglioside GD2 with potential antineoplastic activity. Vaccination with a monoclonal antibody GD2 anti-idiotype vaccine produces an immunoglobulin response against GD2 with subsequent destruction of GD2 positive tumor cells via antibody-dependent cellular cytotoxicity (ADCC). GD2 is overexpressed in melanoma, neuroblastoma, soft tissue sarcoma, and small cell carcinoma of the lung. C26450 257236 valacyclovir The hydrochloride salt of the L-valyl ester of the antiviral drug acyclovir. Orally administered, valacyclovir is rapidly converted to acyclovir which inhibits viral DNA replication after further conversion to the nucleotide analog acyclovir triphosphate by viral thymidine kinase, cellular guanyl cyclase, and a number of other cellular enzymes. Acyclovir triphosphate competitively inhibits viral DNA polymerase; incorporates into and terminates the growing viral DNA chain; and inactivates viral DNA polymerase. The greater antiviral activity of acyclovir against herpes simplex virus (HSV) compared with varicellla-zoster virus (VZV) is due to its more efficient phosphorylation by HSV thymidine kinase. C28235 257309 clofarabine A second generation purine nucleoside analog with antineoplastic activity. Clofarabine is phosphorylated intracellularly to the cytotoxic active 5'-triphosphate metabolite, which inhibits the enzymatic activities of ribonucleotide reductase and DNA polymerase, resulting in inhibition of DNA repair and synthesis of DNA and RNA. This nucleoside analog also disrupts mitochondrial function and membrane integrity, resulting in the release of pre-apoptotic factors, including cytochrome C and apoptotic-inducing factor, which activate apoptosis. C26638 257347 NY-ESO-B A tumor-associated antigen belonging to the family of immunogenic testicular proteins that are aberrantly expressed in human cancers in a lineage-nonspecific fashion. Reverse transcription-PCR analysis showed NY-ESO-1 mRNA expression in a variable proportion of a wide array of human cancers, including melanoma, breast cancer, bladder cancer, prostate cancer, and hepatocellular carcinoma; and restricted expression in normal tissues, with high-level mRNA expression found only in testis and ovary tissues. The gene for NY-ESO-1 maps to Xq28 and codes for an 18-kDa protein having no homology with any known protein. NY-ESO-1 elicits a strong, integrated humoral and cellular immune response in a high proportion of patients with NY-ESO-1-expressing tumors and is under investigation as a cancer immunotherapy agent. C26680 257611 laetrile Originally, the name laetrile was the contraction of laevo-mandelonitrile glucoside, a cyanogenic glycoside found naturally in some plants. Over the years the meaning of laetrile has changed. There are now preparations called Laetrile where amygdalin is the major constituent. Laetrile and amygdalin are often used interchangeably, but are different agents. Cyanide and benzaldehyde are metabolites of both laetrile and amygdalin. Both metabolites may possess antineoplastic properties. Laetrile has been used as an anticancer treatment in humans worldwide, but scientific evidence does not support its effectiveness. It is not approved for use in the United States. 257773 eribulin mesylate The mesylate salt of a synthetic analogue of halichondrin B, a substance derived from a marine sponge (Lissodendoryx sp.) with antineoplastic activity. Eribulin binds to the vinca domain of tubulin and inhibits the polymerization of tubulin and the assembly of microtubules, resulting in inhibition of mitotic spindle assembly, induction of cell cycle arrest at G2/M phase, and, potentially, tumor regression. 257775 RK-0202 An oral polymer matrix-based rinse formulation that contains N-acetylcysteine, an antioxidant amino acid derivative with antiinflammatory properties. RK-0202 may alleviate symptoms of radiation-induced oral mucositis. 257809 etanercept A recombinant soluble dimeric fusion protein consisting of the extracellular ligand-binding region of recombinant human tumor necrosis factor (rhTNF) receptor attached to the constant (Fc) region of human immunoglobulin G (FcIgG). The receptor moiety of etanercept binds to circulating TNF (2 molecules of TNF per receptor) and inhibits its attachment to endogenous TNF cell surface receptors, thereby rendering TNF inactive and inhibiting TNF-mediated mechanisms of inflammation. 257861 epoetin beta A recombinant therapeutic agent that is chemically identical to or similar to the endogenous cytokine human erythropoietin (EPO). Produced primarily by cells of the peritubular capillary endothelium of the kidney in response to hypoxia, circulating EPO binds to EPO receptors on the surface of committed erythroid progenitors in the bone marrow resulting in their replication and maturation into functional erythrocytes. C26639 257914 EGb761 A standardized ginkgo biloba extract with antioxidant and neuroprotective activities. EGb761 has been shown to inhibit the proliferation of certain tumor cells in vitro. 258213 flaxseed Seed isolated from one of several species of the plant genus Linum. Flaxseed-derived foods, lignans, and essential fatty acids such as alpha-linolenic acid, possess anti-inflammatory, lipid-lowering, antioxidant, and antineoplastic properties. C26650 258292 autologous dendritic cell-adenovirus p53 vaccine An autologous vaccine composed of dendritic cells (DC) that have been transduced with a p53 tumor suppressor gene-modified virus. When the autologous dendritic cell-adenovirus p53 vaccine is administered, the host cytotoxic T lymphocytes (CTL) are directed against p53-positive tumor cells, which may result in tumor cell death and decreased tumor growth. C26445 258313 talaporfin sodium An agent consisting of chlorin e6, derived from chlorophyll, and L-aspartic acid with photosensitizing activity. After intratumoral activation by light emitting diodes, taporfin sodium forms an extended high energy conformational state that generates singlet oxygen, resulting in free radical-mediated cell death. C26675 258388 PV701 An attenuated, replication-competent, oncolytic strain of Newcastle disease virus. PV701 selectively lyses tumor cells. The selectivity of this agent is related to defects in the interferon-mediated antiviral response found in tumor cells. 258431 golnerminogene pradenovec A recombinant agent consisting of a genetically-modified adenovirus 5 vector encoding the protein cytokine tumor necrosis factor (TNF) alpha. TNF exhibits potent anti-tumor cytolytic properties; the adenovirus 5 vector efficiently infects tumor cells, delivering tumor-specific TNF. 269063 American ginseng The aromatic root of the perennial herb Panax quinquefolius, native to eastern North America. American ginseng, used in Chinese traditional medicine and available as a nutritional supplement, is classified as an adaptogenic herb with multiple effects, many of which are regulatory in nature. It contains a complex mixture of saponin glycosides, also known as ginsenosides or panaxosides. Although the mechanism of action is unclear, this agent is reported to enhance the immune system and reduce fatigue. 269064 transferrin-CRM107 A synthetic targeted protein toxin which consists of human transferrin (Tf) conjugated to a diphtheria toxin that contains a point mutation (CRM107). After binding to the transferrin receptor expressed on the tumor cell surface, transferrin-CRM107 is internalized, where the diphtheria toxin moiety exerts its cytotoxic effect intracellularly by inhibiting protein synthesis through ADP-ribosylation of elongation factor. 269069 enzastaurin hydrochloride The hydrochloride salt of enzastaurin, a synthetic macrocyclic bisindolemaleimide with potential antineoplastic activity. Binding to the ATP-binding site, enzastaurin selectively inhibits protein kinase C beta, an enzyme involved in the induction of vascular endothelial growth factor (VEGF)-stimulated neo-angiogenesis. This agent may decrease tumor blood supply and so tumor burden. 269130 hexyl 5-aminolevulinate The hexyl ester of 5-aminolevulinic acid (ALA) with photodynamic properties. As a precursor of photoactive porphorins, hexyl 5-aminolevulinate induces the endogenous production of the photosensitizer protoporphyrin IX (PPIX) which accumulates selectively in tumor tissue. When exposed to specific wavelengths of light, PPIX is activated and, depending on the wavelength and/or intensity of light, either fluoresces, thereby allowing tumor imaging, or induces tumor cell apoptosis. 269131 marijuana Any part of, or extract from, the female hemp plant Cannabis sativa. Marijuana contains cannabinoids, substances with hallucinogenic, psychoactive, and addictive properties. This agent has potential use for treating cancer pain and cachexia. 269137 sildenafil citrate The citrate salt of a pyrazolopyrimidinone derivative structurally related to zaprinast. Sildenafil selectively inhibits cyclic guanosine monophosphate (cGMP)-specific type 5 phosphodiesterase, resulting in vasodilation in the corpus cavernosum of the penis and penile erection. C26670 269165 HspE7 A recombinant chimeric protein composed of the heat shock protein 65 (Hsp65) from Mycobacterium bovis, and the human papilloma viral (HPV) protein E7. Hsp65, similar to other members of its family of proteins, elicits a strong immune response and may be used to design vaccines against a number of different cancers. E7 protein is involved in carcinogenesis of anal and cervical tumors, and represents a tumor antigen that may be specifically targeted by lymphocytes. 269166 I 131 monoclonal antibody CC49 A radioimmunoconjugate of the humanized monoclonal antibody CC49 labeled with iodine I 131. Iodine I 131 monoclonal antibody CC49 delivers beta and gamma radiation-emitting I 131 radionuclide specifically to tumor cells that express tumor-associated glycoprotein (TAG)-72, allowing localization of TAG-72-expressing tumor cells with radioimaging devices in diagnostic applications or resulting in specific TAG-72-expressing tumor cell radiocytotoxicity in therapeutic applications. Monoclonal antibody CC49 binds to TAG-72, a pancarcinoma antigen, with high affinity. C26442 269177 vandetanib An orally bioavailable 4-anilinoquinazoline. Vandetanib \nselectively inhibits the tyrosine kinase activity of vascular endothelial growth factor receptor 2 (VEGF2), thereby blocking VEGF-stimulated endothelial cell proliferation and migration and reducing tumor vessel permeability. This agent also blocks the tyrosine kinase activity of epidermal growth factor receptor (EGFR), a receptor tyrosine kinase that mediates tumor cell proliferation and migration and angiogenesis. 269659 lapatinib ditosylate The ditosylate salt of lapatinib, a synthetic, orally-active quinazoline with potential antineoplastic activity. Lapatinib reversibly blocks phosphorylation of the epidermal growth factor receptor (EGFR), ErbB2, and the Erk-1 and-2 and AKT kinases; it also inhibits cyclin D protein levels in human tumor cell lines and xenografts. EGFR and ErbB2 have been implicated in the growth of various tumor types. 269678 pixantrone dimaleate The dimaleate salt of a synthetic, noncardiotoxic aza-anthracenedione analogue with potential antineoplastic activity. Pixantrone intercalates into DNA and induces topoisomerase II-mediated DNA strand crosslinks, resulting in inhibition of DNA replication and tumor cell cytotoxicity. C82398 269682 Juven An orally bioavailable nutritional supplement. Juven contains the amino acids glutamine and arginine in addition to beta-hydroxy-beta-methylbutyrate (HMB). This agent may promote muscle protein synthesis and increase muscle mass. C26656 270391 buspirone hydrochloride The hydrochloride salt of an anxiolytic agent chemically and pharmacologically unrelated to benzodiazepines, barbiturates, or other sedative/hypnotic drugs. Although its exact mechanism of action is unknown, buspirone may exert its anti-anxiety effects via serotonin (5-HT1A) and dopamine receptors (D2) and may indirectly affect other neurotransmitter systems. Unlike typical benzodiazepine anxiolytics, this agent does not exert anticonvulsant or muscle relaxant effects and lacks prominent sedative effects. C26641 270682 YM598 An orally active synthetic substituted phenylethenesulfonamide. As a selective endothelin A receptor antagonist, YM598 inhibits endothelin-mediated mechanisms involved in tumor cell growth and progression, angiogenesis, and metastasis. 271169 T900607 A pentafluorophenylsulfonamide compound with potential antineoplastic activity. T900607 inhibits tubulin polymerization by binding irreversibly to colchicine binding sites, resulting in cell cycle arrest and apoptosis. 271195 custirsen sodium The eicosasodium salt of a mixed-backbone antisense oligodeoxynucleotide with chemosensitizing properties. Custirsen inhibits testosterone-repressed prostate message-2 (TRPM-2). Administration of custirsen abrogates the anti-apoptotic effect of TRPM-2, thereby sensitizing cells to chemotherapy and resulting in tumor cell death. TRPM-2 is an anti-apoptotic clusterin that is overexpressed by prostate cancer cells and is associated with chemoresistance. 271373 recombinant fowlpox-tyrosinase vaccine A recombinant fowlpox virus vaccine with potential antineoplastic activity. Binding to the melanoma antigen tyrosinase, recombinant fowlpox-tyrosinase vaccine generates cellular immune responses against melanoma cells expressing the tyrosinase antigen; this effect is enhanced by the co-administration of interleukin 2 (IL-2). Fowlpox virus is an attractive vector because its genome is easy to manipulate and it is replication incompetent in mammalian cells. 273709 CMV pp65 peptide A peptide derived from cytomegalovirus (CMV) internal matrix protein pp65. CMV pp65 peptide antigen is used in recombinant vaccinia virus as an HLA-A-restricted epitope to produce vaccines and specific CD8+ and CD4+ cell responses against CMV infection, a serious complication of allogeneic bone marrow transplantation (BMT). In BMT, CMV infection may be prevented by passive immunization with donor-derived CMV-pp65-specific T-cell clones if provided early post-BMT. C26640 276471 autologous immunoglobulin idiotype-KLH conjugate vaccine A cancer vaccine composed of tumor-specific idiotype determinants derived from an individual's tumor cells which are conjugated to keyhole limpet hemocyanin, an immunostimulant carrier protein. When injected into the individual from whom the tumor cells were isolated, this vaccine may stimulate an antitumoral cytotoxic T-lymphocytic immune response. C38715 284684 silymarin A mixture of flavonolignans isolated from the milk thistle plant Silybum marianum. Silymarin may act as an antioxidant, protecting hepatic cells from chemotherapy-related free radical damage. This agent may also promote the growth of new hepatic cells. 285619 CP-724,714 An orally bioavailable quinazoline with potential antineoplastic activity. CP-724,714 selectively binds to the intracellular domain of HER2, reversibly inhibiting its tyrosine kinase activity and resulting in suppression of tumor cell growth. HER2, a member of the epidermal growth factor receptor (EGFR) family, is overexpressed in many adenocarcinomas, particularly breast cancers. 285649 zileuton A synthetic derivative of hydroxyurea with antiasthmatic properties. The leukotriene inhibitor zileuton blocks 5-lipoxygenase, which catalyzes the formation of leukotrienes from arachidonic acid; causes bronchodilation; decreases bronchial mucous secretion and edema; and may prevent or decrease the symptoms of asthma. 285686 galiximab A humanized IgG1 monoclonal antibody directed against CD80, the natural ligand for the T-cell antigen CD28 which mediates T-cell and B-cell adhesion. Galiximab binds to CD80 expressed on the cell surfaces of follicular lymphomas, resulting in antibody-dependent cell-mediated cytotoxicity (ADCC). CD80 is expressed on activated B-cells and gamma-interferon-stimulated monocytes and is often expressed at low levels on the surfaces of follicular lymphoma cells and other lymphoid malignancies. 299001 rasburicase A recombinant urate oxidase enzyme isolated from a genetically-modified strain of Saccharomyces cerevisae. Urate oxidase catalyzes the oxidation of uric acid to the excretable mebolite allantoin, a molecule that is 5-10 times more water-soluble than uric acid. An enzyme that occurs endogenously in most mammals, urate oxidase is not found in humans. 299013 sorafenib tosylate The tosylate salt of sorafenib, a synthetic compound targeting growth signaling and angiogenesis. Sorafenib blocks the enzyme RAF kinase, a critical component of the RAF/MEK/ERK signaling pathway that controls cell division and proliferation; in addition, sorafenib inhibits the VEGFR-2/PDGFR-beta signaling cascade, thereby blocking tumor angiogenesis. 299061 sunitinib malate The orally bioavailable malate salt of an indolinone-based tyrosine kinase inhibitor with potential antineoplastic activity. Sunitinib blocks the tyrosine kinase activities of vascular endothelial growth factor receptor 2 (VEGFR2), platelet-derived growth factor receptor b (PDGFRb), and c-kit, thereby inhibiting angiogenesis and cell proliferation. This agent also inhibits the phosphorylation of Fms-related tyrosine kinase 3 (FLT3), another receptor tyrosine kinase expressed by some leukemic cells. 299464 MLN2704 An immunoconjugate that consists of a humanized monoclonal antibody (MLN591), directed against prostate-specific membrane antigen linked to a maytansinoid (DM1). The monoclonal antibody moiety of MLN2704 binds to tumor cells expressing prostate-specific membrane antigen; MLN274 is then internalized into the tumor cell where the DM1 maytansinoid moiety binds to tubulin and inhibits tubulin polymerization and microtubule assembly, resulting in a disruption of microtubule activity and cell division, and cell death. C26660 299488 abagovomab A murine IgG1 monoclonal anti-idiotype antibody, containing a variable antigen-binding region that functionally mimics the three-dimensional structure of a specific epitope on the ovarian cancer tumor-associated antigen CA-125, with potential antineoplastic activity. With a variable antigen-binding region that acts as a surrogate antigen for CA-125, abagovomab may stimulate the host immune system to elicit humoral and cellular immune responses against CA-125-positive tumor cells, resulting in inhibition of tumor cell proliferation. C26449 301635 GTI-2040 A 20-mer antisense oligonucleotide complementary to a coding region in the mRNA of the R2 small subunit component of human ribonucleotide reductase. GTI-2040 decreases mRNA and protein levels of R2 in vitro and may inhibit tumor cell proliferation in human tumors in vivo. 301640 EP-2101 A proprietary cancer DNA vaccine that contains multiple natural and modified epitopes derived from the four tumor associated antigens, CEA, HER2/neu, p53, and MAGE 2/3. EP-2101 also includes CAP1-6D, a heteroclitic CEA analog, and PADRE, a proprietary universal T-cell epitope that serves to enhance the immunogenicity of the epitopes. This agent has been shown to elicit cytotoxic T-lymphocyte responses against tumor cells expressing these multiple epitopes. 301648 forodesine hydrochloride The hydrochloride salt of the synthetic high-affinity transition-state analogue forodesine. Forodesine binds preferentially to and inhibits purine nucleotide phosphorylase (PNP), resulting in the accumulation of deoxyguanosine triphosphate and the subsequent inhibition of the enzyme ribonucleoside diphosphate reductase and DNA synthesis. This agent selectively causes apoptosis in stimulated or malignant T-lymphocytes. A transition state analogue is a substrate designed to mimic the properties or the geometry of the transition state of reaction. C26655 301896 levocarnitine An amino acid derivative. Levocarnitine facilitates long-chain fatty acid entry into mitochondria, delivering substrate for oxidation and subsequent energy production. Fatty acids are utilized as an energy substrate in all tissues except the brain. C26657 301900 monoclonal antibody MDX-060 A monoclonal antibody with potential antineoplastic activity. MDX-060 is a fully humanized antibody that targets CD30, a member of the tumor necrosis factor receptor superfamily found on activated lymphocytes. CD30 is over-expressed in various lymphoproliferative disorders, Hodgkin's disease and other lymphomas, and other cancers. C26441 302635 black cohosh A triterpene-containing herb isolated from the roots and rhizomes of the plant Cimicifuga racemosa (also known as Actaea racemosa). While the mechanism of action of black cohosh is not completely understood, it appears to act as a selective estrogen receptor modulator. In vitro, this preparation has been shown to induce cell cycle arrest and caspase-dependent apoptosis of estrogen-sensitive breast cancer cells. 302644 soblidotin A dolastatin-10 derivative. Soblidotin inhibits tubulin polymerization, resulting in cell cycle arrest and induction of apoptosis. C26672 302921 polyglutamate camptothecin A therapeutic formulation consisting of camptothecin, an alkaloid isolated from the Chinese tree Camptotheca acuminata, conjugated with polyglutamate. During the S phase of the cell cycle, camptothecin selectively stabilizes topoisomerase I-DNA covalent complexes, thereby inhibiting religation of topoisomerase I-mediated single-strand DNA breaks and producing potentially lethal double-strand DNA breaks when encountered by the DNA replication machinery. Conjugation with polyglutamate renders this agent more water soluble and less toxic than the parent molecule. C26664 304320 Morinda citrifolia fruit extract An extract prepared from the fruit of Morinda citrifolia, a plant that yields various herbal preparations. Morinda citrifolia fruit juice has antioxidant properties and may prevent tumorigenesis via inhibition of DNA-carcinogen adduct formation. C26662 304321 pomegranate juice A natural juice isolated from the fruit of the plant Punica granatum with antioxidant, potential antineoplastic, and chemopreventive activities. Pomegranate juice contains flavonoids which promote differentiation and apoptosis in tumor cells by down-regulating vascular endothelial growth factor (VEGF) and stimulating migration inhibitory factor (MIF), thereby inhibiting angiogenesis. The flavanoids in pomegranate juice also scavenge reactive oxygen species (ROS) and, in some cell types, may prevent ROS-mediated cell injury and death. C26665 304345 dextroamphetamine-amphetamine A combination of two synthetic agents with central nervous system stimulant activity. Both agents are non-catecholamine, sympathomimetic agents that elevate blood pressure and cause bronchodilation. These agents are commonly abused psychostimulant drugs that induce psychologic dependence manifested by elevated mood, increased wakefulness, concentration, physical performance and a feeling of well-being. Tolerance to various effects develops unequally, so that tachycardia and enhanced alertness diminish while psychotoxic effects (hallucinations and delusions) may occur. 304435 shark cartilage A nutritional supplement gleaned from the exoskeleton of the shark. Shark cartilage inhibits metalloproteinases (MMPs) and possesses antiangiogenic and antimetastatic properties. 304440 Essiac An herbal formula containing burdock root (Arctium lappa), Turkey rhubarb root (Rheum palmatum), sheep sorrel (Rumex acetosella), and slippery elm bark (Ulmus fulva) with potential immunostimulating, anti-inflammatory and anti-tumor activities. The exact chemical profile, their respective concentrations and the mechanism of action of Essiac are largely unknown due to the proprietary nature of the formula and product inconsistency. Several chemical classes in Essiac are consistently represented and may attribute to its therapeutic effect, including anthraquinone derivatives such as rhein and emodin, high molecular polysaccharides, and lignans such as arctigenin. However, all these chemicals are unlikely to occur in high concentrations in Essiac, and its potential therapeutic effect may be attributed to a potential synergistic effect of these various compounds. 305828 inositol A natural sugar found in cell membrane phospholipids, plasma lipoproteins, and (as the phosphate form) in the nucleus with potential chemopreventive properties. As one of a number of intracellular phosphate compounds, inositol is involved in cell signaling and may stimulate tumor cell differentiation. 305933 fowlpox-PSA-TRICOM vaccine A cancer vaccine consisting of a recombinant fowlpox virus encoding human prostate-specific antigen (PSA) and TRICOM, a combination of three immunostimulants (i.e., B7.1, ICAM-1, and LFA-3). Administration of this agent may induce a cytotoxic T cell response against PSA-expressing tumor cells. Dendritic cells infected with TRICOM vectors greatly enhance naive T-cell activation and peptide-specific T-cell stimulation. Fowlpox virus is an attractive vector because its genome is easy to manipulate and it is replication incompetent in mammalian cells. C38708 305934 vaccinia-PSA-TRICOM vaccine A vaccine formulation consisting of recombinant vaccinia virus encoding prostate specific antigen (PSA) and recombinant vaccinia virus encoding three co-stimulatory molecule transgenes B7.1, ICAM-1, and LFA-3 (TRICOM). Vaccination with PSA in combination with TRICOM may enhance antigen presentation, resulting in the augmentation of a cytotoxic T cell (CTL) immune response against tumor cells expressing PSA. C38681 305941 recombinant interleukin-7 A recombinant protein which is chemically identical to or similar to endogenous interleukin-7 (IL-7) with hematopoietic and immunopotentiating properties. Produced by bone marrow, thymic stromal, and spleen cells, the cytokine interleukin-7 is a hematopoietic growth factor for progenitor B cells and T cells and stimulates proliferation and differentiation of mature T-cells and natural killer cells. C592 306451 sodium borocaptate A boron-carrying compound. After parenteral administration, borocaptate sodium accumulates preferentially in tumor cells. When exposed to neutron irradiation, borocaptate absorbs neutrons and self-destructs releasing short-range alpha radiation and 'recoil' lithium in tumor cells, resulting in alpha radiation-induced tumor cell death. This highly selective, localized radiotargeting of tumor cells, known as boron neutron capture therapy (BNCT), spares adjacent normal tissues. 306453 ursodiol A synthetically-derived form of ursodiol, a bile acid produced by the liver and secreted and stored in the gallbladder. Also produced by the Chinese black bear liver, ursodiol has been used in the treatment of liver disease for centuries. This agent dissolves or prevents cholesterol gallstones by blocking hepatic cholesterol production and decreasing bile cholesterol. Ursodiol also reduces the absorption of cholesterol from the intestinal tract. 306456 moxifloxacin hydrochloride The hydrochloride salt of a fluoroquinolone antibacterial antibiotic. Moxifloxacin binds to and inhibits the bacterial enzymes DNA gyrase (topoisomerase II) and topoisomerase IV, resulting in inhibition of DNA replication and repair and cell death in sensitive bacterial species. 315643 ravuconazole A triazole with antifungal activity. Ravuconazole inhibits 14a demethylase, an enzyme involved in sterol synthesis, resulting in lysis of the fungal cell wall and fungal cell death. C38688 315736 transgenic lymphocyte immunization vaccine A vaccine consisting of a preparation of allogeneic lymphocytes that encode a gene for telomerase. In transgenic lymphocyte immunization, the transgenic cells are infused into the patient, where they serve as antigen- presenting cells (APCs) with the dual function of antigen synthesis and presentation. Vaccination produces an immune response targeting cancer cells expressing telomerase. C38720 315740 paricalcitol A synthetic noncalcemic, nonphosphatemic vitamin D analogue. Paricalcitol binds to the vitamin D receptor and has been shown to reduce parathyroid hormone (PTH) levels. This agent also increases the expression of PTEN ('Phosphatase and Tensin homolog deleted on chromosome Ten'), a tumor-suppressor gene, in leukemic cells and cyclin-dependent kinase inhibitors, resulting in tumor cell apoptosis and tumor cell differentiation into normal phenotypes. C38693 315774 cyproheptadine hydrochloride The hydrochloride salt of a synthetic methyl-piperidine derivative with antihistaminic and anti-serotoninergic properties. Cyproheptadine competes with free histamine (HA) for binding at HA-receptor sites, thereby competitively antagonizing histamine stimulation of HA-receptors in the gastrointestinal tract, large blood vessels, and bronchial smooth muscle. This agent also competes with free serotonin for binding at serotonin receptor sites. Cyproheptadine exhibits anticholinergic and sedative properties and has been shown to stimulate appetite and weight gain. C28949 315883 fruit and vegetable extracts Extracts from fruits and vegetables that contain fiber, vitamins, minerals, and other natural substances with antioxidant, lipid-lowering, and antiproliferative properties. Used in chemoprevention therapy, these extracts may prevent the development or recurrence of cancer. 315885 dasatinib An orally bioavailable synthetic small molecule-inhibitor of SRC-family protein-tyrosine kinases. Dasatinib binds to and inhibits the growth-promoting activities of these kinases. Apparently because of its less stringent binding affinity for the BCR-ABL kinase, dasatinib has been shown to overcome the resistance to imatinib of chronic myeloid leukemia (CML) cells harboring BCR-ABL kinase domain point mutations. SRC-family protein-tyrosine kinases interact with variety of cell-surface receptors and participate in intracellular signal transduction pathways; tumorigenic forms can occur through altered regulation or expression of the endogenous protein and by way of virally-encoded kinase genes. C38713 315898 talampanel A synthetic derivative of dioxolo-benzodiazepine with anti-seizure activity. Talampanel noncompetitively binds to the AMPA (alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid) subtype of glutamate excitatory amino acid receptors and may inhibit the growth of gliomas by interfering with neurotransmitters involved in brain tumor growth. This agent may also protect against traumatic brain injury. 322247 monoclonal antibody HuHMFG1 A humanized monoclonal antibody directed against MUC1, a mucin glycoprotein overexpressed in breast and other carcinomas. Monoclonal antibody HuHMFG1 stimulates antibody-dependent cell-mediated cytotoxicity (ADCC) against tumor cells expressing MUC1, resulting in a decrease in tumor burden. C38697 322808 pertuzumab A humanized recombinant monoclonal antibody directed against the extracellular dimerization domain of the HER-2 tyrosine kinase receptor. Binding of the antibody to the dimerization domain of the HER-2 tyrosine kinase receptor protein directly inhibits the ability of the HER-2 tyrosine kinase receptor protein (the most common pairing partner) to dimerize with other HER tyrosine kinase receptor proteins; inhibiting receptor protein dimerization prevents the activation of HER signaling pathways, resulting in tumor cell apoptosis. 322832 sertraline hydrochloride The hydrochloride salt of sertraline, a synthetic derivative of naphthalenamine with anti-serotoninergic and anti-depressant properties. Sertraline appears to selectively inhibit the neuronal uptake of serotonin, raising serotonin levels in the CNS. 328241 lamotrigine A synthetic phenyltriazine with antiepileptic and analgesic properties. Lamotrigine enhances the action of gamma-aminobutyric acid, an inhibitory neurotransmitter, which may result in a reduction of pain-related transmission of signals along nerve fibers. This agent may also inhibit voltage-gated sodium channels, suppress glutamate release, and inhibit serotonin reuptake. C38703 328242 anidulafungin A cyclic lipopeptide echinocandin derivative with antifungal activity. Anidulafungin inhibits 1,3 beta-D-glucan synthase, an enzyme involved in fungal cell wall synthesis, resulting in cell lysis and death. This agent is active against Candida species and Aspergillus. C38716 331866 oxandrolone A synthetic, anabolic steroid hormone analog of testosterone. Similar to testosterone, oxandrolone binds to and activates specific nuclear receptors. This agent may be used for testosterone replacement therapy in hypogonadal men, in HIV-wasting syndrome, and in other conditions in order to increase nitrogen retention and fat-free muscle mass. C29306 334454 LMP2a-specific cytotoxic T-lymphocytes A preparation of cytotoxic T-lymphocytes (CTL), specifically reactive to Epstein-Barr virus (EBV) latent membrane protein-2A (LMP2A), with potential antineoplastic activity. T-lymphocytes are exposed ex vivo to dendritic cells (DCs) transfected with a replication-deficient adenovirus encoding EBV LMP2A. Subsequently, LMP2A-specific CTLs are exposed to EBV infected cells transfected with adenovirus encoding LMP2A, thereby further stimulating CTLs. Administered to patients with EBV-positive tumors, LMP2A-specific CTLs target LMP2A-positive cells, resulting in cell lysis and inhibition of cancer cell proliferation. EBV LMP2A may be expressed in various malignancies, including nasopharyngeal carcinoma and Hodgkin and non-Hodgkin lymphomas. C62784 334949 autologous heat-shock protein 70 peptide vaccine AG-858 A recombinant cancer vaccine made with tumor-derived heat shock protein 70 (HSP70) peptide complexes. HSP70 associates with antigenic peptides, transporting them into antigen presenting cells (APC) for processing. Tumor-derived HSP70-peptide complexes used in vaccine preparations have been shown to prime tumor immunity and tumor-specific T cells in animal models. 335280 PEG-interferon alfa-2a A covalent conjugate of recombinant interferon alfa, subtype 2a, and polyethylene glycol (PEG), used as an antiviral and antineoplastic agent. The biological activity of this agent is derived from its interferon alpha-2a protein moiety. Interferons alfa bind to specific cell-surface receptors, leading to the transcription and translation of genes whose protein products mediate antiviral, antiproliferative, anticancer and immune-modulating effects. The PEG moiety lowers the clearance of interferon alpha-2a, thereby extending the duration of its therapeutic effects, but may also reduce interferon-mediated stimulation of an immune response. C33987 339378 methoxy polyethylene glycol epoetin beta A pegylated form of recombinant human erythropoietin, a glycosylated protein naturally produced in the kidney that stimulates erythrocyte production in the bone marrow. Methoxypolyethylene glycol epoetin beta may reverse anemias induced by cancer therapy. 339562 PI-88 A mixture of highly sulfated, monophosphorylated mannose oligosaccharides, derived from the extracellular phosphomannan of the yeast Pichia (Hansenula) holstii, with potential antiangiogenic activity. Heparanase inhibitor PI-88 inhibits the endo-beta-D-glucuronidase heparanase, which may interfere with the heparanase-mediated degradation of heparan-sulfate proteoglycans in extracellular matrices, an important step in the metastatic process. This agent may also bind with high affinity to the heparan sulfate-binding domains of vascular endothelial growth factor (VEGF) and fibroblast growth factors 1 and 2, thereby reducing their functional activities and inhibiting VEGF and FGF stimulation of tumor angiogenesis. Increased heparanase activity has been implicated in tumor angiogenesis and metastasis. 339873 recombinant vaccinia-MUC-1 vaccine A vaccine containing a recombinant vaccinia virus that encodes the gene for human mucin-1, a tumor-associated antigen. Upon administration, recombinant vaccinia-MUC-1 vaccine may elicit a MUC-1-specific cytotoxic T cell response against tumor cells bearing MUC-1. 340956 yttrium Y 90 monoclonal antibody Hu3S193 A radioimmunotherapeutic agent consisting of a humanized murine monoclonal antibody (hu3S193) directed against the tumor-associated Lewis Y epithelial antigen chelated to the radioisotope yttrium-90. Yttrium Y 90 monoclonal antibody Hu3S193 binds to Lewis Y epithelial antigen-expressing tumor cells, selectively delivering a cytotoxic dose of beta radiation. C38678 341632 multi-epitope melanoma peptide vaccine A peptide cancer vaccine consisting of a combination of peptides derived form several melanoma epitopes. Vaccination with multi-epitope melanoma peptide vaccine stimulates the host immune system to mount a cytotoxic T lymphocyte (CTL) response against tumor cells expressing the corresponding antigens, resulting in tumor cell lysis. This vaccine may stimulate a broader CTL response compared to single-antigen vaccines. C38695 341633 melanoma helper peptide vaccine A multivalent vaccine consisting of peptides derived from melanoma-associated antigens and an adjuvant peptide derived from tetanus toxoid. Vaccination with this agent may stimulate a host cytotoxic T-cell response against tumor cells expressing melanoma-associated antigens, resulting in tumor cell lysis. C38700 346072 survivin antigen A tumor-associated antigen. Vaccination with survivin antigen may result in a cytotoxic T-cell response against survivin antigen-expressing tumor cells, resulting in decreased tumor cell proliferation and tumor cell death. Overexpressed in many tumors, endogenous survivin inhibits tumor cell apoptosis. C37449 346082 CC-8490 A benzopyran with potential antineoplastic activity. CC-8490 acts as a selective estrogen receptor modulator (SERM), inhibiting the proliferation of estrogen-sensitive breast cancer cells. This agent also inhibits growth and induces apoptosis of glioblastoma cells via a mechanism independent of estrogen receptor-related mechanisms. 346110 BB-10901 An immunoconjugate of a humanized murine monoclonal antibody (huN-901) and DMI, a semi-synthetic derivative of the plant-derived ansa macrolide maytansine. The antibody moiety of BB-10901 selectively attaches to CD56 antigen, a neural cell adhesion molecule (NCAM)) expressed on the surface of cells of small cell lung cancer (SCLC) and other neuroendocrine (NE) tumors. Thus, the DMI conjugate is targeted specifically to CD56-expressing tumor cells, where it inhibits tubulin polymerization and assembly, resulting in inhibition of mitosis and cell cycle arrest in the S phase. 346435 GVAX lung cancer vaccine An autologous lung cancer vaccine consisting of patient-specific lung cancer cells genetically modified to secrete granulocyte-macrophage colony stimulating factor (GM-CSF), an immunostimulatory cytokine. GM-CSF modulates the proliferation and differentiation of a variety of hematopoietic progenitor cells with some specificity towards stimulation of leukocyte production and may reverse treatment-induced neutropenias. This agent also promotes antigen presentation, up-regulates antibody-dependent cellular cytotoxicity (ADCC), and increases interleukin-2-mediated lymphokine-activated killer cell function and may augment host antitumoral immunity. For safety, cells are irradiated prior to vaccination. 346468 TGFa-PE38 immunotoxin A recombinant, chimeric toxin composed of human transforming growth factor alpha (TGF-alpha) fused to a fragment of Pseudomonas exotoxin (PE38) without its cell-binding domain. The TGF-alpha moiety of the agent attaches to tumor cells expressing the epithelial growth factor receptor (EGFR); the exotoxin induces caspase-mediated apoptosis of tumor cells via a mechanism involving mitochondrial damage; it also catalyzes the transfer of ADP ribose from nicotinamide adenine dinucleotide (NAD) to elongation factor-2 in eukaryotic cells, thereby inactivating elongation factor 2 and inhibiting protein synthesis. 346499 siplizumab A monoclonal immunoglobulin G1 antibody with potential antineoplastic activity. Siplizumab binds to CD2, a specific receptor found in T cells and NK cells, thereby triggering a host immune response that results in lysis of CD2+ cells, selective suppression of the immune system, and control of activated T cell growth. C38685 346914 DJ-927 A semi-synthetic, orally bioavailable taxane derivative with potential antineoplastic properties. Oral taxane derivative DJ-927 binds to tubulin, promoting microtubule assembly and stabilization and preventing microtubule depolymerization, thereby inhibiting cell proliferation. As it represents poor substrate for P-glycoprotein-related drug resistance mechanisms, this agent may be useful for treating multi-drug resistant tumors. As the first oral taxane derivative, oral taxane derivative DJ-927 is more potent than paclitaxel and docetaxel. C37451 350047 valproic acid A synthetic derivative of propylpentanoic acid with antiepileptic properties and potential antineoplastic and antiangiogenesis activities. In epilepsy, valproic acid appears to act by increasing the concentration of gamma-aminobutyric acid (GABA) in the brain. This agent's antitumor and antiangiogenesis activities may be related to the inhibition of histone deacetylases and nitric oxide synthase, which results in the inhibition of nitric oxide synthesis. 350071 Valeriana officinalis extract An herbal extract isolated from the root of the plant Valeriana officinalis with sedative and anxiolytic activities. Valeriana officinalis extract contains four distinct classes of phytochemical constituents: volatile oils; sesquiterpenoids, including valerenic acid and its hydroxyl and acetoxyl derivative; valepotriates; and volatile pyridine alkaloids. Although the exact mechanism of action has not been established, the sequiterpenoids in Valeriana officinalis extract, particularly valerenic acid, appear to account for its sedative and anxiolytic effects. Valerenic acid is both a subtype-selective GABA-A receptor agonist and a 5HT-5A receptor partial agonist. The sedative-hypnotic benzodiazepines are GABA-A receptor agonists. C38725 350082 allogeneic tumor cell vaccine A vaccine composed of tumor cells isolated from the tumor of one patient, killed and processed, and administered to another patient in order to stimulate cytotoxic immune responses to a similar tumor cell type. The cells found in this type of whole-cell vaccine express many cell-surface tumor-associated antigens. This vaccine is frequently administered with an adjuvant immunostimulant. 350157 ABT-510 A synthetic peptide that mimics the anti-angiogenic activity of the endogenous protein thrombospondin-1 (TSP-1). ABT-510 inhibits the actions of several pro-angiogenic growth factors important to tumor neovascularization; these pro-angiogenic growth factors include vascular endothelial growth factor (VEGF), basic fibroblast growth factor (bFGF)), hepatocyte growth factor (HGF), and interleukin 8 (IL-8). C37447 350251 bendamustine hydrochloride The hydrochloride salt of bendamustine, a bifunctional mechlorethamine derivative with alkylator and antimetabolite activities. Bendamustine possesses three active moieties: an alkylating group; a benzimidazole ring, which may act as a purine analogue; and a butyric acid side chain. Although its exact mechanism of action is unknown, this agent appears to act primarily as an alkylator. Bendamustine metabolites alkylate and crosslink macromolecules, resulting in DNA, RNA and protein synthesis inhibition, and, subsequently, apoptosis. Bendamustine may differ from other alkylators in that it may be more potent in activating p53-dependent stress pathways and inducing apoptosis; it may induce mitotic catastrophe; and it may activate a base excision DNA repair pathway rather than an alkyltransferase DNA repair mechanism. Accordingly, this agent may be more efficacious and less susceptible to drug resistance than other alkylators. 350384 TAC-101 A retinobenzoic acid with potential antineoplastic activity. TAC-101 inhibits retinoblastoma-gene product (RB) phosphorylation and increases the presence of 2 cyclin-dependent kinase (CDK) inhibitors, resulting in cell cycle arrest. This agent also causes a cytotoxic decline in cyclin A and thymidylate synthase expression. C38684 350433 matuzumab A humanized monoclonal antibody with antineoplastic activity. Matuzumab binds the epidermal growth factor receptor (EGFR) with high\naffinity, competitively blocking natural ligand binding and\nblocking receptor-mediated downstream signalling, resulting in impaired tumor cell proliferation. C2012 352004 inotuzumab ozogamicin A CD22-targeted cytotoxic immunoconjugate composed of a humanized IgG4 anti-CD22 antibody covalently linked to N-acetyl-gamma-calicheamicin dimethyl hydrazide (CalichDMH) with potential antineoplastic activity. Inotuzumab ozogamicin is rapidly internalized upon binding of the antibody moiety to B cell-specific CD22 receptors, delivering the conjugated CalichDMH intracellularly; the CalichDMH moiety binds to the minor groove of DNA in a sequence-specific manner, resulting in double-strand DNA breaks and apoptosis. CalichDMH is a derivative of gamma calicheamicin, a cytotoxic antibiotic produced by the bacterium Micromonospora echinospora. C71542 352016 OSI-7904L A liposome-encapsulated formulation of the benzoquinazoline folate analog OSI-7904 with antineoplastic activity. As a thymidylate synthase inhibitor, OSI-7904 noncompetitively binds to thymidylate synthase, resulting in inhibition of thymine nucleotide synthesis and DNA replication. Liposome encapsulation improves the efficacy and increases the half-life of OSI-7904. 352165 EKB-569 A 3-cyanoquinoline pan-ErbB tyrosine kinase inhibitor with potential antineoplastic activity. EKB-569 irreversibly binds covalently to epidermal growth factor receptors (EGFR) ErbB-1, -2 and -4, thereby inhibiting receptor phosphorylation and signal transduction and resulting in apoptosis and suppression of proliferation in tumor cells that overexpress these receptors. C2713 352181 axitinib An orally bioavailable tyrosine kinase inhibitor. Axitinib inhibits the proangiogenic cytokines vascular endothelial growth factor (VEGF) and platelet-derived growth factor receptor (PDGF), thereby exerting an anti-angiogenic effect. 353146 tandutinib A piperazinyl quinazoline receptor tyrosine kinase inhibitor with antineoplastic activity. Tandutinib inhibits the autophosphorylation of FLT3 (FMS-Like Tyrosine kinase-3), c-KIT and PDGF (platelet-derived growth factor) receptor tyrosine kinases, thereby inhibiting cellular proliferation and inducing apoptosis. C48404 353153 ZD6126 A water-soluble phosphate prodrug of N-acetylcolchinol with potential antiangiogenesis and antineoplastic activities. ZD6126 is converted in vivo into N-acetylcolchinol. N-acetylcolchinol binds to and destabilizes the tubulin cytoskeleton of endothelial cells in tumor blood vessels, which may result in tumor endothelial cel apoptosis, the selective occlusion of tumor blood vessels, cessation of tumor blood flow, and tumor necrosis. C2736 353187 recombinant adenovirus-L523S vaccine A replication-defective adenovirus containing a gene that encodes the human protein L523S with potential antineoplastic activity. Upon administration, recombinant adenovirus-L523S vaccine expresses L523S, which may stimulate antibody and cytotoxic T lymphocyte (CTL) responses against tumor cells expressing L523S. L523S is an RNA-binding protein that belongs to the KOC (K homology domain containing protein over-expressed in cancer) family of proteins. As an oncofetal protein, L523S is normally expressed in early embryonic tissues and certain normal adult tissues such as colon, fallopian tube, gall bladder, and ovary tissues but may be overexpressed in squamous cell cancers of the lung. C49289 353478 cytochlor A radio-sensitizing pyrimidine nucleoside with potential antineoplastic activity. Cytochlor is metabolized first to a phosphate derivative, CldCMP, by the enzyme deoxycytidine kinase and then to the active uracyl derivative, CldUMP, by the enzyme dCMP deaminase; deoxycytidine kinase and dCMP deaminase have been found in abnormally high concentrations in most cancers. CldUMP, the active metabolite, incorporates into DNA and, upon exposure to radiation, induces the formation of uracil radicals and double-strand DNA breaks. 354223 ridaforolimus A small molecule and non-prodrug analogue of the lipophilic macrolide antibiotic rapamycin with potential antitumor activity. Ridaforolimus binds to and inhibits the mammalian target of rapamycin (mTOR), which may result in cell cycle arrest and,consequently, the inhibition of tumor cell growth and proliferation. Upregulated in some tumors, mTOR is a serine/threonine kinase involved in regulating cellular proliferation, motility, and survival that is located downstream of the PI3K/Akt signaling pathway. C49061 354249 EL625 A phosphorothioate oligonucleotide harboring nucleotide sequences complementary to tumor suppressor p53 mRNA. EL625 hybridizes with p53 mRNA molecules, and induces Rnase H dependent hydrolysis of p53 transcripts in the double stranded section of the hybrids, thereby resulting in loss of p53 production. Loss of p53 activity leads to sensitization of cancer cells to other therapeutics. 354256 tezacitabine A synthetic purine nucleoside analogue with potential antineoplastic activity. Phosphorylated by cellular kinases, tezacitabine is converted into its active diphosphate and triphosphate metabolites. Tezacitabine diphosphate binds to and irreversibly inhibits the activity of the enzyme ribonucleotide reductase (RNR), which may result in the inhibition of DNA synthesis in tumor cells and tumor cell apoptosis. Tezacitabine triphosphate acts as a substrate for DNA polymerase, further compromising DNA replication. This agent is relatively resistant to metabolic deactivation by cytidine deaminase. RNR catalyzes the conversion of ribonucleoside 5'-diphosphates to deoxyribonucleoside 5'-diphosphates necessary for DNA synthesis and is overexpressed in many tumor types. C1539 355727 zibotentan An orally available selective antagonist of the endothelin-A (ET-A) receptor with potential antineoplastic activity. Zibotentan binds selectively to the ET-A receptor, thereby inhibiting endothelin-mediated mechanisms that promote tumor cell proliferation. C48430 355732 anti-CD45 monoclonal antibody BC8 A murine IgG1 anti-CD45 monoclonal antibody (MoAb) with immunotherapeutic activity. CD45 antigen, a receptor protein-tyrosine phosphatase essential for T cell development and lymphocyte activation, is expressed on virtually all leukocytes. MoAb BC8 has specificity for hematopoietic tissues and may be used in targeted immunotherapy. C1961 355732 anti-CD45 monoclonal antibody BC8 A murine IgG1 anti-CD45 monoclonal antibody (MoAb) with immunotherapeutic activity. CD45 antigen, a receptor protein-tyrosine phosphatase essential for T cell development and lymphocyte activation, is expressed on virtually all leukocytes. MoAb BC8 has specificity for hematopoietic tissues and may be used in targeted immunotherapy. C1961 355795 ethiodized oil A synthetic iodine addition product of the ethyl ester of the fatty acids of poppyseed oil. Ethiodized oil contains 37% organically bound iodine and is used as a diagnostic radiopaque medium or, labeled with I-131, as an antineoplastic agent. Selectively retained in tumor vessels for long periods, ethiodized oil is used for imaging organs such as liver, lung, stomach, and thyroid. Labeled with I-131 or other beta emitters (Y-90 or P-32), ethiodol can deliver a high internal radiation dose to certain tumors with minimal effect on healthy tissues. 355797 absorbable gelatin sponge A sterile hemostatic agent composed of purified porcine-derived gelatin. In regional chemotherapy, absorbable gelatin sponge may be used to embolize arteries in the region of a tumor in order to block or retard blood flow; this blockage results in a locally increased concentration of chemotherapeutic agents delivered to the tumor when chemotherapeutic agents are infused into the embolized arterial circulation upstream of the blockage. 355804 NM-3 An orally bioavailable antiangiogenic isocoumarin with potential antineoplastic activity. NM-3 inhibits vascular endothelial growth factor (VEGF), a pro-angiogenic growth factor, thereby inhibiting endothelial cell proliferation. This agent also induces apoptosis by a mechanism involving reactive oxygen species. 357490 garlic A bulbous herb isolated from the plant Allium sativum with potential antineoplastic activity. Garlic contains a number of different organosulfur compounds, some of which have displayed antineoplastic activity. C38706 357497 ruthenium Ru 106 A radioactive isotope of the rare element ruthenium, a member of the light platinum group. A radioactive plaque containing ruthenium 106 may be inserted into the eye to irradiate ophthalmic tumors. 357565 beta-lapachone A naphthoquinone compound derived from bark of Tabebuia sp., with antitumor, antibacterial, antifungal and antitrypanosomal activities. Beta-lapachone exerts its anti-tumor effect by indirect actions of inducing p53-independent apoptosis and cell cycle arrest mediated through altered activities of cell cycle control regulatory proteins; including down-regulating retinoblastoma protein (pRB), a transcriptional repressor target at transcription factor E2F-1, as well as induces expression of cyclin dependent kinase inhibitor 1A (CDKN1A or p21). Both E2F-1 and p21 are required for G1/S-phase transition during cell cycle. This agent also inhibits DNA topoisomerase I by a mechanism distinct from that of camptothecin, and thereby blocks the formation of a cleavable complex leading to enzyme inhibition and prevent DNA repair. Furthermore, beta-lapachone could induce reactive oxygen species in vivo, and result in cytotoxicity. 357572 angiostatin Encoded by human PLG Gene (Plasminogen Family) and expressed in the kidney, angiostatin is an angiogenesis inhibitor present in plasma and other extracellular fluids that blocks neovascularization and mediates suppression of metastases. Containing at least three kringles, angiostatin is a 38-kD internal (serine protease) proteolytic fragment of plasminogen. 357600 monoclonal antibody SGN-30 A genetically-engineered, chimeric mouse-human, anti-CD30 monoclonal antibody with potential antineoplastic activity. Monoclonal antibody SGN-30 specifically binds to the receptor CD-30, a member of the tumor necrosis factor receptor super-family, which may be overexpressed on the surfaces of Hodgkin lymphoma cells and anaplastic-large cell lymphoma cells. After binding to CD30, this agent interferes with the G1 phase of the cell cycle, thereby inducing growth arrest and apoptosis in susceptible tumor cell populations. C2007 357620 deslorelin A synthetic nonapeptide analogue of the natural gonadotrophin releasing hormone (GnRH) with potential antineoplastic activity. Deslorelin binds to and activates pituitary gonadotropin releasing hormone (GnRH) receptors. Continuous, prolonged administration of goserelin in males results in pituitary GnRH receptor desensitization and inhibition of pituitary secretion of follicle stimulating hormone (FSH) and luteinizing hormone (LH), leading to a significant decline in testosterone production; in females, prolonged administration results in a decrease in estradiol production. 360459 alprostadil The naturally occuring prostaglandin E1 (PGE1) which displays a variety of pharmacologic actions. Alprostadil is a potent vasodilator agent that increases peripheral blood flow, inhibits platelet aggregation, and induces bronchodilation. Used in the treatment of erectile dysfunction, this agent produces corporal smooth muscle relaxation by binding to PGE receptors, resulting in the activation of adenylate cyclase and the subsequent accumulation of 3'5'-cAMP. 360460 phentolamine mesylate The mesylate salt of a synthetic imidazoline with alpha-adrenergic antagonist activity. As a competitive alpha-adrenergic antagonist, phentolamine binds to alpha-1 and alpha-2 receptors, resulting in a decrease in peripheral vascular resistance and vasodilatation. This agent also may block 5-hydroxytryptamine (5-HT) receptors and stimulate release of histamine from mast cells. 360844 Traumeel S Diluted extracts isolated from plants and minerals, including belladonna, arnica, St. Johns wort, and Echinacea. As a homeopathic mouth rinse preparation, Traumeel S exhibits antiinflammatory activity; the mechanism of action has not been fully elucidated. This agent may reduce the severity and duration of treatment-related stomatitis. 361537 autologous expanded mesenchymal stem cells OTI-010 Multipotent self-renewing adherent non-hematopoietic stromal cells harvested from a patient's bone marrow and grown in vitro. When injected back into the patient, autologous expanded mesenchymal stem cells OTI-010 may differentiate into various mesenchyme-derived cell types and, in some instances, may augment bone marrow engraftment after whole-body irradiation. 361550 lutetium Lu 177 monoclonal antibody J591 A radioimmunoconjugate consisting of a humanized monoclonal antibody directed against the extracellular domain of prostate-specific membrane antigen linked to a beta-emitting radioisotope (lutetium-177). This radioimmunoconjugate binds to tumor cells that express the extracellular domain of prostate-specific membrane antigen, delivering beta particle radiation selectively to tumor cells expressing this antigen and so limiting the exposure of normal tissues to ionizing radiation. C38701 361777 creatine An endogenous amino acid derivative produced by vertebrate animals and occurring primarily in muscle cells. Creatine is important for energy storage; it is phosphorylated to creatine phosphate, which serves as a phosphate donor in the conversion of ADP to ATP and supplies energy necessary for muscle contraction. Dietary supplementation with creatine may improve muscle wasting associated with cancer and other chronic diseases. C37937 361793 posaconazole A broad-spectrum, second generation, triazole compound with antifungal activity. Posaconazole strongly inhibits 14-alpha demethylase, a cytochrome P450-dependent enzyme. Inhibition of 14-alpha-demethylase prevents the conversion of lanosterol to ergosterol, an important component of the fungal cell wall. Inhibition of ergosterol synthesis changes the fungal cell membrane composition and integrity, alters membrane permeability and eventually leads to fungal cell lysis. Compared to other azole antifungals, posaconazole is a significantly more potent inhibitor of sterol 14-alpha demethylase. C61500 361795 sodium citrate The sodium salt of citrate with alkalinizing activity. Upon absorption, sodium citrate dissociates into sodium cations and citrate anions; organic citrate ions are metabolized to bicarbonate ions, resulting in an increase in the plasma bicarbonate concentration, the buffering of excess hydrogen ion, the raising of blood pH, and potentially the reversal of acidosis. In addition, increases in free sodium load due to sodium citrate administration may increase intravascular blood volume, facilitating the excretion of bicarbonate compounds and an anti-urolithic effect. 362071 carbon-11 acetate The acetate salt of the radioisotope carbon-11. Although the mechanism is unclear, carbon-11 acetate preferentially accumulates in tumor tissue, serving as a tracer for imaging tumors with positron emission tomography (PET). C38712 363619 E7820 A small molecule and aromatic sulfonamide derivative with potential antiangiogenic and antitumor activities. E7820 inhibits angiogenesis by suppressing integrin alpha 2, a cell adhesion molecule expressed on endothelial cells. Inhibition of integrin alpha 2 leads to an inhibition of cell-cell interactions, endothelial cell-matrix interactions, vascular endothelial cell proliferation and angiogenesis. C61501 365545 dacetuzumab A humanized monoclonal antibody directed against the CD40 receptor with potential antineoplastic activity. Dacetuzumab specifically binds to and inhibits the CD40 receptor, thereby inducing apoptosis and inhibiting cellular proliferation via antibody-dependent cellular cytotoxicity (ADCC) in cells that overexpress this receptor. The CD40 receptor, a member of the tumor necrosis factor (TNF) receptor super-family, is highly expressed on most B lineage hematologic malignancies including multiple myeloma, non-Hodgkin's lymphoma, chronic lymphocytic leukemia, Hodgkin's disease and acute lymphoblastic leukemia. C62179 365679 iloprost A prostacyclin analogue with potential chemopreventive activity. Iloprost binds to the prostacyclin receptor in various target cells, thereby causing vasodilation, inhibition of platelet aggregation, and decreased tumor cell adhesion to endothelium among other effects. Prostacyclin is a naturally occurring eicosanoid with anti-inflammatory, antineoplastic, and anti-metastatic properties. C48397 365963 ibandronate sodium The sodium salt of ibadronic acid, a synthetic nitrogen-containing bisphosphonate. Ibandronic acid inhibits farnesyl pyrophosphate synthase, resulting in a reduction in geranylgeranyl GTPase signaling proteins and apoptosis of osteoclasts. This agent increases bone mineral density, decreases bone remodeling, inhibits osteoclast-mediated bone resorption, and reduces metastases-related and corticosteroid-related bone pain. 367053 lestaurtinib An orally bioavailable indolocarbazole derivative with antineoplastic properties. Lestaurtinib inhibits autophosphorylation of FMS-like tyrosine kinase 3 (FLT3), resulting in inhibition of FLT3 activity and induction of apoptosis in tumor cells that overexpress FLT3. 367246 esomeprazole magnesium The magnesium salt of esomeprazole, the S-isomer of omeprazole, with gastric proton pump inhibitor activity. In the acidic compartment of parietal cells, esomeprazole is protonated and converted into the active achiral sulphenamide; the active sulphenamide forms one or more covalent disulfide bonds with the proton pump hydrogen-potassium adenosine triphosphatase (H+/K+ ATPase), thereby inhibiting its activity and the parietal cell secretion of H+ ions into the gastric lumen, the final step in gastric acid production. H+/K+ ATPase is an integral membrane protein of the gastric parietal cell. C29032 370808 zolpidem tartrate The tartrate salt of an imidazopyridine with non-benzodiazepine benzodiazepine-receptor agonist and sedative-hypnotic activities. Zolpidem binds selectively to the alpha 1 subunit of the omega-1 (BZ1) receptor of the gamma-aminobutyric acid type A (GABA-A ) receptor-chloride ionophore complex, thereby opening neuronal chloride channels, hyperpolarizing neuronal cell membranes, and inhibiting neuronal firing. In contrast, benzodiazepines non-selectively bind to and activate all omega receptor subtypes, exhibiting anticonvulsant and myorelaxant activities in addition to a sedative-hypnotic activity. C29553 371709 4-hydroxytamoxifen A tamoxifen metabolite with both estrogenic and anti-estrogenic effects. 4-hydroxytamoxifen has a higher affinity for the estrogen receptor than tamoxifen, and functions as an antagonist in breast cancer cells. 371727 AEE788 An orally bioavailable multiple-receptor tyrosine kinase inhibitor. AEE788 inhibits phosphorylation of the tyrosine kinases of epidermal growth factor receptor (EGFR), human epidermal growth factor receptor 2 (HER2), and vascular endothelial growth factor receptor 2 (VEGF2), resulting in receptor inhibition, the inhibition of cellular proliferation, and induction of tumor cell and tumor-associated endothelial cell apoptosis. C48369 372905 everolimus A derivative of the natural macrocyclic lactone sirolimus with immunosuppressant and anti-angiogenic properties. In cells, everolimus binds to the immunophilin FK Binding Protein-12 (FKBP-12) to generate an immunosuppressive complex that binds to and inhibits the activation of the mammalian Target of Rapamycin (mTOR), a key regulatory kinase. Inhibition of mTOR activation results in the inhibition of T lymphocyte activation and proliferation associated with antigen and cytokine (IL-2, IL-4, and IL-15) stimulation and the inhibition of antibody production. 372906 talabostat mesylate The orally bioavailable mesylate salt of an amino boronic dipeptide with antineoplastic and hematopoiesis- stimulating activities. By cleaving N-terminal Xaa-Pro or Xaa-Ala residues, talabostat inhibits dipeptidyl peptidases, such as fibroblast activation protein (FAP), resulting in the stimulation of cytokine and chemokine production and specific T-cell immunity and T-cell- dependent activity. This agent may also stimulate the production of colony stimulating factors, such as granulocyte colony stimulating factor (G-CSF), resulting in the stimulation of hematopoiesis. Dipeptidyl peptidases are involved in the activation of polypeptide hormones and chemokines. C80682 373829 monoclonal antibody G250 A chimeric monoclonal antibody directed against G250, a cell surface antigen found in the majority of renal cell carcinomas. Following binding, monoclonal antibody G250 (mAb G250) may be internalized by G250 antigen-expressing renal carcinoma cells; mAb G250 may be useful as a carrier for radioisotopes and other antineoplastic therapeutic agents. C1960 373865 SB-AS15 adjuvant A vaccine adjuvant containing CpG 7909, monophosphoryl lipid, and QS-21 with potential antineoplastic and immunostimulatory activities. CpG 7909 is a synthetic 24-mer oligonucleotide containing 3 CpG motifs that selectively targets Toll-like receptor 9 (TLR9), thereby activating dendritic and B cells and stimulating cytotoxic T cell and antibody responses against tumor cells bearing tumor antigens. Monophosphoryl lipid is a detoxified derivative of lipid A, a component of Salmonella minnesota lipopolysaccharide (LPS); this agent may enhance humoral and cellular responses to various antigens. QS-21 is a purified, naturally occurring saponin derived from the South American tree Quillaja saponaria Molina and exhibits various immunostimulatory activities. Combinations of monophosphoryl lipid and QS-21 may be synergistic in inducing humoral and cellular immune responses. C48421 373868 technetium Tc 94m sestamibi A radioconjugate consisting of sestamibi labeled with the positron-emitting isotope Tc 94m. Sestamibi is a synthetic molecule of the isonitrile family that diffuses through cell membranes and may preferentially accumulate within mitochondria. Technetium Tc 94m sestamibi may be used in tumor-imaging studies utilizing positron emission tomography (PET). C48423 377345 ferumoxytol A superparamagnetic iron oxide nanoparticle coated with a low molecular weight semi-synthetic carbohydrate, polyglucose sorbitol carboxymethyl ether, with potential anti-anemic and imaging properties. After intravenous administration, ferumoxytol replaces iron stores with fewer side effects compared to the use of oral iron. In addition, this agent generates T1 relaxation, producing a magnetic field and enhancing T2 relaxation, thereby darkening contrast media-containing structures in magnetic resonance imaging (MRI). Due to small particle size, ferumoxytol remains in the intravasculature for a prolonged period and so may be used as a blood pool agent. C38138 377539 elesclomol A small-molecule bis(thio-hydrazide amide) with oxidative stress induction, pro-apoptotic, and potential antineoplastic activities. Elesclomol induces oxidative stress, creating high levels of reactive oxygen species (ROS), such as hydrogen peroxide, in both cancer cells and normal cells. Because tumor cells have elevated levels of ROS compared to normal cells, the increase in oxidative stress beyond baseline levels elevates ROS beyond sustainable levels, exhausting tumor cell antioxidant capacity, which may result in the induction of the mitochondrial apoptosis pathway. Normal cells are spared because the increase in the level of oxidative stress induced by this agent is below the threshold at which apoptosis is induced. C75291 378203 alvespimycin hydrochloride The hydrochloride salt of alvespimycin, an analogue of the antineoplastic benzoquinone antibiotic geldanamycin. Alvespimycin binds to HSP90, a chaperone protein that aids in the assembly, maturation and folding of proteins. Subsequently, the function of Hsp90 is inhibited, leading to the degradation and depletion of its client proteins such as kinases and transcription factors involved with cell cycle regulation and signal transduction. C38142 380753 iodine I 131 monoclonal antibody 8H9 A radioimmunoconjugate consisting of the iodine 131-radiolabeled murine IgG1 monoclonal antibody 8H9 directed against the surface immunomodulatory glycoprotein 4Ig-B7-H3 with potential radioimaging and radioimmunotherapeutic uses. Iodine I 131 monoclonal antibody 8H9 binds to 4Ig-B7-H3 (human B7-H3 with 4 Ig-like domains) and may be used to radioimage and/or destroy tumor cells that express tenascin. 4Ig-B7-H3 inhibits T-cell activation and the production of effector cytokines such as interferon-gamma and interleukin-4; it is expressed on the cell membranes of a wide variety of tumors of neuroectodermal, mesenchymal and epithelial origin and is highly expressed on monocyte-derived dendritic cells (mdDCs). In vitro, it has been shown that monoclonal antibody-mediated masking of 4Ig-B7-H3 on neuroblastoma cells resulted in the enhancement of natural killer (NK)-mediated lysis of target cells. C48400 382134 atiprimod An orally bioavailable small molecule belonging to the azaspirane class of cationic amphiphilic agents with anti-inflammatory, antineoplastic, and antiangiogenic properties. Atiprimod inhibits the phosphorylation of signal transducer and activator of transcription 3 (STAT3), blocking the signalling pathways of interleukin-6 and vascular endothelial growth factor (VEGF) and downregulating the anti-apoptotic proteins Bcl-2, Bcl-XL, and Mcl-1, thereby inhibiting cell proliferation, inducing cell cycle arrest, and inducing apoptosis. 385490 APC8015F A cell-based vaccine composed of previously frozen autologous antigen-presenting peripheral blood mononuclear cells (enriched for a dendritic cell fraction) that have been exposed to a recombinant protein consisting of granulocyte-macrophage colony-stimulating factor (GM-CSF) fused to prostatic-acid phosphatase (PAP), a protein expressed by prostate cancer cells. Upon administration, the vaccine may stimulate an antitumor T-cell response against tumor cells expressing PAP. C48640 385666 inalimarev A cancer vaccine comprised of a recombinant vaccinia viral vector encoding the carcinoembryonic antigen (CEA), MUC-1 (mucin-1), a transmembrane glycoprotein secreted by glandular tissues, and TRICOM, comprised of the three co-stimulatory molecule transgenes B7-1, ICAM-1 and LFA-3. Upon administration, inalimarev may enhance CEA and MUC-1 presentation to antigen presenting cells (APC) and may activate a cytotoxic T lymphocyte (CTL) response against CEA- and MUC-1-expressing tumor cells. C29317 385667 falimarev A cancer vaccine comprised of a recombinant fowlpox viral vector encoding the carcinoembryonic antigen (CEA), MUC-1, a transmembrane glycoprotein secreted by glandular epithelial tissues, and TRICOM, comprised of three co-stimulatory molecule transgenes (B7-1, ICAM-1 and LFA-3). This agent may enhance CEA and MUC-1 presentation to antigen-presenting cells (APC) and may activate a cytotoxic T-cell response against CEA- and MUC-1-expressing tumor cells. C29316 385686 synthetic human corticotropin-releasing factor A synthetic therapeutic agent which is chemically identical to or similar to the endogenous human corticotropin-releasing factor (hCRF). Synthesized in the hypothalamus, hCRF stimulates the anterior pituitary gland to secrete adrenocorticotropic hormone (ACTH). In cerebral edema, hCRF acts by impeding the flow of fluid from blood vessels into brain tissue, thereby decreasing edema and stabilizing intracranial pressure. This agent possesses anti-edema properties independent of adrenal gland function. C394 386168 recombinant interleukin-18 A recombinant therapeutic agent which is chemically identical to or similar to the endogenous cytokine interleukin-18 (IL-18). Produced primarily by macrophages, IL-18 induces the production of interferon-gamma (IFN-gamma), and enhances the activity of natural killer (NK) and cytotoxic T lymphocytes (CTL). As a potential immunotherapeutic agent, IL-18 displays antitumor effects in vitro and in animal models. C1680 386183 XL647 An orally bioavailable small-molecule receptor tyrosine kinase (RTK) inhibitor with potential antineoplastic activity. XL647 binds to and inhibits several tyrosine receptor kinases that play major roles in tumor cell proliferation and tumor vascularization, including epidermal growth factor receptor (EGFR; ERBB1), epidermal growth factor receptor 2 (HER2; ERBB2), vascular endothelial growth factor receptor (VEGFR), and ephrin B4 (EphB4). This may result in the inhibition of tumor growth and angiogenesis, and tumor regression. C62496 387795 talmapimod An orally bioavailable, small-molecule, p38 mitogen-activated protein kinase (MAPK) inhibitor with potential immunomodulating, anti-inflammatory, and antineoplastic activities. Talmapimod specifically binds to and inhibits the phosphorylation of p38 MAPK, which may result in the induction of tumor cell apoptosis, the inhibition of tumor cell proliferation, and the inhibition of tumor angiogenesis. This agent may also enhance proteasome inhibitor-induced apoptosis. p38 MAPK is a serine/threonine protein kinase involved in a MAPK signaling cascade that controls cellular responses to various environmental stresses, cytokines, and endotoxins. C79841 387796 talotrexin ammonium The ammonium salt of an antimetabolite analogue of aminopterin with potential antineoplastic activity. As a folate antagonist, talotrexin binds to and inhibits the function of dihydrofolate reductase, resulting in the inhibition of folate metabolism, DNA synthesis, and cell division. Hydrosoluble, talotrexin is actively transported into cells by the reduced folate carrier (RFC) and, therefore, is unlikely to be associated with P-glycoprotein-mediated multidrug resistance. C29341 387966 HLA-A2, A3-restricted FGF-5 peptides/Montanide ISA-51 vaccine A peptide vaccine comprised of synthetic HLA-A2- and HLA-A3-binding peptides, derived from amino acid sequences of fibroblast growth factor-5 (FGF-5), combined with the adjuvant Montanide ISA-51 with potential antineoplastic activity. HLA-A2, A3-restricted FGF-5 peptides contain motifs recognized by the MHC class I molecules HLA-A2 and HLA-A3 and may stimulate a cytotoxic T-cell response against tumor cells that overexpress FGF-5. Montanide ISA-51 (also known as incomplete Freund's adjuvant or IFA), a stabilized water-in-oil emulsion adjuvant containing mineral oil with mannide oleate added as a surfactant, non-specifically stimulates cell-mediated immune responses to antigens. C48394 387973 ovarian cancer peptide vaccine A cancer vaccine comprised of synthetic peptides corresponding to naturally-occurring peptides derived from ovarian cancer cell antigens. Ovarian cancer peptide vaccine may elicit a cytotoxic T-cell response against tumor cells expressing the related ovarian cancer cell antigens. C48414 390311 alpha fetoprotein adenoviral vector vaccine A vaccine consisting of a recombinant adenoviral vector encoding alpha fetoprotein. After vaccination, expressed alpha fetoprotein may stimulate a cytotoxic T lymphocyte (CTL) response against tumor cells that express alpha fetoprotein, resulting in tumor cell lysis. C48372 390312 alpha fetoprotein plasmid DNA vaccine A vaccine consisting of plasmid DNA encoding alpha fetoprotein. After vaccination, expressed alpha fetoprotein may stimulate a cytotoxic T lymphocyte (CTL) response against tumor cells that express alpha fetoprotein, resulting in tumor cell lysis. C48373 390313 sargramostim plasmid DNA hepatocellular carcinoma vaccine adjuvant A vaccine adjuvant consisting of a plasmid DNA encoding sargramostim (granulocyte-macrophage colony-stimulating factor). Upon administration, expressed sargramostim may stimulate a cytotoxic T cell response enhancing the host immune response to a concomitantly administered hepatocellular carcinoma vaccine. C48420 391228 motesanib diphosphate The orally bioavailable diphosphate salt of a multiple-receptor tyrosine kinase inhibitor with potential antineoplastic activity. Motesanib selectively targets and inhibits vascular endothelial growth factor (VEGFR), platelet-derived growth factor (PDGFR), kit, and Ret receptors, thereby inhibiting angiogenesis and cellular proliferation. C48374 391236 ispinesib A synthetic small molecule, derived from quinazolinone, with antineoplastic properties. Ispinesib selectively inhibits the mitotic motor protein, kinesin spindle protein (KSP), resulting in inhibition of mitotic spindle assembly, induction of cell cycle arrest during the mitotic phase, and cell death in tumor cells that are actively dividing. Because KSP is not involved in nonmitotic processes, such as neuronal transport, ispinesib may be less likely to cause the peripheral neuropathy often associated with the tubulin-targeting agents. C38131 391254 PEP-3-KLH conjugate vaccine A cancer vaccine consisting of PEP-3, a synthetic peptide encompassing a tumor-specific mutated segment of the epidermal growth factor receptor type vIII (EGFRvIII), conjugated to the naturally-occuring immunoadjuvant keyhole limpet hemocyanin (KLH) with potential immunostimulating and antineoplastic activities. Upon administration, PEP-3-KLH conjugate vaccine may induce a cytotoxic immune response against tumor cells that overexpress EGFRvIII; this antitumoral immune response may involve antibody-dependent cellular cytotoxicity (ADCC). C74070 392723 allogeneic GM-CSF-secreting breast cancer vaccine An allogenic vaccine consisting of irradiated breast cancer cells transfected with the granulocyte macrophage-colony-stimulating factor (GM-CSF) gene. Upon vaccination, the genetically modified cells secrete GM-CSF, thereby potentiating a tumor-specific T cell response against breast cancer cell-asociated antigens. C48371 394098 human prostate-specific membrane antigen plasmid DNA vaccine A vaccine consisting of a plasmid DNA encoding the human prostate-specific membrane antigen (PSMA). Upon administration, expressed PSMA may stimulate a cytotoxic T cell response against tumor cells that express this antigen, resulting in tumor cell lysis. C48396 394099 mouse prostate-specific membrane antigen plasmid DNA vaccine A vaccine consisting of a plasmid DNA encoding the murine prostate-specific membrane antigen (PSMA). Upon administration, expressed PSMA may stimulate a cytotoxic T cell response against tumor cells that express PSMA, resulting in tumor cell lysis. C48411 394101 talactoferrin An orally bioavailable recombinant human lactoferrin produced in the fungus Aspergillus niger with potential antineoplastic and immunomodulating activities. Upon oral administration, talactoferrin is transported into small intestinal Peyer's patches of the gut-associated lymphoreticular tissues (GALT), where it recruits circulating immature dendritic cells (DCs) bearing tumor antigens and induces their maturation. In the GALT, DC maturation in the presence of tumor antigens and lymphoid effector cells may induce systemic innate and adaptive immune responses mediated by anti-tumor natural killer (NK) cells, cytotoxic T lymphocytes, and natural killer T (NKT) cells; activation of tumor-draining lymph nodes, cellular infiltration of distant tumors, and tumor-cell death may follow. Raising the initial immune response in the GALT, distant from the primary tumor, may counter local tumor-mediated immunosuppression. C78460 396824 852A A synthetic imidazoquinoline Toll-like receptor 7 (TLR7) agonist with immunostimulating and potential antitumor activities. TLR7 agonist 852A binds to and activates TLR7, thereby stimulating plasmacytoid dendritic cells (pDC) through the TLR7-MyD88-dependent signaling pathway. Activation of pDC results in secretion of interferon alpha, the production of proimflammatory cytokines, the upregulation of co-stimulatory molecules, and enhanced T and B-cell stimulatory responses. C61104 398145 pioglitazone hydrochloride The hydrochloride salt of an orally-active thiazolidinedione with antidiabetic properties and potential antineoplastic activity. Pioglitazone activates peroxisome proliferator-activated receptor gamma (PPAR-gamma), a ligand-activated transcription factor, thereby inducing cell differentiation and inhibiting cell growth and angiogenesis. This agent also modulates the transcription of insulin-responsive genes, inhibits macrophage and monocyte activation, and stimulates adipocyte differentiation. C29367 403156 CNGRC peptide-TNF alpha conjugate A cytokine-peptide conjugate composed of the cytokine tumor necrosis factor alpha (TNF-alpha) chemically linked to the peptide CNGRC. The peptide moiety CNGRC, a ligand for the membrane-bound metalloprotease CD13, binds to endothelial cells of the angiogenic vasculature that express CD13 (also known as aminopeptidase N); subsequently, the TNF-alpha moiety induces apoptosis in endothelial cells expressing CD13, thereby inhibiting tumor-associated angiogenesis. C48383 405819 resveratrol A phytoalexin derived from grapes and other food products with antioxidant and potential chemopreventive activities. Resveratrol induces phase II drug-metabolizing enzymes (anti-initiation activity); mediates anti-inflammatory effects and inhibits cyclooxygenase and hydroperoxidase functions (anti-promotion activity); and induces promyelocytic leukemia cell differentiation (anti-progression activity), thereby exhibiting activities in three major steps of carcinogenesis. This agent may inhibit TNF-induced activation of NF-kappaB in a dose- and time-dependent manner. C1215 405875 5,10-methylenetetrahydrofolate A folate-based biomodulator with potential antineoplastic activity. 5,10-methylenetetrahydrofolate (MTHF) stabilizes the covalent binding of the fluorouracil metabolite 5-5-fluoro-2'-deoxyuridine-5'-O-monophosphate (FdUMP) to its target enzyme, thymidylate synthase, which results in inhibition of thymidylate synthase, depletion of thymidine triphosphate (TTP), a necessary constituent of DNA, and tumor cell death. Unlike leucovorin, MTHF, as the active form of folate, does not require metabolic activation and may increase the chemotherapeutic effects of fluorouracil with lower toxicity. C61304 409603 GM.CD40L cell vaccine A cell-based vaccine composed of irradiated tumor cells transduced with granulocyte-macrophage colony-stimulating factor (GM-CSF) and CD40-ligand (CD40L) genes. Upon administration, this vaccine may stimulate an anti-tumoral dendritic cell-mediated host immune response. C48391 409696 recombinant human interleukin-21 A recombinant peptide similar to or identical to endogenous human cytokine interleukin-21 (IL-21) with potential antineoplastic activity. Recombinant human IL-21 binds to and activates IL-21 receptors, expressed on T-cells, B-cells, dendritic cells (DC), and natural killer (NK) cells, modulating the proliferation and/or differentiation of T and B cells, promoting T cell survival, and increasing the cytolytic activity of cytotoxic T lymphocytes (CTLs) and NK cells. C62492 409722 autologous EBV-transformed B lymphoblastoid-tumor fusion cell vaccine A cell-based vaccine composed of autologous tumor cells fused with Epstein-Barr virus-transformed B-lymphoblastoid cells. Upon administration, this vaccine may stimulate a cytotoxic T cell response against tumor cells, resulting in tumor cell lysis. C48377 410786 plerixafor A bicyclam with hematopoietic stem cell-mobilizing activity. Plerixafor blocks the binding of stromal cell-derived factor (SDF-1alpha) to the cellular receptor CXCR4, resulting in hematopoietic stem cell (HSC) release from bone marrow and HSC movement into the peripheral circulation. 415313 volociximab A chimeric monoclonal antibody with potential antineoplastic activity. Volociximab binds to and inhibits the activity of alpha(5)beta(1) integrin, thereby inhibiting endothelial cell-cell interactions, endothelial cell-matrix interactions, and angiogenesis. C48426 415541 eculizumab A human monoclonal antibody directed against terminal complement protein C5. Eculizumab binds to terminal complement protein C5, thereby blocking C5 cleavage into pro-inflammatory components and blocking the complement-mediated destruction of paroxysmal nocturnal hemoglobinuria (PNH) red blood cells. 415570 abarelix A synthetic decapeptide and antagonist of naturally occurring gonadotropin-releasing hormone (GnRH). Abarelix directly and competitively binds to and blocks the gonadotropin releasing hormone receptor in the anterior pituitary gland, thereby inhibiting the secretion and release of luteinizing hormone (LH) and follicle stimulating hormone (FSH). In males, the inhibition of LH secretion prevents the release of testosterone. As a result, this may relieve symptoms associated with prostate hypertrophy or prostate cancer, since testosterone is required to sustain prostate growth. 415572 PPI-2458 A synthetic derivative of fumagillin with antineoplastic and cytotoxic properties. PPI-2458 irreversibly inhibits the enzyme methionine aminopeptidase type 2 (MetAP2), thereby preventing abnormal cell growth and angiogenesis. PPI-2458 is reported to have a better toxicity profile compared to other agents of its class. C38129 415732 monoclonal antibody RAV12 A chimeric monoclonal antibody directed against a primate-restricted N-linked carbohydrate epitope (glycotope) expressed on various human carcinomas with potential antineoplastic activity. Following binding, monoclonal antibody RAV12 disrupts sodium channels of tumor cells expressing this glycotope, resulting in cell and organelle swelling, loss of membrane integrity, and cell death. C48409 415963 SJG-136 A pyrrolobenzodiazepine dimer with potential antineoplastic activity. SJG-136 binds to the minor groove of DNA and induces interstrand cross-links between two N-2 guanine positions, thereby inhibiting DNA replication and transcription. With a preference for binding to purine-GATC-pyrimidine sequences, SJG-136 adducts do not appear to be subject to p53-mediated DNA excision repair mechanisms. C29435 419548 vinflunine A bi-fluorinated derivative of the semi-synthetic vinca alkaloid vinorelbine with antitubulin, antineoplastic, and antiangiogenic activities. Vinflunine inhibits tubulin assembly without any stablization of assembled microtubules at concentrations comparable to those of other vinca alkaloids such as vincristine, vinblastine and vinorelbine; this effect on microtubule dynamics results in cell cycle arrest in mitosis and apoptosis. Compared to other vinca alkaloids, this agent binds weakly to the vinca-binding site, indicating that vinflunine may exhibit reduced neurotoxicity. 419685 human gp100 plasmid DNA vaccine A vaccine consisting of a plasmid DNA encoding the human melanoma-associated antigen gp100. Upon adminsistration, expressed gp100 antigen may stimulate a cytotoxic T cell HLA-A2.1-restricted immune response against tumor cells that express this antigen, resulting in tumor cell lysis. C2759 419686 mouse gp100 plasmid DNA vaccine A vaccine consisting of a plasmid DNA encoding the murine melanoma-associated antigen gp100. Upon administration, expressed gp100 antigen may stimulate a cytotoxic T cell HLA-A2.1-restricted immune response against tumor cells that express the gp100 antigen, resulting in tumor cell lysis. C48410 423355 ferumoxtran-10 A synthetic ultrasmall superparamagnetic iron oxide composed of dextran-coated iron oxide nanoparticles (also known as 'ultrasmall particulate iron oxides' or USPIO). Ferumoxtran-10, which accumulates in non-cancerous lymphatic tissue, is used as a molecular resonance imaging (MRI) contrast agent. 424450 pravastatin The sodium salt of pravastatin with cholesterol-lowering and potential antineoplastic activities. Pravastatin competitively inhibits hepatic hydroxymethyl-glutaryl coenzyme A (HMG-CoA) reductase, the enzyme which catalyzes the conversion of HMG-CoA to mevalonate, a key step in cholesterol synthesis. This agent lowers plasma cholesterol and lipoprotein levels, and modulates immune responses by suppressing MHC II (major histocompatibility complex II) on interferon gamma-stimulated, antigen-presenting cells such as human vascular endothelial cells. In addition, pravastatin, like other statins, exhibits pro-apoptotic, growth inhibitory, and pro-differentiation activities in a variety of tumor cells; these antineoplastic activities may be due, in part, to inhibition of the isoprenylation of Ras and Rho GTPases and related signaling cascades. C29375 425344 monoclonal antibody HuAFP31 A humanized monoclonal antibody directed against alpha fetoprotein with potential antineoplastic activity. Upon administration, monoclonal antibody HuAFP31 (mAb HuAFP31) binds to and stimulates a cytotoxic T lymphocyte (CTL) response against tumor cells that express alpha fetoprotein. C48407 425347 yttrium Y 90 DOTA monoclonal antibody HuAFP31 A radioimmunoconjugate comprised of the monoclonal antibody HuAFP31, directed against alpha fetoprotein, that is conjugated to the chelating agent tetra-azacyclododecanetetra-acetic acid (DOTA) and radiolabeled with the beta-emitting radioisotope Yttrium Y90. Yttrium Y 90 DOTA monoclonal antibody HuAFP31 binds to tumor cells expressing alpha fetoprotein, selectively delivering a cytotoxic dose of beta radiation. C48428 425350 yttrium Y 90 DOTA monoclonal antibody HuPAM4 A radioimmunoconjugate comprised of the humanized monoclonal antibody HuPAM4, directed against the pancreatic cancer antigen MUC1, that is conjugated to the chelating agent tetra-azacyclododecanetetra-acetic acid (DOTA) and radiolabeled with the beta-emitting radioisotope Yttrium Y90. Yttrium Y 90 DOTA monoclonal antibody HuPAM4 binds to tumor cells expressing MUC1 antigen, selectively delivering a cytotoxic dose of beta radiation. C48429 425351 monoclonal antibody HuPAM4 A humanized monoclonal antibody directed against the pancreatic cancer antigen MUC1 with potential antineoplastic activity. Monoclonal antibody HuPAM4 (mAb HuPAM4) binds to cells expressing MUC1 antigen; mAb HuPAM4 may be useful as a carrier for radioisotopes and other antineoplastic therapeutic agents. C48408 425596 cediranib maleate The maleate salt of an indole ether quinazoline derivative with antineoplastic activities. Competing with adenosine triphosphate, cediranib binds to and inhibits all three vascular endothelial growth factor receptor (VEGF-1,-2,-3) tyrosine kinases, thereby blocking VEGF-signaling, angiogenesis, and tumor cell growth. C48379 427285 autologous dendritic cell-allogeneic melanoma tumor cell lysate vaccine A cell-based vaccine composed of autologous dendritic cells (DCs) pulsed with lysates from heat-treated allogeneic melanoma tumor cells. Upon administration, this vaccine may stimulate anti-tumoral cytotoxic T-cell and antibody responses to melanoma cells bearing shared melanoma antigens such as MelanA/MART-1, gp100, MAGE3, resulting in tumor cell lysis. 427615 fluorine F 18 EF5 A radioconjugate consisting of EF5, a fluorinated derivative of etanidazole, conjugated to fluorine F 18, a positron emitting isotope. EF5 binds to hypoxic tissue; conjugation to Fluorine F 18 allows imaging of hypoxic regions within tumors. C48389 428188 MET/VEGFR2 inhibitor GSK1363089 An orally bioavailable small molecule with potential antineoplastic activity. MET/VEGFR2 inhibitor GSK1363089 binds to and selectively inhibits hepatocyte growth factor (HGF) receptor c-MET and vascular endothelial growth factor receptor 2 (VEGFR2), which may result in the inhibition of tumor angiogenesis, tumor cell proliferation and metastasis. The proto-oncogene c-MET has been found to be over-expressed in a variety of cancers. VEGFR2 is found on endothelial and hematopoietic cells and mediates the development of the vasculature and hematopoietic cells through VEGF signaling. C80058 428314 recombinant vaccinia-NY-ESO-1 vaccine A cancer vaccine consisting of a recombinant vaccinia viral vector encoding an immunogenic peptide derived from the cancer-testis antigen NY-ESO-1, an antigen found in normal testis and various tumors, including bladder, breast, hepatocellular, melanoma, and prostate cancers. Vaccination with recombinant vaccinia- NY-ESO-1 peptide vaccine may stimulate the host immune system to mount a humoral and cytotoxic T lymphocyte (CTL) response against tumor cells expressing NY-ESO-1 antigen, resulting in tumor cell lysis. C48419 428315 fowlpox-NY-ESO-1 vaccine A cancer vaccine consisting of a recombinant fowlpox virus vector encoding an immunogenic peptide derived from the cancer-testis antigen NY-ESO-1, an antigen found in normal testis and various tumors, including bladder, breast, hepatocellular, melanoma, and prostate cancers. Vaccination with NY-ESO-1 peptide vaccine may stimulate the host immune system to mount a humoral and cytotoxic T lymphocyte (CTL) response against tumor cells expressing NY-ESO-1 antigen, resulting in tumor cell lysis. C48465 428486 veltuzumab A fully humanized monoclonal antibody directed against the CD20 antigen with potential antineoplastic activity. Following binding, veltuzumab triggers complement-dependent cell lysis (CDCL) and antibody-dependent cell-mediated cytotoxicity (ADCC) in cells that overexpress CD20. CD20 antigen is a hydrophobic transmembrane protein located on pre-B and mature B lymphocytes. C48406 428488 opioid growth factor An endogenous pentapeptide with potential antineoplastic and antiangiogenic activities. Opioid growth factor (OGF) binds to and activates the opioid growth factor receptor (OGFr), present on some tumor cells and vascular cells, thereby inhibiting tumor cell proliferation and angiogenesis. C48413 428586 iodine I 124 iododeoxyuridine A radiopharmaceutical comprised of the thymidine analog, 5-iodo-2-deoxyuridine (idoxuridine), labeled with the positron emitter iodine I 124. After incorporation into tumor cell DNA, positron emission tomography (PET) is used to image iodine I 124 localized to tumor cells for determining and monitoring tumor burden. C48399 430384 PSA:154-163(155L) peptide vaccine A cancer vaccine comprised of a synthetic peptide with an amino acid sequence corresponding to positions 154-163 of the amino acid sequence for prostate-specific antigen (PSA) with a leucine substitution at position 155. Upon administration, PSA:154-163(155L) peptide vaccine may elicit a cytotoxic T-cell response against tumor cells that express PSA. C29338 432936 lucatumumab A monoclonal antibody directed against the B-cell surface antigen CD40 with potential antineoplastic activity. Lucatumumab binds to and inhibits CD40, thereby inhibiting CD40 ligand-induced cell proliferation and triggering cell lysis via antibody-dependent cellular cytotoxicity (ADCC) in cells overexpressing CD40. CD40, an integral membrane protein found on the surface of B lymphocytes, is a member of the tumor necrosis factor receptor superfamily and is highly expressed in a number of B-cell malignancies. C48405 432941 ingenol 3-angelate A selective small-molecule activator of protein kinase C (PKC) isolated from the plant Euphorbia peplus with potential antineoplastic activity. Ingenol 3-angelate (I3A) activates various protein kinase C (PKC) isoforms, thereby inducing apoptosis in some tumor cells, including myeloid leukemia cells, melanoma cells, and basal cell carcinoma cells. The PKC family consists of signaling isoenzymes that regulate many cell processes including proliferation, differentiation, and apoptosis. 432958 TTI-237 A small synthetic molecule of triazolopyrimidine derivative with potential antitumor activity. With a novel mechanism of action distinct from the action of other vinca alkaloid compounds, TTI-237 specifically binds to tubulin at the vinca site, and promotes the polymerization of tubulin into microtubules. TTI-237 stabilizes tubulin and inhibits microtubule disassembly. This results in cell cycle arrest at the G2/M phase, and leading to cell death. 433196 HLA-A1, A2, B35-restricted survivin peptides/Montanide ISA-51 vaccine A peptide vaccine comprised of synthetic HLA-A1, -A2 and -B35 restricted survivin epitopes combined with the adjuvant Montanide ISA-51 with potential antineoplastic activity. Upon administration, HLA-A1, A2, B35-restricted survivin peptides/Montanide ISA-51 vaccine may stimulate a cytotoxic T cell response against tumor cells that overexpress survivin, resulting in tumor cell lysis. Montanide ISA-51, also known as incomplete Freund's adjuvant or IFA, is a stabilized water-in-oil emulsion adjuvant containing mineral oil with mannide oleate added as a surfactant that non-specifically stimulates cell-mediated immune responses to antigens. C48393 433272 Bowman-Birk inhibitor concentrate An extract of soybeans enriched in Bowman-Birk inhibitor (BBI), a soybean-derived, 71-amino acid, polypeptide and serine protease inhibitor with potential chemopreventive activity. Bowman-Birk inhibitor contains distinct inhibitory sites for trypsin and chymotrypsin. Although the exact mechanism by which BBI suppresses carcinogenesis is unknown, its antiproliferative activity appears to be linked to the chymotrypsin inhibitory region. C48381 434424 synthetic peptide-based erythropoiesis stimulating agent A synthetic, non-recombinant, pegylated, peptidic erythropoiesis stimulating agent. Synthetic peptide-based erythropoiesis stimulating agent binds to and activates the erythropoietin (EPO) receptor on erythroid progenitor cells, thereby inducing their proliferation and differentiation into mature erythrocytes. C48422 434427 paclitaxel-loaded polymeric micelle A biodegradable poly(ethylene glycol)-poly(D,L-lactide) copolymer miceller nanoparticle-entrapped formulation of paclitaxel with antineoplastic activity. Paclitaxel promotes microtubule assembly and prevents depolymerization, thus interfering with normal mitosis. The copolymer residue increases the water-solubility of paclitaxel and allows delivery of higher doses than those achievable with paclitaxel alone. C48415 434519 oncolytic adenovirus encoding GM-CSF A recombinant oncolytic adenovirus encoding the immunohematopoietic cytokine granulocyte-macrophage colony stimulating factor (GM-CSF) with potential antineoplastic activity. Upon administration, the oncolytic adenovirus selectively infects and replicates in tumor cells, which may result in tumor cells lysis. Synergistically, GM-CSF (sargramostim) expressed by the oncolytic adenovirus may promote a cytotoxic T cell response against tumor cells harboring the oncolytic adenovirus, resulting in an immune-mediated tumor cell death. C48412 434520 nesiritide A recombinant version of the cardiac neurohormone, human B-type natriuretic peptide (hBNP) produced by the ventricular myocardium. Nesiritide binds to natriuretic peptide receptors on vascular smooth muscle and endothelial cells, through which it triggers guanylate cyclase dependent signal transduction resulting in increase of intracellular concentrations of cGMP. This leads to smooth muscle cell relaxation causing arterial and venous dilatation. 435986 deferasirox A synthetic, orally bioavailable, achiral, tridentate triazole derived from salicylic acid with iron-chelating activity. Deferasirox chelates iron at a 2:1 (ligand:iron) ratio. Because of its oral availablity,and long plasma half-life, this agent may be superior to desferrioxamine (desferal, DFO), which is orally inactive and has a short plasma half-life. C48384 435988 nilotinib An orally bioavailable aminopyrimidine-derivative Bcr-Abl tyrosine kinase inhibitor with antineoplastic activity. Designed to overcome imatinib resistance, nilotinib binds to and stabilizes the inactive conformation of the kinase domain of the Abl protein of the Bcr-Abl fusion protein, resulting in the inhibition of the Bcr-Abl-mediated proliferation of Philadelphia chromosome-positive (Ph+) chronic myeloid leukemia (CML) cells. This agent also inhibits the receptor tyrosine kinases platelet-derived growth factor receptor (PDGF-R) and c-kit, a receptor tyrosine kinase mutated and constitutively activated in most gastrointestinal stromal tumors (GISTs). With a binding mode that is energetically more favorable than that of imatinib, nilotinib has been shown to have an approximately 20-fold increased potency in kinase and proliferation assays compared to imatinib. 436110 tetanus toxoid helper peptide Obtained by genetic engineering from the bacterial Clostridium tetani toxoid, tetanus toxoid helper peptide QYIKANSKFIGITEL (amino acids 830-844) binds to class II MHC molecules as a nonspecific vaccine helper epitope (adjuvant) and induces an increased (and long term) immune response by increasing the helper T-cell response. C38134 436982 velafermin A recombinant human fibroblast growth factor-20 (rhFGF-20) protein with pro-proliferative activity. Velafermin stimulates DNA synthesis and cell proliferation, specifically promoting epithelial and mesenchymal cell proliferation, and may prevent radiation or chemotherapy-induced oral mucositis. C48425 437784 retaspimycin hydrochloride The hydrochloride salt of a small-molecule inhibitor of heat shock protein 90 (HSP90) with antiproliferative and antineoplastic activities. Retaspimycin binds to and inhibits the cytosolic chaperone functions of HSP90, which maintains the stability and functional shape of many oncogenic signaling proteins and may be overexpressed or overactive in tumor cells. Retaspimycin-mediated inhibition of HSP90 promotes the proteasomal degradation of oncogenic signaling proteins in susceptible tumor cell populations, which may result in the induction of apoptosis. C48401 437863 methylnaltrexone A methyl derivative of noroxymorphone with selective, opioid-receptor antagonistic activity. Methylnaltrexone displaces opioids from peripheral opioid receptors in the gastrointestinal tract, the bladder, and the skin, resulting in decreases in opioid-related constipation, urinary retention, and pruritis, respectively. Methylnaltrexone does not cross the blood-brain barrier and does not affect the centrally-mediated analgesic effect of opioids. 438803 TPI 287 A synthetic, third generation taxane with potential antineoplastic activity. TPI 287 binds to tubulin and stabilizes microtubules, resulting in inhibition of microtubule assembly/disassembly dynamics, cell cycle arrest at the G2/M phase, and apoptosis. C48424 440023 piperine extract (standardized) A standardized extract containing the active alkaloid piperine, derived from the fruit of the plant Piper nigrum (black pepper) and/or the plant Piper longum L. (long pepper), with thermogenic properties. Co-ingestion of piperidine enhances the bioavailability of various nutrients, including beta-carotene, curcumin, selenium, pyridoxine and coenzyme Q10. In addition, this agent may exert anti-inflammatory and anti-tumor activities and may enhance the production of serotonin. C48417 440127 pNGVL4a-Sig/E7(detox)/HSP70 DNA vaccine An antigen-specific DNA cancer vaccine consisting of the coding sequences of a signal peptide (pNGVL4a-Sig), a detox form of the human papillomavirus type 16 (HPV-16) antigen E7, and the heat shock protein 70 (HSP70). Upon administration, this vaccine may generate potent cytotoxic CD8(+) T-cell responses against E7-expressing tumor cells, resulting in tumor cell death. C48418 440314 131I-TM-601 An iodine 131 (I 131) radioconjugate of the synthetic chlorotoxin (CTX) TM-601 with potential antiangiogenic and antineoplastic activities. CTX is a 36 amino acid neurotoxin found in the venom of the giant yellow scorpion Leiurus quinquestriatus that preferentially binds malignant cells of neuroectodermal origin. The recombinant version of this peptide, TM-601, is expressed in and purified from E. coli and then covalently linked to I 131 to produce 131I-TM-601. 131I-TM-601 binds to tumor cells of neuroectodermal origin and is internalized; administered once, it may be used as a radioimaging agent; repeated administration may result in a tumor-specific, cumulative radiocytotoxic dose of I 131. In addition, TM-601 alone, similar to native CTX, may inhibit angiogenesis due to its ability to bind to and inhibit matrix metalloproteinase 2 (MMP-2), an endopeptidase involved in tissue remodeling processes such as angiogenesis. C78857 440740 alpha-lipoic acid A naturally occurring micronutrient, synthesized in small amounts by plants and animals (including humans), with antioxidant and potential chemopreventive activities. Alpha-lipoic acid acts as a free radical scavenger and assists in repairing oxidative damage and regenerates endogenous antioxidants, including vitamins C and E and glutathione. This agent also promotes glutathione synthesis. In addition, alpha-lipoic acid exerts metal chelating capacities and functions as a cofactor in various mitochondrial enzyme complexes involved in the decarboxylation of alpha-keto acids. C61595 440966 racemic XK469 The racemic form of a synthetic quinoxaline phenoxypropionic acid derivative with antineoplastic properties. XK469R selectively inhibits topoisomerase II by stabilizing the enzyme-DNA intermediates in which topoisomerase subunits are covalently linked to DNA through 5-phosphotyrosyl linkages, thereby interfering with DNA repair and replication, RNA and protein synthesis. This agent possesses unusual solid tumor selectivity and activity against multidrug-resistant cancer cells. XK469R is more water soluble and active than the pure isomers, R(+)XK469 and S(-)XK469. C2825 441235 degarelix A long-acting, synthetic peptide with gonadotrophin-releasing hormone (GnRH) antagonistic properties. Degarelix targets and blocks GnRH receptors located on the surfaces of gonadotroph cells in the anterior pituitary, thereby reducing secretion of luteinizing hormone (LH) by pituitary gonadotroph cells and so decreasing testosterone production by interstitial (Leydig) cells in the testes. 441241 adenovector encoding MDA7 A nonreplicating adenoviral vector (adenovector) encoding the melanoma differentiation-associated 7 gene (MDA7) with potential antineoplastic activity. After intratumoral injection and adenovector-mediated gene transfer of MDA7 into tumor cells, the expressed MDA7 transgene may inhibit tumor cell proliferation and induce tumor cell apoptosis. C48368 441243 picoplatin A new generation organic platinum analog with an extended spectrum of antineoplastic activity. Designed to overcome platinum drug resistance, picoplatin alkylates DNA, forming both inter- and intra-strand cross-linkages, resulting in inhibition of DNA replication and transcription, and the induction of apoptosis. C48416 442110 hepatitis A vaccine An inactivated virus vaccine that provides active immunization against hepatitis A virus (HAV). Immunization with hepatitis A vaccine induces the formation of anti-HAV antibodies which provide protection against hepatitis A infection. C29090 442270 human papillomavirus 16/18 L1 virus-like particle/AS04 vaccine A recombinant, bivalent, human papillomavirus (HPV) vaccine, containing virus-like particles for HPV types 16 and 18 linked to the adjuvant ASO4, with potential immunoprotective and antineoplastic properties. Upon administration, HPV 16/18 L1 virus-like particle/ASO4 vaccine may generate humoral and cellular immunity against HPV types-16 and -18 antigens, thereby preventing cervical infection upon exposure to HPV types 16 and 18. In addition, this agent may stimulate an antitumoral cellular immune response against cervical cancer associated with HPV infection. C48395 442901 HER-2-neu, CEA peptides, GM-CSF, Montanide ISA-51 vaccine A vaccine comprised of HER-2-neu and carcinoembryonic antigen synthetic (CEA) peptides, combined with the adjuvants granulocyte-macrophage colony stimulating factor (GM-CSF), and Montanide ISA-51 with potential antineoplastic activity. HER-2-neu, CEA peptides, GM-CSF, Montanide ISA-51 vaccine may stimulate a cytotoxic T-cell response against HER-2-neu- and CEA-expressing tumor cells. The GM-CSF adjuvant stimulates the proliferation of monocytes and monocyte differentiation into macrophages and dendritic cells, immunohematopoietic elements with important antitumoral functions. Montanide ISA-51, also known as incomplete Freund's adjuvant or IFA, is a stabilized water-in-oil emulsion adjuvant containing mineral oil with mannide oleate added as a surfactant that non-specifically stimulates cell-mediated immune responses to antigens. C48392 443682 amrubicin hydrochloride The hydrochloride salt of a third-generation synthetic 9-amino-anthracycline with antineoplastic activity. Amrubicin intercalates into DNA and inhibits the activity of topoisomerase II, resulting in inhibition of DNA replication, and RNA and protein synthesis, followed by cell growth inhibition and cell death. This agent has demonstrated a higher level of anti-tumor activity than conventional anthracycline drugs without exhibiting any indication of the cumulative cardiac toxicity common to this class of compounds. C47948 445421 Hodgkin's antigens-GM-CSF-expressing cell vaccine An allogeneic vaccine consisting of Hodgkin lymphoma cells transfected with the granulocyte macrophage-colony-stimulating factor (GM-CSF) gene with potential antineoplastic activity. Upon vaccination, Hodgkin antigens-GM-CSF-expressing cell vaccine may stimulate a cytotoxic T-lymphocyte (CTL) immune response against Hodgkin lymphoma-associated antigens, which may result in the lysis of tumor cells expressing these antigens. In addition, transfected Hodgkin lymphopma cells secrete GM-CSF, which may potentiate the CTL response against Hodgkin lymphoma-associated antigens. C61592 445461 E7080 A synthetic, orally available inhibitor of vascular endothelial growth factor receptor 2 (VEGFR2, also known as KDR/FLK-1) tyrosine kinase with potential antineoplastic activity. E7080 blocks VEGFR2 activation by VEGF, resulting in inhibition of the VEGF receptor signal transduction pathway, decreased vascular endothelial cell migration and proliferation, and vascular endothelial cell apoptosis. C48636 445462 851B gel A topical gel containing a peptide derived from the human papillomavirus (HPV). Application of 851B gel may stimulate the host immune system to trigger a cytotoxic T-lymphocyte response to cells that express HPV. C48637 445463 recombinant vaccinia-multiepitope melanoma peptides-B7.1-B7.2 vaccine A cancer vaccine consisting of an inactivated recombinant vaccinia virus encoding epitope peptides derived from melanoma-related HLA-A2-restricted tumor-associated antigens (TAAs), including Melan-A(27-35), gp100(280-288) and tyrosinase(1-9), and two co-stimulatory B7 proteins, B7.1 (CD80) and B7.2 (CD86). Upon administration, recombinant vaccinia-multiepitope melanoma peptides-B7.1-B7.2 vaccine may stimulate a cytotoxic T-lymphocyte response against melanoma cells that express TAAs which share epitopes with the epitope peptides expressed by the vaccine viral vector, resulting in tumor cell lysis; vaccine viral vector-expressed co-stimulatory proteins B7.1 and B7.2 may enhance the cytotoxic T-lymphocyte immune response to the TAAs. C48638 445465 synthetic melanoma-associated antigens vaccine A cancer vaccine containing synthetic epitope peptides derived from melanoma tumor-associated antigens (TAAs), including melanoma-melanocyte antigen gp100(280-288), melanoma-associated antigen tyrosinase(1-9), and melanoma-associated antigen melan-A(27-35). Upon administration, synthetic melanoma-associated antigens vaccine may stimulate a cytotoxic T-lymphocyte immune response against melanoma cells that express TAAs which share epitopes with the vaccine epitope peptides, resulting in tumor cell lysis. C48639 446541 MK0752 A synthetic small molecule with potential antineoplastic activity. MK0752 inhibits the Notch signaling pathway, which may result in induction of growth arrest and apoptosis in tumor cells in which the Notch signaling pathway is overactivated. The Notch signaling pathway plays an important role in cell-fate determination, cell survival, and cell proliferation. C49175 446551 MK0731 A synthetic small molecule with potential antineoplastic activity. MK0731 selectively inhibits kinesin spindle protein (KSP), which may result in the inhibition of mitotic spindle assembly, induction of cell cycle arrest during the mitotic phase, and apoptosis in tumor cells that overexpress KSP. C49174 446576 ethanol A colorless organic liquid also known as ethyl alcohol or grain alcohol. Ethanol's primary physiologic effects involve the central nervous system. Depending on the dose delivered, ethanol behaves as an anxiolytic, a depressant, or a general anesthetic. Ethanol-induced immunosuppression involves dysregulation of CD4+ T cells. 446577 retrovector encoding mutant anti-cyclin G1 A replication-incompetent, pathotropic, tumor matrix (collagen)-targeted, retroviral vector encoding an N-terminal deletion mutant form of the cyclin G1 gene with potential antineoplastic activity. Under the control of a hybrid long-terminal repeat/cytomegalovirus (CMV) promoter, retrovector encoding mutant anti-cyclin G expresses the mutant cyclin G1 construct, resulting in disruption of tumor cell cyclin G1 activity and decreased cellular proliferation and angiogenesis. This agent preferentially targets collagen of the tumor matrix because of the incorporation of the collagen-binding domain of von Willebrand factor (vWF) on the retrovector surface. Exploiting the collagen-targeting mechanism of vWF permits delivery of the retrovector to tumor sites where angiogenesis and collagen matrix exposure occur. C49082 447049 hemiasterlin analog E7974 An analog of the sponge-derived anti-microtubule tripeptide hemiasterlin with antimitotic and potential antineoplastic activities. Hemiasterlin analog E7974 binds to the Vinca domain on tubulin, resulting in inhibition of tubulin polymerization and microtubule assembly; depolymerization of exsiting microtubules; inhibition of mitosis; and inhibition of cellular proliferation. This agent may have more affinity for the beta-3 tubulin isotype. C49083 447136 imetelstat sodium The sodium salt of imetelstat, a synthetic lipid-conjugated, 13-mer oligonucleotide N3' P5'-thio-phosphoramidate with potential antineoplastic activity. Complementary to the template region of telomerase RNA (hTR), imetelstat acts as a competitive enzyme inhibitor that binds and blocks the active site of the enzyme (a "telomerase template antagonist"), a mechanism of action which differs from that for the antisense oligonucleotide-mediated inhibition of telomerase activity through telomerase mRNA binding. Inhibition of telomerase activity in tumor cells by imetelstat results in telomere shortening, which leads to cell cycle arrest or apoptosis. C49084 448620 tremelimumab A human IgG2 monoclonal antibody directed against the T-cell receptor protein cytotoxic T-lymphocyte-associated protein 4 (CTLA4). Tremelimumab binds to CTLA4 and blocks the binding of the antigen-presenting cell ligands B7-1 and B7-2 to CTLA4, resulting in inhibition of B7-CTLA4-mediated downregulation of T-cell activation; subsequently, B7-1 or B7-2 may interact with another T-cell surface receptor protein, CD28, resulting in a B7-CD28-mediated T-cell activation unopposed by B7-CTLA4-mediated inhibition. C49085 449664 olanzapine A synthetic derivative of thienobenzodiazepine with antipsychotic, antinausea, and antiemetic activities. As a selective monoaminergic antagonist, olanzapine binds with high affinity binding to the following receptors: serotoninergic, dopaminergic, muscarinic M1-5, histamine H1, and alpha-1-adrenergic receptors; it binds weakly to gamma-aminobutyric acid type A, benzodiazepine, and beta-adrenergic receptors. The antinausea and antiemetic effects of this agent appear to be due to the blockade of 5-HT2 and 5-HT3 receptors for serotonin. Although its exact mechanism of action in schizophrenia is unknown, it has been proposed that olanzapine's antipsychotic activity is mediated through antagonism to dopamine D2 receptors with rapid ligand-receptor dissociation kinetics that help to minimize extrapyramidal symptoms (EPS). Olanzapine may also stimulate appetite. C47639 449683 recombinant modified vaccinia Ankara-5T4 vaccine A cancer vaccine comprised of a recombinant modified vaccinia Ankara (MVA) viral vector encoding the 5T4 fetal oncoprotein (MVA-h5T4). Vaccination with recombinant modified vaccinia Ankara-5T4 vaccine may stimulate the host immune system to mount a humoral and cytotoxic T lymphocyte (CTL) response against tumor cells expressing 5T4 fetal oncoprotein antigen, resulting in tumor cell lysis. The MVA viral vector, derived from the replication-competent strain Ankara, is a highly attentuated, replication-defective vaccinia strain incapable of virion assembly. C49087 450954 chimeric anti-phosphotidylserine monoclonal antibody An IgG3 monoclonal antibody directed against anionic phospholipids with potential antineoplastic activity. Chimeric anti-phosphotidylserine monoclonal antibody binds to anionic phospholipids in a beta 2-glycoprotein I-dependent manner, inhibiting tumor growth by stimulating antibody-dependent cellular cytotoxicity (ADCC) to tumor vessels. C49088 452040 Boswellia serrata extract A standardized extract derived from the plant Boswellia serrata of the family Burseraceae with anti-inflammatory activity. Boswellia serrata extract contains terpenoid boswellic acids, which are potent inhibitors of 5-lipoxygenase activity and, so, leukotriene synthesis. C49089 452041 ketamine hydrochloride The hydrochloride salt of a synthetic derivative of cyclohexanone with analgesic and anesthetic activities. Although its mechanism of action is not well understood, ketamine appears to non-competitively block N-methyl-D-aspartate (NMDA) receptors and may interact with opiod mu receptors and sigma receptors, thereby reducing pain perception, inducing sedation, and producing dissociative anesthesia. C29142 452042 XL820 An orally bioavailable, small molecule receptor tyrosine kinase inhibitor with potential antineoplastic activity. XL820 binds to and inhibits the receptor tyrosine kinases for vascular endothelial drowth factor (VEGF), c-kit, and platelet-derived growth factor (PDGF). In tumor models of breast carcinomas, gliomas, and leukemia, this agent exhibits dose-dependent growth inhibition and has been shown to cause tumor regression. C49090 452943 BI 2536 A small molecule compound with potential antineoplastic activities. BI 2536 binds to and inhibits Polo-like kinase 1 (Plk1), resulting in mitotic arrest, disruption of cytokinesis, and apoptosis in susceptible tumor cell populations. Plk1, a serine/threonine-protein kinase, is a key regulator of multiple processes fundamental to mitosis and cell division. C49091 453546 AVR118 A peptide-nucleic acid immunomodulator with proinflammatory, broad-spectrum antiviral, and potential antineoplastic activities. AVR118 stimulates the peripheral blood mononuclear cell (PBMC) production of the proinflammatory cytokines IFN-y, IL-1b, IL-6 and TNF-a. This agent may reduce HIV-1 p24 antigen; viral reverse transcriptase activity; syncitial cell formation; and viral mRNA in infected PBMCs and human CD4+ lymphocyte H9 cells, and may decrease viral loads and increase CD4+ and CD8+ T-cell counts in HIV patients. In vitro, AVR118 has been shown to induce the maturation of HL60 leukemic cells and to inhibit the invasive and metastatic properties of a highly malignant breast cancer cell line. 453547 3'-deoxy-3'-[18F]fluorothymidine A radioconjugate consisting of a thymidine analogue radiolabeled with fluorine F 18, a positron emitting isotope. Phosphorylated by S-phase-specific thymidine kinase 1, 3'-deoxy-3'-[18F]fluorothymidine (18F-FLT) is trapped intracellularly by entering the salvage pathway of DNA synthesis without incorporation into DNA. 18F-FLT serves a marker of tumor cell proliferation for imaging with positron emission tomography (PET); as a marker of proliferation rather than metabolism, it is more specific to tumor tissue than 2-deoxy-2-[18F] fluoro-D-glucose (18F-FDG). This agent is metabolically stable, accumulates in the normal bone marrow and the liver, and does not cross the blood-brain barrier. C49093 453548 neratinib An orally available, 6,7-disubstituted-4-anilinoquinoline-3-carbonitrile irreversible inhibitor of the HER-2 receptor tyrosine kinase with potential antineoplastic activity. Neratinib binds to the HER-2 receptor irreversibly, thereby reducing autophosphorylation in cells, apparently by targeting a cysteine residue in the ATP-binding pocket of the receptor. Treatment of cells with this agent results in inhibition of downstream signal transduction events and cell cycle regulatory pathways; arrest at the G1-S (Gap 1/DNA synthesis)-phase transition of the cell division cycle; and ultimately decreased cellular proliferation. Neratinib also inhibits the epidermal growth factor receptor (EGFR) kinase and the proliferation of EGFR-dependent cells. C49094 453549 tranexamic acid A synthetic derivative of the amino acid lysine with antifibrinolytic activity. With strong affinity for the five lysine-binding sites of plasminogen, transexamic acid competitively inhibits the activation of plasminogen to plasmin, resulting in inhibition of fibrinolysis; at higher concentrations, this agent noncompetitively inhibits plasmin. This agent has a longer half-life, is approximately ten times more potent, and is less toxic than aminocaproic acid, which possesses similar mechanisms of action. C47765 453550 CC-401 A second generation ATP-competitive anthrapyrazolone c-Jun N terminal kinase (JNK) inhibitor with potential antineoplastic activity. Based on the chemistry of SP600125, another anthrapyrazolone inhibitor of JNK, CC-401 competitively binds the ATP binding site of JNK, resulting in inhibition of the phosphorylation of the N-terminal activation domain of transcription factor c-Jun; decreased transcription activity of c-Jun; and a variety of cellular effects including decreased cellular proliferation. C49095 453551 alvimopan A synthetic trans-3,4-dimethyl-4-(3-hydroxyphenyl) piperidine with peripherally selective opioid mu receptor antagonist activity. Alvimopan is a selective and competitive antagonist at mu-opioid receptors, found in myenteric and submucosal neurons and\nthe immune cells of the lamina propria in the human gut. Upon administration, this agent binds to mu-opioid receptors in the gut, thereby reversing opiod-related disturbances in gut motility. Alvimopan is approximately three to nine times more potent than naloxone. 453584 AFP464 A synthetic lysyl prodrug of the amino-substituted flavone derivate aminoflavone with antiproliferative and antineoplastic activities. AFP464 is rapidly converted to aminoflavone in plasma. Aminoflavone activates the aryl hydrocarbon receptor (AhR) signaling pathway leading to an increase in cytochrome P450 1A1 (CYP1A1) and cytochrome P450 1A2 (CYP1A2) expression and, to a lesser extent, an increase in cytochrome P450 1B1 (CYP1B1) expression. Subsequently, aminoflavone is metabolized to toxic metabolites by the cytochromome P450 enzymes that it induces; these toxic metabolites covalently bind to DNA, resulting in the phosphorylation of p53, the induction of the p53 downstream target p21Waf1/Cip1, and apoptosis. Pulmonary toxicity may be dose-limiting. C48370 453588 AZD0530 An orally available 5-, 7-substituted anilinoquinazoline with anti-invasive and anti-tumor activities. AZD0530 is a dual-specific inhibitor of Src and Abl, protein tyrosine kinases that are overexpressed in chronic myeloid leukemia cells. This agent binds to and inhibits these tyrosine kinases and their effects on cell motility, cell migration, adhesion, invasion, proliferation, differentiation, and survival. Specifically, AZD0530 inhibits Src kinase-mediated osteoclast bone resorption. C48378 453589 bardoxolone A synthetic triterpenoid compound with potential antineoplastic and anti-inflammatory activities. Bardoxolone blocks the synthesis of inducible nitric oxide synthase (iNOS) and inducible cyclooxygenase (COX-2), two enzymes involved in inflammation and carcinogenesis. This agent also inhibits the interleukin-1 (IL-1)-induced expression of the pro-inflammatory proteins matrix metalloproteinase-1 (MMP-1) and matrix metalloproteinase-13 (MMP-13) and the expression of Bcl-3; Bcl-3 is an IL-1-responsive gene that preferentially contributes to MMP-1 gene expression. C48382 453590 iodine I 131 monoclonal antibody CC49-deltaCH2 A radioimmunoconjugate consisting of the humanized CH2 domain-deleted monoclonal antibody CC49 and iodine I 131 with antineoplastic activity. Monoclonal antibody CC49-deltaCH2 targets the tumor-associated glycoprotein 72 (TAG-72) that is expressed by a wide range of human neoplasms including colorectal, gastric, pancreatic, ovarian, endometrial, breast, non-small cell lung, and prostate cancers. Iodine I 131 monoclonal antibody CC49-deltaCH2 binds to tumor cells expressing TAG-72, selectively delivering a cytotoxic dose of beta and gamma radiation. 454314 11C topotecan A semisynthetic derivative of camptothecin, a cytotoxic, quinoline-based alkaloid extracted from the Asian tree Camptotheca acuminata radiolabeled with carbon 11 (11C) with antineoplastic and radiotracer properties. During the S phase of the cell cycle, topotecan inhibits topoisomerase I activity by stabilizing the cleavable complex between topoisomerase I and DNA, resulting in DNA breaks that inhibit DNA replication and trigger apoptotic cell death. Quantitation of 11C topotecan accumulated in tumor tissues by positron emission tomography (PET) may help predict responses to topotecan therapy. C49172 454517 aprepitant A small molecule, high-affinity substance P antagonist (SPA) with antiemetic activity. Crossing the blood brain barrier, aprepitant binds selectively to the human substance P/neurokinin 1 receptor in the central nervous system (CNS), thereby inhibiting receptor binding of endogenous substance P and substance P-induced emesis. This agent has little or no affinity for serotonin type 3 (5-HT3), dopamine, and corticosteroid receptors. C49173 454583 belinostat A novel hydroxamic acid-type histone deacetylase (HDAC) inhibitor with antineoplastic activity. Belinostat targets HDAC enzymes, thereby inhibiting tumor cell proliferation, inducing apoptosis, promoting cellular differentiation, and inhibiting angiogenesis. This agent may sensitize drug-resistant tumor cells to other antineoplastic agents, possibly through a mechanism involving the down-regulation of thymidylate synthase. C48812 454586 PD-0332991 An orally available pyridopyrimidine-derived cyclin-dependent kinase (CDK) inhibitor with potential antineoplastic activity. PD-0332991 selectively inhibits cyclin-dependent kinases (particularly Cdk4/cyclin D1 kinase), which may inhibit retinoblastoma (Rb) protein phosphorylation; inhibition of Rb phosphorylation prevents Rb-positive tumor cells from entering the S phase of the cell cycle (arrest in the G1 phase), resulting in suppression of DNA replication and decreased tumor cell proliferation. C49176 454589 recombinant dHER2 vaccine A cancer vaccine consisting of a truncated recombinant HER2 peptide (dHER2) with potential antineoplastic activity. Upon administration, recombinant dHER2 vaccine may stimulate the host immune response to mount a cytotoxic T-lymphocyte response against tumor cells that overexpress the HER2 protein, resulting in tumor cell lysis. The HER2 protein is a tumor-associated antigen (TAA) that is overexpressed in a variety of cancers. dHER2 includes the extracellular domain (ECD) and a part of the intracellular domain (ICD) of the HER2 protein. C49177 454593 EGEN-001 A novel non-viral vector consisting of a plasmid DNA encoding the human gene for interleukin 12 (IL-12) and a biocompatible, biodegradable delivery polymer with potential antineoplastic activity. EGEN-001 is designed to increase the local concentration of IL-12 in the tumor microenvironment. IL-12 stimulates T-cell-independent production of IFN-gamma by peripheral blood mononuclear cells (PBMCs); enhances natural killer (NK) cell lytic activity; acts as a growth factor for T- and NK-cells; and is important for T-cell differentiation. IL-12 may potentiate antitumoral functions of the host immune system, resulting in immune-mediated tumor regression. C49178 455226 simvastatin A lipid-lowering agent derived synthetically from a fermentation product of the fungus Aspergillus terreus. Hydrolyzed in vivo to an active metabolite, simvastatin competitively inhibits hepatic hydroxymethyl-glutaryl coenzyme A (HMG-CoA) reductase, the enzyme which catalyzes the conversion of HMG-CoA to mevalonate, a key step in cholesterol synthesis. This agent lowers plasma cholesterol and lipoprotein levels, and modulates immune responses by suppressing MHC II (major histocompatibility complex II) on interferon gamma-stimulated, antigen-presenting cells such as human vascular endothelial cells. C29454 455227 cefpodoxime proxetil A third generation semi-synthetic cephalosporin and a beta-lactam antibiotic with bactericidal activity. Cefpodoxime's effect is dependent on its binding to penicillin-binding proteins (PBPs) located in the bacterial cytoplasmic membrane. Binding results in the inhibition of the transpeptidase enzymes, thereby preventing cross-linking of the pentaglycine bridge with the fourth residue of the pentapeptide and interrupting consequent synthesis of peptidoglycan chains. As a result, cefpodoxime inhibits bacterial septum and cell wall synthesis formation. C28916 455271 broccoli sprout extract A cruciferous vegetable extract with potential chemopreventive activities. Broccoli sprout extract contains a high amount of sulforaphane, a naturally occurring isothiocyanate. Sulforaphane activates the transcription factor NF-E2-related factor 2 (Nrf2), a member of the basic leucine zipper family, which binds to and activates antioxidant-response elements (AREs). Subsequently, activated AREs mediate the transcription of antioxidant enzymes (particularly glutathione-S-transferase and quinone oxidoreductase), resulting in the detoxification of highly reactive carcinogens. AREs are cis-acting regulatory enhancer elements found in the 5’ flanking region of many phase II detoxification enzymes. C52174 456262 SB-743921 A synthetic small molecule with potential antineoplastic properties. SB-743921 selectively inhibits kinesin spindle protein (KSP), an important protein involved in the early stages of mitosis that is expressed in proliferating cells. Inhibition of KSP results in inhibition of mitotic spindle assembly and interrupts cell division, thereby causing cell cycle arrest and induction of apoptosis. C52199 456264 recombinant human growth hormone A recombinant form of endogenous human growth hormone (GH), a polypeptide produced by the anterior lobe of the human pituitary gland. GH exhibits growth-promoting effects and metabolic effects on carbohydrate, fat, protein and bone metabolism. GH stimulates protein synthesis and the uptake of amino acids into cells, and induces lipolysis in adipose tissues. The secretion of GH increases with sexual maturation and then declines steadily. C837 456358 tucotuzumab celmoleukin A recombinant fusion protein comprised of a human monoclonal antibody directed against the epithelial cell adhesion molecule (EpCAM or KS) linked to an active interleukin-2 (IL2) molecule with potential antineoplastic activity. The humanized monoclonal antibody moiety of tucotuzumab celmoleukin recognizes and binds to EpCAM, a cell surface epithelial protein that is expressed on a wide variety of cancer cells, thereby concentrating IL2 in EpCAM-expressing tumor tissue. Subsequently, the localized IL2 moiety of this fusion protein may stimulate a cytotoxic T-cell antitumor immune response. C2630 456780 PD0325901 An orally bioavailable, synthetic organic molecule targeting mitogen-activated protein kinase kinase (MAPK/ERK kinase or MEK) with potential antineoplastic activity. MEK inhibitor PD325901, a derivative of MEK inhibitor CI-1040, selectively binds to and inhibits MEK, which may result in the inhibition of the phosphorylation and activation of MAPK/ERK and the inhibition of tumor cell proliferation. The dual specific threonine/tyrosine kinase MEK is a key component of the RAS/RAF/MEK/ERK signaling pathway that is frequently activated in human tumors. C52195 456793 figitumumab A human monoclonal antibody directed against the insulin-like growth factor type I receptor (IGF1R) with potential antineoplastic activity. Figitumumab selectively binds to IGF1R, preventing insulin-like growth factor type 1 (IGF1) from binding to the receptor and subsequent receptor autophosphorylation. Inhibition of IGF1R autophosphorylation may result in a reduction in receptor expression on tumor cells that express IGF1R, a reduction in the anti-apoptotic effect of IGF, and inhibition of tumor growth. IGF1R is a receptor tyrosine kinase expressed on most tumor cells and is involved in mitogenesis, angiogenesis, and tumor cell survival. C52187 458064 18F-fluoromisonidazole A radiofluorinated 2-nitroimidazole derivate with hypoxia-specific tracer activity. Misonidazole is reduced under hypoxic conditions and in reduced form covalently binds to macromolecules in hypoxic cells. 18F (fluorine-18) radiofluorination of misonidazole to form 18F-fluoromisonidazole allows radioisotopic imaging of reduced misonidazole bound to macromolecules in hypoxic cells. C52180 458103 MUC-1 peptide vaccine A cancer vaccine comprised of a synthetic peptide derived from the mucin 1 (MUC-1) antigen with potential antineoplastic activity. Upon administration, MUC-1 peptide vaccine may stimulate the host immune system to mount a cytotoxic T lymphocyte (CTL) response against tumor cells positive for the MUC-1 antigen, resulting in decreased tumor growth. Overexpressed by many tumor cell types, MUC-1 antigen, a mammary-type apomucin, is a high-molecular-weight transmembrane glycoprotein. C2407 459491 AG-024322 A cyclin-dependent kinase (CDK) inhibitor with antineoplastic activity. AG-024322 selectively inhibits cyclin-dependent kinases (particularly CDK1,2 and 4), enzymes that regulate cell cycle progression. Inhibition of CDK may result in cell cycle arrest, induction of apoptosis, and inhibition of DNA replication and tumor cell proliferation. C52182 459750 fenofibrate A synthetic phenoxy-isobutyric acid derivate and prodrug with antihyperlipidemic activity. Fenofibrate is hydrolyzed in vivo to its active metabolite fenofibric acid that binds to and activates perioxisome proliferator activated receptor alpha (PPARalpha), resulting in the activation of lipoprotein lipase and reduction of the production of apoprotein C-III, an inhibitor of lipoprotein lipase activity. Increased lipolysis and a fall in plasma triglycerides, in turn, leads to the modification of the small, dense low density lipoporotein (LDL) particles into larger particles that are catabolized more rapidly due to a greater affinity for cholesterol receptors. In addition, activation of PPARalpha also increases the synthesis of apoproteins A-I, A-II, and high density lipoprotein (HDL)-cholesterol. Overall, fenofibrate reduces total cholesterol, LDL cholesterol, apolipoprotein B, total triglycerides and triglyceride rich lipoprotein (VLDL) while increasing HDL cholesterol. C29047 459751 carfilzomib An epoxomicin derivate with potential antineoplastic activity. Carfilzomib irreversibly binds to and inhibits the chymotrypsin-like activity of the 20S proteasome, an enzyme responsible for degrading a large variety of cellular proteins. Inhibition of proteasome-mediated proteolysis results in an accumulation of polyubiquinated proteins, which may lead to cell cycle arrest, induction of apoptosis, and inhibition of tumor growth. C52196 459753 romiplostim A recombinant protein with megakaryopoiesis stimulating activity. Romiplostim mimics endogenous thrombopoietin (TPO), directly binding to and activating the platelet thrombopoietin receptor (TpoR, Mpl, or CD110 antigen), a cytokine receptor belonging to the hematopoietin receptor superfamily. Activation of TpoR stimulates the proliferation and differentiation of megakaryocytes, resulting in an increase in the production of blood platelets. 459755 menatetrenone A menaquinone compound and form of vitamin K2 with potential antineoplastic activity. Menatetrenone may act by modulating the signalling of certain tyrosine kinases, thereby affecting several transcription factors including c-myc and c-fos. This agent inhibits tumor cell growth by inducing apoptosis and cell cycle arrest. C52194 459758 recombinant human endostatin A recombinant human proteolytic fragment of the C-terminal end of type XVIII collagen. Endostatin induces microvascular endothelial cell apoptosis and inhibits endothelial proliferation and angiogenesis, which may result in a reduction in tumor burden. This agent also may decrease hepatic metastasis by inhibiting proinflammatory cytokines and vascular cell adhesion molecule (VCAM)-dependent cell attachment to the hepatic microvasculature. C45515 459774 ATN-161 A small peptide antagonist of integrin alpha5beta1 with potential antineoplastic activity. ATN-161 selectively binds to and blocks the receptor for integrin alpha5beta1, thereby preventing integrin alpha5beta1 binding. This receptor blockade may result in inhibition of endothelial cell-cell interactions, endothelial cell-matrix interactions, angiogenesis, and tumor progression. Integrin alpha5beta1 is expressed on endothelial cells and plays a crucial role in endothelial cell adhesion and migration. C52185 459776 5-hydroxytryptophan An aromatic amino acid with antidepressant activity. In vivo, 5-hydroxytryptophan (5-HTP) is converted into 5-hydroxytryptamine (5-HT or serotonin) as well as other neurotransmitters. 5-HTP may exert its antidepressant activity via conversion to serotonin or directly by binding to serotonin (5-HT) receptors within the central nervous system (CNS). Endogenous 5-HTP is produced from the essential amino acid L-tryptophan. Exogenous therapeutic 5-HTP is isolated from the seeds of the African plant Griffonia simplicifolia. 459900 recombinant human 6Ckine A therapeutic recombinant analogue of a member of the endogenous CC chemokines with potential antineoplastic activity. Expressed by various lymphoid tissues, endogenous 6Ckine is chemotactic for B and T lymphocytes and dendritic cells. C1792 459953 ropivacaine hydrochloride The hydrochloride salt of ropivacaine, a local anesthetic of the amide type with analgesic activity. Ropivacaine binds to voltage-gated sodium ion channels in the neuronal membrane, thereby preventing the permeability of sodium ions and resulting in. a stabilization of the neuronal membrane and inhibition of depolarization; nerve impulse generation and propagation are blocked, resulting in a reversible loss of sensation. C52198 459956 basiliximab A recombinant, chimeric, human-murine monoclonal antibody directed against the alpha subunit of the interleukin-2 receptor (IL-2R alpha) with immunosuppressant activity. Basiliximab selectively binds to and blocks IL-2R alpha, expressed on the surface of activated T-lymphocytes, thereby preventing interleukin-2 binding and inhibiting the interleukin-2-mediated activation of lymphocytes. 459958 milk thistle A substance derived from any of several Old World coarse prickly-leaved shrubs and subshrubs including the plant Silybum marianum. Milk thistle's active chemical component is silymarin, which is a combination of flavonoids such as silibinin, dehydrosilibinin, silychristin and silydianin. These compounds are antioxidants and may alter the membrane structure of the liver cell, thereby blocking the absorption of toxins; they may also stimulate the production of new liver cells. In addition, milk thistle may increase cellular adenosine triphosphate (ATP) levels, exhibiting dose-dependent cardiac myocyte cytoprotection against doxorubicin. The silibinin component of milk thistle has been shown to inhibit growth factor receptor-mediated mitogenic and cell survival signaling, thereby inhibiting tumor growth. (NCI04) C29261 459959 bromelain A proteolytic enzyme obtained from the pineapple plant that cleaves sulhydryl groups. The enzyme is adsorbed intact through the gastrointestinal tract and has demonstrated therapeutic benefit. Bromelain has the ability to modulate cytokines, and has also demonstrated anti-inflammatory activity, immune response activity, and fibrinolytic activity. C28134 459961 goldenrod A group of North American weedy herbs belonging to the genus Solidago (family Asteraceae) with potential chemopreventive activities. Goldenrod may also possess anti-inflammatory, antiseptic properties, diuretic and antifungal properties, and may relieve chemotherapy-induced side-effects. C52191 459973 ex vivo-expanded HER2-specific T cells T cells specific for the human epidermal growth factor receptor 2 (HER2) with potential immunopotentiating activity. T cells directed against HER2, overexpressed on many tumor cells, are collected from HER2-expressing tumor tissue, expanded ex vivo and, then re-introduced in the patient. Re-introduction of ex vivo-expanded HER2-specific T cells may enhance the cytotoxic T cell response against tumor cells overexpressing HER2, resulting in inhibition of tumor growth. C52192 459975 levonorgestrel-releasing intrauterine system A long-acting, hormone-releasing, intrauterine device consisting of a small, T-shaped, polyethylene frame and a reservoired synthetic progesterone with progestational and potential antineoplastic activities. After insertion of this system into the uterus, the device slowly and gradually releases the hormone. Levonorgestrel acts by binding to the progesterone receptor in the nuclei of target cells, resulting in transcription activation and an alteration in protein synthesis. Subsequently, luteinizing hormone (LH) activity and ovulation are suppressed. Levonorgestrel may also exhibit antiproliferative activity in endometrial tissue. C52193 460052 plitidepsin A cyclic depsipeptide isolated from the marine tunicate Aplidium albicans. Plitidepsin displays a broad spectrum of antitumor activities, inducing apoptosis by triggering mitochondrial cytochrome c release, initiating the Fas/DC95, JNK pathway and activating caspase 3 activation. This agent also inhibits elongation factor 1-a, thereby interfering with protein synthesis, and induces G1 arrest and G2 blockade, thereby inhibiting tumor cell growth. C1689 460131 anamorelin hydrochloride The orally bioavailable hydrochloride salt of a synthetic, small-molecule ghrelin mimetic with appetite-stimulating and anabolic activities. Anamorelin binds to and stimulates the growth hormone secretagogue receptor (GHSR) centrally, thereby mimicking the appetite-stimulating and growth hormone-releasing effects of grhelin. Stimulation of GHSR may also reduce the production of the pro-inflammatory cytokines TNF-alpha and interleukin-6, which may play a direct role in cancer-related loss of appetite. C52197 460239 atorvastatin calcium The calcium salt of atorvastatin, a synthetic lipid-lowering agent. Atorvastatin competitively inhibits hepatic hydroxymethyl-glutaryl coenzyme A (HMG-CoA) reductase, the enzyme which catalyzes the conversion of HMG-CoA to mevalonate, a key step in cholesterol synthesis. This agent increases the number of LDL receptors on hepatic cell surfaces, enhancing the uptake and catabolism of LDL and reducing LDL production and the number of LDL particles, and lowers plasma cholesterol and lipoprotein levels. Like other statins, atorvastatin may also display direct antineoplastic activity, possibly by inhibiting farnesylation and geranylgeranylation of proteins such as small GTP-binding proteins, which may result in the arrest of cells in the G1 phase of the cell cycle. This agent may also sensitize tumor cells to cyctostatic drugs, possibly through the mTOR-dependent inhibition of Akt phosphorylation. 460926 GM-K562 cell vaccine A cell-based vaccine comprised of K562 cells transfected with the granulocyte macrophage-colony stimulating factor (GM-CSF) gene with potential immunopotentiating properties. Vaccination with GM-K562 cells may stimulate the host immune system to produce an antitumoral T-lymphocyte response, thereby inhibiting tumor growth. K562 cells are derived from the human erythroleukemia cell line K562. GM-CSF (also known as sagramostim) expressed by vaccine cells binds to specific cell surface receptors, modulating the proliferation and differentiation of a variety of hematopoietic progenitor cells with some specificity towards stimulation of leukocyte production. GM-CSF also promotes antigen presentation, up-regulates antibody-dependent cellular cytotoxicity (ADCC), and increases interleukin-2-mediated lymphokine-activated killer cell function; it may also augment host antitumoral immunity. C52190 461103 XL184 An orally bioavailable, small molecule receptor tyrosine kinase (RTK) inhibitor with potential antineoplastic activity. XL184 strongly binds to and inhibits several tyrosine receptor kinases. Specifically, XL184 appears to have a strong affinity for the hepatocyte growth factor receptor (Met) and vascular endothelial growth factor receptor 2 (VEGFR2), which may result in inhibition of tumor growth and angiogenesis, and tumor regression. This agent has also been shown to inhibit mast/stem cell growth factor (KIT), FMS-like tyrosine kinase 3 (Flt3) and tyrosine-protein kinase receptor (Tie-2). C52200 461135 tegafur-uracil A formulated therapeutic oral agent consisting of a combination of the 5-fluorouracil (5-FU) congener prodrug tegafur (tetrahydrofuranyl-5-fluorouracil) and uracil (1:4). The high concentration of uracil reversibly inhibits the uracil-reducing enzyme dihydropyrimidine dehydrogenase (DPD), thereby inhibiting first-pass DPD-mediated hepatic metabolism of the uracil analogue 5-FU and permitting administration of 5-FU as the orally bioavailable prodrug tegafur. Tegafur is bioactivated to 5-FU by liver microsomal cytochrome P450 enzymes. 5-FU is subsequently converted into its active metabolites 5-fluoro-deoxyuridine-monophosphate (FdUMP) and 5-fluorouridine-triphosphate (FUTP) intracellularly; these metabolites inhibit the enzyme thymidylate synthase and intercalate into RNA, resulting in decreased thymidine synthesis, reduced DNA synthesis, disrupted RNA function, and tumor cell cytotoxicity. 461189 propofol A hypnotic alkylphenol derivative. Formulated for intravenous induction of sedation and hypnosis during anesthesia, propofol facilitates inhibitory neurotransmission mediated by gamma-aminobutyric acid (GABA). This agent is associated with minimal respiratory depression and has a short half-life with a duration of action of 2 to 10 minutes. 461218 remifentanil hydrochloride The hydrochloride salt form of remifentanil, a synthetic anilidopiperidine derivative and short-acting opiate agonist with analgesic and anesthetic properties. Remifentanil selectively binds to and activates the mu-opioid receptor, thereby producing analgesia, respiratory depression, miosis, reduced gastrointestinal motility, and euphoria. 462092 etoricoxib A synthetic, nonsteroidal anti-inflammatory drug (NSAID) with antipyretic, analgesic ,and potential antineoplastic properties. Etoricoxib specifically binds to and inhibits the enzyme cyclooxygenase-2 (COX-2), resulting in inhibition of the conversion of arachidonic acid into prostaglandins. Inhibition of COX-2 may induce apoptosis and inhibit tumor cell proliferation and angiogenesis. 462160 IRX-2 A cell-free mixture comprised of a variety of naturally-derived cytokines obtained from normal, unrelated donor lymphocytes with potential immunostimulatory activity. The cytokines in IRX-2, including interleukin (IL)-1, -2, -6, -8, -10, -12, tumor necrosis factor alpha (TNF-a), interferon-gamma (IFN-g) and colony stimulating factors (CSFs), play vital roles in regulating cellular immunity and may synergistically stimulate a cellular immune response against tumor cells. C53396 462279 recombinant interferon alfa-2b A non-glycosylated recombinant interferon with antiviral and antineoplastic activities. Alfa interferons bind to specific cell-surface receptors, resulting in the transcription and translation of genes whose protein products mediate antiviral, antiproliferative, anticancer, and immune-modulating effects. C1953 462346 midostaurin A synthetic indolocarbazole multikinase inhibitor with potential antiangiogenic and antineoplastic activities. Midostaurin inhibits protein kinase C alpha (PKCalpha), vascular endothelial growth factor receptor 2 (VEGFR2), c-kit, platelet-derived growth factor receptor (PDGFR) and FMS-like tyrosine kinase 3 (FLT3) tyrosine kinases, which may result in disruption of the cell cycle, inhibition of proliferation, apoptosis, and inhibition of angiogenesis in susceptible tumors. C1872 462366 tadalafil A carboline-based compound with vasodilatory activity. Tadalafil selectively inhibits the cyclic guanosine monophosphate (cGMP)-specific type 5 phosphodiesterase- (PDE-5)-mediated degradation of cGMP, which is found in the smooth muscle of the corpus cavernosa and corpus spongiosum of the penis. Inhibition of cGMP degradation by tadalafil results in prolonged muscle relaxation, vasodilation, and blood engorgement of the corpus cavernosa, and, so, prolonged penile erection. 462556 brivanib alaninate The alaninate salt of a vascular endothelial growth factor receptor 2 (VEGFR2) inhibitor with potential antineoplastic activity. Brivanib strongly binds to and inhibits VEGFR2, a tyrosine kinase receptor expressed almost exclusively on vascular endothelial cells; inhibition of VEGFR2 may result in inhibition of tumor angiogenesis, inhibition of tumor cell growth, and tumor regression. C53397 462567 PF-00299804 A highly selective, orally bioavailabe small-molecule inhibitor of the HER family of tyrosine kinases with potential antineoplastic activity. PF-00299804 specifically and irreversibly binds to and inhibits human Her-1, Her-2, and Her-4, resulting in the proliferation inhibition and apoptosis of tumor cells that overexpress these receptors. C53398 462569 ADH-1 A small, cyclic pentapeptide vascular-targeting agent with potential antineoplastic and antiangiogenic activities. ADH-1 selectively and competitively binds to and blocks N-cadherin, which may result in disruption of tumor vasculature, inhibition of tumor cell growth, and the induction of tumor cell and endothelial cell apoptosis. N-cadherin, a cell- surface transmembrane glycoprotein of the cadherin superfamily of proteins involved in calcium-mediated cell-cell adhesion and signaling mechanisms; may be upregulated in some aggressive tumors and the endothelial cells and pericytes of some tumor blood vessels. C53399 462587 diindolylmethane A phytonutrient and plant indole found in cruciferous vegetables including broccoli, brussels sprouts, cabbage, cauliflower and kale, with potential antiandrogenic and antineoplastic activities. As a dimer of indole-3-carbinol, diindolylmethane (DIM) promotes beneficial estrogen metabolism in both sexes by reducing the levels of 16-hydroxy estrogen metabolites and increasing the formation of 2-hydroxy estrogen metabolites, resulting in increased antioxidant activity. Although this agent induces apoptosis in tumor cells in vitro, the exact mechanism by which DIM exhibits its antineoplastic activity in vivo is unknown. C53434 463333 lanreotide acetate copolymer microparticles A prolonged-release depot suspension of microparticles containing the acetate salt of lanreotide, a synthetic peptide analog of the naturally occurring somatostatin, and copolymers. Lanreotide inhibits the secretion of growth hormone (GH) by binding to pituitary somatostatin receptors, and may inhibit various other hormones, including thyroid stimulating hormone (TSH) and the gastroenteropancreatic hormones insulin, glucagon and gastrin. This agent has a much longer duration of action than natural somatostatin and is selective towards the inhibition of growth hormone. C53437 463367 bemiparin sodium The sodium salt of bemiparin, a second generation, synthetic, low-molecular-weight heparin (LMWH) with anticoagulant activity. Derived, after depolymerisation and fractionation, from medical-grade porcine unfractionated heparin (UFH), bemiparin has an average molecular weight of 3,600 daltons and has a higher anti-factor Xa/anti-factor IIa ratio (8:1) than first-generation LMWHs. This anticoagulant binds to antithrombin III, thereby enhancing the inactivation of activated Factor X (Factor Xa) and, to a lesser extent, activated factor II (Factor IIa). Compared to unfractionated heparins, the use of bemiparin is associated with lower incidences of major bleeding, osteoporosis, and heparin-induced thrombocytopenia. Bemiparin also promotes a greater release of tissue factor pathway inhibitor than UFH or dalteparin. C53400 463937 PV-10 An injectable ten percent solution of rose bengal disodium, an iodinated fluorescein derivative, with potential antineoplastic and radiosensitizing activities. When injected into tumor tissue, PV-10 specifically targets and concentrates in tumor cells, producing cytotoxic singlet oxygen when exposed to ionizing radiation. In addition, PV-10 may stimulate an anti-tumor immune response. C53412 463939 CP-4055 The lipophilic 5'-elaidic acid ester of the deoxycytidine analog cytosine arabinoside (cytarabine; Ara-C) with potential antineoplastic activity. As a prodrug, CP-4055 is converted intracellularly into cytarabine triphosphate by deoxycytidine kinase and subsequently competes with cytidine for incorporation into DNA, thereby inhibiting DNA synthesis. Compared to cytarabine, CP-4055 shows increased cellular uptake and retention, resulting in increased activation by deoxycytidine kinase to cytarabine triphosphate, decreased deamination and deactivation by deoxycytidine deaminase, and increased inhibition of DNA synthesis. This agent also inhibits RNA synthesis, an effect not seen with cytarabine. C53401 464172 valsartan An orally active nonpeptide triazole-derived antagonist of angiotensin (AT) II with antihypertensive properties. Valsartan selectively and competitively blocks the binding of angiotensin II to the AT1 subtype receptor in vascular smooth muscle and the adrenal gland, preventing AT II-mediated vasoconstriction, aldosterone synthesis and secretion, and renal reabsorption of sodium, and resulting in vasodilation, increased excretion of sodium and water, a reduction in plasma volume, and a reduction in blood pressure. 464795 L-citrulline A non-essential amino acid. In hepatocytes, L-citrulline is synthesized in the urea cycle by the addition of carbon dioxide and ammonia to ornithine. L-citrulline is converted into L-arginine by the enzymes argininosuccinate synthetase and argininosuccinate lyase in the presence of L-aspartate and ATP. Subsequently, L-arginine is converted to nitric oxide by nitric oxide synthase and L-citrulline is regenerated as a by-product . C53406 465178 vascular endothelial growth factor antisense oligonucleotide An antisense oligonucleotide with potential antiangiogenesis activity. Vascular endothelial growth factor (VEGF) antisense oligonucleotide binds directly to binds VEGF A/C/D mRNA, leading to mRNA degradation and the inhibition of VEGF A-mediated angiogenesis and VEGF C/D-mediated lymphangiogenesis. C53435 465181 autologous Epstein-Barr virus-transformed B-lymphoblastoid cell vaccine A cell-based vaccine composed of autologous lymphoblastoid B cells activated against Epstein-Barr virus (EBV) in vitro with potential immunoprotective activity. Upon prophylactic administration, this vaccine may stimulate specific cytotoxic T-lymphocyte (CTL) and antibody responses against EBV-transformed B cells, thereby preventing an EBV-induced post-transplantation lymphoproliferative disorder. C53443 465193 G250 peptide vaccine A cancer vaccine containing of a synthetic form of the renal cell carcinoma (RCC)-associated antigen G250 with potential antineoplastic activity. Vaccination with G250 peptide vaccine may stimulate the host immune system to mount a cytotoxic T lymphocyte (CTL) response against tumor cells positive for the G250 antigen, resulting in decreased tumor growth. Found in the majority of renal cell carcinomas, G250 is a cell surface tumor-associated antigen (TAA) that contains an HLA-A2.1-restricted epitope that is recognized by CTLs. C53410 465382 saponin-cholesterol-phospholipid adjuvant An adjuvant comprised of saponin, derived from the bark of Quillaia saponaria Molina, cholesterol and phospholipid with antigen-delivery and immunostimulatory activities. This saponin-based adjuvant in combination with various antigens, including those for human papilloma virus (HPV), hepatitis C virus (HCV), and the human cancer antigen NY-ESO-1, may result in potent antibody, CD4+ T-helper-cell, and CD8+ cytotoxic T-cell responses against the targeted antigen. In addition, this agent may reduce the amount of antigen necessary to induce an efficient immune response in the host. C53436 465493 iodine I 124 chimeric monoclonal antibody G250 A radioimmunoconjugate comprised of the chimeric monoclonal antibody G250 conjugated with the positron emitter iodine I 124. The antibody moiety of iodine I 124 chimeric monoclonal antibody G250 may bind to renal cell carcinoma (RCC) cells that express the RCC-associated antigen G250, allowing detection of tumor-localized iodine I 124 with positron emission tomography (PET). G250 is a cell surface tumor-associated antigen (TAA) that is found in the majority of renal cell carcinomas. C53407 465648 alfuzosin hydrochloride The hydrochloride salt of alfuzosin, a quinazoline compound with smooth muscle-relaxing activity. Alfuzosin selectively binds to and antagonizes post-synaptic alpha1-adrenoreceptors in smooth muscle of the prostate, bladder base, bladder neck, prostatic capsule, and prostatic urethra, initiating relaxation of smooth muscle and resulting in improvement of urine flow and the symptoms of benign prostatic hyperplasia (BPH). This agent also blocks alpha1-adrenoreceptors in peripheral vascular smooth muscle, resulting in vasodilatation and a decrease in peripheral vascular resistance. C53408 465788 yttrium Y 90-DOTA-chimeric monoclonal antibody cG250 A radioimmunoconjugate comprised of the chimeric monoclonal antibody cG250 conjugated with the bifunctional, macrocyclic chelating agent tetra-azacyclododecanetetra-acetic acid (DOTA) and lableled with the beta-emitting radioisotope yttrium Y 90. The antibody moiety of yttrium Y 90 DOTA chimeric monoclonal antibody cG250 binds to renal cell carcinoma cells expressing the G250 antigen, thereby selectively delivering a cytotoxic dose of beta radiation. C53409 466062 caseinate protein isolate An isolate comprised of the sodium or calcium salt of the glycoprotein casein, the primary protein found in milk and other dairy products, with anti-catabolic activity. C53440 466520 recombinant interferon alpha-1b The non-glycosylated recombinant interferon alpha, subtype 1b, with immunostimulatory and antineoplastic activities. Alpha interferon-1b binds to specific cell-surface receptors, resulting in the transcription and translation of genes whose protein products mediate antiviral, antiproliferative, anticancer, and immune-modulating effects. C53411 466602 soy isoflavones A dietary supplement isolated from soybeans containing phytoestrogen isoflavones. Although the mechanism of action is unclear, soy isoflavones mimic estrogen action mediated through estrogen receptors. In addition, this agent also modulates estrogen metabolism. As a result, soy isoflavones have been shown to reduce tumor cell proliferation and induce tumor cell apoptosis, as well as to be able to regulate hormone balance and reduce the risks of breast cancer, heart disease, and osteoporosis. C65152 467169 CpG oligodeoxynucleotide A synthetic oligodeoxynucleotide, containing unmethylated CpG motifs derived from bacterial DNA, with immunostimulatory activities. A CpG oligodeoxynucleotide (CpG ODN) binds to and activates a Toll-like receptor 9 (TLR9) and is taken up into cells by endocytosis; once internalized, it may activate numerous signaling transduction pathways resulting in the release of multiple cytokines. Through activation of TLR9, a CpG ODN can directly stimulate B-lymphocytes, dendritic and NK cells, resulting in an increase in innate immunity and antibody-dependant cell cytotoxicity (ADCC). Additionally, a CpG ODN can indirectly modulate T-cell responses, through the release of cytokines (IL-12 and IFN gamma), to induce a preferential shift to the Th1 (helper) phenotype resulting in enhanced CD8+ cellular cytotoxicity. C62280 467177 F-18 fluoroethyltyrosine An amino acid analog radiolabeled with fluorine F 18, a positron emitting isotope, used as a tracer in positron emission tomography (PET). Reflecting the increased amino acid transport capacity of tumor cells, F-18 fluroethyltyrosine (F-18 FET) is actively taken up in tumor cells via amino acid transport system L, but is neither incorporated into proteins nor readily degraded, resulting in high intracellular concentrations of this imaging agent. Radiolableled amino acid-based agents are useful in PET brain tumor imaging because F-18 fluoro-deoxyglucose (F-18 FDG), commonly used in PET tumor imaging, is relatively insensitive for detecting tumors in the brain due the high levels of glycolytic metabolism in the normal cortex and to a lesser extent in white matter. C60818 467183 recombinant bispecific single-chain antibody rM28 A recombinant, bispecific, single chain antibody directed against both the T-cell surface-associated costimulatory molecule CD28 and a melanoma-associated proteoglycan (MAPG) with potential antitumor activity. By targeting both CD28 and MAPG, recombinant bispecific single-chain antibody rM28 enhances cytotoxic T-cell recognition of melanoma cells, which may result in immune effector cell-mediated tumor cell death and a decrease in distant metastases. This agent appears to have a long serum half-life secondary to the formation of dimers. When activated, CD28 facilitates interactions between T-cells and other immune effector cells resulting in cytotoxic T-lymphocyte responses; MAPG is a surface antigen expressed on the majority of melanomas, including primary cutaneous, ocular and metastatic melanomas. C60882 467184 herba scutellaria barbata A Chinese herb isolated from the plant Scutellaria barbata D. Don (Lamiaceae) with potential antineoplastic activity. Containing the antioxidant flavone scutellarin, herba Scutellaria barbata has been shown to induce apoptosis of ovarian and breast tumor cells in vitro. C2661 467189 recombinant interferon alpha-2a A non-glycosylated recombinant human alpha interferon, subtype 2a, produced in the bacterium E. coli. Interferon alpha-2a binds to its specific cell-surface receptor, resulting in the transcription and translation of genes whose protein products have antiviral, antiproliferative, anticancer, and immune modulating effects. 467218 ammonium tetrathiomolybdate An ammonium salt with potential antiangiogenic and antitumor activities. Tetrathiomolybdate has been found to deplete systemic copper reserves through an unknown mechanism. This agent has been shown to inhibit the activities of cuproenzymes, including superoxide dismutase 1 (SOD1) and cytochrome c oxidase (COX), which may contribute to its antiangiogenic and antitumor effects. C74001 467222 bosutinib A synthetic quinolone derivative and dual kinase inhibitor that targets both Abl and Src kinases with potential antineoplastic activity. Unlike imatinib, bosutinib inhibits the autophosphorylation of both Abl and Src kinases, resulting in inhibition of cell growth and apoptosis. Because of the dual mechanism of action, this agent may have activity in resistant CML disease, other myeloid malignancies and solid tumors. Abl kinase is upregulated in the presence of the abnormal Bcr-abl fusion protein which is commonly associated with chronic myeloid leukemia (CML). Overexpression of specific Src kinases is also associated with the imatinib-resistant CML phenotype. C60809 467737 tinzaparin sodium The sodium salt of a low molecular weight heparin (LMWH) obtained by controlled enzymatic depolymerization of heparin from porcine intestinal mucosa with antithrombotic properties. Tinzaparin is a potent inhibitor of several activated coagulation factors, especially Factors Xa and IIa (thrombin); its primary activity is mediated through the plasma protease inhibitor antithrombin. In addition, this agent may inhibit angiogenesis through: 1) competitive binding of the heparin-binding sites on endothelial cells for the proangiogenic cytokines vascular endothelial growth factor (VEGF) and beta-fibroblast growth factor (beta-FGF) and 2) increasing the release of tissue factor pathway inhibitor (TFPI), a negative regulator of angiogenesis. C60810 467739 polyamine analogue PG11047 A second generation polyamine analogue, synthesized through the restriction of molecular conformations of parent polyamine compounds, with potential antineoplastic activity. Polyamine analogue PG11047 may displace endogenous polyamines from DNA binding sites, thereby interfering with cell cycle processes dependent upon polyamine binding and function, and resulting in cell-cycle arrest, induction of apoptosis, depletion of polyamines, and interference with gene and ligand-receptor activities involved with cell growth.\n This agent may exhibit decreased toxicity and enhanced cytotoxicity profiles compared to first-generation polyamine compounds. In tumor cells, there is an increase dependence on polyamines as well as a dysregulated polyamine metabolic pathway resulting in abnormal or sustained tumor growth. C60816 467750 vitamin D A family of lipo-soluble steroids important to the absorption, metabolism, and function of calcium and phosphorus and the growth and development of bone and tooth enamel. Found naturally in animal tissues, cholecalciferol (vitamin D3) is formed in the skin when ultraviolet light activates cholesterol conversion into vitamin D3. Ultraviolet irradiation of ergosterol (plant vitamin D) forms ergocalciferol (vitamin D2). 467926 monoclonal antibody KW-2871 A low-fucose, human-mouse chimeric IgG1 monoclonal antibody directed against the ganglioside GD3, a surface antigen expressed on many malignant melanoma cells, with potential antineoplastic activity. Monoclonal antibody KW-2871 binds to GD3-positive cells, thereby initiating antibody-dependent cytotoxicity against GD3-positive cells. This agent is prepared by fusing murine immunoglobulin (Ig) light and heavy variable regions derived from the murine IgG3 antibody KM-641 to a human constant (Fc) region. The low fucose content of the oligosaccharide side chains of this antibody may enhance binding of the antibody Fc region to lymphocyte Fc receptors. C61095 467927 Angelica sinensis root extract An herbal extract derived from the root of the plant Angelica sinensis with possible antiinflammatory, antispasmodic, vasodilatory, estrogenic, and antitumor activities. Angelica sinensis contains volatile oils, including safrole, isosafrole, and n-butylphthalide; coumarin derivatives, including psoralens, bergapten, osthol, imperatorin, and oxypeucedanin; and ferulic acid. The coumarin derivatives in this agent may vasodilate and relax smooth muscle and may exhibit additive anticoagulant effects. Ferulic acid, a phenolic phytochemical present in plant cell walls, may neutralize free radicals such as reactive oxygen species. In addition, Angelica sinensis extract has been shown to inhibit the growth and induce apoptosis of glioblastoma mutltiforme brain tumor cells through p53-dependent and p53-independent pathways. C60817 467928 hypertonic saline Any solution of sodium chloride (NaCl) in water with a concentration of NaCl higher than that found in physiological saline (0.9% w/v). When administered in vivo, hypertonic saline (HTS) exhbits several physiological effects beneficial to cerebral injury including: 1) osmotic and vasoregulatory - by promoting the flow of excess water from cerebral tissue to the blood via osmosis and decreasing edema in the vascular endothelium of injured tissues, thus lowering vascular resistance and allowing more blood flow; 2) hemodymanic - by effectively expanding plasma volume; 3) immunomodulatory - by preventing leukocytes from becoming activated and adhering to injured neurons and; 4) neurochemical - by counteracting detrimental excitatory amino acids through the normalization of neuronal cell membranes and by restoration of normal electrolyte and neurotransmitter levels in brain cells, and normal cell volumes. C60814 467929 ferrous sulfate A sulfate salt of mineral iron formulated for oral administration and used as a dietary supplement, ferrous sulfate is absorbed in the stomach and small intestine and combines with apoferritin to form ferritin, which is stored in the liver, spleen, red bone marrow, and intestinal mucosa. Important in transport of oxygen by hemoglobin to the tissues, iron is also found in myoglobin, transferrin, and ferritin, and is a component of many enzymes such as catalase, peroxidase, and cytochromes. 467930 iron sucrose injection A sterile aqueous complex of polynuclear iron (III)-hydroxide in sucrose for intravenous use. Following intravenous administration, iron sucrose is dissociated by the reticuloendothelial system into iron and sucrose; the sucrose component is eliminated mainly by urinary excretion. Iron sucrose can be administered with or without erythropoietin to raise hemoglobin levels and may be used in cases of oral iron therapy intolerance or ineffectiveness. Hypersensitivity reactions are less common with iron sucrose compared to other parenteral iron products, such as iron dextran. C60883 468469 imexon A 2-cyanoaziridine derivative with antitumor activity in multiple myeloma. Although its mechanism of action is not clearly known, imexon may induce apoptosis via a pathway involving cleaved caspase-3, caspase-9, and/or caspase-8. Other cytotoxic mechanisms of action of this agent may involve thiol depletion, generation of reactive oxygen species (ROS), and decreases in the mitochondrial membrane potential. 468556 fenretinide lipid matrix An orally bioavailable powder formulation of a synthetic phenylretinamide analogue of retinol with potential chemopreventive and antineoplastic activities. Fenretinide binds to and activates retinoic acid receptors (RARs), thereby inducing cell differentiation and apoptosis in some tumor cell types, including those of the colon, breast, prostate, and neuroblastoma. Independent of RAR activation, this agent also modulates gene expression that leads to ceramide-induced, caspase-independent programmed cell death (PCD) via effectors such as ganglioside GD3 and reactive oxygen species (ROS). Compared to the capsule form, the powder contains a mixture of wheat flour, fats, and sugar that may contribute to the enhanced bioavailability of fenretinide. C63482 468834 triptorelin pamoate The pamoate salt of triptorelin, a synthetic decapeptide agonist analog of luteinizing hormone releasing hormone (LHRH). Possessing greater potency than endogenous LHRH, triptorelin reversibly represses gonadotropin secretion after prolonged administration. After chronic, continuous administration, a sustained decrease in LH, FSH and testicular and ovarian steroidogenesis is observed. The serum testosterone concentration may fall to levels typically seen in surgically castrated men. 468837 pNGVL3-hICD vaccine A plasmid DNA cancer vaccine encoding the intracellular domain (ICD) of the HER-2/neu proto-oncogene. Upon administration and after cellular uptake by skin or muscle cells, the pNGVL3-hICD vaccine plasmid expresses the HER-2/neu protein, which, after intracellular processing, may elicit both antigen-specific cytotoxic T-lymphocyte (CTL) and humoral immune responses against tumor cells expressing HER-2. The HER-2/neu ICD protein is highly immunogenic and, as a subdominant epitope, may be associated with decreased immune tolerance. C61146 468840 Lactobacillus rhamnosus GG A live specific strain of the species, Lactobacillus rhamnosus (a subspecies of Lactobacillus casei) with probiotic activity. When administered orally, Lactobacillus rhamnosus GG adheres to the mucous membrane of the intestine and may help to restore the balance of the GI microflora; promote gut-barrier functions; diminish the production of carcinogenic compounds by other intestinal bacteria; and activate the innate immune\nresponse and enhance adaptive immunity, especially during infections. C61097 468842 adenovirus HER2-transduced autologous dendritic cell vaccine A cell-based cancer vaccine composed of autologous dendritic cells (DCs) transduced with a replication-deficient adenovirus vector encoding HER-2 with potential antineoplastic activity. Upon administration, adenovirus HER2-transduced autologous dendritic cell vaccine may stimulate a cytotoxic T lymphocyte (CTL) response against HER-2-positive tumor cells, which may result in tumor cell death and decreased tumor growth.\nHER-2, a tyrosine kinase receptor for epidermal growth factor (EGF) (also known as neu and ErbB2), is overexpressed by some breast, ovarian, and gastric cancers. C61098 468844 nedaplatin A second-generation cisplatin analogue with antineoplastic activity. Containing a novel ring structure in which glycolate is bound to the platinum by a bidentate ligand, nedaplatin forms reactive platinum complexes that bind to nucelophillic groups in DNA, resulting in intrastrand and interstrand DNA cross-links, apoptosis and cell death. This agent appears to be less nephrotoxic and neurotoxic compared to both cisplatin and carboplatin. C61099 468927 glycopeptide antibiotic One of a class of antibiotics originally isolated from plant and soil bacteria with structures containing either a glycosylated cyclic or polycyclic nonribosomal peptide. These antibiotics inhibit the cell wall structure of susceptible organisms (principally Gram-positive cocci) by inhibiting peptidoglycan synthesis.\nFirst-generation glycopeptide antibiotics include vancomycin, teicoplanin, and ramoplanin; second-generation semi-synthetic glycopeptide antibiotics include oritavancin, dalbavancin, and telavancin. C61101 469006 D-cycloserine An analogue of the amino acid D-alanine with broad-spectrum antibiotic and glycinergic activities. D-cycloserine interferes with bacterial cell wall synthesis by competitively inhibiting two enzymes, L-alanine racemase and D-alanine:D-alanine ligase, thereby impairing peptidoglycan formation necessary for bacterial cell wall synthesis. This agent may be bactericidal or bacteriostatic, depending on its concentration at the infection site and the susceptibility of the organism. In addition, D-cycloserine is an excitatory amino acid and partial agonist at the glycine binding site of the NMDA receptor in the central nervous system (CNS); binding to the central NMDA receptor may result in amelioration of neuropathic pain. 469015 daptomycin A semi-synthetic cyclic lipopeptide antibiotic isolated form the bacterium Streptomyces roseosporus with broad-spectrum anitbiotic activity against Gram-positive bacteria. Daptomycin has a distinct mechanism of action, in which it binds to bacterial membrane and causes rapid depolarization of the cell membrane due to calcium-dependant potassium efflux; the loss of membrane potential leads to inhibition of DNA, RNA and protein synthesis, resulting in bacterial cell death. This agent does not penetrate the outer membrane of gram-negative bacteria. 469731 XL844 A synthetic small-molecule inhibitor of checkpoint kinases 1 and 2 (Chk1 and Chk2) with potential antineoplastic activity. XL844 binds to and inhibits Chks 1 and 2, resulting in inhibition of cell cycle arrest, progressive DNA damage, inhibition of DNA repair, and, ultimately, tumor cell apoptosis. This agent also inhibits vascular endothelial growth factor receptor 1 (VEGFR1) and vascular endothelial growth factor receptor 3 (VEGFR3), important mediators of tumor angiogenesis and lymphogenesis, respectively. In the presence of DNA damage or incomplete DNA replication, eukaryotic cells activate cell cycle checkpoints that temporarily halt the cell cycle to permit DNA repair or completion of DNA replication to take place. In the presence of extensive damage or absence of timely repair, these checkpoint-signaling pathways may also trigger a pathway that effects apoptosis. Normal functions of Chks involve the initiation of cell-cycle arrest and the up-regulation of transcription genes involved with DNA excision repair and dNTP synthesis. C61102 469778 noscapine hydrochloride The orally bioavailable hydrochloride salt of the opioid agonist noscapine, a phthalideisoquinoline alkaloid derived from the opium poppy Papaver somniferum, with mild analgesic, antitussive, and potential antineoplastic activities. Noscapine binds to tubulin and alters its conformation, resulting in a disruption of the dynamics of microtubule assembly (by increasing the time that microtubules spend idle in a paused state) and, subsequently, the inhibition of mitosis and tumor cell death. Unlike other tubulin inhibitors such as the taxanes and vinca alkaloids, noscapine does not affect microtubule polymerization. C61103 470233 therapeutic triiodothyronine A therapeutic formulation of the primary physiologically active form of endogenous thyroid hormone. In vivo, triiodothyronine enters the nucleus and binds to nuclear thyroid hormone receptors that subsequently bind to thyroid response elements (TREs) located in target genes. Receptor binding by triiodothyronine in combination with recruited coactivators results in maximal transcriptional activation after binding to TREs; in general, binding of thyroid hormone receptor alone to TREs leads to repression of gene transcription. 470235 ranimustine A chloroethylnitrosourea derivative that inhibits proliferation and growth of tumor cells by alkylation and cross-linkage of DNA strands of tumor cells. 470241 tetracycline antibiotic Any of a group of broad spectrum naphthacene antibiotics isolated from various species of Streptomyces or produced semisynthetically. In bacteria, tetracycline antibiotics block binding of aminoacyl-tRNA to the mRNA-ribosome complex, thereby inhibiting protein synthesis. 471234 perflutren protein-type A microspheres A sterile non-pyrogenic suspension of microspheres of human serum albumin with the stable, high-molecular-weight fluorocarbon gas perflutren, used as a contrast enhancement agent for ultrasound procedures. Because the acoustic impedance of perflutren protein-type A microspheres is much lower than that of blood, impinging ultrasound waves are scattered and reflected at the microsphere-blood interface and\nmay be visualized with ultrasound imaging. At the frequencies used in adult echocardiography (2-5 MHZ), the microspheres resonate which further increases the extent of ultrasound scattering and reflection. C61105 471236 allogeneic dendritic cell-myeloma idiotype vaccine A cell-based vaccine composed of allogeneic dendritic cells pulsed ex-vivo with an autologous myeloma idiotype with potential antineoplastic activity. Upon administration, allogeneic dendritic cell-myeloma idiotype vaccine may stimulate the host immune system to mount a specific cytotoxic T-lymphocyte (CTL) response against myeloma cells, resulting in cell lysis. C61434 471256 SR31747A A synthetic peripheral sigma receptor ligand with immunomodulatory and potential antitumor activities. Although the exact mechanism by which SR31747A exerts its antitumor effects has not been fully established, SR31747A binds to and inhibits the sigma1 receptor (SR31747A-binding protein-1 or SR-BP1), human sterol isomerase (emopamil-binding protein) and the sigma2 receptor, which may result in a reduction in tumor cell proliferation and tumor cell apoptosis. In addition, this agent inhibits the production of pro-inflammatory cytokines while increasing anti-inflammatory cytokines. Upregulated in various cancers, the sigma1 and sigma2 receptors and human sterol isomerase are proteins that are involved in the regulation of cell proliferation and survival. C61435 471831 amantadine hydrochloride The hydrochloride salt of amantadine, a synthetic tricyclic amine with antiviral, antiparkinsonian, and antihyperalgesic activities. Amantadine appears to exert its antiviral effect against the influenza A virus by interfering with the function of the transmembrane domain of the viral M2 protein, thereby preventing the release of infectious viral nucleic acids into host cells; furthermore, this agent prevents virus assembly during virus replication. Amantadine exerts its antiparkinsonian effects by stimulating the release of dopamine from striatal dopaminergic nerve terminals and inhibiting its pre-synaptic reuptake. This agent may also exert some anticholinergic effect through inhibition of N-methyl-D-aspartic acid (NMDA) receptor-mediated stimulation of acetylcholine, resulting in antihyperalgesia. 471833 licorice root extract An herbal extract derived from the root of the plant Glycyrrhiza glabra with potential anti-inflammatory, antioxidant, and antineoplastic activities. Licorice root extract contains glycoside glycyrrhizinic acid and numerous flavonoids. Glycyrrhizinic acid in licorice root extract is hydrolyzed to glycyrrhetic acid (GA); GA inhibits 11 beta-hydroxysteroid dehydrogenase, resulting in inhibition of the conversion of cortisol to the inactive steroid cortisone and elevated cortisol levels. In addition, GA inhibits 17,20-lyase and 17 beta-hydroxysteroid dehydrogenase, resulting in decreased conversions of 17-hydroxyprogesterone to androstenedione and androstenedione to testosterone. The primary antioxidant found in licorice root, the flavonoid glabridin, may inactivate or inhibit the activities of some cytochrome P450 enzymes. In tumor cells, beta-hydroxy-DHP, another flavonoid, may induce Bcl-2 phosphorylation, apoptosis, and G2/M cell cycle arrest. C61436 471934 S-CKD602 A sterically stabilized, pegylated liposomal formulation containing CKD602, a semi-synthetic analogue of campthotecin with potential antitumor activity. CKD602 inhibits the action of topoisomerase I, an enzyme that produces reversible single-strand breaks in DNA during DNA replication. CDK602 stabilizes the topoisomerase I and DNA complex, resulting in the inhibition of religation of DNA breaks, inhibition of DNA replication, and apoptotic cell death. The polyethylene glycol coating of S-CKD602 allows for greater plasma circulation time, thus enhancing the concentration of CKD602 at the tumor site. Encapsulation of CKD602 preserves the active lactone form, resulting in an increased cytotoxic effect of CKD602. C61437 472077 pegylated anti-GFR antibody fragment A pegylated, cross-linked, humanized divalent-Fab' antibody fragment directed against vascular endothelial growth factor receptor-2 (VEGFR-2) with potential antiangiogenic and antitumor activities. Pegylated anti-GFR antibody fragment binds to and inhibits VEGFR-2, which may inhibit angiogenesis and tumor cell proliferation. Multivalent Fab' antibody fragments may exhibit improved retention and internalization properties compared to their parent IgGs. C61438 472195 meloxicam An oxicam derivative and a non-steroidal anti-inflammatory drug (NSAID) with anti-inflammatory, antipyretic and analgesic activities. Unlike traditional nonselective NSAIDs, meloxicam preferentially inhibits the activity of cyclo-oxygenase II (COX-II), resulting in a decreased conversion of arachidonic acid into prostaglandin precursors. The resulting decrease in prostaglandin synthesis is responsible for the therapeutic effects of meloxicam. 472200 transdermal estrogen A transdermal formulation containing the synthetic form of estradiol, the most potent, endogenously produced estrogen. Upon topical administration, estradiol diffuses through the cell membrane and binds to and activates specific intracellular estrogen receptors located on estrogen-responsive tissues, including the reproductive tract, breast, pituitary, hypothalamus, liver, and bone. The activated ligand-receptor complex binds to estrogen response elements on DNA and promotes the transcription of genes involved in the functioning of the female reproductive system and secondary sex characteristics. In addition, estradiol inhibits the pituitary secretion of the gonadotropins luteinizing hormone (LH) and follicle stimulating hormone (FSH) through a negative feedback mechanism. C61440 472205 terameprocol A synthetic tetra-methylated derivative of nordihydroguaiaretic acid (NDGA) and transcriptional inhibitor with potential antiviral, antiangiogenic, and antineoplastic activities. Terameprocol competes with the transcription factor Sp1 for specific Sp1 DNA binding domains within gene promoter regions during DNA synthesis. In virally-infected cells, blocking of the Sp1 binding site suppresses Sp1-regulated viral promoter activity and gene expression, thereby inhibiting viral transcription and replication. In tumor cells, blockage of Sp1 binding sites by this agent interferes with the transcription of the Sp1-dependant genes cyclin-dependant kinase (Cdc2), survivin, and vascular endothelial growth factor (VEGF), which are overexpressed in a variety of cancers. By suppressing Sp1-regulated transcription of these genes, terameprocol may reduce tumor angiogenesis and tumor cell proliferation and induce tumor cell apoptosis. C61441 472216 WT1 126-134 peptide vaccine A synthetic peptide vaccine consisting of the amino acids 126 through 134 of the human Wilms' Tumor protein-1 (WT1) with potential antitumor activity. WT1, a tumor associated antigen, is overexpressed in most types of leukemia and in a variety of solid cancers. Vaccination with WT1 126-134 peptide vaccine may induce a WT1-specific cytotoxic T-lymphocyte (CTL) response against WT1 expressing cells, resulting in cell lysis and inhibition of cancer cell proliferation. C61442 473030 V930 vaccine A novel cancer vaccine designed to treat HER-2- and/or CEA-expressing cancers. C61069 473196 human anti-alpha-v integrin monoclonal antibody A pan alpha-v human monoclonal antibody that recognizes alpha-v beta-1, alpha-v beta-3, alpha-v beta-5, and alpha-v beta-6 integrins with antiangiogenic and antitumor activities. Human anti-alpha-v integrin monoclonal antibody competitively binds to and blocks both alpha-v beta-3 and alpha-v beta-5 integrins, resulting in inhibition of integrin-mediated tumor angiogenesis and tumor growth. \nIntegrins facilitate\nthe adhesion of stimulated endothelial cells to the extracellular matrix (ECM); trigger the secretion of ECM-rearranging proteases; and propagate\nsignaling events that promote the survival and differentiation of\ncells in newly formed vasculature. C61070 473242 aerosolized liposomal 9-nitro-20 (S) camptothecin An aerosolized liposomal preparation of a water-insoluble derivative of camptothecin with potential antineoplastic activity. 9-nitro-20 (S)-camptothecin and its active metabolite 9-aminocamptothecin (9-AC) selectively stabilize topoisomerase I-DNA covalent complexes during S-phase, thereby inhibiting religation of topoisomerase I-mediated single-strand DNA breaks and producing potentially lethal double-strand DNA breaks when encountered by the DNA replication machinery.\n This agent is formulated with dilauroylphosphatidylcholine and nebulized in particle sizes of 1.2-1.6 micrometer mass median aerodynamic diameter. C61071 473738 epothilone ZK-219477 A novel synthetic epothilone with potential antineoplastic activity. Epothilone ZK-219477 binds to microtubules, predominantly in tumor cells, thereby inducing microtubule bundling, formation of multipolar spindles, and mitotic arrest in a manner similar to taxanes. Epothilones are poor substrates for the multidrug resistance 1 (MDR1) P-glycoprotein drug efflux pump and, unlike the taxanes, appear to be able to evade some drug-resistance mechanisms. C61072 473873 gp96-Ig fusion protein-expressing non-small cell lung cancer cell vaccine A cancer vaccine consisting of irradiated non-small cell lung cancer cells, manipulated to express and secrete heat shock protein gp96-Ig fusion protein, with potential antineoplastic activity. Vaccination with gp96-Ig fusion protein-expressing non-small cell lung cancer cell vaccine may elicit a cytotoxic T cell response against non-small lung cancer cells. Monomorphic heat shock protein gp96 participates in the major histocompatibility complex class I-restricted antigen presentation pathway. C61073 473901 Aurora kinase inhibitor MLN8054 An orally bioavailable, highly selective small molecule inhibitor of the serine/threonine protein kinase Aurora A kinase with potential antineoplastic activity. Auora kinase inhibitor MLN8054 binds to and inhibits Aurora kinase A, resulting in disruption of the assembly of the mitotic spindle apparatus, disruption of chromosome segregration, and inhibition of cell proliferation. Aurora A localizes in mitosis to the spindle poles and to spindle microtubules and is thought to regulate spindle assembly. Aberrant expression of Aurora kinases occurs in a wide variety of cancers, including colon and breast cancers. C61075 474021 synthetic breast cancer peptides-tetanus toxoid-Montanide ISA-51 vaccine A cancer vaccine comprised of multiple synthetic breast cancer peptides and the adjuvant tetanus toxoid helper peptide emulsified in the adjuvant Montanide ISA-51 with immunopotentiation activity. Vaccination with this cancer vaccine may elicit a specific cytotoxic T-lymphocyte response against breast cancer cells. Synthetic breast cancer peptides may stimulate the immune response against cells that produce breast cancer markers such as erbB2 (HER2/neu) while tetanus toxoid helper peptide binds to class II MHC molecules as a nonspecific vaccine helper epitope, resulting in a long-term immunopotentiation by increasing the helper T-cell response. Montanide ISA-51, also known as incomplete Freund's adjuvant or IFA, is a stabilized water-in-oil emulsion adjuvant containing mineral oil with mannide oleate added as a surfactant that non-specifically stimulates cell-mediated immune responses to antigens. C61076 474024 autologous dendritic cell-autologous tumor mRNA-human CD40L vaccine A cancer vaccine consisting of autologous dendritic cells transfected with autologous tumor mRNA and the human CD40 ligand (CD40L) gene with immunostimulatory and antitumor activities. Vaccination with autologous dendritic cell-autologous tumor mRNA-human CD40L vaccine may elicit a cytotoxic T cell response against tumor cells from which the autologous tumor mRNA was derived. When expressed by dendritic cells, tumor antigens and the co-stimulatory molecule CD40L, which binds to CD40 receptors on antigen presenting cells (APC), facilitate both humoral and cellular immune responses against tumor cells. C61077 474798 paclitaxel vitamin E-based emulsion formulation A cremophor-free, P-glycoprotein-inhibiting, vitamin E-based emulsion particle formulation of paclitaxel with antineoplastic activity. Paclitaxel binds to tubulin and inhibits the disassembly of microtubules, thereby resulting in the inhibition of cell division. This agent also induces apoptosis by binding to and blocking the function of the apoptosis inhibitor protein Bcl-2 (B-cell Leukemia 2). The vitamin-E based emulsion allows bolus infusion without steroid premedication and may diminish hypersensitivity reactions; tumor tissue may be passively targeted due to preferential deposition of emulsion particles while an emulsion formulation component inhibits the P-glycoprotein drug efflux pump. C61079 474964 ISS 1018 CpG oligodeoxynucleotide A short, synthetic, unmethylated CpG motif-based oligodeoxynucleotide (CpG ODN) with immunostimulatory activity. As an immunostimulatory sequence (ISS) that signals through Toll-like receptor 9 (TLR9), ISS 1018 CpG ODN induces the production of immunoglobulin by B cells and interferon (IFN) -alpha, IFN-beta, interleukin (IL) -12, and tumor necrosis factor (TNF) -alpha by plasmacytoid dendritic cells (pDC). In turn, pDC, through cell-cell contact and secretion of and IFN-alpha and -beta induce natural killer (NK) cell proliferation, NK cell production of IFN-gamma, and NK cell-mediated cytotoxicity; secreted IFNs also stimulate bystander T cell activation and differentiation of naive CD4+ T cells into T-helper 1 cells on specific antigen challenge. In addition, ISS 1018 CpG ODN promotes antigen presentation and co-stimulatory molecule expression. Unmethylated CpG motifs are regions of genomic DNA containing the cytosine-guanine dinucleotide in which cytosine remains unmethylated, especially in prokaryotic DNA. C61080 475676 3,4-methylenedioxymethamphetamine A ring-substituted amphetamine derivative, structurally related to the hallucinogen mescaline, with entactogenic, neurotoxic, and motor-stimulatory activities. 3,4-methylenedioxymethamphetamine (MDMA) produces an acute, rapid enhancement in both the release of serotonin from and the inhibition of serotonin reuptake by serotonergic nerve endings in the brain. Once within the cell, MDMA depletes stores of tryptophan hydroxylase (TPH) via acute oxidative inactivation; in turn, depleted stores of TPH leave cell terminals open to damage from oxidative stress, possibly a source of MDMA neurotoxicity. This agent also induces norepinephrine, dopamine, and acetylcholine release and can act directly on a number of receptors, including alpha 2-adrenergic and 5-hydroxytryptamine (5-HT) 2A receptors. MDMA may suppress the dyskinesia associated with long-term use of L-dopamine (L-DOPA) without affecting the efficacy of L-DOPA treatment. C61081 475734 alpha-1,3-galactosyltransferase-expressing allogeneic pancreatic tumor cell vaccine A cancer vaccine comprised of irradiated allogeneic pancreatic cancer cells transfected to express murine alpha-1,3-galactosyltransferase with potential antitumor activity. Vaccination is associated with the expression of murine alpha-1,3-galactosyl (alpha-gal) carbohydrate residues on cell membrane glycoproteins and glycolipids of the vaccine pancreatic cancer cell allograft; murine alpha-gal epitopes, not present on human cells, then induce a hyperacute rejection of the vaccine pancreatic cancer cell allograft. The hyperacute rejection involves the binding of pre-existing human anti-alpha-gal antibodies (which naturally occur against gut flora) to murine alpha-gal epitopes, resulting in the rapid activation of antibody-dependent cell-mediated cytotoxicity (ADCC) towards allograft cells. The host immune system then attacks endogenous pancreatic cancer cells, resulting in ADCC towards endogenous pancreatic cancer cells. C61082 475763 sodium stibogluconate Pentavalent antimony (Sb) in differential complex formation with gluconic acid with leishmanicidal and potential antineoplastic activities. The Sb moiety of sodium stibogluconate (SSG) may inhibit protein tyrosine phophorylases (PTPases) by covalently modifying sulfhydryl groups in PTPase cysteine residues, resulting in specific inactivation of SH2 domain-containing tyrosine phosphatases-1 and -2 (SHP-1 and SHP-2), PTPases which negatively regulate interferon (IFN) signaling; enhancement of IFN-induced Stat1 tyrosine phosphorylation; and induction of cellular protein tyrosine phosphorylation. SSG in combination with IFN-alpha may synergize to overcome tumor cell resistance to IFN-alpha-mediated apoptosis. C61083 475765 anti-IL-6 chimeric monoclonal antibody A human-mouse chimeric antibody, constructed from a murine antiinterleukin 6 (IL-6) monoclonal antibody, with antitumor and antiinflammatory activities. Containing the antigen-binding variable region of the murine antibody, CLB-IL-6-8, and the constant region of a human IgG1kappa immunoglobulin, anti-IL-6 chimeric monoclonal antibody has high affinity for recombinant as well as native IL-6 and inhibits the binding of IL-6 to the IL-6 receptor (IL-6R), resulting in the blockade of the IL-6/IL-6R/gp130 signal transduction pathway, and, subsequently, antitumor and antiinflammatory activities. C61084 475797 atomoxetine hydrochloride The hydrochloride salt of atomoxetine, a phenoxy-3-propylamine derivative and selective non-stimulant, norepinephrine reuptake inhibitor with cognitive-enhancing activity. Although its precise mechanism of action is unknown, atomoxetine appears to selectively inhibit the pre-synaptic norepinephrine transporter, resulting in inhibition of the presynaptic reabsorption of norepinephrine and prolongation of norepinephrine activity in the synaptic cleft; the effect on cognitive brain function may result in improved attention and decreased impulsivity and activity levels. C47405 476316 demineralized bone matrix Demineralized allograft bone with osteoinductive activity. Demineralized\nbone matrices are prepared by acid extraction of allograft\nbone, resulting in loss of most of the mineralized component\nbut retention of collagen and noncollagenous proteins, including\ngrowth factors.\nThe efficacy of a demineralized\nbone matrix (DBM) as a bone-graft substitute or extender may be related to the total amount of bone morphogenetic\nprotein (BMP) present, and the ratios of the different BMPs\npresent. BMPs belong to the transforming growth factor (TGF) superfamily of proteins. C61085 476335 gp100:209-217(210M) peptide vaccine A synthetic peptide cancer vaccine consisting of amino acid residues 209 through 217 of the glycoprotein 100 (gp100) melanoma antigen, with a methionine substitution at position 210 designed to improve immunogenicity. Vaccination with gp100:209-217(210M) peptide may stimulate the host immune system to mount a cytotoxic T lymphocyte (CTL) response against tumor cells expressing gp100. 476336 MART-1:27-35 peptide vaccine A natural or synthetic peptide cancer vaccine consisting of amino acid residues 27 through 35 of the melanoma-associated antigen MART-1 with potential antineoplastic activity. Vaccination with MART-1:27-35 peptide may induce cytotoxic host immune responses against melanoma cells that express this peptide. 476479 pazopanib hydrochloride The hydrochloride salt of a small molecule inhibitor of multiple protein tyrosine kinases with potential antineoplastic activity. Pazopanib selectively inhibits vascular endothelial growth factor receptors (VEGFR)-1, -2 and -3, c-kit and platelet derived growth factor receptor (PDGF-R), which may result in inhibition of angiogenesis in tumors in which these receptors are upregulated. C60779 476572 casopitant mesylate The mesylate salt of a centrally-acting neurokinin 1 (NK1) receptor antagonist with antidepressant and antiemetic activities. Casopitant competitively binds to and blocks the activity of the NK1 receptor, thereby inhibiting NK1-receptor binding of the endogenous tachykinin neuropeptide substance P (SP), which may result in antiemetic effects. SP is found in neurons of vagal afferent fibers innervating the brain-stem nucleus tractus solitarii and the area postrema, which contains the chemoreceptor trigger zone (CTZ), and may be elevated in response to chemotherapy. The NK1 receptor is a G-protein receptor coupled to the inositol phosphate signal-transduction pathway and is found in both the nucleus tractus solitarii and the area postrema. C61086 476576 quadrivalent human papillomavirus (types 6, 11, 16, 18) recombinant vaccine A non-infectious recombinant, quadrivalent vaccine prepared from the highly purified\nvirus-like particles (VLPs) of the major capsid (L1) protein of human papillomavirus (HPV) Types 6, 11, 16, and 18 with immunoprophylactic activity. The immunoprohylactic efficacy of L1 VLP vaccines, such as quadrivalent human papillomavirus (types 6, 11, 16, 18) recombinant vaccine, appear to be mediated by the development of humoral immune\nresponses. HPV Types 16 and 18 account for approximately 70% of cervical cancers and HPV Types 6 and 11 account for approximately 90% of genital warts. C61087 476771 survivin inhibitor YM155 A small-molecule proapoptotic agent with potential antineoplastic activity. Survivin inhibitor YM155 selectively inhibits survivin expression in tumor cells, resulting in inhibition of survivin antiapoptotic activity (via the\nextrinsic or intrinsic apoptotic pathways) and tumor cell apoptosis. Survivin, a member of the inhibitor of apoptosis (IAP) gene family, is expressed during embryonal development and is absent in most normal, terminally differentiated tissues; upregulated in a variety of human cancers, its expression in tumors is associated with a more aggressive phenotype, shorter survival times, and a decreased response to chemotherapy. C61091 478746 MAGE-A3/HPV 16 peptide vaccine A multi-epitope "Trojan antigen" ("TA") construct vaccine consisting of human melanoma antigen A3 (MAGE-A3) and human papillomavirus (HPV) 16 peptide epitopes linked by the furin-sensitive linker peptide RVKR (arginine-serine-lysine-arginine) with immunostimulatory and antitumor activities. The TA construct enters the cytoplasm of antigen-presenting cells (APC) and is processed by the endoplasmic reticulum (ER) and the trans-Golgi network (TGN), where the endopeptidase furin releases the epitopes from the RVKR linker peptide and, together with various exopeptidases, generates MHC class I-binding peptides. Expressed on the cell surfaces of APC, these MHC class I-binding peptides stimulate a cytotoxic T lymphocyte (CTL) response against tumor cells that display the same peptide epitopes on their cell surfaces. C61088 479148 tamsulosin hydrochloride The hydrochloride salt of tamsulosin, a sulfonamide derivative with adrenergic antagonist activity. Tamsulosin selectivity binds to and blocks the activity of alpha1 adrenoreceptors in the human prostate and bladder neck; blockade of these adrenoceptors can cause smooth muscle in the prostate and bladder neck to relax, resulting in an improvement in urinary flow rate. C29486 479183 dutasteride A synthetic 4-azasteroid compound with antiandrogenic activity. Dutasteride competitively and specifically binds to isoenzymes 1 and 2 of 5-alpha-reductase, forming stable enzyme complexes and inhibiting the conversion of testosterone to 5α-dihydrotestosterone (DHT); the reduction in DHT activity may mitigate or prevent enlargement of the prostate gland. The type 2 5-alpha-reductase isoenzyme is primarily active in the reproductive tissues while the type 1 isoenzyme is also active in skin and the liver. 479648 nordihydroguaiaretic acid A naturally occurring antioxidant dicatechol originally derived from the creosote bush Larrea divaricatta with antipromoter, anti-inflammatory, and antineoplastic activities. Nordihydroguaiaretic acid (NDGA) directly inhibits activation of two receptor tyrosine kinases (RTKs), the insulin-like growth factor receptor (IGF-1R) and the c-erbB2/HER2/neu receptor, resulting in decreased proliferation of susceptible tumor cell populations. This agent may induce apoptosis in susceptible tumor cell populations as a result of disruption of the actin cytoskeleton in association with the activation of stress activated protein kinases (SAPKs). In addition, NDGA inhibits arachidonic acid 5-lipoxygenase (5LOX), resulting in diminished synthesis of inflammatory mediators such as prostaglandins and leukotrines; it may prevent leukocyte infiltration into tissues and the release of reactive oxygen species and, at higher concentrations, may also inhibit cyclooxygenase. 480388 aprotinin bovine A single chain polypeptide isolated from bovine lung with antifibrinolytic and anti-inflammatory activities. As a broad-spectrum serine protease inhibitor, aprotinin bovine competitively and reversibly inhibits the activity of a number of different esterases and proteases, including trypsin, chymotrypsin, kallikrein, plasmin, tissue plasminogen activator, and tissue and leukocytic proteinases, resulting in attenuation of the systemic inflammatory response (SIR), fibrinolysis, and thrombin generation. This agent also inhibits pro-inflammatory cytokine release and maintains glycoprotein homeostasis. C47402 480399 xaliproden hydrochloride The hydrochloride salt of xaliproden, an orally-active, synthetic, non-peptidic 5-hydroxytryptamine (5-HT) 1A receptor agonist with neurotrophic and neuroprotective activities. Although its mechanism of action is not fully understood, xaliproden appears to either mimic the effects of neurotrophins or stimulate their synthesis, thereby stimulating neuronal cell differentiation and proliferation and inhibiting neuronal cell death. The neuroprotective effect of this agent involves the activation of MAP kinase pathways via stimulation of the 5-HT1A receptor. C61328 480407 senna fruit The fruit of Cassia acutifolia and Cassia angustifolia (Cassia) with laxative and purgative activities. The active ingredients in senna fruit include the hydroxyanthracene glycosides sennosides A and B (rhein dianthrones) and sennosides C and D (rhein aloe-emodin heterodianthrones). \n\nSennosides irritate the bowel lining and stimulate the bowel muscular coat, particularly in the colon, resulting in accelerated bowel transit and evacuation. C29447 480408 senna extract An extract made from the dried leaflets on the pods of Cassia angustifolia or Cassia acutifolia with cathartic activity. Dimeric glycosides in dried senna extract are converted to the active monoanthrones by bacterial action in the colon. Through direct effects on enterocytes, enteric neurons, and muscle, monoanthrones produce giant migrating colonic contractions in addition to water and electrolyte secretion. As do other stimulant laxatives, monoanthrones may induce a limited low-grade inflammation in the colon through activation of prostaglandin/cyclic AMP and nitric oxide/cyclic GMP pathways and perhaps inhibition of Na+, K+-ATPase. C61324 480467 magnesium citrate The citrate salt of the element magnesium with cathartic activity. The cathartic action of magnesium cations appears to result, in part, from osmotically mediated water retention, which subsequently stimulates peristalsis. In addition, magnesium ions may also stimulate the activity of nitric oxide (NO) synthase and increase the biosynthesis of the phospholipid proinflammatory mediator platelet activating factor (PAF) in the gut. NO may stimulate intestinal secretion via prostglandin- and cyclic GMP-dependent mechanisms while PAF produces significant stimulation of colonic secretion and gastrointestinal motility. C29241 481255 doxifluridine A fluoropyrimidine derivative and oral prodrug of the antineoplastic agent 5-fluorouracil (5-FU) with antitumor activity. Doxifluridine, designed to circumvent the rapid degradation of 5-FU by dihydropyrimidine dehydrogenase in the gut wall, is converted into 5-FU in the presence of pyrimidine nucleoside phosphorylase. 5-FU interferes with DNA synthesis and subsequent cell division by reducing normal thymidine production and interferes with RNA transcription by competing with uridine triphosphate for incorporation into the RNA strand. C978 481277 recombinant thyrotropin alfa A recombinant form of the human anterior pituitary glycoprotein thyroid stimulating hormone (TSH) with use in the diagnostic setting. With an amino acid sequence identical to that of human TSH, thyrotropin alfa binds to TSH receptors on normal thyroid epithelial cells or well-differentiated thyroid cancer cells, stimulating iodine uptake and organification, synthesis and secretion of thyroglobulin (Tg), triiodothyronine (T3), and thyroxine (T4). C61322 481301 liposome-encapsulated doxorubicin citrate A formulation of the citrate salt of the antineoplastic anthracycline antibiotic doxorubicin, encapsulated within liposomes, with antitumor activity. Doxorubicin intercalates into DNA and interacts with topoisomerase II, thereby inhibiting DNA replication and RNA synthesis. This agent also interacts with cell membrane lipids causing lipid peroxidation. Liposomal delivery of doxorubicin improves drug penetration into tumors and decreases drug clearance, thereby increasing the duration of therapeutic drug effects while lowering the toxicity profile. C61317 481348 denosumab A humanized monoclonal antibody directed against the receptor activator of nuclear factor kappa beta ligand (RANKL) with antiosteoclast activity. Denosumab specifically binds to RANKL and blocks the interaction of RANKL with RANK, a receptor located on osteoclast cell surfaces, resulting in inhibition of osteoclast activity, a decrease in bone resorption, and a potential increase in bone mineral density. RANKL, a protein expressed by osteoblastic cells, plays an important role in osteoclastic differentiation and activation. C61313 481366 bupivacaine hydrochloride A long-acting, amide-type local anesthetic. Bupivicaine reversibly binds to specific sodium ion channels in the neuronal membrane, resulting in a decrease in the voltage-dependent membrane permeability to sodium ions and membrane stabilization; inhibition of depolarization and nerve impulse conduction; and a reversible loss of sensation. 483042 barium sulfate The sulfate salt of barium, an alkaline, divalent metal. Barium sulfate is quite insoluble in water, and is used as a radiopaque agent to diagnose gastrointestinal medical conditions. Barium sulfate is taken by mouth or given rectally. C28859 483101 lansoprazole A substituted benzimidazole prodrug with selective and irreversible proton pump inhibitor activity. Lansoprazole prodrug is converted to an active sulfonamide derivative in the acidic environment of the gastric parietal cell; the sulfonamide derivative binds to the gastric proton pump H+/K+ ATPase and forms a stable disulfide bond with the sulfhydryl group near the potassium-binding site on the luminal side, resulting in inactivation of the ATPase and a reduction in gastric acid secretion. This agent does not have anticholinergic or histamine H2 -receptor antagonistic properties. C29150 483128 nadroparin calcium A low molecular weight heparin (LMWH) composed of a heterogeneous mixture of sulfated polysaccharide glycosaminoglycan chains obtained by depolymerisation of porcine mucosal sodium heparin, extraction/purification and conversion to the calcium salt. Nadroparin binds to antithrombin III (ATIII) and inhibits the activity of activated factor X (factor Xa), thereby inhibiting the final common pathway of the coagulation cascade and preventing the formation of a cross-linked fibrin clot. C61320 483132 palladium-bacteriopheophorbide A novel palladium-substituted bacteriochlorophyll derivative and photosensitizer with potential antitumor activity. Upon administration, inactive palladium-bacteriophephorbide is activated locally when the tumor bed is exposed to photoirradiation; the activated form induces local cytotoxic processes, resulting in local tissue damage, disruption of tumor vasculature, and tumor hypoxia and necrosis. C61321 484444 apixaban An orally active inhibitor of coagulation factor Xa with anticoagulant activity. Apixaban directly inhibits factor Xa, thereby interfering with the conversion of prothrombin to thrombin and preventing formation of cross-linked fibrin clots. C61308 484456 CHIR-265 An orally bioavailable small molecule with potential antineoplastic activity.CHIR-265 binds and inhibits Raf kinases, which may result in a reduction of tumor cell growth and proliferation, and tumor cell death. In addition, this agent inhibits vascular endothelial growth factor receptor type 2 (VEGFR-2), thereby disrupting tumor angiogenesis. \nRaf kinases are critical enzymes in the Ras/Raf/MEK/ERK signaling pathway and are frequently upregulated in neoplasms. C61311 484587 methazolamide A sulfonamide derivate and carbonic anhydrase inhibitor with potential antineoplastic activity. Methazolamide inhibits tumor-associated carbonic anhydrase IX (CAIX), which may result in increased cell death in hypoxic tumors. As a hypoxia-inducible transmembrane glycoprotein, CAIX catalyzes the rapid interconversion of carbon dioxide and water into carbonic acid, protons, and bicarbonate ions, helping to maintain acidification of the tumor microenvironment and enhance resistance to cytotoxic therapy in some hypoxic tumors. C61318 484642 Jin Fu Kang A traditional Chinese herbal medicine derived from the plant Astragalus membranaceus with potential immunopotentiation activity. \nJin Fu Kang may stimulate anti-tumor macrophage and natural killer cell\nactivity and may enhance immune recognition of tumor cells by\ninhibiting the production of T-helper cell type 2 (Th2) cytokines such as interleukin-4 (IL-4) amd interleukin-10 (IL-10). C61316 484826 reduced glutathione-L-cysteine-anthocyanins gel A gel formulation containing reduced glutathione, L-cysteine, and anthocyanins with potential antioxifdant, immunostimulating, and chemoprotective activities. Reduced glutathione is the primary cellular antioxidant and plays important roles in the antioxidation of reactive oxygen species and free radicals and, as a thiol-containing co-enzyme, in the detoxification of xenobiotic compounds. In addition, glutathione affects DNA synthesis and repair and exerts immunostimulating activity by increasing the production of interleukin-2 (IL-2), promoting antigen presentation, and stimulating T-suppressor/cytotoxic (CD8 cells) cells. The flavonoid anthocyanins, derived from various blue and purple flowering plants, are potent scavengers of reactive oxygen species. C61323 484893 bcr-abl (b3a2)-derived peptide vaccine A peptide vaccine consisting of the bcr-abl b3a2 fusion oncoprotein, frequently expressed in chronic myelogenous leukemia (CML), with potential antineoplastic activity. Vaccination with the bcr-abl (b3a2)-derived peptide vaccine may stimulate the host immune system to mount a cytotoxic T lymphocyte (CTL) response against tumor cells that express the bcr-abl b3a2 fusion protein. \nFusion genes in CML typically result from the fusion of either BCR exon b2 or BCR exon b3 to ABL exon a2, a 'b3a2' or a 'b2a2' fusion. C61310 484895 bcr-abl (b2a2)-derived peptide vaccine A peptide vaccine consisting of the bcr-abl b2a2 fusion oncoprotein, frequently expressed in chronic myelogenous leukemia (CML), with potential antineoplastic activity. Vaccination with the bcr-abl (b2a2)-derived peptide vaccine may stimulate the host immune system to mount a cytotoxic T lymphocyte (CTL) response against tumor cells that express the bcr-abl b2a2 fusion protein. Fusion genes in CML typically result from the fusion of either BCR exon b2 or BCR exon b3 to ABL exon a2, a 'b3a2' or a 'b2a2' fusion. C61309 485164 anti-EpCAM antibody fragment -Pseudomonas exotoxin fusion protein A fusion protein immunotoxin consisting of a humanized, single-chain monoclonal antibody fragment specific for the epithelial cell adhesion molecule (EpCAM) conjugated with a truncated form of Pseudomonas exotoxin A with potential antineoplastic activity. Anti-EpCAM-Pseudomonas-exotoxin fusion protein binds to Ep-CAM-positive tumor cells, thereby delivering the Pseudomonas exotoxin A moiety specifically; the Pseudomonas exotoxin A moiety then inactivates elongation factor 2 (EF-2) through ADP ribosylation, resulting in inhibition of protein synthesis in target cells. EpCAM, a cell surface protein, is expressed by a variety of tumor cells and is frequently found in head and neck cancers. C61307 485165 INO-1001 A isoindolinone derivative and potent inhibitor of the nuclear enzyme poly (ADP-ribose) polymerase (PARP) with chemosensitization and radiosensitization properties. INO-1001 inhibits PARP, which may result in inhibition of tumor cell DNA repair mechanisms and, so, tumor cell resistance to chemotherapy and radiation therapy. PARP enzymes are activated by DNA breaks and have been implicated in the repair of DNA single-strand breaks (SSB). C61315 485171 amonafide L-malate The malate salt of amonafide, an imide derivative of naphthalic acid, with potential antineoplastic activity. Amonafide intercalates into DNA and inhibits topoisomerase II, resulting in DNA double-strand breaks (DSB) and inhibition of DNA replication and RNA synthesis. C61306 485244 ezatiostat hydrochloride The hydrochloride salt of a liposomal small-molecule glutathione analog inhibitor of glutathione S-transferase (GST) P1-1 with hematopoiesis-stimulating activity. After intracellular de-esterification, the active form of ezatiostat binds to and inhibits GST P1-1, thereby restoring Jun kinase and MAPK pathway activities and promoting MAPK-mediated cellular proliferation and differentiation pathways. This agent promotes the proliferation and maturation of hematopoietic precursor cells, granulocytes, monocytes, erythrocytes and platelets. C61326 485249 digoxin A cardiac glycoside. Digoxin inhibits the sodium potassium adenosine triphosphatase (ATPase) pump, thereby increasing intracellular calcium and enhancing cardiac contractility. This agent also acts directly on the atrioventricular node to suppress conduction, thereby slowing conduction velocity. Apparently due to its effects on intracellular calcium concentrations, digoxin induces apoptosis of tumor cells via a pathway involving mitochondrial cytochrome c and caspases 8 and 3. 485262 delta-8-tetrahydrocannabinol An analogue of tetrahydrocannabinol (THC) with antiemetic, anxiolytic, appetite-stimulating, analgesic, and neuroprotective properties. Delta-8-tetrahydrocannabinol (delta-8-THC) binds to the cannabinoid G-protein coupled receptor CB1, located in the central nervous system; CB1 receptor activation inhibits adenyl cyclase, increases mitogen-activated protein kinase activities, modulates several potassium channel conductances and inhibits N- and P/Q-type Ca2+ channels. This agent exhibits a lower psychotropic potency than delta-9-tetrahydrocannabinol (delta-9-THC), the primary form of THC found in cannabis. C61312 485272 oligonucleotide SPC2996 A synthetic antisense oligonucleotide against Bcl-2 messenger RNA with potential antitumor activity. Oligonucleotide SPC2996 binds to and inactivates Bcl-2 mRNA, thereby inhibiting the expression of Bcl-2 protein, promoting tumor cell apoptosis, and potentially enhancing the efficacy of standard cytotoxic chemotherapy. Linked to tumor drug resistance, the antiapoptotic protein Bcl-2 is upregulated in several types of cancers. C61325 485274 sivifene gel The phenylhydrazone 4,4'-dihydroxybenzophenone-2,4-dinitrophenylhydrazone formulated as a topical agent with immunomodulating and potential antineoplastic activities. Applied topically as a gel, sivifene may stimulate a local immune response against human papillomavirus (HPV)-induced cervical intraepithelial neoplasia (CIN). C61305 485276 VCL-CB01 vaccine A vaccine consisting of two plasmids encoding the human cytomegalovirus (CMV) tegument phosphoprotein 65 (pp65), a major internal matrix protein, and glycoprotein B (gB), an important CMV component responsible for attachment and entry into cells, with immunostimulatory properties. Vaccination with VCL-CB01 may stimulate the host immune system to mount cellular and humoral immune responses against CMV positive cells, resulting in cell lysis. C61327 485295 Z-360 A selective, orally available, 1,5-benzodiazepine-derivative gastrin/cholecystokinin 2 (CCK-2) receptor antagonist with potential antineoplastic activity. Z-360 binds to the gastrin/CCK-2 receptor, thereby preventing receptor activation by gastrin, a peptide hormone frequently associated with the proliferation of gastrointestinal and pancreatic tumor cells. C61329 485296 GM-CSF-encoding oncolytic herpes simplex virus An oncolytic, recombinant herpes simplex type-1 virus (HSV) encoding thuman cytokine granulocyte-macrophage colony stimulating factor (GM-CSF) with potential immunostimulating and antineoplastic activities. Upon administration, GM-CSF-encoding oncolytic HSV selectively infects and replicates in tumor cells, thereby inducing tumor cell lysis. In addition, expressed GM-CSF may stimulate a cytotoxic T cell response against tumor cells, resulting in immune-mediated tumor cell death in addition to HSV-mediated oncolytic tumor cell death. C61314 485305 tozasertib lactate The lactate salt of tozasertib, a synthetic, small-molecule Aurora kinase inhibitor with potential antitumor activity. Tozasertib binds to and inhibits Aurora kinases (AKs), thereby inducing apoptosis in tumor cells in which AKs are overexpressed.\nAKs, a family of serine-threonine kinases, are essential for mitotic progression, spindle formation, centrosome maturation, chromosomal segregation, and cytokinesis. C61319 486259 GI-4000 vaccine A vaccine containing a heat-killed recombinant Saccharomyces cerevisiae yeast transfected with mutated forms of Ras, an oncogene frequently found in solid tumors, with potential immunostimulant and antitumor activity. Upon administration, GI-4000 vaccine elicits an immune response by stimulating a specific cytotoxic T-cell response against the mutated forms of Ras. This may lead to a destruction of cancer cells expressing a Ras mutation. C61489 486303 recombinant human mannan-binding lectin A recombinant protein similar or identical to human mannan-binding lectin (MBL) with opsonin activity. MBL, a soluble pattern recognition receptor (PRR) collectin in the C-type lectin superfamily, is a plasma protein that plays an important role in innate immunity; MBL contains a carbohydrate recognition domain at one end and a collagen-like stalk domain at the other. Upon MBL binding to mannose residues on mannose-containing polysaccharides (mannans) on the surfaces of a microorganisms, activation of the complement system results in the deposition of complement components (opsonization) and the clearance of the opsonized microorganisms by phagocytic cells. MBL is part of the mannan-binding lectin pathway (also known as the Ali/Krueger pathway), which has similarities to the classical complement pathway in that activation of C4 and C2 produce activated complement proteins further down the complement cascade. However, unlike the classical complement pathway, activation of this pathway is not antibody dependent. C1151 486305 darinaparsin A small-molecule organic arsenical with potential antineoplastic activity. Although the exact mechanism of action is unclear, darinaparsin, a highly toxic metabolic intermediate of inorganic arsenicals (iAs) that occurs in vivo, appears to generate volatile cytotoxic arsenic compounds when glutathione (GSH) concentrations are low. The arsenic compounds generated from darinaparsin disrupt mitochondrial bioenergetics, producing reactive oxygen species (ROS) and inducing ROS-mediated tumor cell apoptosis; in addition, this agent or its byproducts may initiate cell death by interrupting the G2/M phase of the cell cycle and may exhibit antiangiogenic effects. Compared to inorganic arsenic compounds such as arsenic trioxide (As2O3), darinaparsin appears to exhibit a wide therapeutic window. C61490 486329 adenovirus encoding recombinant human endostatin A replication-defective, recombinant oncolytic adenovirus encoding human endostatin with potential antineoplastic activity. Endostatin, a 20 kDa C-terminal proteolytic fragment of collagen XVIII, is an important angiogenesis inhibitor. Upon intratumoral administration, the adenovirus infects and replicates in tumor cells. The expressed endostatin may inhibit endothelial cell proliferation and angiogenesis which may result in a reduction of tumor growth. 486330 coxsackievirus A21 A naturally occurring enterovirus with potential antitumor activity. Upon intratumoral administration, coxsackievirus A21 targets and binds to intracellular adhesion molecule 1 (ICAM-1) and decay acceleration factor (DAF), both cell surface molecules that are both overexpressed on certain malignant cells. After entering the cells, coxsackievirus A21 replicates in these cancer cells, thereby causing cancer cell lysis. This results in a reduction of tumor cell growth. 486333 AVN944 An orally available, synthetic small molecule with potential antineoplastic activity. AVN944 inhibits inosine monosphosphate dehydrogenase (IMPDH), an enzyme involved in the de novo synthesis of guanosine triphosphate (GTP), a purine molecule required for DNA and RNA synthesis. Inhibition of IMPDH deprives cancer cells of GTP, resulting in disruption of DNA and RNA synthesis, inhibition of cell proliferation, and the induction of apoptosis. AVN944 appears to have a selective effect on cancer cells in that deprivation of GTP in normal cells results in a temporary slowing of cell growth only. IMPDH is overexpressed in some cancer cells, particularly in hematological malignancies. C49181 486347 TAS-108 A synthetic, antiestrogenic steroidal compound with potential antitumor activity. TAS-108 binds to and inhibits estrogenic receptor alpha (ERa), mainly expressed in the mammary gland and uterus and upregulated in estrogen-dependent tumors. Blockage of ERa by TAS-108 prevents the binding and effects of estrogen and may lead to an inhibition of estrogen-dependent cancer cell proliferation. TAS-108 also is a partial agonist of the estrogenic receptor beta (ERb), expressed in many tissues including the central nervous system, urogenital tract, bone and cardiovascular system, thereby exerting a positive effect on these tissues. In addition, TAS-108 activates the co-repressor Silencing Mediator for Retinoid and Thyroid hormone receptor (SMRT), a protein that inhibits the activities of the estrogen receptors, which may contribute to the antitumor activity of TAS-108. 486348 Melan-A VLP vaccine A vaccine consisting of the melanocyte differentiation antigen Melan A (also called MART-1) encapsulated in noninfectious virus-like particles (VLP) with potential immunostimulating and antineoplastic activities. Upon administration, Melan-A VLP vaccine may activate the immune system to exert a specific cytotoxic T lymphocyte (CTL) response against cancer cells expressing the Melan A antigen, resulting in tumor cell lysis. Melan A is an antigen that is upregulated in most melanomas. VLP stimulates the immune system and promotes the CTL response. 486351 MKC-1 An orally bioavailable, small-molecule, bisindolylmaleimide cell cycle inhibitor with potential antineoplastic activity. MKC-1 and its metabolites inhibit tubulin polymerization, blocking the formation of the mitotic spindle, which may result in cell cycle arrest at the G2/M phase and apoptosis. In addition, this agent has been shown to inhibit the activities of the oncogenic kinase Akt, the mTOR pathway, and importin-beta, a protein essential to the transport of other proteins from the cytosol into the nucleus. C2507 486366 palonosetron hydrochloride The hydrochloride salt of palonosetron, a carbazole derivative and a selective serotonin receptor antagonist with antiemetic activity. Palonosetron competitively blocks the action of serotonin at 5-hydroxytryptamine type 3 (5-HT3) receptors located on vagal afferents in the chemoreceptor trigger zone (CTZ), resulting in suppression of chemotherapy-induced nausea and vomiting. The CTZ is located in the area postrema on the dorsal surface of the medulla oblongata at the caudal end of the fourth ventricle and outside the blood-brain barrier (BBB). 486413 RFT5-dgA immunotoxin A recombinant immunotoxin consisting of the anti-CD25 monoclonal antibody RFT5 fused to the deglycosylated ricin A-chain (dgA) with potential antitumor activity. The monoclonal antibody moiety of RFT5-dgA immunotoxin attaches to CD25 (the alpha chain of the IL-2 receptor complex) on the cell membrane; after internalization, the dgA moiety cleaves the N-glycosidic bond between the ribose and adenine base at position 4324 in 28S ribosomal RNA, resulting in ribosome inactivation, inhibition of protein synthesis, and cell death. CD25 is expressed on activated normal T and B cells and macrophages and is frequently upregulated in many hematologic malignancies. C61498 486415 nitric oxide-releasing acetylsalicylic acid derivative A nitric oxide (NO) donating derivative of acetylsalicyclic acid with anti-inflammatory, analgesic, antipyretic, antithrombotic, gastroprotective and potential antitumor activities. The acetylsalicylic acid derivative moiety of this agent inhibits the activities of cyclooxygenase (COX) I and II, preventing the formation of prostaglandins and thromboxanes. A reduction in prostaglandin synthesis accounts for this agent's anti-inflammatory, anti-pyretic and analgesic activities; a reduction in thromboxane A2 synthesis results in an irreversible inhibition of platelet aggregation. NO donation by this agent, after cleavage from the acetylsalicylic acid derivative in vivo, may protect the gastric mucosa against the damaging effects of the aspirin derivative by modulating prostaglandins. In tumor cells, the NO donating moiety may block the cell cycle in the G1 and G2 phases and may induce apoptosis through caspase-mediated mechanisms. C61499 486428 oral fludarabine phosphate An oral formulation of the phosphate salt of fludarabine, a synthetic purine nucleoside analogue antimetabolite with antineoplastic activity. Fudarabine is preferentially transported into malignant cells and metabolized by deoxycytidine kinase to its active form, 2-fluoro-ara-ATP; 2-fluoro-ara-ATP competes directly with deoxyadenosine triphosphate (dATP) and inhibits alpha DNA polymerase, RNA reductase, and DNA primase, which may result in inhibition of DNA synthesis and cell death. C64338 486610 ixabepilone (oral) An orally bioavailable semisynthetic analogue of epothilone B with antineoplastic activity. Ixabepilone binds to tubulin and promotes tubulin polymerization and microtubule stabilization, thereby arresting cells in the G2-M phase of the cell cycle and inducing tumor cell apoptosis. This agent demonstrates antineoplastic activity against taxane-resistant cell lines. 486626 mapatumumab A fully human agonistic monoclonal antibody to tumor necrosis factor-related apoptosis-inducing ligand receptor-1 (TRAIL-R1) with apoptosis promoting and potential antitumor activities. TRAIL-R1 is a cell surface receptor expressed on many malignant cell types. Mapatumumab selectively binds to and activates the TRAIL cell receptor, thereby inducing apoptosis and reducing tumor growth. 486728 anti-GP-3 monoclonal antibody A humanized, immunoglobulin G1 monoclonal antibody with potential antitumor activity. MORab-003 specifically targets at glycoprotein 3 (GP-3), a cell surface antigen that is overexpressed on many epithelial-derived cancer cells. Upon binding to the GP-3 antigen, MORab-003 triggers a host immune response against GP-3 expressing cells resulting in cell lysis. C61503 486735 recombinant human hyaluronidase A human recombinant form of the naturally occurring human enzyme hyaluronidase with potential chemoadjuvant activity. Upon local administration, recombinant human hyaluronidase hydrolyzes hyaluronic acid, a glucosaminoglycan responsible for the viscosity of the interstitial barrier. The digestion of hyaluronic acid lowers the viscosity in the interstitial space, thereby increasing permeability and facilitating local penetration of chemotherapeutic agents into cancer cells. 486744 live freeze-dried lactic acid bacteria probiotic A probiotic containing live, cultivated, freeze-dried lactic acid bacteria with gastrointestinal (GI) protective, anti-inflammatory, immunomodulating and potential antitumor properties. Oral administration of probiotic bacteria help maintain adequate colonization of the GI tract and modulate the composition of the normal microflora. Upon colonization of the GI tract, the probiotic bacteria form a protective barrier, interfere with the attachment of pathogenic bacteria and other harmful substances and may bind to and degrade carcinogens. This may prevent inflammation and possibly cancer. In addition, these bacteria produce lactic acid, thereby creating an acidic environment that is unfavorable for pathogens. C61505 486745 inulin A naturally occurring, indigestible and non-absorbable oligosaccharide produced by certain plants with prebiotic and potential anticancer activity. Inulin stimulates the growth of beneficial bacteria in the colon, including Bifidobacteria and Lactobacilli, thereby modulating the composition of microflora. This creates an environment that protects against pathogens, toxins and carcinogens, which can cause inflammation and cancer. In addition, fermentation of inulin leads to an increase in short-chain fatty acids and lactic acid production, thereby reducing colonic pH, which may further control pathogenic bacteria growth and may contribute to inulin's cancer protective properties. 486831 SU014813 An orally-active, tyrosine kinase receptor inhibitor with potential antitumor activity. SU014813 binds to and inhibits the phosphorylation of vascular endothelial growth factor receptor 2 (VEGFR2), platelet-derived growth factor receptor (PDGFR) alpha and beta, c-Kit and Fms-related tyrosine kinase 3 (Flt-3). This leads to an inhibition of cellular proliferation and angiogenesis and an induction of apoptosis. C61507 486925 18F-fluoroazomycin arabinoside A radiofluorinated 2-nitroimidazole derivative with hypoxia-specific tracer activity. 18F-fluoroazomycin arabinoside is reduced under hypoxic conditions and is often seen in various malignant tumors, forming highly reactive intermediates. In its reduced form, 18F-fluoroazomycin arabinoside covalently binds to macromolecules, thereby accumulating in hypoxic cells and allowing radioisotopic imaging of these particular cells. Compared to 18F-misonidazole, 18F-fluoroazomycin arabinoside has a lower octanol:water partition coefficient; it therefore has less tendency to accumulate in lipophilic tissues and exhibits a faster renal clearance, leading to an improved imaging ability of hypoxic tissue. C62520 486941 mocetinostat A rationally designed, orally available, Class 1-selective, small molecule, 2-aminobenzamide HDAC inhibitor with potential antineoplastic activity. Mocetinostat binds to and inhibits Class 1 isoforms of HDAC, specifically HDAC 1, 2 and 3, which may result in epigenetic changes in tumor cells and so tumor cell death; although the exact mechanism has yet to be defined, tumor cell death may occur through the induction of apoptosis, differentiation, cell cycle arrest, inhibition of DNA repair, upregulation of tumor suppressors, down regulation of growth factors, oxidative stress, and autophagy, among others. Overexpression of Class I HDACs 1, 2 and 3 has been found in many tumors and has been correlated with a poor prognosis. C62521 486962 lanreotide long-acting aqueous gel A long-acting aqueous gel preparation of lanreotide, a synthetic cyclic octapeptide analogue of somatostatin. Lanreotide inhibits the secretion of growth hormone (GH) by binding to pituitary somatostatin receptors, and may inhibit the release of various other hormones, including thyroid stimulating hormone (TSH) and the gastroenteropancreatic hormones insulin, glucagon and gastrin. This agent also decreases circulating total and free insulin-like growth factor 1 (IGF-I). Lanreotide exhibits a high binding affinity for somatostatin receptor 2 (SSTR-2) and a lesser binding affinity for SSTR-5. However, compared to octreotide, this agent is less potent in inhibiting the release of growth hormone from the pituitary gland. 487002 catumaxomab A trifunctional bispecific monoclonal antibody with potential antineoplastic activity. Catumaxomab has two antigen-recognition sites: one for human CD3, a T cell surface antigen; and one for human epithelial cell adhesion molecule (EpCAM), a cell surface antigen expressed by a variety of epithelial tumor cells. In addition, the modified Fc portion of this antibody binds Fc receptors on antingen presenting cells (APCs) such as macrophages and dendritic cells (DCs). Catumaxomab brings T cells, EpCAM-expressing epithelial tumor cells and APCs together into tricellular complexes, which may result in a potent cytotoxic T-lymphocyte (CTL) response against EpCAM-expressing epithelial tumor cells. Fc-mediated binding of APCs in the tricellular complex potentiates EpCAM antigen presentation to T cells and the activation of anti-tumor cytotoxic T cell functions. C62445 487160 attenuated Listeria monocytogenes CRS-100 A live-attenuated strain of the Gram-positive bacterium Listeria monocytogenes (Lm) with potential immunostimulatory and antineoplastic activities. Upon intravenous administration, attenuated Listeria monocytogenes CRS-100 may accumulate in and infect liver cells where it may activate a potent innate immune response and an adaptive immune response involving the by recruitment and activation of T lymphocytes. This agent may potentiate the immune response to vaccines against various liver neoplasms. C62409 487486 14C BMS-275183 The orally bioavailable C-4 methyl carbonate analogue of paclitaxel, labeled with radioactive carbon 14, with radioisotope and potential antineoplastic activities. 14C BMS-275183 binds to tubulin and inhibits microtubule disassembly, which may result in cell cycle arrest at the G2/M phase and inhibition of cell division, and subsequently cell death. This agent may be useful for treating multi-drug resistant (MDR) tumors because it does not appear to be a substrate for P-glycoprotein. C62553 487509 indium In 111 chimeric monoclonal antibody 806 A recombinant chimeric, mouse-human monoclonal antibody IgG1, directed against the epidermal growth factor receptor (EGFR) and labeled with the radioisotope indium-111, with potential radioimaging activity. Indium 111 chimeric monoclonal antibody 806 binds to a specific epitope on EGFR-expressing tumor cells, allowing imaging of EGFR-expressing tumor cells using gamma scintigraphy. EGFR is a receptor tyrosine kinase that is involved in the regulation of cell growth and is found to be overexpressed on the cell surfaces of many tumor cell types. C62407 487522 oligofructose-enriched inulin A mixture of non-digestible carbohydrates, containing the fermentable plant fructans oligosaccharide and inulin, with potential prebiotic activity. Resisting hydrolysis by intestinal digestive enzymes, inulin and oligofructose serve as growth media and energy substrates for bifidobacteria in the colon; beneficial colonic commensal bacteria such as bifidobacteria may inhibit the colonization of the intestine by pathogenic bacteria and have been inplicated to inhibit colon carcinogenesis. Oligofructose-enriched inulin may be administered in combination with probiotic bifidobacteria. In addition, this agent may promote the absorption of calcium and magnesium from the gastrointestinal tract. 487523 fluphenazine hydrochloride The hydrochloride salt of fluphenazine, a phenothiazine with antipsychotic activity and potential antineoplastic activity. Fluphenazine blocks postsynaptic dopamine D2 receptors in the limbic system, cortical system and basal ganglia, resulting a reduction of schizophrenia-associated hallucinations and delusions. In addition, as a serotonin antagonist, this agent may inhibit lymphocyte and myeloma cell proliferation by blocking 5-hydroxytrptamine type 1B (5-HT type 1B) receptors for serotonin. 487532 ARRY-334543 An orally bioavailable inhibitor of the epidermal growth factor receptor family with potential antineoplastic activity. ARRY-334543 selectively and reversibly binds to both EGFR (ErbB-1) and Her-2/neu (ErbB-2) and prevents their phosphorylation and activation, which may result in inhibition of the associated signal transduction pathways, inhibition of cellular proliferation and cell death. EGFR and Her-2 play important roles in cell proliferation and differentiation and are upregulated in various human tumor cell types. Due to the dual inhibition of both EGFR and Her-2, this agent may be therapeutically more effective than agents that inhibit EGFR or Her-2 alone. C62530 487535 psilocybin A tryptamine alkaloid, isolated from various genera of fungi including the genus Psilocybe, with hallucinogenic, anxiolytic, and psychoactive activities. In vivo, psilocybin is rapidly dephosphorylated into the active compound psilocin, which activates serotonin 2A (5-HT2A) receptors in the central nervous system (CNS), mimicking the effects of serotonin. C62529 487588 fluvastatin sodium The sodium salt of a synthetic lipid-lowering agent with potential antineoplastic activity. Fluvastatin competitively inhibits hepatic 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase, the enzyme that catalyzes the conversion of HMG-CoA to mevalonate, a key step in cholesterol synthesis. This agent lowers plasma cholesterol and lipoprotein levels, and modulates immune responses through the suppression of MHC II (major histocompatibility complex II) on interferon gamma-stimulated, antigen-presenting cells such as human vascular endothelial cells. Through the inhibition of mevalonate synthesis, statins, like fluvastatin, have been shown to inhibit the production of dolichol, geranylpyrophosphate (GPP) and farnesylpyrophosphate (FPP) and the isoprenylation of the intracellular G-proteins Ras and Rho, which may result in antiangiogenic, apoptotic, and antimetastatic effects in susceptible tumor cell populations. 487684 blinatumomab A recombinant, single-chain, anti-CD19/anti-CD3 bispecific monoclonal antibody with potential immunostimulating and antineoplastic activities. Blinatumomab posesses two antigen-recognition sites, one for the CD3 complex, a group of T cell surface glycoproteins that complex with the T cell receptor (TCR), and one for CD19, a tumor-associated antigen (TAA) overexpressed on the surface of B cells. This bispecific monoclonal antibody brings CD19-expressing tumor B-cells and cytotoxic T lymphocytes (CTLs) and helper T lymphocytes (HTLs) together, which may result in the CTL- and HTL-mediated cell death of CD19-expressing B-lymphocytes. C62528 488459 adenovirus encoding rat Her-2/neu A replication-defective oncolytic adenovirus, encoding rat Her-2/neu (ErbB-2), with potential antineoplastic activity. Upon administration, adenovirus encoding rat HER-2/neu may induce an immune response against tumor cells expressing the HER-2/neu antigen, which may result in the immune-mediated inhibition of tumor cell proliferation and tumor cell death. Her-2/neu, a tumor-associated antigen and member of the epidermal growth factor receptor (EGFR) family of tyrosine kinases, is overexpressed in various tumor cell types. C62527 488465 PARP-1 inhibitor BSI-201 A small-molecule prodrug inhibitor of the nuclear enzyme poly(ADP-ribose) polymerase-1 (PARP-1) with potential chemosensitizing, radiosensitizing and antineoplastic activities. In vivo, PARP-1 inhibitor BSI-201 is converted to the active drug, which selectively binds to PARP-1 and inhibits PARP-1- mediated DNA repair. Consequently, this agent may enhance the cytotoxicity of DNA-damaging agents and reverse tumor cell resistance to chemotherapy and radiation therapy. In addition, PARP-1 inhibitor BSI-201 may exhibit direct antineoplastic activity against cancers defective in DNA repair. PARP-1 catalyzes post-translational ADP-ribosylation of nuclear proteins and is activated by single-strand DNA (ssDNA) breaks. C62526 488467 human monoclonal antibody 216 A naturally-occurring human IgM monoclonal antibody with potential antineoplastic activity. Human monoclonal antibody 216, derived from the gene VH4-34, binds to the glycosylated epitope CDIM on the surface of both malignant and normal B cells. Upon binding to B cells, this antibody may crosslink two or more CDIM molecules, resulting in the formation of cell membrane pores, the disruption of cell membrane integrity, and B cell lysis; this mechanism of antibody-mediated cell death is direct and does not involve mechanisms of complement-mediated cytotoxicity or antibody-depndent cell-mediated cytotoxicity (ADCC). CDIM is the glyco-moiety of a 75 kD MW B-cell cell surface glycoprotein. C62532 488470 folate-vinca alkaloid conjugate EC145 A water-soluble, folate-receptor-targeted conjugate of folate and the vinca alkaloid desacetylvinblastine monohydrazide (DAVLBH) with potential antineoplastic activity. The folate moiety of folate-vinca alkaloid conjugate EC145 binds to folic acid receptors on the tumor cell surface and the agent is internalized via folate receptor-mediated endocytosis, delivering the tubulin-binding DAVLBH moiety directly into the tumor cell; DAVLBH binding to tubulin results in the disruption of microtubule assembly-disassembly dynamics, cell cycle arrest, and tumor cell apoptosis. Folic acid receptors are frequently upregulated on the surfaces of many tumor cell types. DAVLBH is a derivative of the natural product vinblastine. C62525 488475 18F-FHBG A fluorine-18-labeled acycloguanosine derivative substrate for herpes simplex virus type-1 thymidine kinase (HSV1-tk). 18F-FHBG is used as a reporter probe to image the expression of the herpes simplex virus type-1 thymidine kinase (HSV1-tk) gene in gene transfer therapy. HSV1-tk and and HSV1-tk-metabolized 18F-FHBG co-localize, allowing positron emission tomography (PET) localization of HSV1-tk gene-transfected tissue and the assessment of gene transfer efficiency. C62533 488482 Seneca Valley virus-001 A native, replication-competent oncolytic picornavirus with potential antineoplastic activity. Administered systemically, Seneca Valley virus-001 (SVV-001) specifically targets and infects tumor cells with neuroendocrine characteristics. Upon infection, this agent replicates intracellularly, resulting in tumor cell lysis and reduced tumor cell proliferation. The selective tropism of virus replication may involve receptor-mediated internalization. C62524 488948 CDK inhibitor SNS-032 A 2-aminothiazole-derived, small-molecule cyclin dependent kinase (CDK) inhibitor with potential antineoplastic activity. CDK inhibitor SNS-032 selectively binds to CDKs 2, 7, and 9, preventing their phosphorylation and activation; inhibition of CDK activity may result in cell cycle arrest, the induction of apoptosis and decreased tumor cell proliferation in susceptible tumor cell populations. This agent has been shown to sensitize radioresistant tumor cells to ionizing radiation. C62523 488957 c-Met inhibitor ARQ 197 An orally bioavailable small molecule inhibitor of c-Met with potential antineoplastic activity. c-Met inhibitor ARQ 197 binds to the c-Met protein and disrupts c-Met signal transduction pathways, which may induce cell death in tumor cells overexpressing c-Met protein or expressing consitutively activated c-Met protein. c-Met protein, the product of the proto-oncogene c-Met, is a receptor tyrosine kinase also known as hepatocyte growth factor receptor (HGFR); this protein is overexpressed or mutated in many tumor cell types and plays key roles in tumor cell proliferation, survival, invasion, and metastasis, and tumor angiogenesis. C62437 488976 dovitinib lactate The orally bioavailable lactate salt of a benzimidazole-quinolinone compound with potential antineoplastic activity. Dovitinib strongly binds to fibroblast growth factor receptor 3 (FGFR3) and inhibits its phosphorylation, which may result in the inhibition of tumor cell proliferation and the induction of tumor cell death. In addition, this agent may inhibit other members of the RTK superfamily, including the vascular endothelial growth factor receptor; fibroblast growth factor receptor 1; platelet-derived growth factor receptor type 3; FMS-like tyrosine kinase 3; stem cell factor receptor (c-KIT); and colony-stimulating factor receptor 1; this may result in an additional reduction in cellular proliferation and angiogenesis, and the induction of tumor cell apoptosis. The activation of FGFR3 is associated with cell proliferation and survival in certain cancer cell types. C62435 488984 vascular-disrupting agent NPI-2358 An orally active diketopiperazine derivative with potential antineoplastic activity. Vascular disrupting agent NPI-2358 selectively binds to the colchicine-binding site of tubulin, thereby interrupting equilibrium of microtubule dynamics; mitotic spindle assembly is disrupted, resulting in cell cycle arrest at the M phase and blockage of cell division in tumor cells. In addition, this agent induces tubulin depolymerization in vascular endothelial cells, resulting in the disruption of tumor blood vessel architecture and a selective collapse of tumor vasculature. C62444 489092 PHA-739358 A small-molecule 3-aminopyrazole derivative with potential antineoplastic activity. Aurora kinase inhibitor PHA-739358 binds to and inhibits the Aurora kinases, which may result in cell growth arrest and apoptosis in tumor cells in which Aurora kinases are overexpressed. This agent may preferentially bind to and inhibit Aurora B kinase. Aurora kinases, a family of serine-threonine kinases, are important regulators of cellular proliferation and division. C61587 489119 recombinant parathyroid hormone A recombinant therapeutic agent that is identical or similar to an 84-amino-acid polypeptide produced by the parathryoid gland which functions to maintain a constant concentration of calcium ions (Ca2+) in the extracellular fluid. In target tissues, parathyroid hormone (PTH) binds to and activates the parathryorid hormone receptor (PTHR), a cell surface G protein-coupled receptor; there are two types of receptors, parathyroid hormone receptor 1 (PTH1R) found in bone and the kidney and parathyroid hormone receptor 2 (PTH2R) found primarily in the central nervous system (CNS), pancreas, testis, and placenta. Activation of PTHRs results in the activation of adenylyl cyclase and phospholipase C in target tissue cells, which, depending upon the specific target tissue, results in the enhancement of intestinal Ca2+ absorption, mobilization of bone Ca2+, and renal Ca2+ reabsorption. C62555 489120 anti-CD137 monoclonal antibody A humanized agonistic monoclonal antibody targeting the CD137 receptor with potential immunostimulatory and antineoplastic activities. Anti-CD137 monoclonal antibody specifically binds to and activates CD137-expressing immune cells, stimulating an immune response, in particular a cytotoxic T cell response, against tumor cells. CD137 is a member of the tumor necrosis factor (TNF)/nerve growth factor (NGF) family of receptors and is expressed by activated T- and B-lymphocytes and monocytes; its ligand has been found to play an important role in the regulation of immune responses. C62449 489121 NY-ESO-1 plasmid DNA cancer vaccine A plasmid DNA encoding an immunogenic peptide derived from the cancer-testis antigen NY-ESO-1 with potential immunostimulating and antitumor activities. Upon adninstration, NY-ESO-1 plasmid DNA cancer vaccine may stimulate the host immune system to mount a cytotoxic T lymphocyte (CTL) response against tumor cells expressing the NY-ESO-1 antigen, resulting in tumor cell lysis. NY-ESO-1 is a tumor associated antigen (TAA) found in normal testes and expressed on the surfaces of various tumor cells, including melanoma, breast, bladder, prostate, lung, ovarian, and hepatocellular tumor cells. C62452 489122 oral topotecan hydrochloride An oral formulation of the hydrochloride salt of topotecan, a semisynthetic derivative of the quinoline alkaloid camptothecin, with potential antineoplastic activity. Topotecan selectively inhibits topoisomerase I activity by stabilizing topoisomerase I-DNA covalent complexes during the S phase of the cell cycle, thereby inhibiting religation of topoisomerase I-mediated single-strand DNA breaks and producing potentially lethal double-strand DNA breaks when encountered by the DNA replication machinery. C63477 489132 CHP-NY-ESO-1 peptide vaccine IMF-001 A peptide cancer vaccine containing nanoparticles of cholesteryl hydrophobized pullulan (CHP) complexed with the cancer-testis antigen NY-ESO-1 protein, with potential immunostimulating and antineoplastic activities. Upon administration, CHP-NY-ESO-1 peptide vaccine IMF-001 may stimulate the host immune system to mount a humoral and cytotoxic T-cell response against tumor cells expressing NY-ESO-1 antigen, resulting in tumor cell lysis. The self-aggregating CHP, composed of a pullulan backbone and cholesterol branches, forms stable colloidal nanoparticles in water.\n\nNY-ESO-1, an antigen found in normal testis, is upregulated in various cancers, including bladder, breast, hepatocellular, melanoma, and prostate cancers. C62598 489137 picibanil A lyophilized formulation containing cultures of a low-virulent strain of Streptococcus pyogenes, treated and killed with pencillin G, with potential sclerosing, immunostimulating and antineoplastic activities. Besides its activity as a sclerosing agent, picibanil appears to have multiple effects on the immune system as a non-specific immunostimulant. This agent activates the host immune system by stimulating the activity of natural killer (NK) cells, macrophages and lymphocytes, and by enhancing the production of several key immune mediators, including interleukins (ILs) and tumor necrosis factor (TNF). 489285 KLH-FITC A conjugate consisting of keyhole-limpet hemocyanin (KLH) and fluorescein isothiocyanate (FITC) with potential immunostimulating activity. Vaccination with KLH-FITC may elicit an immune response against fluorescein and the production of anti-fluorescein IgG antibodies. KLH, a natural protein isolated from the marine mollusk keyhole limpet, is an immunostimulant carrier protein. C62478 489286 folate-FITC A conjugate consisting of fluorescein isothiocyanate (FITC) conjugated with folate with potential antineoplastic activity. Folate-FITC binds to folate receptors, which are overexpressed on the surfaces of many cancer cells including kidney and ovarian cancer cells. Once bound to the cancer cell through the folate moiety of the conjugate, curculating anti-fluorescein antibodies.may recognize and bind to the FITC moiety, resulting in antibody-dependent cellular cytotoxicity. C62479 489294 indium In 111-CMD-193 A radiolabeled antibody-targeted antineoplastic antibiotic consisting of the enediyne antibiotic calicheamicin conjugated with anti-Lewis Y antibody and labeled with indium In 111. In 111 CMD-193 binds to Lewis Y antigen-expressing tumor cells via its antibody moiety and is internalized; subsequently, the calicheamicin moiety binds to the minor groove of tumor cell DNA, causing double-strand DNA breaks, the inhibition of DNA synthesis, and apoptosis. The indium In 111 radiolabel allows the detection of CMD-193 distribution and tumor localization using gamma scintigraphy. C62481 489295 immunoconjugate CMD-193 A humanized monoclonal antibody directed against the Lewis Y antigen conjugated with calicheamicin, a hydrophobic enediyne antibiotic, with potential antineoplastic activity. Upon binding to Lewis Y antigen-expressing tumor cells, immunoconjugate CMD-193 is internalized, delivering the calicheamicin moiety specifically; calicheamicin binds non-covalently to the minor groove of DNA and prompts conformational changes and DNA oxidation, thereby inhibiting DNA synthesis and inducing apoptosis. Lewis Y antigen is a tetrasaccharide that is expressed on the cell surfaces of many tumor cell types. C52176 489297 anti-IGF-1R recombinant monoclonal antibody MK-0646 A recombinant monoclonal antibody directed against the insulin-like growth factor 1 receptor (IGF1R) with potential antineoplastic activity. Anti-IGF1R recombinant monoclonal antibody MK-0646 binds to membrane-bound IGF1R, preventing binding of the ligand IGF1 and the subsequent triggering of the PI3K/Akt signaling pathway; inhibition of this survival signaling pathway may result in the inhibition of tumor cell proliferation and the induction of tumor cell apoptosis. The activation of IGF1R, a tyrosine kinase and a member of the insulin receptor family, stimulates cell proliferation, enables oncogenic transformation, and suppresses apoptosis; IGF1R signaling has been highly implicated in tumorigenesis and metastasis. C74011 489323 CS-1008 A humanized agonistic monoclonal antibody directed against human tumor necrosis factor-related apoptosis-inducing ligand receptor 2 (TRAIL-R2) with potential antitumor activity. Mimicking the natural receptor ligand TRAIL, CS-1008 binds to TRAIL-R2, activating signal transduction pathways that may result in tumor cell apoptosis and a reduction in tumor growth. A member of the tumor necrosis factor (TNF) receptor family, TRAIL-R2, also known as DR5 (death receptor 5), is expressed on the surfaces of many types of malignant cells. C62482 489384 anti-mesothelin monoclonal antibody MORAb-009 A humanized IgG1 monoclonal antibody directed against human mesothelin with potential antineoplastic activity. Anti-mesothelin monoclonal antibody MORAb-009 binds to mesothelin, triggering an antibody dependent cellular cytotoxicity (ADCC)-mediated host immune response against mesothelin-expressing tumor cells, which may result in tumor cell lysis. Mesothelin, a 40kDa cell surface glycoprotein, is overexpressed in several human tumors, including mesothelioma and ovarian and pancreatic adenocarcinomas. C62483 489385 AR antagonist BMS-641988 A nonsteroidal androgen receptor (AR) antagonist with anti-androgenic and potential antineoplastic activities. AR antagonist BMS-641988 binds to ARs in target tissues and prevents AR activation, which may result in the inhibition of AR-mediated transcriptional activity and tumor cell death in susceptible tumor cell populations. Global gene expression analysis has shown that exposure to this agent may result in a phenotype that is closer to a castration phenotype than is achievable with other antiandrogens such as bicalutamide. C62522 489463 ferumoxsil oral suspension An orally administered aqueous suspension of silicone-coated,\nsuperparamagnetic iron oxide used as a magnetic resonance imaging (MRI) contrast agent. After oral administration, ferumoxsil fills the stomach and intestines. Upon exposure to the strong external magnetic field during MRI, ferumoxsil exhibits strong T1 relaxation properties and a strongly varying local magnetic field; T2 relaxation is enhanced, thereby darkening the contrast agent-containing portion of the gastrointestinal tract. Delineation of the bowel is thus enhanced, distinguishing bowel from\norgans and tissues adjacent to the upper regions of the gastrointestinal\ntract. C62485 489464 arginine/omega-3 fatty acids/nucleotides oral supplement An oral nutritional supplement, containing substantial amounts of polyunsaturated fatty acids, arginine, and nucleotides, with potential immunostimulating activity. Omega-3 fatty acids/arginine/nucleotides oral supplement may enhance activities of key components of the immune system, including lymphocytes, antigen presenting cells (APCs), and various cytokines. C62534 489507 camptothecin-polymer conjugate IT-101 A formulation consisting of camptothecin conjugated to a hydrophilic, cyclodextrin-based linear polymer with potential antineoplastic activity. Upon intravenous administration, camptothecin is slowly released from camptothecin-polymer conjugate IT-101 at the tumor site and taken up by tumor cells. During the S phase of the cell cycle, camptothecin selectively stabilizes topoisomerase I-DNA covalent complexes, thereby inhibiting religation of topoisomerase I-mediated single-strand DNA breaks and producing potentially lethal double-strand DNA breaks when encountered by the DNA replication machinery. Compared to camptothecin alone, this formulation exhibits a prolonged half life and improved biodistribution, enhancing tumor exposure while reducing systemic side effects. In addition, camptothecin-polymer conjugate IT-101 may overcome certain types of multidrug resistance (MDR). C62600 489533 ondansetron hydrochloride The hydrochloride salt of the racemic form of ondansetron, a carbazole derivative and a selective, competitive serotonin 5-hydroxytrptamine type 3 (5-HT3) receptor antagonist with antiemetic activity. Although its mechanism of action has not been fully characterized, ondansetron appears to competitively block the action of serotonin at 5HT3 receptors peripherally in the gastrointestinal tract as well as centrally in the area postrema of the CNS, where the chemoreceptor trigger zone (CTZ) for vomiting is located, resulting in the suppression of chemotherapy- and radiotherapy-induced nausea and vomiting. 491866 radium-223 chloride The chloride salt of the radioisotope radium-223 with bone-targeting, radioisotopic and potential antineoplastic activities. Upon administration, short-lived alpha-particle-emitting radium-223 localizes to bone metastases and kills tumor cells, with minimal effects on the surrounding population of normal cells. C62535 491929 berubicin hydrochloride The hydrochloride salt of the anthracycline derivative berubicin with potential antineoplastic activity. Berubicin intercalates into DNA and interrupts topoisomerase II activity, resulting in the inhibition of DNA replication and repair, and RNA and protein synthesis. Unlike other anthracycline derivatives, this agent crosses the blood-brain barrier (BBB). 491931 polyvinylpyrrolidone-sodium hyaluronate gel An oral bioadherent gel containing polyvinylpyrrolidone (PVP) and sodium hyaluronate with muco-protective activity. Upon oral application, this gel adheres to the mucosal surface of the mouth and throat, forming a thin layer that acts as a barrier to protect exposed and sensitized nerve endings from the painful stimuli associated with eating, drinking, and talking. C61593 491935 lyso-thermosensitive liposome doxorubicin A temperature-sensitive liposomal formulation of the anthracycline antibiotic doxorubicin with potential antineoplastic activity. Upon intravenous administration, circulating thermosensitive liposomes are activated locally by increasing the tumor temperature to 40-41 degrees Celsius using an external heat source. The elevated temperature causes compositional changes in the liposomes, creating openings that allow for the release of encapsulated doxorubicin. Compared to non-thermosensitive liposomes, lyso-thermosensitive liposomes deliver higher concentrations of a cytotoxic agent to a heat-treated tumor site while sparing normal tissues unexposed to heat treatment. C61571 491973 eltrombopag olamine The orally active ethanolamine salt of eltrombopag, a small-molecule, nonpeptide thrombopoietin receptor agonist with megakaryopoiesis-stimulating activity. Eltrombopag binds to and stimulates the transmembrane domain of the platelet thrombopoietin receptor (TPO-R or CD110), a member of the hematopoietin receptor superfamily. Activation of TPO-R leads to the proliferation and differentiation of cells in the megakaryocytic lineage and an increase in platelet production. C62501 491988 gp100-fowlpox vaccine A cancer vaccine comprised of a recombinant fowlpox virus vector encoding the melanoma antigen glycoprotein 100 (gp 100) with potential antineoplastic activity. The expression of gp100 may generate a cellular immune response to melanoma cells; this effect is enhanced by the co-administration of interleukin 2 (IL-2). 492218 AEG35156 A second-generation synthetic antisense oligonucleotide with potential antineoplastic activity. AEG35156 selectively blocks the cellular expression of X-linked inhibitor of apoptosis protein (XIAP), a pivotal inhibitor of apoptosis that is overexpressed in many tumors. This agent reduces total levels of XIAP in tumor cells, working synergistically with cytotoxic drugs to overcome tumor cell resistance to apoptosis. XIAP interferes with both the intrinsic and extrinsic program-death signaling pathways, which may render tumor cells resistant to apoptosis. C49180 492222 PR-104 A non-toxic, small-molecule, hypoxia-activated, 3,5-dinitrobenzamide nitrogen mustard pre-prodrug with potential antitumor activity. Upon intravenous administration, PR-104 is converted by systemic phosphatases to the alcohol intermediate PR-104A, which is reduced to form the active DNA-crosslinking mustard species hydroxylamine PR-104H intracellularly under hypoxic conditions. PR-104H specifically crosslinks hypoxic tumor cell DNA, resulting in the inhibition of DNA repair and synthesis, cell-cycle arrest, and apoptosis in susceptible hypoxic tumor cell populations while sparing normoxic tissues. 492229 siRNA-expressing SV40 vector A simian virus 40 (SV40)-based shuttle vector, encoding small interfering RNA (siRNA), with potential antineoplastic activity. The expression of siRNA in target tumor cells transfected with an siRNA-expressing SV40 vector may result in siRNA-mediated silencing of target oncogenes and, so, the inhibition of tumor cell growth and the induction of tumor cell death. C62536 492706 HuC242-DM4 An immunotoxin of a humanized monoclonal antibody C242 (MoAb HuC242) conjugated with a derivative of cytotoxic agent maytansine, DM4, with potential antitumor activity. huC242-DM4 is generated based on MoAb C242, which is raised against a cell surface superantigen, CA242, found in a variety of human tumor cells. Upon binding and entry, the immunoconjugate releases the maytansinoid agent DM4, which binds to tubulin, thereby affecting microtubule assembly/disassembly dynamics. As a result, this agent prevents cell division and reduces cell growth of cancer cells that express CA242. C61576 492712 gp100:280-288(288V) peptide vaccine A peptide vaccine consisting of the amino acids 280 through 288 of the melanoma antigen glycoprotein 100 (gp100) with potential antineoplastic activity. gp100:280-288(288V) peptide has a valine substitution at amino acid position 288 to improve immunogenicity. Vaccination with gp100:280-288(288V) peptide may stimulate the host immune system to mount a cytotoxic T lymphocyte (CTL) response against tumor cells positive for the gp100 antigen, resulting in decreased tumor growth. 492715 colloidal gold-bound tumor necrosis factor A nanoparticle delivery system for recombinant human tumor necrosis factor (TNF) consisting of recombinant TNF bound to pegylated colloidal gold nanoparticles with potential antineoplastic activity. Upon intravenous administration, colloidal gold-bound recombinant human TNF travels through the bloodstream, avoiding immune detection and uptake by the reticuloendothelial system because of nanoparticle pegylation. Due to their size, the colloidal gold nanoparticles exit the circulatory system only at hyperpermeable tumor neovasculature sites; TNF then binds to and activates tumor cell TNF receptors, which may result in an increase in tumor cell apoptosis and a reduction in tumor cell proliferation. Compared to the administration of unbound TNF, colloidal gold-bound TNF may improve the efficacy and safety of TNF administration by delivering TNF specifically to tumor tissue. C62538 494632 dapsone gel, 5% A gel containing 5% (w/w) dapsone, a synthetic derivative of diamino-sulfone with anti-infective properties. A structural analog of p-aminobenzoic acid (PABA), dapsone inhibits dihydropteroate synthase (DHPS), an enzyme important in folate synthesis, resulting in a depletion of the folate pool and a reduction in the amount of thymidylate available for DNA synthesis. 494707 fluoxymesterone A halogenated derivative of 17-alpha-methyltestosterone. Similar to testosterone, fluoxymesterone binds to and activates specific nuclear receptors, resulting in an increase in protein anabolism, a decrease in amino acid catabolism, and retention of nitrogen, potassium, and phosphorus. This agent also may competitively inhibit prolactin receptors and estrogen receptors, thereby inhibiting the growth of hormone-dependent tumor lines. Fluoxymesterone is approximately five times more potent than methyltestosterone. 494748 APF530 A controlled-release formulation of the 5-hydroxytryptamine 3 (5-HT3) antagonist granisetron, in which granisteron is encapsulated in a biodegradable poly(ortho ester) polymer, with antiemetic activity. Upon subcutaneous administration, APF530 slowly erodes and releases the active ingredient granisetron over a period of approximately 5 days. As a selective serotonin receptor antagonist, granisetron competitively blocks the action of serotonin at 5-HT3 receptors, resulting in the suppression of nausea and vomiting. C61567 494994 glutathione disulfide NOV-002 A stabilized formulation of disodium glutathione disulfide (GSSG; oxidized glutathione) and cisplatin (1000:1) with potential chemoprotective and immunomodulating activities. Mimicking endogenous GSSG, glutathione disulfide NOV-002 acts as a competitive substrate for gamma-glutamyl-transpeptidase (GGT), which may result in the S-glutathionylation of proteins, predominantly actin, a redox stress on endoplasmic reticulum (ER), and ER stress-induced apoptosis; S-glutathionylation may be stimulated by reactive oxygen species (ROS) liberated by a glutathione disulfide NOV-002-induced increase in GGT activity. Glutathione disulfide NOV-002 may also induce phosphorylation of proteins such as ERK and p38, two kinases that play critical regulatory roles in cell proliferation and apoptosis. The cisplatin component of this agent does not provide an effective therapeutic concentration of cisplatin in vivo. C62537 496464 veliparib A poly(ADP-ribose) polymerase (PARP) -1 and -2 inhibitor with chemosensitizing and antitumor activities. With no antiproliferative effects as a single agent at therapeutic concentrations, ABT-888 inhibits PARPs, thereby inhibiting DNA repair and potentiating the cytotoxicity of DNA-damaging agents. PARP nuclear enzymes are activated by DNA single or double strand breaks, resulting in the poly(ADP-ribosyl)ation of other nuclear DNA binding proteins involved in DNA repair; poly(ADP-ribosyl)ation contributes to efficient DNA repair and to survival of proliferating cells exposed to mild genotoxic stresses as induced by as oxidants, alkylating agents or ionizing radiation. 496932 betulinic acid A pentacyclic lupane-type triterpene derivative of betulin (isolated from the bark of Betula alba, the common white birch) with antiinflammatory, anti-HIV and antineoplastic activities. Betulinic acid induces apoptosis\nthrough induction of changes in mitochondrial membrane potential, production of reactive oxygen\nspecies, and opening of mitochondrial permeability transition pores, resulting in the release of mitochondrial\napogenic factors, activation of caspases, and DNA fragmentation. Although originally thought to exhibit specific cytotoxicity against melanoma cells, this agent has been found to be cytotoxic against non-melanoma tumor cell types including neuroectodermal.and brain tumor cells. 496937 Aurora kinase inhibitor AZD1152 An orally bioavailable, small-molecule, dihydrogen phosphate prodrug of the pyrazoloquinazoline Aurora kinase inhibitor AZD1152–hydroxyquinazoline pyrazol anilide (AZD1152-HQPA) with potential antineoplastic activity. Upon administration and rapid conversion from the prodrug form in plasma, AZD1152-HQPA specifically binds to and inhibits Aurora kinase B, which results in the disruption of spindle checkpoint functions and chromosome alignment and, so, the disruption of chromosome segregation and cytokinesis. Consequently, cell division and cell proliferation are inhibited and apoptosis is induced in Aurora kinase B-overexpressing tumor cells. Aurora kinase B, a serine/threonine protein kinase that functions in the attachment of the mitotic spindle to the centromere, is overexpressed in a wide variety of cancer cell types. C62502 496938 TLN-4601 A small-molecule inhibitor of the RAS/RAF/MAPK signaling pathway with potential antineoplastic activity. TLN-4601 binds to and inhibits Ras kinase, thereby preventing the phosphorylation and activation of proteins downstream of the Ras signal transduction pathway, including serine/threonine kinase RAF (BRAF) and extracellular signal-regulated kinases 1 and 2 (ERK1 and ERK-2). This agent also selectively binds to the peripheral benzodiazepine receptor (PBR), a receptor highly expressed in certain tumor cell types cells, inducing cell cycle arrest and apoptosis in PBR-expressing cells. TLN-4601 can cross the blood-brain barrier (BBB). C62508 496939 IMP321 A T-cell immunostimulatory factor derived from the soluble form of lymphocyte-activation gene 3 (LAG-3) protein with potential antineoplastic activity. Upon administration, alone or in combination with tumor antigens, IMP321 binds, with high affinity, to MHC class II molecules expressed by dendritic cells (DC), which may result in DC maturation, DC migration to lymph nodes, enhanced DC cross-presentation of antigens to T cells, and antitumor cytotoxic T cell responses. C62509 496940 phosphorodiamidate morpholino oligomer AVI-4126 A c-Myc antisense phosphorodiamidate morpholino oligomer (PMO) with potential antineoplastic activity. Phosphorodiamidate morpholino oligomer AVI-4126 binds to c-Myc mRNA and blocks its translation, which may result in the death of tumor cells overexpressing c-Myc. Differing from traditional antisense oligodeoxynucleotides (ODNs), neutrally charged PMOs are composed of subunits of nucleic acid bases linked to a synthetic backbone and, so, are less prone to enzymatic degradation. c-Myc, a proto-oncogene overexpressed in a variety of cancers, is involved in cellular proliferation, differentiation, and apoptosis. C62518 497050 Hsp90 inhibitor CNF2024 An orally active, purine-scaffold, small-molecule inhibitor of heat shock protein 90 (HSP90) with potential antineoplastic activity. HSP90 inhibitor CNF2024 specifically blocks active HSP90, inhibiting its chaperone function and promoting the degradation of oncogenic signaling proteins involved in tumor cell proliferation and survival; this may result in the inhibition of cellular proliferation in susceptible tumor cell populations. HSP90, a chaperone protein upregulated in a variety of tumor cell types, regulates the folding and degradation of many oncogenic signaling proteins. C62517 497135 escitalopram oxalate The oxalate salt of escitalopram, a pure S-enantiomer of the racemic bicyclic phthalane derivative citalopram, with antidepressant activity. As a selective serotonin reuptake inhibitor (SSRI), escitalopram blocks the reuptake of serotonin by neurons in the central nervous system (CNS), thereby potentiating CNS serotonergic activity. 500040 SOD1 inhibitor ATN-224 An orally bioavailable, second-generation tetrathiomolybdate analog with potnetial antiangiogenic and antineoplastic activities. SOD1 inhibitor ATN-224 selectively chelates the copper ion in copper-zinc superoxide dismutase 1 (SOD1), inhibiting SOD1 activity; this may result in a decrease in intra-cellular H2O2 levels and, in turn, increased activity of intracellular phosphatases. The ATN-224-mediated increase in phosphatase activity may interfere with the activation of multiple kinase signaling pathways required for cellular proliferation and angiogenesis. This agent has been shown to inhibit VEGF and FGF-2 signaling in endothelial cells, \nIGF-1, EGF, NF-kB, and integrin signaling in tumor cells, \nand PDGF signaling in pericytes. C62514 500041 bafetinib An orally bioavailable 2-phenylaminopyrimidine derivative with potential antineoplastic activity. Bafetinib specifically binds to and inhibits the Bcr/Abl fusion protein tyrosine kinase, an abnormal enzyme produced by Philadelphia chromosomal translocation associated with chronic myeloid leukemia (CML). This agent also inhibits the Src-family member Lyn tyrosine kinase, upregulated in imatinib-resistant CML cells and in a variety of solid cancer cell types. The inhibitory effect of bafetinib on these specific tyrosine kinases may decrease cellular proliferation and induce apoptosis in tumor cells that overexpress these kinases. CML patients may be refractory to imatinib, which sometimes results from point mutations occurring in the kinase domain of the Bcr/Abl fusion product. Due to its dual inhibitory activity, the use of bafetinib has been shown to overcome this particular drug resistance. C62516 500055 anti-CD20 monoclonal antibody AME-133v An Fc-engineered monoclonal antibody directed against human CD20 with potential antineoplastic activity. Anti-CD20 monoclonal antibody AME 133v specifically binds to CD20 antigen (B1), preventing mitogen-induced B-cell proliferation; inhibiting B-cell differentiation; and promoting antibody-dependent cell-mediated cytotoxicity (ADCC) and apoptosis of B cells expressing CD20. The Fc portion of this monoclonal antibody has been engineered to possess a higher binding affinity for variant Fc receptors on T helper cells, resulting in an augmentation of the anti-tumor immune response. Because of Fc engineering, this agent may be significantly more potent than rituximab in inducing B cell-directed ADCC. CD20 is a non-glycosylated cell surface phosphoprotein that is exclusively expressed on B cells during most stages of B cell development. C2524 500062 F-18 16 alpha-fluoroestradiol A radiopharmaceutical consisting of an estradiol analogue radiolabeled with the positron-emitting isotope fluorine F 18. F-18 16 alpha-fluoroestradiol is actively taken up in tumor cells expressing the estrogen receptor (ER), allowing visualization of ER-positive tumor cells with positron emiision tomography (PET). Uptake of this agent depends upon the ER status of target tissues. C62541 500063 citalopram hydrobromide The orally bioavailable hydrobromide salt of the racemic bicyclic phthalene derivative citalopram with antidepressant activity. As a selective serotonin reuptake inhibitor (SSRI), citalopram selectively inhibits the CNS neuronal reuptake of serotonin, thereby potentiating serotonergic activity in the central nervous system (CNS). This agent has minimal effects on the CNS neuronal reuptake of norepinephrine (NE) and dopamine (DA). C28932 500066 titanium dioxide/zinc oxide sunscreen cream SPF 60 A sunscreen formulated with titanium dioxide and zinc oxide with broad UV spectrum-blocking properties. Upon topical application, titanium dioxide and zinc oxide reflect and block both UVA and UVB ultraviolet light rays, protecting the skin against UVA and UVB radiation that causes sunburn, premature aging of the skin and skin cancer.SPF30 and SPF60 contain 5% titanium dioxide and zinc oxide, and 7.5% titanium dioxide and zinc, oxide respectively. C62540 500373 liposomal oxaliplatin A liposomal formulation of the prodrug oxaliplatin, an organoplatinum complex in which the platinum atom is complexed with 1,2-diaminocyclohexane (DACH) and with an oxalate ligand as a 'leaving group', with antineoplastic activity. After displacement of the labile oxalate ligand leaving group, the active oxaliplatin derivatives monoaquo and diaquo DACH platinum alkylate macromolecules, and form both inter- and intra-strand platinum-DNA crosslinks; inhibition of DNA replication and transcription and cell-cycle nonspecific cytotoxicity ensue. The DACH side chain appears to inhibit alkylating-agent resistance. A leaving group is an atom or a group of atoms that is displaced as a stable species taking with it its bonding electrons. C65110 500377 ampicillin sodium/sulbactam sodium A combination formulation of the sodium salts of the antibiotic ampicillin and the beta-lactamase inhibitor sulbactam with antibacterial activity. Ampicillin, a broad-spectrum, semisynthetic penicillin, binds to and inactivates penicillin-binding proteins (PBP) located on the inner membrane of the bacterial cell wall, thereby interfering with the cross-linking of peptidoglycan chains necessary for bacterial cell wall strength and rigidity. As a result, the cell wall is weakened and the cell lyses. The sulbactam component irreversibly binds to bacterial beta-lactamase at or near its active site, thereby interfering with substrate binding and inhibiting bacterial metabolism of penicillin and cephalosporin beta-lactam antibiotics, effectively extending their antibiotic spectrum to include many beta-lactam-resistant bacteria. C28823 500479 KW-0761 A humanized monoclonal antibody directed against C-C chemokine receptor 4 (CCR4) with potential anti-inflammatory and antineoplastic activities. KW-0761 selectively binds to and blocks the activity of CCR4, which may inhibit CCR4-mediated signal transduction pathways and, so, chemokine-mediated cellular migration and proliferation of T cells, and chemokine-mediated angiogenesis. In addition, this agent may induce antibody-dependent cell-mediated cytotoxicity (ADCC) against CCR4-positive T cells. CCR4, a G-coupled-protein receptor for C-C chemokines such MIP-1, RANTES, TARC and MCP-1, is expressed on the surfaces of some types of T cells, endothelial cells, and some types of neurons. CCR4, also known as CD194, may be overexpressed on adult T-cell lymphoma (ATL) and peripheral T-cell lymphoma (PTCL) cells. C62510 502114 telomerase peptide vaccine GV1001 A synthetic peptide vaccine containing a 16-amino-acid human telomerase reverse transcriptase peptide(hTERT: 611-626) with potential antineoplastic activity. Vaccination with telomerase peptide vaccine GV1001, which binds multiple HLA class II molecules and harbors putative HLA class I epitopes, may activate the immune system to mount a cytotoxic T-lymphocyte (CTL) response against telomerase-expressing tumor cells. Telomerase, a reverse transcriptase normally repressed in healthy cells, is overexpressed in most tumor cell types and plays a key role in cellular proliferation. C62756 502157 Clostridium novyi-NT spores Spores of Clostridium novyi-NT, an attenuated strain of the obligate anaerobe Clostridium novyi, with potential immunostimulating and oncolytic activities. Upon intravenous administration, Clostridium novyi-NT spores germinate exclusively in hypoxic tissue, such as avascular regions of tumors. Germination results in lysis and destruction of surrounding viable tumor cells. Although C. novyi-NT spores do not proliferate in oxygenated tumor regions, they may stimulate the immune system to mount a cytolytic immune response against tumor cells, both hypoxic and well-oxygenated. C62762 502184 PM00104 A synthetic tetrahydroisoquinoline alkaloid related to the marine natural compounds Jorumycin and the family of Renieramycins, obtained from molluscs and sponges, respectively, with potential antineoplastic activity. PM00104 reversibly binds to DNA and interferes with DNA replication, transcription, and translation. DNA binding by this agent does not trigger DNA damage checkpoint responses, hence PM00104 exhibits a reversible cytotoxicity. C62763 504100 obatoclax mesylate The mesylate salt of obatoclax, a synthetic small-molecule inhibitor of the bcl-2 family of proteins with potential pro-apoptotic and antineoplastic activities. Obatoclax binds to members of the Bcl-2 protein family, preventing the binding of these anti-apoptotic proteins to the pro-apoptotic proteins Bax and Bak and so promoting the activation of the apoptotic pathway in Bcl-2-overexpressing cells. The Bcl-2 family of proteins (bcl-2, bcl-xl, bcl-w, and Mcl-1) are overexpressed in a wide variety of cancers, including those of the lymphatic system, breast, lung, prostate, and colon. 504524 multitargeted tyrosine kinase inhibitor BIBF 1120 An orally bioavailable, indolinone-derived, receptor tyrosine kinase (RTK) inhibitor with potential antiangiogenic and antineoplastic activities. Multitargeted tyrosine kinase inhibitor BIBF 1120 selectively binds to and inhibits vascular endothelial growth factor receptor (VEGFR), fibroblast growth factor receptor (FGFR) and platelet-derived growth factor receptor (PDGFR) tyrosine kinases, which may result in the induction of endothelial cell apoptosis; a reduction in tumor vasculature; and the inhibition of tumor cell proliferation and migration. In addition, this agent also inhibits members of the Src family of tyrosine kinases, including Src, Lck, Lyn, and FLT-3 (fms-like tyrosine kinase 3). VEGFR, FGFR and PDGFR RTKs play key roles in tumor angiogenesis. C79846 504594 LMP-2:340-349 peptide vaccine A peptide cancer vaccine containing amino acid residues 340-349 of the Epstein-Barr virus (EBV) latent membrane protein-2 (LMP-2) with potential immunostimulating and antineoplastic activities. Vaccination with LMP-2:340-349 peptide may boost the immune system to mount a specific cytotoxic T-lymphocyte (CTL) response against LMP-2-expressing tumor cells, resulting in cell lysis and inhibition of tumor cell proliferation. LMP-2, an EBV transmembrane protein, is expressed in various malignancies including nasopharyngeal cancer and EBV-positive Hodgkin disease. 62767 504596 LMP-2:419-427 peptide vaccine A peptide cancer vaccine containing amino acid residues 419-427 of the latent membrane protein-2 (LMP-2) of the Epstein-Barr virus (EBV) with potential immunostimulating and antineoplastic activities. Vaccination with the LMP-2:49-427 peptide vaccine may boost the immune system to mount a specific cytotoxic T-lymphocyte response against LMP-2-expressing tumor cells, resulting in cell lysis and inhibition of tumor cell proliferation. LMP-2, an EBV transmembrane protein, is expressed in various malignancies including nasopharyngeal cancer and EBV-positive Hodgkin disease. 505287 gossypol An orally-active polyphenolic aldehyde with potential antineoplastic activity. Derived primarily from unrefined cottonseed oil, gossypol induces cell cycle arrest at the G0/G1 phase, thereby inhibiting DNA replication and inducing apoptosis. This agent also inhibits cell-signaling enzymes, resulting in inhibition of cell growth, and may act as a male contraceptive. 506041 defined green tea catechin extract A defined, decaffeinated green tea extract, containing polyphenolic flavonol catechins, isolated from the plant Camellia sinensis with antiviral, antioxidant, and potential chemopreventive activities. The primary catechins found in green tea are epicatechin (EC), epigallocatechin (EGC), epicatechin-3 gallate (ECG), and epigallocatechin-3-gallate (EGCG), the most potent. As potential chemopreventive agents, catechins scavenge free radicals; inhibit enzymes involved in cell replication and DNA synthesis; interfere with cell-to-cell contact adhesion; and inhibit various intracellular communication pathways required for cell division. In addition, it has been postulated that EGCG may "trap" growth factors such platelet-derived growth factor (PDGF) on cell membranes, immobilizing growth factors on cell membranes and preventing ligand-receptor crosslinking and growth factor receptor activation. C38689 506045 MAGE-A1, Her-2/neu, FBP peptides ovarian cancer vaccine A cancer vaccine containing multiple synthetic antigen peptides derived from MAGE-A1, Her-2/neu, and folate binding protein (FBP) with potential immunostimulating and antineoplastic properties. MAGE-A1, Her-2/neu, FBP peptides cancer vaccine includes the antigen peptides MAGE-A1:161-169, FBP:191-199, Her-2/neu:369-377, MAGE-A1:96-104, and Her-2/neu:754-762. Upon administration, this cancer vaccine may stimulate the immune system to mount a cytotoxic T-cell (CTL) response against tumor cells expressing these antigen peptides, resulting in tumor cell lysis. MAGE-A1, Her-2/neu, and FBP proteins may be over-expressed in various cancer cell types, such as epithelial ovarian cancer cells. C62775 506112 Melan-A VLP vaccine A vaccine consisting of the melanocyte differentiation antigen Melan A (also called MART-1) encapsulated in noninfectious virus-like particles (VLPs) with potential immunostimulating and antineoplastic activities. Upon administration, Melan-A VLP vaccine may stimulate the immune system to exert a specific cytotoxic T lymphocyte (CTL) response against tumor cells expressing the Melan A antigen, resulting in tumor cell lysis. Melan A is upregulated in most melanomas. VLPs stimulate the immune system and promotes the CTL response. C61495 506118 tasisulam sodium The sodium salt of an acyl-sulfonamide with potential antineoplastic activity. Selectively toxic towards tumor cells, tasisulam appears to induce tumor cell apoptosis by a mitochondrial-targeted mechanism involving the loss of mitochondrial membrane potential and induction of reactive oxygen species (ROS). In combination with an angiogenesis inhibitor, this agent may exhibit synergistic antiangiogenic activity. 507579 vinorelbine liposomes injection An injectable, sphingomyelin/cholesterol liposome-encapsulated formulation of the semisynthetic vinca alkaloid vinorelbine with antineoplastic activity. Vinorelbine binds to tubulin and prevents formation of the mitotic spindle, resulting in cell cycle arrest in metaphase. Like other vinca alkaloids, vinorelbine may also interfere with the metabolism of nucleic acids, lipids, amino acids, cAMP, and glutathione, as well as other biological processes including calmodulin-dependent Ca2+-transport, ATPase activity, or cellular respiration. Liposomal delivery of vinorelbine may improve drug penetration into tumors and decreases drug clearance, increasing the duration of therapeutic effects while lowering the toxicity profile. C62790 507582 nimotuzumab A humanized monoclonal antibody directed against the epidermal growth factor receptor (EGFR) with potential antineoplastic activity. Nimotuzumab binds to and inhibits EGFR, resulting in growth inhibition of tumor cells that overexpress EGFR. This agent may act synergistically with radiation therapy. 508976 dextropropoxyphene hydrochloride The hydrochloride salt of the d-isomer of the synthetic opiate propoxyphene with weak narcotic analgesic activity. Dextropropoxyphene mimics the effects of endogenous opiates by binding to mu receptors located throughout the central nervous system. The binding results in GTP to GDP exchanges on the mu-G-protein complex, by which the effector adenylate cyclase is inactivated, decreasing intracellular cAMP. This, in turn, inhibits the release of various nociceptive neurotransmitters, such as substance P, gamma-aminobutyric acid (GABA), dopamine, acetylcholine, noradrenaline, vasopressin, and somatostatin. In addition, dextropropoxyphene closes N-type voltage-gated calcium channels and opens calcium-dependent inwardly rectifying potassium channels, which results in neuronal hyperpolarization, a reduction in neuronal excitability, and a further decrease in the perception of pain. C63538 508980 oxycodone hydrochloride The hydrochloride salt of oxycodone, a methylether of oxymorphone and semisynthetic opioid agonist with analgesic and antitussive properties. Oxycodone binds to mu-receptors in the central nervous system (CNS), thereby mimicking the effects of endogenous opiates. In addition to analgesia and a depressive effect on the cough center in the medulla, this agent may cause euphoria, anxiolysis, miosis, sedation, physical dependence, constipation, and respiratory depression, depending on dosage and variations in individual metabolism. 509172 minocycline-EDTA A combination preparation containing the broad-spectrum, semi-synthetic tetracycline antibiotic minocycline and the chelator ethylenediaminetetraacetate (EDTA) with antimicrobial and antibiofilm activities. Minocycline exhibits bacteriostatic activity by binding to the bacterial 30S ribosomal subunit and preventing binding of aminoacyl-tRNA to the mRNA-ribosome complex during protein translation; this results in an inhibition of bacterial protein synthesis and, consequently, an inhibition of bacterial cell growth. EDTA may cause the dispersal and killing of biofilms by chelating metal ions important to the stabilization of biofilm structure. The two agents in this combination may act synergistically to eradicate bacteria embedded in biofilms. C63545 509184 5-fluoro-2-deoxycytidine A fluorinated pyrimidine analogue antimetabolite with potential antineoplastic activity. As a prodrug, 5-fluoro-2-deoxycytidine is converted by intracellular deaminases to the cytotoxic agent 5-fluorouracil (5-FU). 5-FU is subsequently metabolized to active metabolites including 5-fluoro-2-deoxyuridine monophosphate (FdUMP) and 5-fluorouridine triphosphate (FUTP). FdUMP binds to and inhibits thymidylate synthase, thereby reducing the production of thymidine monophosphate, which leads to depletion of thymidine triphosphate and the inhibition of DNA synthesis and cell division. FUTP competes with uridine triphosphate (UTP) for incorporation into the RNA strand, which results in the inhibition of RNA and protein synthesis and cell proliferation. Other fluorouracil metabolites also get incorporated into both DNA and RNA, with further inhibition of cellular growth. C62785 510285 fondaparinux sodium The sodium salt form of fondaparinux, a synthetic glucopyranoside with antithrombotic activity. Fondaparinux sodium selectively binds to antithrombin III, thereby potentiating the innate neutralization of activated factor X (Factor Xa) by antithrombin. Neutralization of Factor Xa inhibits its activity and interrupts the blood coagulation cascade, thereby preventing thrombin formation and thrombus development. 511023 seliciclib An orally bioavailable, small-molecule cyclin-dependent kinase (CDK) inhibitor with potential proapoptotic and antineoplastic activities. Seliciclib primarily inhibits CDK2/E, CDK2/A, CDK7 and CDK9 by competing for their ATP binding sites, leading to a disruption of cell cycle progression. In addition, this agent appears to interfere with CDK-mediated phosphorylation of the carboxy-terminal domain of RNA polymerase II, inhibiting RNA polymerase II-dependent transcription, which may result in the down-regulation of antiapoptotic proteins such as induced myeloid leukemia cell differentiation protein Mcl-1. CDKs, serine/threonine kinases that play an important role in cell cycle regulation, are overexpressed in various malignancies. Mcl-1 belongs to the Bcl-2 family of antiapoptotic proteins and is a protein crucial to the survival of a range of tumor cell types. C62783 511037 dihydrotestosterone The most potent androgen, required for sex development. Dihydrotestosterone is synthesized from testosterone in the prostate gland, testes, hair follicles and adrenal glands by 5-alpha reductase. Dihydrotestosterone exerts its action similar to testosterone, which binds to and activates specific nuclear androgen receptors. After translocation into the nucleus, the activated hormone-receptor complex binds to the androgen response elements on the DNA and activates gene expressions that are required for sex development. Dihydrotestosterone is responsible for the formation of male primary sex characteristics and most male secondary sex characteristics during puberty, such as muscular growth, facial and body hair growth, and deepening of the voice. 512990 VEGFR-2 inhibitor peptide CT-322 A highly specific, synthetic peptide vascular endothelial growth factor receptor-2 (VEGFR-2) antagonist with potential antiangiogenic activity. Derived from human fibronectin using a proprietary protein engineering process, VEGFR-2 inhibitor peptide CT-322 may block the activation of VEGFR-2 by all known activating ligands, thereby inhibiting the growth of new tumor blood vessels. C62791 513165 sapacitabine An orally bioavailable pyrimidine analogue prodrug with potential antineoplastic activity. Sapacitabine is hydrolyzed by amidases to the deoxycytosine analogue CNDAC (2'-Cyano-2'-deoxyarabinofuranosylcytosine), which is then phosphorylated into the active triphosphate form. As an analogue of deoxycytidine triphosphate, CNDAC triphosphate incorporates into DNA strands during replication, resulting in single-stranded DNA breaks during polymerization due to beta-elimination during the fidelity checkpoint process; cell cycle arrest in the G2 phase and apoptosis ensue. The unmetabolized prodrug may exhibit antineoplastic activity as well. C64541 513166 ZYC300 A plasmid DNA encoding an inactivated form of the carcinogen activator cytochrome P450 1B1 (CYP1B1) encapsulated in biodegradable poly-DL-lactide-coglycolide microparticles with potential antineoplastic activity. Vaccination with ZYC300 may stimulate the immune system to elicit a cytotoxic T lymphocyte (CTL) response against the tumor-associated antigen (TAA) CYP1B1, which may result in the lysis of tumor cells expressing CYP1B1. CYP1B1, an extrahepatic monooxygenase of the cytochrome P450 family, is overexpressed in many cancers with only restricted expression in normal tissues. C64631 513167 EGFR/HER2 inhibitor AV-412 A second-generation, orally bioavailable dual kinase inhibitor with potential antineoplastic activity. EGFR/HER2 inhibitor AV-412 binds to and inhibits the epidermal growth factor receptor (EGFR) and the human epidermal growth factor receptor 2 (HER2), which may result in the inhibition of tumor growth and angiogenesis, and tumor regression in EGFR/HER2-expressing tumors. This agent may be active against EGFR/HER2-expressing tumor cells that are resistant to first-generation kinase inhibitors. EGFR and HER2 are receptor tyrosine kinases that play major roles in tumor cell proliferation and tumor vascularization. C64627 513177 CDKI AT7519 An orally bioavailable small molecule with potential antineoplastic activity. AT7519M selectively binds to and inhibits cyclin dependent kinases (CDKs), which may result in cell cycle arrest, induction of apoptosis, and inhibition of tumor cell proliferation. CDKs are serine/theronine kinases involved in regulation of the cell cycle and may be overexpressed in some types of cancer cells. C64761 513178 alpha-type-1 polarized dendritic cells A population of mature polarized dendritic cells with potent immunostimulating activity. Treating bone marrowed-derived dendritic cells (DCs) with interferon-alpha (IFN-a), polyinosinic:polycytidylic acid (poly I:C) and bacterial CpG-DNA produces mature but not exhausted alpha type-1 polarized DCs (alphaDC1) that are capable of: 1) high responsiveness to other lymphoid chemokines, and 2) producing high levels of interleukin-12p70 (IL-12p70), characteristics found in human type-1 polarized dendritic cells. When pulsed with specific tumor associated antigens (TAAs), alphaDC1 may induce a potent cytotoxic T lymphocyte (CTL) response against TAA-expressing tumor cells. C64846 514473 ciclopirox olamine lotion A lotion preparation of the olamine salt of ciclopirox, a synthetic hydroxypyridone derivative with broad-spectrum antifungal and anti-inflammatory activities. Although its mechanism of action is not well understood, ciclopirox may chelate trivalent cations, such as Fe3+ and Al3+, thereby inhibiting the availability of essential metal co-factors for enzymes, which may result in a loss of enzyme activities that are essential for cellular metabolism, organization of cell wall structure, and other crucial cell functions in a wide variety of fungal species. This agent may also disrupt DNA repair, cell division signals and mitotic spindles as well as some elements of intracellular transport in susceptible fungi. Ciclopirox exhibits anti-inflammatory activity by inhibiting 5-lipoxygenase and cyclooxygenase (COX). C65327 516002 DT(388)IL3 fusion protein A recombinant protein consisting of human interleukin 3 (IL3) fused to the first 388 amino acids of diphtheria toxin [DT(388)] with potential antineoplastic activity. Upon administration, the IL3 moiety of the DT(388)IL3 fusion protein binds to IL3 receptors on cells expressing the receptor. Subsequently, the DT(388) toxin moiety, containing both translocation and catalytic domains, translocates across the cell membrane endocytotically; within the cytosol, the catalytic domain catalyzes the ADP-ribosylation of, and inactivates, translation elongation factor 2 (EF-2), resulting in the inhibition of translation during protein synthesis. IL3 may be overexpressed by acute myeloid leukemia (AML) cells. C64769 517173 PRX302 A targeted prodrug consisting of a recombinant modified form of the Aeromonas protoxin proaerolysin (PA), bearing a prostate-specific protease cleavage site, with potential antineoplastic activity. When injected directly into the prostate, PRX302 is hydrolyzed to the active toxin aerolysin by the serine protease prostate specific antigen (PSA), a protein overexpressed by prostate cancers and prostate cells in hyperplastic prostatic tissue. Aaerolysin molecules then oligomerize to form ring-like heptamers that are incorporated into the lipid bilayers of cell membranes, forming large membrane channels and resulting in the leakage of cellular contents and lysis of PSA-expressing prostate cells. C64779 518286 iodine I 123 A radioactive isotope of iodine, a nonmetallic element of the halogen group with an atomic mass of 123 and a half-life of 13.2 hours with radioisotopic activity. Selectively accumulating in the thyroid tissue, iodine I 123 emits gamma rays that can be detected with gamma scintigraphy, allowing localization of thyroid tissue. This agent may be used as a tracer in whole body scintigraphy (WBS) to localize thyroid carcinoma metastases. C64794 518287 iodine I 124 A radioactive isotope of iodine, a nonmetallic element of the halogen group, with an atomic mass of 124 and a half-life of 4.18 days with radioisotopic activity. Selectively accumulating in thyroid tissue, iodine I 124 emits positrons that can be detected by positron emission tomography (PET), allowing localization of thyroid tissue. This radiosiotope also emits gamma rays. C64624 518288 pregabalin A 3-isobutyl derivative of gamma-amino butyric acid (GABA) with anti-convulsant, anti-epileptic, anxiolytic, and analgesic activities. Although the exact mechanism of action is unknown, pregabalin selectively binds to alpha2delta (A2D) subunits of presynaptic voltage-dependent calcium channels (VDCCs) located in the central nervous system (CNS). Binding of pregabalin to VDCC A2D subunits prevents calcium influx and the subsequent calcium-dependent release of various neurotransmitters, including glutamate, norepinephrine, serotonin, dopamine, and substance P, from the presynaptic nerve terminals of hyperexcited neurons; synaptic transmission is inhibited and neuronal excitability is diminished. Pregabalin does not bind directly to GABA-A or GABA-B receptors and does not alter GABA uptake or degradation. C64625 518289 zalutumumab A fully human IgG1 monoclonal antibody directed against the epidermal growth factor receptor (EGFR) with potential antineoplastic activity. Zalutumumab selectively binds to the EGFR receptor and blocks receptor binding of EGF and transforming growth factor-alpha (TGF-a), which results in the disruption of EGFR-mediated cell signaling, cell growth inhibition and apoptosis in EGFR-expressing tumor cells. In addition, this agent triggers antibody dependent cellular cytotoxicity (ADCC) in EGFR-expressing cells. EGFR is a cell surface receptor tyrosine kinase, overexpressed on many cancer cells. C64620 518315 tenifatecan A lipophilic preparation of 7-ethyl-10-hydroxycamptothecin (SN-38) with potential antineoplastic activity. Tenifatecan is an oil-in-water emulsion of tocopherol covalently linked, via a succinate linker, to SN-38, an active metabolite of the camptothecin derivative irinotecan. After the succinate linker is hydrolyzed in vivo, the active moiety SN-38 is released and selectively stabilizes topoisomerase I-DNA covalent complexes, thereby inhibiting religation of topoisomerase I-mediated single-stranded DNA breaks and inducing lethal double-stranded DNA breaks; DNA replication is inhibited and apoptosis is triggered. This agent may provide greater delivery and exposure of SN-38 to the tumor than can be achieved with irinotecan. C64772 518316 salinosporamide A A naturally-occurring salinosporamide, isolated from the marine actinomycete Salinospora tropica, with potential antineoplastic activity. Salinosporamide A irreversibly binds to and inhibits the 20S catalytic core subunit of the proteasome by covalently modifying its active site threonine residues; inhibition of ubiquitin-proteasome mediated proteolysis results in an accumulation of poly-ubiquitinated proteins, which may result in the disruption of cellular processes, cell cycle arrest, the induction of apoptosis, and the inhibition of tumor growth and angiogenesis. This agent more may more potent and selective than the proteasome inhibitor bortezomib. C64634 518325 PDGFR inhibitor CP-868596 An orally bioavailable small molecule, targeting the platelet-derived growth factor receptor (PDGFR), with potential antineoplastic activity. PDGFR inhibitor CP-868596 binds to and inhibits PDGFR, which may result in the inhibition of PDGFR-related signal transduction pathways, and, so, the inhibition of tumor angiogenesis and tumor cell proliferation. PDGFR, up-regulated in many tumor cell types, is a receptor tyrosine kinase essential to cell migration and the development of the microvasculature. C64639 518351 WT-1 analog peptide vaccine A peptide vaccine containing a human Wilms tumor 1 (WT-1) protein-derived epitope with potential antineoplastic activity. Vaccination with the WT-1 analog peptide vaccine may induce a cytotoxic T-lymphocyte (CTL) response against WT-1 expressing cells, resulting in tumor cell lysis and inhibition of tumor cell proliferation. WT-1, a zinc finger transcription factor, is overexpressed in most types of leukemia and in some solid cancers. C64635 520344 recombinant human mannose-binding lectin A recombinant protein similar or identical to human mannose-binding lectin (MBL) with antimicrobial activity. MBL is a plasma protein containing a carbohydrate recognition domain at one end and a collagen-like stalk domain at the other. The presence of multiple carbohydrate binding sites in a single molecule of MBL (also called mannose-binding protein, mannan-binding protein or or MBP) allows strong binding to mannose residues on the phospholipid bilayer of microbial pathogens. Upon binding, activation of the complement system leads to the deposition of complement components on the surface of the microorganisms (opsonisation), followed by their clearance by phagocytic cells. Administration of the agent to deficient individuals may restore lectin function in vivo. C1151 522717 KSP inhibitor AZD4877 A synthetic kinesin spindle protein (KSP) inhibitor with potential antineoplastic activity. KSP inhibitor AZD4877 selectively inhibits microtubule motor protein KSP (also called kinesin-5 or Eg5), which may result in the inhibition of mitotic spindle assembly; activation of the spindle assembly checkpoint; induction of cell cycle arrest during the mitotic phase; and cell death in tumor cells that are actively dividing. Because KSP is not involved in postmitotic processes, such as neuronal transport, this agent may be less likely to cause the peripheral neuropathy often associated with the tubulin-targeting agents. Eg5 is essential for the formation of bipolar spindles and the proper segregation of sister chromatids during mitosis. C64522 522726 silatecan AR-67 A synthetic, highly lipophilic derivative of camptothecin, with potential antineoplastic and radiosensitizing activities. Silatecan DB-67 binds to and stabilizes the topoisomerase I-DNA covalent complex, inhibiting the religation of topoisomerase I-mediated single-stranded DNA breaks and producing lethal double-stranded DNA breaks when encountered by the DNA replication machinery; inhibition of DNA replication and apoptosis follow. Camptothecin readily undergoes hydrolysis at physiological pH, changing its conformation from the active lactone structure to an inactive carboxylate form. Modifications on the E ring of camptothecin prevent binding of human serum albumin, which prefers the inactive carboxylate form, thereby enhancing the stability of the active lactone structure and resulting in prolonged agent activity. In addition, this agent may radiosensitize tumor cells. C64618 522734 Aurora kinase inhibitor R763 An orally bioavailable, synthetic, small-molecule multi-Aurora kinase inhibitor with potential antineoplastic activity. Aurora kinase inhibitor R763 selectively binds to and inhibits multiple Aurora kinases (AKs), which may result in the inhibition of cell division and proliferation, and the induction of apoptosis in tumor cells that overexpress AKs. Overexpressed in certain tumor cell types, AKs, a family of serine-threonine kinases, are important regulators of cell division and proliferation that are involved in controlling chromatid segregation. C64540 523273 anti-p53 T-cell receptor-transduced peripheral blood lymphocytes Human autologous peripheral blood lymphocytes (PBLs) transduced with an anti-p53 T cell receptor gene with potential antineoplastic activity. PBLs are harvested from a patient and pulsed with a retroviral vector that encodes the T-cell receptor gene specific for a mutated form of p53. The transduced PBLs are then expanded in culture. When reintroduced to the patient, these modified PBLs express the anti-p53 T cell receptor which binds to mutant p53-overexpressing tumor cells; PBL-mediated tumor growth inhibition may follow. Many tumor cell types overexpress mutant p53 proteins, which are associated with the loss of apoptosis regulation and abnormal cell proliferation. C64773 523327 recombinant interleukin-1-alpha A recombinant agent which is chemically identical to or similar to the endogenous protein cytokine interleukin-1 (IL-1). The IL-1 precursor is produced by monocytes, activated macrophages, and other cell types; mature IL-1 is generated by proteolytic cleavage by proteases such as IL-1-beta converting enzyme (ICE). This agent enhances T cell proliferation and B cell growth and differentiation and induces the expression of proinflammatory cytokines. 523412 carcinoembryonic antigen-expressing measles virus An attenuated oncolytic Edmonston (Ed) strain of measles virus (MV) encoding the soluble extracellular N-terminal domain of human carcinoembryonic antigen (CEA) (MV-CEA) with potential antineoplastic activity. The cellular receptor of MV is human CD46 antigen, a type 1 integral membrane glycoprotein found on nearly all human tissues and overexpressed on many cancer cell types. Mediated through CD46, both haemagglutinin and fusion glycoproteins of MV are required for the attachment to and fusion of host cell membranes, thereby leading to syncytia and cell lysis. The expressed CEA, a tumor associated antigen, can be detected in serum and used as a sensitive marker to monitor viral gene expression in order to easily optimize individual therapy. Compared to wild-type MV, the Ed strain of MV has a lower affinity for the MV receptor signaling lymphocyte-activation molecule (CD150), mainly expressed in B- and T-lymphocytes, but a higher affinity for CD46. C64775 523413 navitoclax An orally bioavailable, synthetic small-molecule antagonist of a subset of the B-cell leukemia 2 (Bcl-2) family of proteins with potential antineoplastic activity. BcI-2 family protein inhibitor ABT-263 selectively binds to apoptosis suppressor proteins Bcl-2, Bcl-XL, and Bcl-w and prevents their binding to the apoptotic effectors Bax and Bak proteins, which may trigger apoptosis in tumor cells overexpressing Bcl-2, Bcl-XL, and Bcl-w. Bcl-2, Bcl-XL, and Bcl-w are frequently overexpressed in a wide variety of cancers, including those of the lymphatic system, breast, lung, prostate, and colon, and have been linked to tumor drug resistance. C64776 523414 yttrium Y 90 resin microspheres An injectable formulation of the radioisotope yttrium Y 90 encapsulated in resin microspheres with potential antineoplastic activity. When injected into arterial vasculature supplying the tumor, yttrium Y 90 resin microspheres occlude tumor blood vessels and selectively deliver a cytotoxic dose of beta emitting yttrium Y 90 to the tumor site, which may result in tumor cell death and tumor regression. C64539 524060 sufentanil citrate The citrate salt form of sufentanil, a synthetic congener of fentanyl and related to the phenylpieridines, with analgesic property. Sufentanil citrate binds to and activates the mu-opioid receptor, thereby producing analgesia, respiratory depression, miosis, reduced gastrointestinal motility, and euphoria. In addition, this agent has a more rapid onset of action and shorter duration of action compared to fentanyl. 524061 sevoflurane A fluorinated isopropyl ether with general anesthetic activity. Although the mechanism of action has not been fully elucidated, sevoflurane may interfere with the release and re-uptake of neurotransmitters at post-synaptic terminals, and/or alter ionic conductance following receptor activation by a neurotransmitter. This agent may also interact directly with the lipid matrix of neuronal membranes, thereby affecting gating properties of ion channels. In addition, sevoflurane may activate gamma-aminobutyric acid (GABA) receptors, hyperpolarizing cell membranes and resulting in a general anesthetic effect, a decrease in myocardial contractility and mean arterial pressure, and an increased respiratory rate. 525721 DTA-H19 plasmid A plasmid DNA encoding the A chain of the diphtheria toxin (DT-A) driven by the transcriptional regulatory sequences of human H19, with potential antineoplastic activity. Because the expression of DT-A is under the control of H19 promotor elements, DT-A is selectively expressed in tumor cells capable of turning on H-19. DT-A catalyzes ADP-ribosylation of translation elongation factor 2 (EF-2), resulting in the inhibition of protein synthesis and apoptosis. In addition, DT-A protein released from lysed cells cannot enter and kill neighboring cells because of the absence of the DT-B chain, further enhancing the selective cytotoxicity of this agent. Human H19 is a paternally-imprinted, oncofetal gene encoding an RNA product; it acts as a "riboregulator" in gene expression and is found at substantial levels in different human tumor cell types while its expression in normal adult tissue is limited. C64845 526173 levetiracetam A pyrrolidine with antiepileptic activity. The exact mechanism through which levetiracetam exerts its effects is unknown but does not involve inhibitory and excitatory neurotransmitter activity. Stereoselective binding of levetiracetam was confined to synaptic plasma membranes in the central nervous system with no binding occurring in peripheral tissue. Levetiracetam inhibits burst firing without affecting normal neuronal excitability, which suggests that it may selectively prevent hyper-synchronization of epileptiform burst firing and propagation of seizure activity. 526175 DACH polymer platinate AP5346 A low molecular weight polymer-conjugated platinum complex with potential antineoplastic activity. This polymer drug delivery system consists of cytotoxic diaminocyclohexane (DACH)-platinum (Pt) coupled to a water-soluble biocompatible hydroxypropylmethacrylamide (HPMA) copolymer via a pH sensitive linker. Due to decreased pH in tumor sites, the linker is cleaved and the chelated active moiety DACH-Pt is released in tumor cells. DACH-Pt alkylates macromolecules and causes both inter- and intra-strand platinum-DNA crosslinks, which impede DNA replication and transcription, resulting in cell-cycle independent cytotoxicity. The HPMA-based drug delivery system increases the concentration and prolongs the half-life of DACH-Pt in tumor sites, while minimizing adverse effects on normal tissues. C64784 526176 MPC-6827 A quinazoline derivative with potential dual antineoplastic activities. MPC-6827 binds to and inhibits tubulin polymerization and interrupts microtubule formation, resulting in disruption of mitotic spindle assembly, cell cycle arrest in the G2/M phase, and cell death. This agent is not a substrate for several subtypes of multidrug resistance ABC transporters, such as P-glycoprotein, multidrug resistance-associated protein 1 (MRP1), and breast cancer resistance protein 1 (BCRP1); therefore, it may be useful for treating multidrug resistant (MDR) tumors that express these transporters. In addition, as a vascular disrupting agent (VDA), MPC-6827 appears to disrupt tumor microvasculature specifically, which may result in acute ischemia and massive tumor cell death. C64782 526178 apoptosis inducer MPC-2130 A broad-acting, apoptosis-inducing, small molecule with potential antineoplastic activity. Although the exact mechanism of action has yet to be fully elucidated, apoptosis inducer MPC-2130 exhibits proapoptotic activities in tumor cells, including membrane phosphatidylserine externalization, release of cytochrome C from mitochondria, caspase activation, cell condensation, and DNA fragmentation. In addition, because this agent is not a substrate for several types of multidrug resistance (MDR) ABC superfamily transporters, such as P-glycoprotein 1 (MDR-1), multidrug resistance-associated protein 1 (MRP1), and breast cancer resistance protein 1 (BCRP1/ABCG2), it may be useful in treating MDR tumors that express these particular MDR efflux pumps. C64781 526653 recombinant thyroid-stimulating hormone A peptide hormone secreted by the anterior pituitary. It promotes the growth of the thyroid gland and stimulates the synthesis of thyroid hormones and the release of thyroxine by the thyroid gland. 526788 meclocycline sulfosalicylate The sulfosalicylate salt form of meclocycline, a tetracycline antibiotic with broad-spectrum antibacterial and antiprotozoal activity. Meclocycline sulfosalicylate is bacteriostatic and inhibits bacterial protein synthesis by binding to the 30S ribosomal subunit, thereby preventing the addition of amino acids to the growing peptide chain. This tetracycline is active against a wide range of gram-positive and gram-negative bacteria. 526815 AdRTVP-1-transduced prostate cancer cell-based vaccine A cell-based vaccine comprised of prostate cancer cells transduced with an adenoviral vector encoding human RTVP-1 (AdRTVP-1), with potential immunostimulating and antineoplastic activities. RTVP-1, also referred to as glioma pathogenesis-related protein 1 (GLIP1), is down-regulated in prostate tumors. Regulated by tumor suppressor p53, the expression of RTVP-1 functions as a tumor suppressor, and is abundant in normal human prostate epithelial cells as well as in differentiated macrophages. Administration of AdRTVP-1-transduced prostate cancer cell-based vaccine leads to an induction of apoptosis through the expression of RTVP-1, which may result in a reduction in prostate cancer cellular proliferation. In addition, this vaccine may induce a cytotoxic T lymphocyte (CTL) response against prostate specific tumor- associated antigens. C64785 528015 lexatumumab A fully human monoclonal agonistic antibody directed against tumor necrosis factor-alpha (TNF-alpha)-related apoptosis-inducing ligand receptor-2 (TRAIL-R2) with potential antitumor activity. Mimicking the natural ligand TRAIL, lexatumumab binds to and activates TRAIL-R2, which may trigger apoptosis in and inhibit the growth of TRAIL-R2-expressing tumor cells. TRAIL-R2, also known as death receptor 5 (DR5), is a member of the TNF receptor family and is expressed on many malignant cell types. C64621 528273 thyroxine A hormone synthesized and secreted by the thyroid gland containing four iodine atoms and is converted to triiodothyronine (T3) in the body, influencing metabolism and organ function. 528954 BRAF(V600E) kinase inhibitor RO5185426 An orally bioavailable, ATP-competitive, small-molecule inhibitor of BRAF(V600E) kinase with potential antineoplastic activity. BRAF(V600E) kinase inhibitor RO5185426 selectively binds to the ATP-binding site of BRAF(V600E) kinase and inhibits its activity, which may result in an inhibition of an over-activated MAPK signaling pathway downstream in BRAF(V600E) kinase-expressing tumor cells and a reduction in tumor cell proliferation. Approximately 90% of BRAF gene mutations involve a valine-to-glutamic acid mutation at residue 600 (V600E); the oncogene protein product, BRAF(V600E) kinase, exhibits a markedly elevated activity that over-activates the MAPK signaling pathway. The BRAF(V600E) gene mutation has been found to occur in approximately 60% of melanomas, and in about 8% of all solid tumors, including melanoma, colorectal, thyroid and other cancers. C64768 529189 CDKI R547 An orally bioavailable diaminopyrimidine cyclin-dependent kinase inhibitor (CDKI) with potential antineoplastic activity. CDKI R547 selectively binds to and inhibits CDKs, especially CDK1/cyclin B, CDK2/cyclin E, and CDK4/cyclin D1. The inhibition of CDKs results in cell cycle arrest, inhibition of tumor cell proliferation, and induction of apoptosis. Through CDK inhibition, this agent also reduces phosphorylation of the retinoblastoma (Rb) protein, thus preventing activation of transcription factor E2F and so further suppressing tumor cell proliferation.\n\nCDKs are ATP-dependent serine/threonine kinases that are important regulators of cell cycle progression and are frequently overexpressed in tumor cells. C64544 529297 recombinant TNF-related apoptosis-inducing ligand TNF-related apoptosis-inducing ligand (TRAIL) is a homotrimeric type II membrane protein that rapidly induces oligomerization of receptor intracellular death domains and apoptosis in a variety of tumor cells. TRAIL mRNA is up regulated in response to IFNA and IFNB. TRAIL demonstrated antineoplastic activity in vivo without significant toxicity. 529341 BLP25 liposome vaccine A liposome-encapsulated peptide vaccine consisting of a synthetic peptide derived from the mucin 1 (MUC-1) antigen with potential antineoplastic activity. Upon vaccination, MUC-1 peptide vaccine may stimulate the host immune system to mount a cytotoxic T lymphocyte (CTL) response against MUC-1-expressing tumor cells, resulting in growth inhibition. MUC-1 antigen is a high-molecular-weight transmembrane glycoprotein that is overexpressed on the cell surfaces of many epithelial tumor cells as well as on the cell surfaces of some B-cell lymphoma cells and multiple myeloma cells. 529342 E2F1 pathway activator ARQ 171 A second-generation E2F1 pathway activator with potential antineoplastic activity. ARQ 171 induces the expression of E2F transcription factor 1, thereby activating the E2F1-mediated checkpoint process. As a result, this agent exerts anti-tumor activity through checkpoint activation independent of p53 mediated tumor suppression. E2F1, down-regulated in cancer cells, regulates expression of genes involved in the cell cycle progression from G1 into S phase. The G1/S checkpoint process selectively induces cell cycle arrest in cancer cells with irreparable DNA damages and triggers subsequent apoptosis, while allowing cell division to proceed in cells without or with minor reparable DNA damage. C64767 529346 Cocculus/nux vomica/tabacum/petroleum extract A homeopathic herbal formulation with potential anti-emetic activity. Cocculus/nux vomica/tabacum/petroleum extract contains equal homeopathic units of the following extracts: extract of Cocculus indicus (fish berry), the fruit of the southeast Asian/Indian climbing plant Anamirta cocculus; extract of the seeds of Strychnos nux vomica (poison nut), an evergreen tree native to southeast Asia; extract of Nicotiana tabacum (tobacco); and petroleum. Although the exact mechanism(s) of action for this formulation has yet to be fully elucidated, alkaloids in these plant extracts have been shown to relieve nausea, vomiting, and, in some cases, dizziness. C66805 529352 mycobacterial cell wall-DNA complex A proprietary preparation of mycobacterial DNA oligonucleotides embedded in mycobacterial cell wall fragments derived from cultures of Mycobacterium phlei, with potential immunomodulatory and antineoplastic activities. DNA oligonucleotides in the mycobacterial cell wall-DNA complex (MCC) induce apoptosis by increasing BAX protein levels, releasing cytochrome C from mitochondria, and activating caspase-3 and -7, which results in the cleavage of poly (ADP-ribose) polymerase and the release of nuclear matrix proteins. In addition to its pro-apoptotic effect, MCC activates monocytes and macrophages to produce various cytokines, including interleukin 6 (IL-6), IL-8, IL-12, IL-18, and tumor necrosis factor alpha (TNF-a). This results in the activation of natural killer (NK) cells and cytotoxic T lymphocytes (CTLs) and interferon gamma (IFN-gamma) synthesis. C64765 529357 isavuconazole A water-soluble triazole prodrug with broad-spectrum antifungal activity. Administered intravenously or orally with high oral bioavailability, isavuconazole is hydrolyzed to the active moiety BAL4815 by plasma esterases. BAL4815 inhibits fungal cytochrome P450 lanosterol 14-alpha-demethylase (CYP51), which catalyzes the conversion of lanosterol to ergosterol, an important component of the fungal cell membrane. CYP51 inhibition by this agent leads to a decrease in ergosterol pool, thus disturbing synthesis of the fungal cell membrane; increasing fungal cell membrane permeability; promoting the loss of essential intracellular elements; and resulting in fungal cell lysis and death. C64543 529839 fermented wheat germ extract An extract of fermented wheat germ containing a concentrated, standardized amount of methoxy-substituted benzoquinones with immunomodulatory and potential antineoplastic activities. Fermented wheat germ extract (FWGE) inhibits the activities of several enzymes involved in de novo nucleic acid synthesis and in supplying the dNTP pool required for DNA replication. This agent also induces caspase-3- mediated inactivation of poly(ADP)ribose polymerase (PARP), a key enzyme in DNA repair that is overexpressed in many cancers; cleavage of PARP prevents DNA repair and induces apoptosis. The benzoquinones may contribute to the immunomodulatory effects of FWGE, down-regulating major histocompatibility complex class I (MHC-1) protein on the surface of cancer cells, allowing natural killer (NK) cell surveillance; and up-regulating the expression of intracellular adhesion molecule 1 (ICAM-1) on tumor endothelial cells. C64763 529846 inolitazone dihydrochloride The orally bioavailable dihydrochloride salt of the thiazolidinedione inolitazone with potential antineoplastic activity. Inolitazone binds to and activates peroxisome proliferation-activated receptor gamma (PPAR-gamma), which may result in the induction of tumor cell differentiation and apoptosis, and so a reduction in tumor cell proliferation. PPAR-gamma is a nuclear hormone receptor and ligand-activated transcription factor controlling gene expression involved in such cellular processes as differentiation, apoptosis, cell-cycle control, carcinogenesis, and inflammation. C64764 530015 ofatumumab A fully human, high-affinity IgG1 monoclonal antibody directed against the B cell CD20 cell surface antigen with potential antineoplastic activity. Ofatumumab binds specifically to CD20 on the surfaces of B cells, triggering complement-dependent cell lysis (CDCL) and antibody-dependent cell-mediated cytotoxicity (ADCC) of B cells overexpressing CD20. The CD20 antigen, found on over 90% of B cells, B cell lymphomas, and other B cells of lymphoid tumors of B cell origin, is a non-glycosylated cell surface phosphoprotein that acts a calcium ion channel; it is exclusively expressed on B cells during most stages of B cell development. C66952 530060 adenovirus-interferon-gamma TG1042 A replication-defective adenoviral vector encoding human interferon-gamma (IFN-g) cDNA with potential antineoplastic and immunoregulatory activities. Upon intratumoral administration, the prolonged expression of IFN-g by adenovirus-interferon-gamma TG1042 promotes a T helper type 1 (Th1-type) immune response and inhibits the Th2-mediated cytokine production observed in many cutaneous lymphomas. IFN-g also mediates interleukin-12 (IL-12) production by antigen-presenting cells (APCs); activates macrophages, cytotoxic T-cells, and natural killer (NK) cells; upregulates major histocompatibility complex (MHC) molecules; and stimulates antibody-dependent cellular cytotoxicity (ADCC). Altogether, these IFN-g-mediated effects may result in an inhibition of tumor cell proliferation and tumor cell death. C66972 530302 fresolimumab A pan-specific, recombinant, fully human monoclonal antibody directed against human transforming growth factor (TGF) -beta 1, 2 and 3 with potential antineoplastic activity. Fresolimumab binds to and inhibits the activity of all isoforms of TGF-beta, whcih may result in the inhibition of tumor cell growth, angiogenesis, and migration. TGF-beta, a cytokine often over-expressed in various malignancies, may play an important role in promoting the growth, progression, and migration of tumor cells. C63546 530629 tiacumicin B A narrow-spectrum, 18-membered macrolide antibiotic isolated from the actinomycete Dactylosporangium aurantiacum subsp. hamdenensis with potential antibacterial activity. Although the exact mechanism of action has yet to be fully elucidated, tiacumicin B may bind to and inhibit bacterial DNA-dependent RNA polymerase, thereby inhibiting the initiation of bacterial RNA synthesis. When orally administered, this agent is minimally absorbed into the systemic circulation, acting locally in the gastrointestinal tract. Tiacumicin B appears to be active against pathogenic Gram-positive bacteria, such as clostridia, enterococci, and staphylococci, but does not appear to be active against other beneficial intestinal bacteria. C66979 530758 brentuximab vedotin An antibody-drug conjugate (ADC) directed against the tumor necrosis factor (TNF) receptor CD30 with potential antineoplastic activity. Brentuximab vedotin is generated by conjugating the humanized anti-CD30 monoclonal antibody SGN-30 to the cytotoxic agent monomethyl auristatin E (MMAE) via a valine-citrulline peptide linker. Upon administration and internalization by CD30-positive tumor cells, brentuximab vedotin undergoes enzymatic cleavage, releasing MMAE into the cytosol; MMAE binds to tubulin and inhibits tubulin polymerization, which may result in G2/M phase arrest and tumor cell apoptosis. Transiently activated during lymphocyte activation, CD30 (tumor necrosis factor receptor superfamily, member 8;TNFRSF8) may be constitutively expressed in hematologic malignancies including Hodgkin lymphoma and some T-cell non-Hodgkin lymphomas. The linkage system in brentuximab vedotin is highly stable in plasma, resulting in cytotoxic specificity for CD30-positive cells. C66944 530784 checkpoint kinase inhibitor AZD7762 A synthetic small molecule inhibitor of checkpoint kinases (Chks) with potential chemosensitizing activity. AZD7762 binds to and inhibits Chks, which may prevent cell cycle arrest and subsequent nucleotide excision repair in DNA-damaged tumor cells, resulting in tumor cell apoptosis. This agent may enhance the cytotoxicity of DNA-damaging agents. Chks are protein kinases that regulate either G1/S or G2/M transitions in the cell cycle. In the presence of DNA damage or incomplete DNA replication, Chks become activated and initiate cell cycle arrest to allow DNA repair or the completion of DNA replication. C66961 530790 panobinostat A cinnamic hydroxamic acid analogue with potential antineoplastic activity. Panobinostat selectively inhibits histone deacetylase (HDAC), inducing hyperacetylation of core histone proteins, which may result in modulation of cell cycle protein expression, cell cycle arrest in the G2/M phase and apoptosis. In addition, this agent appears to modulate the expression of angiogenesis-related genes, such as hypoxia-inducible factor-1alpha (HIF-1a) and vascular endothelial growth factor (VEGF), thus impairing endothelial cell chemotaxis and invasion. HDAC is an enzyme that deacetylates chromatin histone proteins. C66948 530791 elisidepsin A marine-derived, synthetic cyclic depsipeptide with potential antineoplastic activity. Elisidepsin is a derivative of a natural marine compound that belongs to a family of dehydro aminobutyric acid-containing peptides (kahalalides) isolated from the herbivorous marine mollusk Elysia rufescens. Although the primary mechanism of action has yet to be elucidated, this agent exhibits anti-proliferative activity in a wide variety of cancer cell types, including breast, colon, pancreas, lung, and prostate; it appears to induce oncolytic rather than apoptotic cell death. C66949 530794 tibolone A synthetic anabolic steroid with estrogenic, androgenic and progestagenic activities. The 3alpha- and 3beta-hydroxy metabolites of tibilone activate estrogenic receptors (ERs) in bone and vaginal tissue leading to a decrease in bone turnover, and decreased vaginal dryness, respectively; derived from the 3beta-hydroxy metabolite, its delta4-isomer activates androgenic receptors (ARs) in the brain and liver and progestogenic receptors (PRs) in endometrial tissue, affecting sexual function, lipid metabolism, and endometrial function, respectively. In breast and endometrial tissue, tibolone metabolites inhibit sulfatase, preventing the conversion of circulating estrone sulfate and estradiol sulfate to estrone and estradiol, respectively; estrogen-mediated effects in the breast and uterus are thus reduced. C66955 530928 vitamin B12 An essential nutrient and natural water-soluble vitamin of the B-complex family that must combine with an intrinsic factor for absorption by the intestine, Vitamin B12 (cyanocobalamin) is necessary for hematopoiesis, neural metabolism, DNA and RNA production, and carbohydrate, fat, and protein metabolism. B12 improves iron functions in the metabolic cycle and assists folic acid in choline synthesis. B12 metabolism is interconnected with that of folic acid. Vitamin B12 deficiency causes pernicious anemia, megaloblastic anemia, and neurologic lesions. C939 531049 mometasone furoate The furoate salt form of mometasone, a synthetic topical glucocorticosteroid receptor agonist with anti-inflammatory, anti-pruritic and vasoconstrictive properties. Mometasone furoate exerts its effect by binding to cytoplasmic glucocorticoid receptors and subsequently activates glucocorticoid receptor mediated gene expression. This results in synthesis of certain anti-inflammatory proteins, while inhibiting the synthesis of certain inflammatory mediators.. Specifically, mometasone furoate appears to induce phospholipase A2 inhibitory proteins, thereby controlling the release of the inflammatory precursor arachidonic acid from phospholipid membrane by phospholipase A2. C29268 531051 lutetium Lu-177-DOTA-chimeric monoclonal antibody cG250 A radioimmunoconjugate consisting of the chimeric monoclonal antibody cG250 linked to the low energy beta-emitting radioisotope Lutetium 177, via the bifunctional macrocyclic chelating agent tetra-azacyclododecanetetra-acetic acid (DOTA), with potential antineoplastic activity. The antibody moiety of lutetium Lu-177-DOTA-chimeric monoclonal antibody cG250 binds to renal cell carcinoma (RCC) cells expressing the RCC-associated antigen G250; a cytotoxic dose of beta radiation is selectively delivered to G250-expressing RCC cells upon internalization of the radioimmunoconjugate. C66978 531055 human MHC non-restricted cytotoxic T-cell line TALL-104 An allogeneic human cytotoxic T-lymphocyte cell line with potential antineoplastic activity. Human MHC non-restricted cytotoxic T-cell line TALL-104 is an IL-2-dependent human leukemic T cell line, expressing CD8 and CD3 but not CD16. Upon administration, human MHC non-restricted cytotoxic T-cell line TALL-104 interacts with tumor cells and activates apoptotic and necrotic pathways, resulting in tumor cell lysis. Endowed with MHC-non-restricted killer activity, these cells are cytotoxic against a broad range of tumor cells, sparing normal cells. In addition, TALL-104 may induce secretion of various cytokines, such as interferon-gamma, potentially enhancing its cytotoxic activity. C66980 531122 quinacrine dihydrochloride The dihydrochloride salt of the 9-aminoacridine derivative quinacrine with potential antineoplastic and antiparasitic activities. Quinacrine may inhibit the transcription and activity of both basal and inducible nuclear factor-kappaB (NF-kappaB), which may result in the induction of tumor suppressor p53 transcription, the restoration of p53-dependent apoptotic pathways, and tumor cell apoptosis. Continuous NF-kappaB signaling, present in many tumors and in chronic inflammatory processes, promotes the expression of antiapoptotic proteins and cytokines while downregulating the expression of proapoptotic proteins, such as p53. C67059 531150 odanacatib An inhibitor of cathepsin K with potential anti-osteoporotic activity. Odanacatib selectively binds to and inhibits the activity of cathepsin K, which may result in a reduction in bone resorption, improvement of bone mineral density, and a reversal in osteoporotic changes. \nCathepsin K, a tissue-specific cysteine protease that catalyzes degradation of bone matrix proteins such as collagen I/II, elastin, and osteonectin plays an important role in osteoclast function and bone resorption. C66981 531798 alefacept A recombinant dimeric fusion protein consisting of the extracellular CD2-binding domain of the human leukocyte function-associated antigen 3 (LFA-3; CD58) linked to the Fc portion of human immunoglobulin G1 (IgG1) with potential immunosuppressive activity. Alefacept binds to the CD2 receptor expressed on the majority of T lymphocytes, blocking the binding of endogenous LFA-3, located on antigen-presenting cells (APCs), to the CD2 receptor; the activation and proliferation of T lymphocytes in response to LFA-3 binding is thus inhibited. In addition, binding of the IgG1 moiety of this agent to the Fc gamma receptor on the surface of natural killer (NK)cells may bridge NK cells and target T lymphocytes, initiating NK cell-mediated apoptosis of T lymphocytes. C65220 531923 acyclovir sodium The sodium salt form of acyclovir, a synthetic analog of the purine nucleoside, guanosine, with potent antiviral activity against herpes simplex viruses type 1 and 2, varicella-zoster virus and other viruses. After conversion in vivo to the active metabolite acyclovir triphosphate, acyclovir competitively inhibits viral DNA polymerase, incorporates into and terminates the growing viral DNA chain, and inactivates viral DNA polymerase. The greater antiviral activity of acyclovir against HSV compared to VZV is due to its more efficient phosphorylation by the thymidine kinase of HSV. C47956 532249 anti-CS1 monoclonal antibody HuLuc63 A humanized monoclonal antibody directed against the human CS1 (CD2 subset 1, CRACC, SLAMF7) antigen with potential antineoplastic activity. Anti-CS1 monoclonal antibody HuLuc63 binds to the CS1 antigen, which may trigger antibody-dependent cellular cytotoxicity (ADCC) in cells expressing CS1. CS1 is a cell surface glycoprotein belonging to the CD2 subset of the immunoglobulin superfamily (IgSF) and is highly expressed by multiple myeloma cells, but minimally expressed by normal cells. C66982 532253 antisurvivin antisense oligonucleotide LY2181308 A second-generation antisense oligonucleotide directed against survivin mRNA with potential antitumor activity. Antisurvivin antisense oligonucleotide LY2181308 hybridizes to survivin mRNA, thereby blocking translation of survivin protein, a member of the inhibitor of apoptosis (IAP) family. Silencing the expression of survivin may result in the restoration of the apoptotic process in tumor cells, facilitating chemotherapeutic treatment. Survivin, expressed during embryonal development, is upregulated in a variety of human cancers while absent in most normal adult cells; its expression in tumors is associated with a more aggressive phenotype, shorter survival times, and a decreased response to chemotherapy. C66935 532294 MEK inhibitor AZD6244 An orally bioavailable small molecule with potential antineoplastic activity. MEK inhibitor AZD6244 inhibits mitogen-activated protein kinase kinases (MEK or MAPK/ERK kinases) 1 and 2, which may prevent the activation of MEK1/2-dependent effector proteins and transcription factors, and so may inhibit cellular proliferation in MEK-overexpressing tumor cells. MEK 1 and 2 are dual-specificity kinases that are essential mediators in the activation of the RAS/RAF/MEK/ERK pathway, are often upregulated in various tumor cell types, and are drivers of diverse cellular activities, including cellular proliferation. C66939 532310 hepatitis B vaccine (recombinant) A non-infectious mixture containing recombinant hepatitis B surface antigen (HBsAg) in a liquid vehicle. Immunization with the hepatitis B vaccine induces the formation of specific anti-hepatitis B antibodies and an active immunity against hepatitis B infection. C29091 533894 green tea lozenge A lozenge formulation of green tea, derived from the dried leaves of Camellia sinensis, with potential antioxidant and chemopreventive activities. Green tea lozenge contains polyphenols that may be responsible for its chemopreventive effect. The polyphenol fraction contains mainly epigallocatechin-3-gallate (EGCG) and other catechins, such as epicatechin (EC), gallocatechin gallate (GCG), epigallocatechin (EGC), and epicatechin gallate (ECG). Green tea polyphenols act as antioxidants and free radical scavengers, protecting cells from the damaging effects of reactive oxygen species (ROS). C67058 533908 green tea Tea derived from the dried leaves of the plant Camellia sinensis with potential antioxidant, chemopreventive, and lipid-lowering activities. Green tea contains polyphenols that may be responsible for its chemopreventive effect. The polyphenol fraction contains mainly epigallocatechin-3-gallate (EGCG) and other catechins, such as epicatechin (EC), gallocatechin gallate (GCG), epigallocatechin (EGC), and epicatechin gallate (ECG). Green tea polyphenols act as antioxidants and free radical scavengers and may affect enzymes involved in cellular replication and tumor angiogenesis by modulating angiogenic factors, such as vascular endothelial growth factor (VEGF). C67048 533915 kunecatechins ointment A topical ointment containing a green tea polyphenol mixture (kunecatechins) with potential antiviral, antibacterial, antioxidant, and chemopreventive activities. Kunecatechins is a partially purified fraction of the aqueous extract of green tea leaves from Camellia sinensis and contains catechins and other green tea components. Catechins, polyphenolic antioxidant plant metabolites or flavonoids, comprise most of the drug substance in kunecatechins with epigallocatechin gallate (EGCG) present as the primary catechin. Catechins may inhibit basic functions of human papillomavirus (HPV), counteract specific changes in tumor cells, affect cell signaling, and stimulate the immune system. Topical application of kunecatechins ointment has been reported to reduce HPV-induced genital and anal warts through a not yet fully understood mechanism, which may involve anti-oxidative activity. C67049 534127 monoclonal antibody hLL1 A humanized monoclonal antibody directed against human CD74 with potential antineoplastic activity. Monoclonal antibody hLL1 specifically binds to CD74 on CD74-positive cells. Although the exact mechanism through which this agent induces apoptosis is unknown, it may involve antibody-dependent cellular cytotoxicity (ADCC) or complement-mediated cytotoxicity (CMC). Alternatively, as CD74 is the cellular receptor for the cytokine migration-inhibitory factor (MIF), the cytotoxicity of this agent may be related to inhibition of CD74 activation by MIF. CD74, an integral membrane protein that functions as an MHC class II chaperone, may also be an accessory-signaling molecule; activation of CD74 may initiate cell survival mechanisms involving induction of a signaling cascade resulting in NFkB activation, entry of stimulated cells into the S phase of the cell cycle, elevation of DNA synthesis, cell division, and augmented expression of Bcl-xL. C66983 534131 cabazitaxel A semi-synthetic derivative of the natural taxoid 10-deacetylbaccatin III with potential antineoplastic activity. Cabazitaxel binds to and stabilizes tubulin, resulting in the inhibition of microtubule depolymerization and cell division, cell cycle arrest in the G2/M phase, and the inhibition of tumor cell proliferation. Unlike other taxane compounds, this agent is a poor substrate for the membrane-associated, multidrug resistance (MDR), P-glycoprotein (P-gp) efflux pump and may be useful for treating multidrug-resistant tumors. In addition, cabazitaxel penetrates the blood-brain barrier (BBB). C66937 534284 fluorine F 18 FEQA The anilinoquinazoline derivative FEQA radiolabeled with the positron-emitting radioisotope fluorine F 18 with epidermal growth factor receptor (EGFR) binding and radioisotopic activities. Fluorine F 18 FEQA irreversibly binds to (EGFR), allowing imaging of EGFR-positive tumor cells with positron emission tomography (PET). C66936 534287 multikinase inhibitor AT9283 A small-molecule inhibitor of several kinases with potential antineoplastic activity. Multikinase inhibitor AT9283 binds to and inhibits Aurora kinases A and B, JAK2 (Janus kinase 2) and the kinase BCR-ABL, which may result in the inhibition of cellular division and proliferation and the induction of apoptosis in tumor cells that overexpress these kinases. Aurora kinases are serine-threonine kinases that play essential roles in mitotic checkpoint control during mitosis; JAK2 is a kinase that transduces signals from the single chain and IL-3 cytokine receptor families, and from the\n\nIFN-gamma receptors; BCR-ABL is a fusion protein with tyrosine kinase activity that is commonly found in CML. C66947 534399 levonorgestrel The levorotatory form of norgestrel and synthetic progestogen with progestational and androgenic activity. Levonorgestrel binds to the progesterone receptor in the nucleus of target cells, thereby stimulating the resulting hormone-receptor complex, initiating transcription, and increasing the synthesis of certain proteins. This results in a suppression of luteinizing hormone (LH) activity and an inhibition of ovulation, as well as an alteration in the cervical mucus and endometrium. 536018 sodium phenylbutyrate The sodium salt of phenylbutyrate, a derivative of the short-chain fatty acid butyrate, with potential antineoplastic activity. Phenylbutyrate reversibly inhibits class I and II histone deacetylases (HDACs), which may result in a global increase in gene expression, decreased cellular proliferation, increased cell differentiation, and the induction of apoptosis in susceptible tumor cell populations. C1440 536028 microtubulin inhibitor EPC2407 A small molecule tubulin polymerization inhibitor with potential antineoplastic activity. Microtubulin inhibitor EPC2407 binds to the colchicine-binding site on beta-tubulin and inhibits the polymerization of tubulin into microtubules, which may result in cell cycle arrest, the induction of apoptosis, and the inhibition of tumor cell proliferation. As a vascular disruption agent (VDA), this agent also disrupts tumor neovascularization, which may result in a reduction in tumor blood flow and tumor hypoxia and ischemic necrosis. C66938 536034 DNA plasmid vector pPRA-PSM vaccine A cancer vaccine consisting of a DNA plasmid encoding epitopes of the human preferential antigen of melanoma (PRAME) and the prostate specific membrane antigen (PSMA) with potential immunostimulating activity. Upon direct administration of this vaccine into lymph nodes, peptides expressed by DNA plasmid vector pPRA-PSM may activate the immune system, resulting in a cytotoxic T-lymphocyte (CTL) response against PRAME- and PSMA-expressing cells. PRAME and PSMA are tumor associated antigens upregulated in a number of cancer cell types. As part of the MKC1106-PP regimen exploiting the 'prime-boost strategy', this plasmid is responsible for priming the immune response and is used in conjunction with a peptide vaccine consisting of PRAME and PSMA that boosts the immune system against PRAME- and PSMA-expressing tumor cells. C67089 536035 Aurora kinase inhibitor PF-03814735 An orally bioavailable, ATP-competitive, reversible small-molecule Aurora kinase inhibitor with potential antineoplastic activity. Aurora kinase inhibitor PF-03814735 binds to and inhibits Aurora kinases A and B, which may result in the inhibition of cellular division and proliferation in tumor cells that overexpress these kinases. Aurora kinases are serine-threonine kinases that play essential roles in mitotic checkpoint control during mitosis. C66946 536220 cell cycle checkpoint/DNA repair antagonist IC83 A proprietary agent with potential antineoplastic activity. Cell cycle checkpoint/DNA repair antagonist IC83 IC83 inhibits cell cycle checkpoint/DNA repair enzymes, which may result in enhanced cytotoxicity of DNA damaging agents and diminished tumor cell resistance to chemotherapy and radiation therapy.\n\nCell cycle checkpoint/DNA repair enzymes are involved in the recognition and repair of damaged DNA and are overexpressed in many types of cancer cells. C67075 536232 lenograstim A glycosylated form of a recombinant therapeutic agent which is chemically identical to or similar to an endogenous human granulocyte colony-stimulating factor (G-CSF). Produced endogenously by monocytes, fibroblasts, and endothelial cells, G-CSF binds to and activates specific cell surface receptors, stimulating neutrophil progenitor proliferation and differentiation and selected neutrophil functions. C49234 536240 anti-HGF monoclonal antibody AMG 102 A fully human IgG2 monoclonal antibody directed against the human hepatocyte growth factor (HGF) with potential antineoplastic activity. Anti-HGF monoclonal antibody AMG 102 binds to and neutralizes HGF, preventing the binding of HGF to its receptor c-Met and so c-Met activation; inhibition of c-Met-mediated signal transduction may result in the induction of apoptosis in cells expressing c-Met.\nc-Met (HGF receptor or HGFR), a receptor tyrosine kinase overexpressed or mutated in a variety of epithelial cancer cell types, plays a key role in cancer cell growth, survival, angiogenesis, invasion, and metastasis. C67079 536241 pyruvate kinase inhibitor TLN-232 A synthetic cyclic heptapeptide with potential antineoplastic activity. Pyruvate kinase (PK) inhibitor TLN-232 targets pyruvate kinase M2 (M2PK), which may disrupt tumor cell anaerobic glycolysis. M2PK is a dimeric isoform of PK and the predominant PK isoform found in tumor cells. C67087 536528 HSV-TK-transduced donor lymphocytes A preparation of donor lymphocytes transduced with the "suicide" gene herpes simplex virus thymidine kinase (HSV-TK) with potential immunomodulating activity. Administration of HSV-TK-transduced lymphocytes after T cell-depleted allogeneic stem cell transplantation allows an early controllable immune reconstitution, which takes advantage of the antitumor effect of donor lymphocytes and helps to mitigate the risk of post-transplant opportunistic infection. To control graft-versus-host disease (GvHD) due to donor lymphocyte infusion, HSV-TK-transduced donor lymphocytes are selectively eliminated by administration of the antiviral agent ganciclovir. Ganciclovir, a prodrug, is readily phosphorylated by the suicide gene HSV-TK within HSV-TK-transduced lymphocytes to its monophosphate form and, subsequently, converted into its active triphosphate form, which specifically kills HSV-TK- transduced donor lymphocytes. C67047 537355 belotecan hydrochloride The hydrochloride salt of the semi-synthetic camptothecin analogue belotecan with potential antitumor activity. Belotecan binds to and inhibits the activity of topoisomerase I, stabilizing the cleavable complex of topoisomerase I-DNA, which inhibits the religation of single-stranded DNA breaks generated by topoisomerase I; lethal double-stranded DNA breaks occur when the topoisomerase I-DNA complex is encountered by the DNA replication machinery, DNA replication is disrupted, and the tumor cell undergoes apoptosis. Topoisomerase I is an enzyme that mediates reversible single-strand breaks in DNA during DNA replication. C66954 537368 human lactoferrin peptide hLF1-11 A synthetic peptide corresponding to the first 11 N-terminal amino acids of human lactoferrin (hLF1-11) with potential antimicrobial activity. Although the exact mechanism through which this peptide exerts its effect has yet to be fully elucidated, hLF1-11 binds ferric iron, limiting the availability of free iron for microbial functions. hLF1-11 may be effective against a variety of bacteria and fungi, including multidrug-resistant (MDR) strains of Acinetobacter baumannii and Staphylococcus aureus, and fluconazole-resistant Candida albicans strains. Human lactoferrin, a 692 amino acid glycoprotein belonging to the transferrin family of metal-binding proteins, can be found in human milk and other secretory fluids, and the secondary granules of polymorphonuclear (PMN) cells. Human lactoferrin plays a role in the innate defense of mucosal surfaces. C67046 537376 eicosapentaenoic acid An essential, polyunsaturated, 20-carbon omega-3 fatty acid with anti-inflammatory and potential antineoplastic and chemopreventive activities. Eicosapentaenoic acid (EPA) may activate caspase 3, resulting in apoptosis in susceptible tumor cell populations. In addition, this agent may inhibit cyclooxygenase-2 (COX-2), resulting in inhibition of prostaglandin synthesis and prostaglandin-mediated inflammatory processes. C67080 537378 indium In 111-labeled autologous peripheral blood mononuclear cells A preparation of autologous peripheral blood mononuclear cells (PBMCs) radiolabeled with indium In 111 with radioisoptoic activity. Autologous PBMCs are isolated, expanded ex vivo, radiolabeled with indium In 111, and then infused back into the patient. Gamma scintigraphy may then be used to image gamma ray-emitting indium In 111 PBMCs localized in lymhoma tissue. C67085 537379 indium In 111-labeled autologous polymorphonuclear leukocytes A preparation of autologous peripheral polymorphonuclear (PMNLs) radiolabeled with indium In 111 with radioisoptic activity. Autologous PMNLs are isolated, expanded ex vivo, radiolabeled with indium In 111, and then infused back into the patient. Gamma scintigraphy may then be used to image gamma ray-emitting indium In 111 PMNLs localized in lymphoma tissue. C67086 537395 allogeneic adult mesenchymal stem cells Human mesenchymal stem cells (MSCs) harvested from bone marrow of healthy adult donors and expanded ex vivo, with potential immunosuppressive activity. Allogeneic adult MSCs are hypo-immunogenic due to lack of major histocompatibility II (MHC II) molecule expression, eliciting little, if any, host immune response upon intravenous infusion. Infusion of allogeneic MSCs may result in: a) increased production of anti-inflammatory cytokines, such as interleukin-10, prostaglandin E, and hepatocyte growth factor; b) decreased mononuclear phagocyte expression of indoleamine 2,3,-dioxygenase, which catabolizes L-tryptophan into its pro-inflammatory metabolites; and c) modulated dendritic cell (DC)maturation and disrupted activities of natural killer (NK) cells and CD8+ and CD4+ T cells. In addition, pluripotent MSCs, upon administration, may be recruited to damaged tissue sites, differentiating along specific lineages when stimulated. C67082 537396 NMPRTase inhibitor APO866 A small molecule with potential antineoplastic and antiangiogenic activities. NMPRTase inhibitor APO866 binds to and inhibits nicotinamide phosphoribosyltransferase (NMPRTase), inhibiting the biosynthesis of nicotinamide adenine dinucleotide (NAD+) from niacinamide (vitamin B3), which may deplete energy reserves in metabolically active tumor cells and induce tumor cell apoptosis. In addition, this agent may inhibit tumor cell prioduction of vascular endothelial growth factor (VEGF), resulting in the inhibition of tumor angiogenesis. The coenzyme NAD+ plays an essential role in cellular redox reactions, including the redox reaction linking the citric acid cycle and oxidative phosphorylation. C67043 537549 topical vitamin E A topical preparation of the fat-soluble vitamin E with potential antioxidant and cytoprotective activities. As a potent antioxidant and radical scavenger, vitamin E ameliorates free-radical damage to cell membranes, thereby protecting cells from reactive oxygen species and maintaining the integrity of cellular macromolecules. In addition, vitamin E noncompetitively inhibits cyclooxygenase (COX) activity in many tissues, which may decrease inflammation. Vitamin E is a generic name for a group of compounds known as tocopherols and tocotrienols (tocols). C67081 537550 tocophersolan A water-soluble amphipathic formulation of d-alpha-tocopherol succinate coupled, through a succinate linker, to polyethylene glycol (PEG) 1000. Due to its amphipathic property in which it forms its own micelles, tocophersolan is easily taken up into enterocytes, even in the absence of bile salts; fat soluble d-alpha-tocopherol is then released after hydrolysis. This formulation enhances the absorption of d-alpha-tocopherol compared to the administration of free d-alpha-tocopherol. In addition, tocophersolan may enhance the absorption of water-insoluble agents and other fat-soluble vitamins. C67044 537572 EGFR/HER2 tyrosine kinase inhibitor BIBW 2992 An orally bioavailable dual receptor tyrosine kinase (RTK) inhibitor with potential antineoplastic activity. EGFR/HER2 tyrosine kinase inhibitor BIBW 2992 irreversibly binds to and inhibits human epidermal growth factor receptors 1 and 2 (EGFR-1; HER2), which may result in the inhibition of tumor growth and angiogenesis. EGFR/HER2 are RTKs that belong to the EGFR superfamily; both play major roles in tumor cell proliferation and tumor vascularization and are overexpressed in many cancer cell types. C66940 537610 magnesium hydroxide A solution of magnesium hydroxide with antacid and laxative properties. Milk of magnesium exerts its antacid activity in low doses such that all hydroxide ions that enter the stomach are used to neutralize stomach acid. This agent exerts its laxative effect in higher doses so that hydroxide ions are able to move from the stomach to the intestines where they attract and retain water, thereby increasing intestinal movement (peristalsis) and inducing the urge to defecate. C29262 537638 gimatecan An orally bioavailable, semi-synthetic lipophilic analogue of camptothecin, a quinoline alkaloid extracted from the Asian tree Camptotheca acuminate, with potential antineoplastic and antiangiogenic activities. Gimatecan binds to and inhibits the activity of topoisomerase I, stabilizing the cleavable complex of topoisomerase I-DNA, which inhibits the religation of single-stranded DNA breaks generated by topoisomerase I; lethal double-stranded DNA breaks occur when the topoisomerase I-DNA complex is encountered by the DNA replication machinery, DNA replication is disrupted, and the tumor cell undergoes apoptosis. Although the mechanism of its antiangiogenic activity has yet to be full elucidated, this agent may inhibit endothelial cell migration, tumor neovascularization, and the expression of proangiogenic basic fibroblast growth factor (bFGF). C65804 537707 L-arginine/Korean ginseng/ Gingko biloba/damiana-based supplement An amino acid and herbal supplement with libido-enhancing activity. L-arginine/korean ginseng/Ginkgo biloba/damiana-based supplement contains a blend of the amino acid L-arginine and the herbs Korean ginseng, Ginkgo biloba, and damiana (Turnera aphrodisiaca) in addition to 14 other vitamins and minerals. The semi-essential amino acid L-arginine is a precursor for nitric oxide (NO); Korean ginseng may enhance the conversion of L-arginine into NO by NO synthase; and Ginkgo biloba may promote microvascular circulation. This agent may increase NO production, resulting in vasodilatation and an enhanced circulation critical to sexual function and arousal. The damiana component may exert an anxiolytic effect and stimulate sexual behavior. C67093 537716 fluorine F 18 sodium fluoride A radiopharmaceutical consisting of the sodium salt of fluorine F 18 fluoride with radioisotopic and bone mineralizing activities. Fluoride binds to calcium ions in hydroxyapatite crystals in bone. The uptake and incorporation of positron-emitting fluorine F 18 fluoride into bone can be imaged using positron emission tomography (PET) or single-photon emission computed tomography (SPECT), allowing visualization of malignant bone lesions in which regional blood flow and bone turnover are increased. C66941 537722 technetium Tc 99m methylene diphosphonate A radiopharmaceutical containing methylene diphosphonate (medronate; MDP) complexed with the gamma-emitting radionuclide technetium Tc 99m with radioisotopic activity and hydroxyapatite affinity. Upon intravenous administration, skeletal uptake of technetium Tc 99m methylene diphosphonate occurs as a function of skeletal blood flow and osteogenic activity. The MDP moiety of this agent has affinity for hydroxyapatite crystals in bone with abnormal accumulation at sites with increased osteoid mineralization; labeling of MDP with Tc 99m allows scinitgraphic imaging of areas of abnormal osteogenesis associated with malignant bone lesions. C67060 538262 oncolytic measles virus encoding thyroidal sodium iodide symporter An attenuated oncolytic Edmonston (Ed) strain of measles virus encoding the human thyroidal sodium iodide symporter (MV-NIS) with potential gene expression and antineoplastic activities. After attachment to and fusion with host tumor cell membranes, MV-NIS may induce tumor cell syncytia and tumor cell lysis. When combined with iodine 123 (I-123), expressed NIS facilitates uptake of I-123 by MV-NIS-infected tumor cells, allowing noninvasive imaging of these cells. MV-NIS may also enhance the oncolytic activity of MV against radiosensitive tumor cells by facilitating the uptake of iodine 131 (I-131) by MV-NIS-infected cells. The cellular receptor for MV is the human CD46 antigen, a type 1 integral membrane glycoprotein found on nearly all human tissues and overexpressed on many cancer cell types. C66942 538399 vinorelbine tartrate emulsion An emulsion containing the tartrate salt of the semisynthetic vinca alkaloid vinorelbine with antineoplastic activity. Vinorelbine binds to tubulin, inhibiting tubulin polymerization into microtubules; cell division is prevented, the cell cycle is arrested metaphase and cell death ensues. In this formulation vinorelbine is emulsified in a homogeneous suspension of nanoparticles, which protects the venous endothelium from coming into direct contact with the active ingredient, potentially reducing vinorelbine-associated venous toxicity at the venous injection site. C66943 538436 deglycosylated ricin A chain-conjugated anti-CD19/anti-CD22 immunotoxins A combination preparation of 1:1 mixture of the immunotoxins HD37-dgA and RFB4-dgA with potential antineoplastic activity. Anti-CD19 IgG monoclonal antibody HD37 and anti-CD22 IgG monoclonal antibody RFB4 are attached individually to a deglycosylated ricin A chain (dgA) via N-succinimidyl-oxycarbonyl-alpha-methyl-alpha-(2-pyridyldithio) toluene (SMPT) linker. Deglycosylated ricin A chain-conjugated anti-CD19/anti-CD22 immunotoxins bind to CD19- and CD22-expressing tumor cells, specifically delivering cytotoxic ricin A chain to leukemia cells expressing these antigens. Ricin A chain is toxic to ribosomal activity and protein synthesis, and inhibits cell growth. CD19 and CD22 molecules are cell surface antigens present on the majority of B acute lymphoblastic leukemia (ALL) cells. C67061 538747 MDR modulator CBT-1 A naturally-occurring, orally bioavailable bisbenzylisoquinoline plant alkaloid with potential chemosensitization activity. MDR modulator CBT-1 binds to and inhibits the MDR efflux pump P-glycoprotein (P-gp), which may inhibit the efflux of various chemotherapeutic agents from tumor cells and reverse P-gp-mediated tumor cell MDR. P-gp is a transmembrane ATP-binding cassette (ABC) transporter and is overexpressed by some multidrug resistant tumors. C67042 538994 eszopiclone A nonbenzodiazepine cyclopyrrolone and active dextrorotatory stereoisomer of zopiclone with hypnotic and sedative activities and without significant anxiolytic activity. Although the exact mechanism of action remains to be fully elucidated, eszopiclone binds to and activates the omega-1 subtype of the alpha subunit of the gamma-aminobutyric acid-benzodiazepine GABA receptor complex (GABA-A), a chloride ionophore complex in the central nervous system (CNS). This leads to the opening of chloride channels, causing hyperpolarization and inhibition of neuronal firing, which may result in a hypnotic effect and the induction of sleep. C65545 538996 palifosfamide A synthetic mustard compound with potential antineoplastic activity. An active metabolite of ifosfamide covalently linked to the amino acid lysine for stability, palifosfamide irreversibly alkylates and cross-links DNA through GC base pairs, resulting in irreparable 7-atom inter-strand cross-links; inhibition of DNA replication and cell death follow. Unlike ifosfamide, this agent is not metabolized to acrolein or chloroacetaldehyde, metabolites associated with bladder and CNS toxicities. In addition, because palifosfamide does not require activation by aldehyde dehydrogenase, it may overcome the tumor resistance seen with ifosfamide. C66990 539029 daniquidone A water-insoluble heterocyclic amide with potential antineoplastic activity. Daniquidone inhibits topoisomerases I and II, thereby inhibiting DNA replication and repair, and RNA and protein synthesis. The acetylated form of daniquidone is highly toxic and is capable of inducing unscheduled DNA synthesis; rapid acetylators are more likely to experience toxicity with this agent. C66984 539100 alpha-1,3-galactosyltransferase-expressing allogeneic lung tumor cell vaccine An allogeneic lung cancer vaccine with potential immunostimulating and antineoplastic activities. Derived from allogeneic lung tumor cells, alpha-1,3-galactosyltransferase-expressing allogeneic lung tumor cell vaccine is engineered to express the murine alpha-1,3-galactosyltransferase (GalT), an enzyme humans lack. GalT catalyzes the expression of foreign alpha-1,3-galactosyl (alpha-gal) carbohydrate epitopes in glycoproteins and in glycolipids on the cell membranes of the allogeneic lung tumor cells present in the vaccine, essentially producing a "xenograft". The hyperacute rejection involves pre-existing human anti-alpha-gal antibodies that bind the foreign alpha-gal epitopes expressed by the vaccine tumor cell “xenograft”, resulting in complement-mediated cytotoxicity (CMC) and antibody-dependent cell-mediated cytotoxicity (ADCC) towards endogenous lung tumor cells with unmodified carbohydrate epitopes. C66985 539307 Fas receptor agonist APO010 A recombinant, soluble, hexameric fusion protein consisting of three human Fas ligand (FasL) extracellular domains fused to the dimer-forming collagen domain of human adiponectin with potential pro-apoptotic and antineoplastic activities. Assembled into a soluble hexameric structure mimicking the ligand clustering of endogenous active FasL, Fas receptor agonist APO010 activates the Fas receptor, resulting in caspase-dependent apoptosis in susceptible tumor cell populations. FasL is a transmembrane protein of the tumor necrosis factor (TNF) superfamily and a pro-apoptotic ligand for the death receptor Fas. C67041 539359 polyunsaturated fatty acid A fatty acid containing more than one double bond (C=C). The essential fatty acids omega-3 and omega-6 are polyunsaturated fatty acids (PUFAs) that contain 2 or more cis double bonds. Dietary intake of some PUFAs may have beneficial effects on blood pressure, serum lipds, and inflammation. Some PUFAs, such as omega-3 PUFAs, may have antineoplastic or chemopreventive activities. C67038 539361 phytochemical The term 'phyto' originated from a Greek word meaning plant. Phytonutrients are certain organic components of plants, and these components are thought to promote human health. Fruits, vegetables, grains, legumes, nuts and teas are rich sources of phytonutrients. Unlike the traditional nutrients (protein, fat, vitamins, minerals), phytonutrients are not 'essential' for life, so some people prefer the term 'phytochemical'. (USDA Agricultural Research Service) 539362 anti-IL-13 humanized monoclonal antibody TNX-650 A humanized monoclonal antibody directed against interleukin-13 (IL-13) with potential antineoplastic activity. Anti-IL-13 humanized monoclonal antibody TNX-650 binds to and blocks the activity of IL-13, which may result in the inhibition of Hodkin lympoma cell proliferation. IL-13 cytokine, an important mediator in allergic inflammation, may be an autocrine growth factor for Hodgkin lymphoma cells. C66988 539691 folate receptor-targeted vinca alkaloid/mitomycin C EC0225 A folate receptor-targeting cytotoxic agent with potential antineoplastic activity. Folate receptor-targeted vinca alkaloid/mitomycin C EC0225 contains two potent cytotoxic agents, a vinca alkaloid and mitomycin C, linked to a single folate molecule. Mediated through the folate moiety, this agent delivers the cytotoxic agents directly into cells expressing folic acid receptors, frequently upregulated in many types of tumor cells. After ligand-receptor internalization, the vinca alkaloid moiety binds to tubulin and disrupts microtubule assembly-disassembly dynamics, resulting in cell cycle arrest and apoptosis. Mitomycin C alkylates DNA, producing DNA cross-links and inhibiting DNA replication. The relative tumor cell specificity of EC0225 reduces the toxicity profiles of its cytotoxic agent moieties. C66987 539695 folate receptor-targeted technetium Tc 99m EC20 A folate receptor-targeting radiopharmaceutical consisting of a folate-containing tetrapeptide chelator to which technetium Tc 99m is linked. The folate component of folate receptor-targeted technetium Tc 99m EC20 binds to folic acid receptors, which are frequently upregulated in many types of tumor cells and activated macrophages. Gamma scintigraphy may then be used to image folate receptor-positive tumors. C66986 539702 lutetium Lu 177-capromab A radioimmunoconjugate consisting of capromab linked to lutetium Lu 177 via the bifunctional macrocyclic chelator methoxy-tetraazacyclododecane-tetraacetic acid (MeO-DOTA) with potential antineoplastic activity. Lutetium Lu 177-capromab binds to human prostate specific membrane antigen (PSMA) expressed on tumor cell surfaces via its capromab moiety and, upon internalization, delivers cytotoxic beta radiation directly to PSMA-expressing tumor cells. PSMA is a cell surface glycoprotein abundantly expressed by prostate epithelium and is typically overexpressed by prostate cancer cells. C67039 539730 povidone-iodine solution An iodophor solution containing a water-soluble complex of iodine and polyvinylpyrrolidone (PVP) with broad microbicidal activity. Free iodine, slowly liberated from the povoiodine-iodine (PVPI) complex in solution, kills eukaryotic or prokaryotic cells through iodination of lipids and oxidation of cytosplasmic and membrane compounds. This agent exhbits a broad range of microbicidal activity against bacteria, fungi, protozoa, and viruses.\nSlow release of iodine from the PVPI complex in solution minimizes iodine toxicity towards mammalian cells. C766 539733 anti-PD-1 human monoclonal antibody MDX-1106 A fully human monoclonal antibody directed against the negative immunoregulatory human cell surface receptor PD-1 (programmed death-1 or programmed cell death-1/PCD-1) with immunopotentiation activity. Anti-PD-1 human monoclonal antibody MDX-1106 binds to and blocks the activation of PD-1, an Ig superfamily transmembrane protein, by its ligands PD-L1 and PD-L2, resulting in the activation of T-cells and cell-mediated immune responses against tumor cells or pathogens.\nActivated PD-1 negatively regulates T-cell activation and effector function through the suppression of P13k/Akt pathway activation. C68814 539740 chk1 inhibitor PF-477736 A proprietary compound targeting cell cycle checkpoint kinase 1 (chk1) with potential chemopotentiation activity. Chk1 inhibitor PF-477736 inhibits chk1, an ATP-dependent serine-threonine kinase that is a key component in the DNA replication-monitoring S/G2 checkpoint system. By overriding the last checkpoint defense against DNA damaging agent-induced lethal damage, chk1 inhibitor PF-477736 may potentiate the antitumor efficacy of various chemotherapeutic agents against tumor cells with intrinsic checkpoint defects. C68820 539834 opium tincture Also known as laudanum and formulated for oral administration, opium tincture is made of air-dried poppy (Papaver somniferum) latex and contains alkaloids such as morphine and codeine. As an antidiarrheal agent, it slows transit of intestinal contents by increasing intestinal smooth muscle tone and inhibiting motility; water is absorbed from fecal contents, decreasing diarrhea. 540032 anti-CD22 immunotoxin CAT-8015 A recombinant immunotoxin consisting of the Fv portion of the anti-CD22 antibody covalently fused to a 38 KDa fragment of Pseudomonas exotoxin-A (PE38) with potential antineoplastic activity. The Fv portion of anti-CD22 immunotoxin CAT-8015 binds to CD22, a cell surface receptor expressed on a variety of malignant B-cells, thereby delivering the toxin moiety PE38 directly to tumor cells. Once internalized, PE38 induces caspase-mediated apoptosis via a mechanism involving mitochondrial damage and blocks translational elongation by binding to elongation factor 2 (EF-2). Anti-CD22 immunotoxin CAT-8015 exhibits a greater affinity for CD22 than its predecessor, anti-CD22 immunotoxin CAT-3888 (BL22 immunotoxin), and hence may be more effective against tumor cells expressing lower levels of CD22. C68819 540122 indocyanine green solution A sterile solution of a nontoxic tricarbocyanine dye with a peak spectral absorption at 790 nm, used for determining cardiac output, hepatic function, and liver blood flow, as well as for ophthalmic angiography. Designed to be administered intravenously, indocyanine green solution (ICG) contains less than 5% sodium iodide. Upon intravenous injection, ICG rapidly binds to its principle carrier, plasma protein, and is thereby confined to the vascular space. This agent, with a half-life of 150 to 180 seconds, is removed exclusively by the liver from circulation to bile juice. Furthermore, due to poor uptake, ICG is not suitable for angiography or functional output analysis of kidney, lung, cerebro-spinal, or peripheral tissues. C69127 540197 fostamatinib disodium An orally available disodium salt of the Syk kinase inhibitor fostamatinib with potential anti-inflammatory and immunomodulating activities. Fostamatinib inhibits Syk kinase-mediated IgG Fc gamma receptor signaling, resulting in inhibition of the activation of mast cells, macrophages, and B-cells and related inflammatory responses and tissue damage.\nSyk kinase, widely expressed in hematopoietic cells, is a nonreceptor tyrosine kinase that is involved in coupling activated immunoreceptors to signal downstream events that mediate diverse cellular responses, including proliferation, differentiation, and phagocytosis. C69128 540244 D-methionine formulation MRX-1024 A proprietary oral formulation of D-methionine with antioxidant and antimucositis activities. D-methionine formulation MRX-1024 may selectively protect the oral mucosa from the toxic effects of chemotherapy and radiation therapy without compromising antitumor activity. \nD-methionine may be converted into the L- isomer in vivo, particlualry in instances of L-methionine deprivation; both isomers have antioxidant activity which may be due, in part, to their sulfur moieties and chelating properties. L-methionine, an essential amino acid, also may help to maintain the ratio of reduced glutathione to oxidized glutathione in cells undergoing oxidative stress and may provide a source of L-cysteine for glutathione synthesis. C69140 540312 cesium Cs 137 A radioactive isotope of cesium with an atomic mass of 139 and potential application in radiotherapy. Cesium Cs 137 is prevalent due to its spontaneous production, which occurs as a result of nuclear fission of other radioactive materials, such as uranium and plutonium. This radionuclide has a relatively long half-life, 30 years, and decays by emitting beta particles. Both Cs 137 and its metastable nuclear isomer, barium-137m, emit gamma radiation of moderate energy and so are used in sterilization procedures in the food industry or in hospital environments. C68812 540319 recombinant nematode anticoagulant protein c2 An 85-amino acid recombinant peptide derived from protein c2 of the hemophagocytic hookworm Ancylostoma caninum (a common canine parasite) with anticoagulant activity. Recombinant nematode anticoagulant protein c2 (rNAPc2) binds to circulating activated factor X (FXa) or zymogen factor X (FX) to form a binary complex which subsequently binds to and inhibits membrane-bound activated factor VII/tissue factor complex (FVIIa/TF). When administered prophylactically, this agent may reduce the incidence of deep venous thrombosis without hemostatic compromise. Because rNAPc2 inhibits the formation of the FVIIa/TF protease complex, which may play a role in the cellular signaling of both metastatic and angiogenic processes, it may impede tumor progression. C69129 540440 pasireotide A synthetic long-acting cyclic peptide with somatostatin-like activity. Pasireotide activates a broad spectrum of somatostatin receptors, exhibiting a much higher binding affinity for somatostatin receptors 1, 3, and 5 than octreotide in vitro, as well as a comparable binding affinity for somatostatin receptor 2.\nThis agent is more potent than somatostatin in inhibiting the release of human growth hormone (HGH), glucagon, and insulin. C69131 540623 lopinavir A protease inhibitor used against human immunodeficiency virus (HIV). Lopinavir competitively inhibits the HIV-1 protease, an enzyme that mediates the cleavage of Gag, Gag-Pol and Nef precursor polypeptides into their mature proteins, including protease, reverse transcriptase, and integrase. Inhibition of HIV-1 protease prevents cleavage of the viral polyprotein precursor and results in the release of immature, noninfectious virions. 540635 tenofovir A synthetic antiviral acyclic nucleotide analogue of adenosine 5-monophosphate. Tenofovir is incorporated into human immunodeficiency viral DNA instead of the natural substrate deoxyadenosine 5-triphosphate, thereby inhibiting HIV-1 reverse transcriptase (RT), an RNA-dependent DNA polymerase, and resulting in DNA chain termination and impairment of viral replication and propagation. This agent prevents HIV from reproducing in uninfected cells only. Tenofovir exhibits activity against the hepatitis B virus (HBV). C29490 540650 efavirenz A synthetic non-nucleoside reverse transcriptase (RT) inhibitor with antiviral activity. Efavirenz binds directly to the human immunodeficiency virus type 1 (HIV-1) RT, an RNA-dependent DNA polymerase, blocking its function in viral DNA replication. In combination with other antiretroviral drugs, this agent has been shown to significantly reduce HIV viral load, retarding or preventing damage to the immune system and reducing the risk of developing AIDS. Efavirenz induces activity of the cytochrome P450 system, accelerating its own metabolism. C29027 540668 emtricitabine A synthetic nucleoside analogue of cytidine with activity against human immunodeficiency virus type 1 reverse transcriptase (RT). Emtricitabine is phosphorylated by cellular enzymes to form emtricitabine 5'-triphosphate. Emtricitabine 5'-triphosphate inhibits the activity of HIV-1 RT by competing with the RT natural substrate deoxycytidine 5'-triphosphate and by being incoprorated into nascent viral DNA which results in the termination of viral DNA chain elongation. 542697 collagen/aloe vera/vitamin E/lidocaine topical hydrogel A topical preparation containing collagen, aloe vera, vitamin E, and lidocaine hydrochloride with wound-healing activity. The four ingredients of collagen/aloe vera/vitamin E/lidocaine topical hydrogel may promote wound repair and new tissue growth in which : collagen, a structural protein in connective tissue, provides a connective tissue matrix for the attachment of various cells involved in wound repair; aloe vera carbohydrate polymers provide a moist wound environment; vitamin E promotes blood vessel formation; and lidocaine acts as a local anesthetic. C69133 543136 cationic liposome-encapsulated paclitaxel A cationic liposome preparation of paclitaxel with antineoplastic activity. Paclitaxel, the active ingredient in cationic liposome-encapsulated paclitaxel, binds to tubulin and inhibits the disassembly of microtubules, resulting in the inhibition of mitosis and cellular proliferation, and apoptosis. Cationic liposome encapsulation of paclitaxel allows the delivery of high doses of paclitaxel to target tissues while minimizing systemic toxicity. Tumor endothelial cells may preferentialy bind and internalize cationic liposomes. C69130 543155 iodine I 123 iodometomidate An iodine I-123 conjugate of metomidate (MTO) with potential application in adrenal imaging. Metomidate is a potent and selective inhibitor of the cytochrome P-450 enzymes, especially CYP11B1 (11 beta-hydroxylase) and CYP11B2 (aldosterone synthase). Because both CYP11B1 and CYP11B2 are expressed exclusively in the adrenal cortex, I-123 iodometomidate can be used as a radiotracer for adrenal scintigraphy. C69137 543515 Raf kinase inhibitor XL281 An orally active, small molecule with potential antineoplastic activity. XL281 specifically inhibits RAF kinases, located downstream from RAS in the RAS/RAF/MEK/ERK kinase signaling pathway, which may result in reduced proliferation of tumor cells. RAS mutations may result in constitutive activation of the RAS/RAF/MEK/ERK kinase signaling pathway, and have been found to occur frequently in human tumors. C69135 543519 apoptosis inducer BZL101 An orally active aqueuous extract derived from the plant Scutellaria barbata with potential antineoplastic activity. Sparing normal cells, apoptosis inducer BZL101 specifically facilitates translocation of the protein apoptosis-inducing factor (AIF) from the mitochondrial membrane into the nucleus in tumor cells, thereby causing tumor cell-specific chromatin condensation and DNA degradation followed by the induction of caspase-independent apoptosis. AIF is both a mitochondrial intermembrane flavoprotein with oxidoreductase activity and a caspase-independent death\neffector that, similar to cytochrome c, is released from mitochondria early\nin the apoptotic process. C69134 543526 MEK inhibitor AZD8330 An orally active, selective MEK inhibitor with potential antineoplastic activity. MEK inhibitor AZD8330 specifically inhibits mitogen-activated protein kinase kinase 1 (MEK or MAP/ERK kinase1), resulting in inhibition of growth factor-mediated cell signaling and tumor cell proliferation. MEK is a key component of the RAS/RAF/MEK/ERK signaling pathway that regulates cell growth; constitutive activation of this pathway has been implicated in many cancers. C69143 543723 indium In 111 CHX-A DTPA trastuzumab An indium I 111-labeled trastuzumab with potential use as an imaging agent. Indium In 111 CHX-A DTPA trastuzumab is chemically conjugated via a bifunctional metal chelator molecule, 2-(p-isothiocyanatobenzyl)-cyclohexyl-diethylenetriaminepentaacetic acid (CHX-A DTPA), a backbone-substituted derivative of DTPA. This agent may allow radioimmunolocalization of HER2-positive cells. Trastuzumab, a recombinant humanized monoclonal antibody that selectively binds with high affinity to the extracellular domain of human epidermal growth factor receptor 2 (HER2), may elicit an antibody-dependent cellular cytotoxicity (ADCC) against tumor cells that overexpress HER2. C60766 543726 bcr-abl p210-b3a2 breakpoint-derived multipeptide vaccine A multipeptide vaccine consisting of five peptides derived from the bcr-abl p210-b3a2 breakpoint fusion protein with potential antineoplastic activity. Vaccination with bcr-abl p210-b3a2 breakpoint-derived multipeptide vaccine may stimulate the host immune system to mount a cytotoxic T lymphocyte (CTL) response against tumor cells that express the bcr-abl p210-b3a2 breakpoint fusion protein.\n In chronic myelogenous leukemia (CML), fusion genes typically result from the fusion of either bcr exon b2 or exon b3 to abl exon a2, resulting in either a b3a2 or a b2a2 gene fusion product. C69082 543797 synthetic peptides E-PRA and E-PSM vaccine A cancer vaccine consisting of E-PRA and E-PSM, two synthetic peptide analogs of PRAME (PReferential Antigen MElanoma) and PSMA (Prostate Specific Membrane Antigen), with potential immunostimulating activity. Upon direct administration into lymph nodes, synthetic peptides E-PRA and E-PSM vaccine may sitmulate a cytotoxic T-lymphocyte (CTL) response against PRAME- and PSMA-expressing tumor cells. PRAME and PSMA are tumor-associated antigens upregulated and expressed on the cell surfaces of certain tumor cell types. C67098 543940 therapeutic angiotensin-(1-7) A synthetic heptapeptide identical to endogenous angiotensin-(1-7) with vasodilator and antiproliferative activities. Therapeutic angiotensin 1-7 may inhibit cyclooxygenase 2 (COX-2) and the production of proinflammatory prostaglandins and may activate the angiotensin-(1-7) receptor Mas, resulting in diminished tumor cell proliferation. \nActivation of the angiotensin-(1-7) receptor Mas, a G-protein coupled, seven transmembrane protein, may down-regulate the phophorylation and activation of Erk1 and Erk2 in the Erk1/Erk2 Mapk signaling pathway. In the renin-angiotensin system, the vasodlilating activity of angiotensin- (1-7), hydrolysed from angiotensin II by the type I transmembrane metallopeptidase and carboxypeptidase angiotensin converting enzyme 2 (ACE2) in vivo, counteracts the vasoconstricting activity of angiotensin II. C68962 543979 adefovir dipivoxil An acyclic nucleotide adenine analogue with potent antiviral activity. Adefovir is activated in vivo to a diphosphate metabolite which is incorporated into viral DNA, leading to viral RNA-dependent DNA polymerase inhibition, DNA chain termination and impairment of viral replication. This agent inhibits the reverse transcriptases of hepatitis B, herpes and HIV viruses, induces natural killer cell activity, and stimulates endogenous interferon production. Viral resistance to adefovir develops at a slower rate compared to other antivirals. 544199 NY-ESO-1b peptide vaccine A recombinant nonapeptide used as an antineoplastic vaccine. NY-ESO-1b peptide vaccine contains the amino acid sequence SLLMWITQC, derived from the cancer-testis tumor antigen (NY-ESO-1), which is expressed on tumor cells of many different types, including melanomas. Vaccination with this peptide vaccine may elicit strong humoral and cellular immune responses to NY-ESO-1-expressing cancers. C68999 544217 resiquimod An imidazoquinolinamine Toll-like receptor (TLR) agonist with potential immunostimulatory activity. Resiquimod binds to and activates TLRs 7 and 8, mainly on dendritic cells (DCs), macrophages, and B-lymphocytes, which results in the activation of the TLR signaling pathway and nuclear translocation of the transcription activator NF-kB another transcription factors; subsequently, the production of cytokines, especially interferon-alpha (INF-a), increases, enhancing T-helper 1 (Th1) immune responses. In addition, topical application of resiquimod appears to activate Langerhans cells, which may result in enhanced activation of T-lymphocytes. Due to its immunostimulatory activity, this agent may potentially be useful as a vaccine adjuvant. 544559 sialyl Lewisª-keyhole limpet hemocyanin conjugate vaccine A vaccine consisting of the oligosaccharide antigen sialyl Lewisª (CA19-9) conjugated to the nonspecific immunomodulator keyhole limpet hemocyanin (KLH), with potential antineoplastic activity. Upon administration, sialyl Lewisª-keyhole limpet hemocyanin conjugate vaccine may induce production of IgG and IgM antibodies as well as trigger an antibody-dependent cell-mediated cytotoxicity (ADCC) against tumor cells expressing the sialyl Lewisª antigen.\nSialyl Lewisª is a blood group antigen and a tumor-associated antigen associated with epithelial cancers such as breast cancer and various digestive cancers. Sialyl Lewisª serves as a ligand for the cytokine-inducible cell adhesion molecule (CAM) E-selectin, an endothelial cell-specific type I transmembrane surface protein, thus facilitating hematogenous metastasis by mediating the adhesion of circulating cancer cells to vascular endothelium. C69000 544567 polymeric camptothecin prodrug XMT-1001 A polymeric prodrug of camptothecin (CPT) with potential antineoplastic activity. Polymeric camptothecin prodrug XMT-1001 consists of CPT conjugated to the 60-70 kDa, inert, bio-degradable, hydrophilic copolymer poly[1-hydroxymethylene hydroxymethyl formal] (PHF). Through a dual-phase, non-enzymatic release mechanism, CPT is first released in plasma from XMT-1001 as the lipophilic prodrugs CPT-SI (a succinimidoglycinate derivative) and CPT-SA (a succinamidoyl glycinate derivative), which are then hydrolyzed within tissues to release the lactone form of CPT. CPT inhibits the catalytic activity of DNA topoisomerase I, thereby inhibiting DNA replication and inducing apoptosis. This agent may exhibit a more favorable pharmacokinetic profile than other agents in the same class. C69079 544572 ranibizumab A second-generation, recombinant humanized IgG1 kappa monoclonal antibody fragment directed against human vascular endothelial growth factor (VEGF) alpha. Ranibizumab binds to VEGF alpha and inhibits VEGF alpha binding to its receptors, VEGFR1 and VEGFR2, thereby preventing the growth and maintenance of tumor blood vessels. The molecular weight of this agent (48 kD) is much smaller than the molecular weight of bevacizumab (MW ~149 kD), allowing complete penetration of the retina and the subretinal space following intravitreal injection. In contrast to other anti-VEGF aptamers such as pegaptanib, ranibizumab has a high specificity and affinity for all soluble human isoforms of VEGF. C67562 546970 anti-EGFRvIII vaccine CDX-110 A cancer vaccine consisting of a human epidermal growth factor receptor variant III (EGFRvIIi)-specific peptide conjugated to the non-specific immunomodulator keyhole limpet hemocyanin (KLH) with potential antineoplastic activity. Vaccination with anti-EGFRvIII vaccine CDX-110 may elicit a cytotoxic T-lymphocyte (CTL) immune response against tumor cells expressing EGFRvIII. EGFRvIII, a functional variant of EGFR that is not expressed in normal tissues, was originally discovered in glioblastoma multiforme (GBM) and has also been found in various other cancers such as breast, ovarian, metastatic prostate, colorectal, and head and neck cancers. EGFRvIII contains an 83 amino acid deletion in its extracellular domain and has been shown to transform NIH/3T3 mouse embryonic fibroblast cells in vitro. C69076 546971 candesartan cilexetil A synthetic, benzimidazole-derived angiotensin II receptor antagonist prodrug with antihypertensive activity. After hydrolysis of candesartan cilexetil to candesartan during gastrointestinal absorption, candesartan selectively competes with angiotensin II for the binding of the angiotensin II receptor subtype 1 (AT1) in vascular smooth muscle, blocking angiotensin II-mediated vasoconstriction and inducing vasodilatation. In addition, antagonism of AT1 in the adrenal gland inhibits angiotensin II-stimulated aldosterone synthesis and secretion by the adrenal cortex; sodium and water excretion increase, followed by a reduction in plasma volume and blood pressure. C28903 546978 serine/threonine kinase inhibitor XL418 A selective, orally active small molecule, targeting protein kinase B (PKB or AKT) and ribosomal protein S6 Kinase (p70S6K), with potential antineoplastic activity. XL418 inhibits the activities of PKB and p70S6K, both acting downstream of phosphoinosotide-3 kinase (PI3K). These kinases are often upregulated in a variety of cancers. Inhibition of PKB by this agent will induce apoptosis, while inhibition of p70S6K will result in the inhibition of translation within tumor cells. C68963 546981 pladienolide derivative E7107 A synthetic urethane derivative of pladienolide D with potential antineoplastic activity. Pladienolide derivative E7107 is generated from the 12-membered macrolide pladienolide D, one of several macrolides derived from the bacterium Streptomyces platensis Mer-11107. This agent appears to bind to the 130-kDa subunit 3 (spliceosome-associated protein 130; SAP130) of the splicing factor 3b (SF3b), resulting in inhibition of pre-messenger RNA splicing and the arrest of cell-cycle progression. The splicing factor SF3b is a multiprotein complex integral to the accurate excision of introns from pre-messenger RNA; the subunit SAP130 associates with U2 snRNP and is recruited to prespliceosomal complexes. C69005 546990 KSP inhibitor ARRY-520 A synthetic, small molecule targeting the kinesin spindle protein (KSP) with potential antineoplastic activity. KSP inhibitor ARRY-520 specifically inhibits KSP (kinesin-5 or Eg5), resulting in activation of the spindle assembly checkpoint, induction of cell cycle arrest during the mitotic phase, and consequently cell death in tumor cells that are actively dividing. Because KSP is not involved in postmitotic processes, such as neuronal transport, this agent does not cause the peripheral neuropathy that is often associated with tubulin-targeting agents.\nKSP is an ATP-dependent microtubule motor protein that is essential for the formation of bipolar spindles and the proper segregation of sister chromatids during mitosis. C68937 547019 class III receptor tyrosine kinase inhibitor AC220 An orally available small molecule with potential antineoplastic activity. Class III receptor tyrosine kinase inhibitor AC220 selectively inhibits class III receptor tyrosine kinases, including FMS-related tyrosine kinase 3 (FLT3/STK1), colony-stimulating factor 1 receptor (CSF1R/FMS), stem cell factor receptor (SCFR/KIT), and platelet derived growth factor receptors (PDGFRs), resulting in inhibition of ligand-independent leukemic cell proliferation and apoptosis. Mutations in FLT3, resulting in constitutive activation, are the most frequent genetic alterations in acute myeloid leukemia (AML) and occur in approximately one-third of AML cases. C68936 547027 clobetasol propionate The propionate salt form of clobetasol, a topical synthetic corticosteroid with anti-inflammatory, anti-pruritic, and vasoconstrictive properties. Clobetasol propionate exerts its effect by binding to cytoplasmic glucocorticoid receptors and subsequently activates glucocorticoid receptor mediated gene expression. This results in synthesis of certain anti-inflammatory proteins, while inhibiting the synthesis of certain inflammatory mediators. Specifically, clobetasol propionate appears to induce phospholipase A2 inhibitory proteins, thereby controlling the release of the inflammatory precursor arachidonic acid from membrane phospholipids by phospholipase A2. 547030 mast cell stabilizer TF002 A small molecule with mast cell stabilizing activity. Mast cell stabilizer TF002 inhibits the formation of lipid rafts of mast cell membranes that contain the signaling machinery which triggers the release of mast cell allergic and inflammatory mediators. Inhibition of lipid raft assembly by this agent results in mast cell stabilization, preventing mast cell degranulation and the release of the inflammatory mediators involved in type I allergic reactions (histamine, leukotrienes, prostaglandins, and cytokines). The assembly of the signaling machinery in mast cell lipid rafts, specialized membrane microdomains rich in cholesterol and sphingolipids, is initiated by IgE binding to its receptor on the mast cell surface; subsequently, allergens crosslink with the IgE/receptor complex and other proteins and lipids are recruited into the signaling machinery. C69146 547044 ketamine/amitriptyline NP-H cream A topical preparation containing the antidepressant amitriptyline and the excitatory amino acid antagonist ketamine with potential topical analgesic activity. In addition to activating adenosine A1 receptors and inhibiting the neuronal reuptake of norepinephrine and serotonin, amitriptyline produces antinociceptive effects, which appear to be mediated through the modulation of multiple subtypes of glutamate receptors including the N-methyl D-aspartate (NMDA) receptor. Ketamine inhibits biogenic amine uptake, agonistically binds to mu-opioid receptors, and inhibits NMDA receptors. NDMA receptor antagonists such as amitriptyline and ketamine interfere with the role of NMDA receptors in the process of central sensitization in which NMDA receptors on spinal dorsal horn neurons are activated, resulting in an increase in synaptic efficacy and so an amplification of the response to sensory input. C67250 547184 adenovirus encoding human aquaporin-1 A replication-deficient, recombinant adenovirus encoding human aquaporin-1 with potential membrane water channel activity. Upon transfection of salivary glands, adenovirus encoding human aquaporin-1 (AdhAQP1) directs human aquaporin-1 (hAQP1) expression in the apical and basolateral plasma membranes of salivary secretory cells, which may result in increased saliva production. hAQP1, a water channel protein, is one of several highly conserved water channel proteins that mediate water permeability in cells of water-transporting tissues. C68932 547294 choline magnesium trisalicylate A nonsteroidal anti-inflammatory drug (NSAID) belonging to the salicylate family. Choline magnesium trisalicylate inhibits inflammation-related prostaglandin synthesis. This agent's analgesic effect is mediated through peripheral and central pathways, resulting in a decrease in pain perception; its antipyretic effect is mediated via the hypothalamic heat regulation center. 547816 teglarinad chloride A water-soluble prodrug of a cyanoguanidine compound with potential antineoplastic activity. In vivo, teglarinad chloride is rapidly converted into active drug through hydrolytic cleavage of a carbonate ester bond. Although the exact mechanism of action has yet to be fully elucidated, the active drug appears to antagonize nuclear factor-kappa B (NF-kB) transcription, resulting in the induction of tumor cell apoptosis. C68931 548017 Hsp90 antagonist KW-2478 An agent that targets the human heat-shock protein 90 (Hsp90) with potential antineoplastic activity. Although the mechanism of action remains to be fully elucidated, Hsp90 antagonist KW-2478 appears to inhibit Hsp90, resulting in impaired signal transduction, inhibition of cell proliferation, and the induction of apoptosis in tumor cells. HSP90 is a molecular chaperone that plays a key role in the conformational maturation of oncogenic signaling proteins, such as HER2/ERBB2, AKT, RAF1, BCR-ABL, and mutated p53, as well as many other molecules that are important in cell cycle regulation or immune responses. C69139 549001 tyrosine kinase inhibitor XL228 A synthetic molecule that targets multiple tyrosine kinases with potential antineoplastic activity. Tyrosine kinase inhibitor XL228 binds to and inhibits the activities of multiple tyrosine kinases, such as the insulin-like growth factor 1 receptor (IGF1R), Src tyrosine kinase, and Bcr-Abl tyrosine kinase. Blockade of these kinases may result in the inhibition of tumor angiogenesis, cell proliferation, and metastasis.\nIn addition, this agent may be a potent inhibitor of the T315I mutant form of the\nAbl protein, which is associated with the resistance of chronic myelogenous leukemia (CML) to other tyrosine kinase inhibitors. IGF1R and Src tyrosine kinases are upregulated in many tumor cells and play important roles in tumor cell proliferation and metastasis. Bcr-Abl translocation leads to constitutive activation of ABL kinase and is commonly associated with Philadelphia-positive acute lymphocytic leukemia (ALL). C68929 549337 anti-HIF-1alpha LNA antisense oligonucleotide EZN-2968 A synthetic antisense oligodeoxynucleotide (AS ODN) targeting hypoxia-inducible factor-1alpha (HIF-1alpha) with potential antineoplastic activity. Anti-HIF-1alpha LNA antisense oligonucleotide EZN-2968 hybridizes with HIF-1alpha mRNA and blocks t HIF-1 alpha protein expression, which may result in the inhibition of angiogenesis, the inhibition of tumor cell proliferation, and apoptosis. \nHIF-1alpha, normally activated in response to hypoxia-induced stress, is a key transcription regulator of a large number of genes important in cellular adaptation to low-oxygen conditions, including angiogenesis, cell proliferation, apoptosis, and cell invasion. C68930 549539 therapeutic estetrol A synthetic steroid similar or identical to endogenous estetrol, a short-acting estrogen with both agonistic and antagonistic estrogen receptor activity. Administered orally, therapeutic estetrol binds to the estrogen receptor and as a selective estrogen receptor modulator (SERM) exhibits estrogen agonism in certain tissues and estrogen antagonism in others. Displaying weak estrogen activity in the uterus, estetrol acts as an estrogen antagonist in breast tissue. Produced solely by the human fetal liver, endogenous estetrol is the primary estrogen metabolite of estrogen biosynthesis in the human fetal liver. C68928 549681 anti-CEA/anti-DTPA-In (F6-734) bispecific antibody A bispecific monoclonal antibody (BsMAb) consisting of the Fab fragment of an anti-CEA monoclonal antibody (F6) coupled to the Fab fragment of an anti-DTPA-In monoclonal antibody (734) with potential radioimmunotherapeutic activity. In a two-step "pretargeted" radioimmunotherapeutic approach, this BsMAb, localizing to CEA-expressing tumor cells via the F6 Fab fragment, is introduced into patient first, followed by injection of indium 131-radiolabeled DTPA, which is recognized by the 734 Fab fragment of the BsMAb. Accordingly, a potentially lethal dose of indium 131 is delivered specifically to CEA-expressing tumor cells while minimizing radiotoxicity to normal tissues. CEA (carcinoembryonic antigen) is a tumor antigen overexpressed in many cancer types, including gastrointestinal, breast, non-small cell lung, and thyroid cancers. DTPA (diethylenetriaminepentaacetic acid) is a bivalent hapten. C68927 549706 therapeutic hemin A sterile, lyophilized powder of hemin, the Fe3+ oxidation product of heme (Fe2+), derived from processed red blood cells. Therapeutic hemin appears to inhibit delta-aminolevulinic acid (ALA) synthetase, a rate-limiting enzyme in the porphyrin/heme biosynthetic pathway, resulting in inhibition of the hepatic and/or marrow synthesis of porphyrin precursors. The mechanism by which therapeutic hematin produces symptomatic improvement in patients with acute episodes of the hepatic porphyrias has not been determined. C68925 551562 oral picoplatin An oral preparation of picoplatin, a third generation platinum compound with antineoplastic activity. Designed to overcome platinum drug resistance, picoplatin alkylates DNA, forming both inter- and intra-strand cross-linkages, resulting in inhibition of DNA replication and RNA transcription and the induction of apoptosis.\nBecause of the increase in steric bulk around the platinum center, there is a relative reduction in the inactivation of picoplatin by thiol-containing\nspecies such as glutathione and metallothionein in comparison to cisplatin. C68924 551564 selective androgen receptor modulator GTx-024 A non-steroidal agent with anabolic activity. Selective androgen receptor modulator (SARM) GTx-024 is designed to work like testosterone, thus promoting and/or maintaining libido, fertility, prostate growth, and muscle growth and strength. Mimicking testosterone's action, this agent may increase lean body mass, thereby ameliorating muscle wasting in the hypermetabolic state of cancer cachexia. C69161 551654 MEK inhibitor GDC-0973 An orally bioavailable small-molecule inhibitor of mitogen-activated protein kinase kinase 1 (MAP2K1 or MEK1), with potential antineoplastic activity. MEK inhibitor GDC-0973 specifically binds to and inhibits the catalytic activity of MEK1, resulting in inhibition of extracellular signal-related kinase 2 (ERK2) phosphorylation and activation and decreased tumor cell proliferation. Preclinical studies have demonstrated that this agent is effective in inhibiting the growth of tumor cells bearing a B-RAF mutation, which has been found to be associated with many tumor types. A threonine-tyrosine kinase and a key component of the RAS/RAF/MEK/ERK signaling pathway that is frequently activated in human tumors, MEK1 is required for the transmission of growth-promoting signals from numerous receptor tyrosine kinases. C68923 551718 iron dextran complex A colloidal solution containing ferric oxyhydroxide complexed with\npolymerized dextran, used as a form of parenteral iron-replacement\ntherapy. Upon administration and absorption, the iron dextran complex is\nremoved from plasma by the reticuloendothelial system which cleaves it\ninto the components iron and dextran; ferric iron subsequently binds to\ntransferrin or is stored as hemosiderin or ferritin. Transferrin-bound\niron is transported in the plasma to the liver, spleen and bone marrow,\nwhere is it is incorporated into hemoglobin (Hgb) and to muscle where it\nis incorporated into myoglobin (Mb). Use of this agent circumvents the\ngastrointestinal adverse effects commonly encountered with the use of\norally administered iron salt preparations. Because of cross-reactivity with antibodies targeted against\npolysaccharides similar to dextran, anaphylactic reactions may occur with\nthis type of iron formulation. 551892 transferrin receptor-targeted liposomal p53 cDNA A cationic liposomal, tumor-targeting p53 (TP53) gene delivery system with potential anti-tumor activity. Transferrin receptor-targeted liposomal p53 cDNA contains plasmid DNA encoding the tumor suppressor protein p53 packaged in membrane-like liposome capsules that are complexed with anti-transferrin receptor single-chain antibody (TfRscFv). Upon systemic administration, the anti-TfRscFv selectively binds to tumor cells expressing transferrin receptors. The p53 plasmid is delivered into the nucleus and as a result, p53 protein is produced in tumor cells that have altered p53 function. This results in the restoration of normal cell growth control mechanisms as well as normal response mechanisms to DNA damage. C29474 551902 xenogeneic tyrosinase DNA vaccine A plasmid DNA vaccine, encoding an epitope of mouse tyrosinase, with potential antineoplastic activity. Administered via intramuscular electroporation, vaccination with xenogeneic tyrosinase DNA vaccine may induce both humoral and cytotoxic lymphocyte (CTL) immune responses against melanoma cells that express tyrosinase, resulting in decreased tumor growth. . C68839 552648 doxorubicin prodrug INNO-206 A 6-maleimidocaproyl hydrazone derivative prodrug of the anthracycline antibiotic doxorubicin (DOXO-EMCH) with antineoplastic activity. Following intravenous administration, doxorubicin prodrug INNO-206 binds selectively to the cysteine-34 position of albumin via its maleimide moiety. Doxorubicin is released from the albumin carrier after cleavage of the acid-sensitive hydrazone linker within the acidic environment of tumors and, once located intracellularly, intercalates DNA, inhibits DNA synthesis, and induces apoptosis. Albumin tends to accumulate in solid tumors as a result of high metabolic turnover, rapid angiogenesis, hyervasculature, and impaired lymphatic drainage. Because of passive accumulation within tumors, this agent may improve the therapeutic effects of doxorubicin while minimizing systemic toxicity. C68921 552699 minocycline hydrochloride The hydrochloride salt of minocycline, a broad spectrum long-acting derivative of the antibiotic tetracycline, with antibacterial and anti-inflammatory activities. Minocycline binds to the bacterial 30S ribosomal subunit and interferes with the binding of tRNA to the ribosomal complex, thereby inhibiting protein translation in bacteria. In addition, minocycline inhibits the inflammatory enzyme 5-lipoxygenase (5LOX) and may impede T cell-microglia interactions; both activities may contribute to minocycline's neuroprotective effects. 5LOX catalyzes the synthesis of inflammatory mediators such as prostaglandins and leukotrienes. 552702 clindamycin/hydrocortisone lotion A topical lotion, containing clindamycin and hydrocortisone, with antibacterial and anti-inflammatory activities. Clindamycin, a lincomycin antibiotic, binds to the 50S subunit of the bacterial ribosome, thereby inhibiting bacterial protein synthesis. As a glucocorticoid agonist, hydrocortisone promotes protein catabolism, gluconeogenesis, capillary wall stability, renal excretion of calcium, and suppression of immune and inflammatory responses. C68844 552704 abiraterone acetate An orally active acetate salt of the steroidal compound abiraterone with antiandrogen activity. Abiraterone inhibits the enzymatic activity of steroid 17alpha-monooxygenase (17alpha-hydrolase/C17,20 lyase complex), a member of the cytochrome p450 family that catalyzes the 17alpha-hydroxylation of steroid intermediates involved in testosterone synthesis. Administration of this agent may suppress testosterone production by both the testes and the adrenals to castrate-range levels. C68845 552929 tapentadol hydrochloride ER An orally active, extended-release preparation of the hydrochloride salt of tapentadol with analgesic activity. Tapentadol is a synthetic, centrally acting analgesic with a dual mechanism of action involving mu-opioid receptor agonism and norepinephrine reuptake inhibition. This agent may be effective in the management of pain, cancer-related and other. C68922 552982 autologous Ad-CD154-transduced CLL B cells An autologous tumor cell vaccine containing chronic lymphocytic leukemia (CLL) B cells transduced with an adenoviral vector carrying chimeric CD154 (ad-CD154) with potential antineoplastic activity. Administration of autologous ad-CD154 transduced CLL B cells may result in increases in the numbers of leukemia-specific CD4+ T cells and high serum-levels of IL-12 and IFN-gamma. Due to ligation of CD154 to CD40 on CLL cells, this agent may induce CLL cells to express the proapoptotic molecule Bid and death receptors CD95 (Fas) and DR5, rendering CLL B cells first resistant and then sensitive to Fas-mediated apoptosis. In addition, autologous ad-CD154 transduced CLL B cells may induce MHC class I-dependent cytotoxic T lymphocyte (CTL) responses against autologous leukemia cells. CD154 is a type II membrane glycoprotein and ligand for CD40; both molecules are important in cognate co-stimulatory cell-cell interactions. C68842 553253 pan HER/VEGFR2 receptor tyrosine kinase inhibitor BMS-690154 A pyrrolotriazine-based compound and a pan inhibitor of receptor tyrosine kinases with potential antineoplastic activity. Pan HER/VEGFR2 receptor tyrosine kinase inhibitor BMS-690154 binds to human epidermal growth factor receptors 1 and 2 (HER1, HER2) and vascular endothelial growth factor receptor 2 (VEGFR-2), all three of which are frequently overexpressed by a variety of tumor types. Binding of this agent to these receptors may result in the inhibition of tumor cell proliferation; the inhibition of endothelial cell migration and proliferation and angiogenesis; and tumor cell death. C68832 553413 efalizumab A humanized IgG1 monoclonal antibody directed against CD11a, the alpha subunit of human leukocyte-function-associated antigen type 1 (LFA-1), with immunosuppressant activity. Efalizumab binds to CD11a, which is expressed on all leukocytes, resulting in a reduction in the cell surface expression of CD11a. In addition, this agent inhibits the binding of LFA-1 to intercellular adhesion molecule-1 (ICAM-1), resulting in the inhibition of leukocyte adherence and the suppression of cell-mediated immunity. LFA-1 binding to ICAM-1 is involved in the activation of T lymphocytes, adhesion of\n\nT lymphocytes to endothelial cells, and migration of T lymphocytes to sites of inflammation. C68831 553530 tazarotene A synthetic, topical retinoid. Tazarotene induces the expression of tazarotene-induced gene 3 (TIG3), a tumor suppressor gene. In psoriasis, tazarotene normalizes abnormal keratinocyte differentiation and reduces their hyperproliferation. 553625 HDAC inhibitor CRA-024781 A novel, broad-spectrum hydroxamic acid-based inhibitor of histone deacetylase (HDAC) with potential antineoplastic activity. HDAC inhibitor CRA-024781 inhibits several isoforms of HDAC, resulting in an accumulation of highly acetylated histones, followed by the induction of chromatin remodeling; the selective transcription of tumor suppressor genes; and the tumor suppressor protein-mediated inhibition of tumor cell division and induction of tumor cell apoptosis.\n HDAC, upregulated in many tumor types, is an an enzyme that is responsible for the deacetylation of chromatin histone proteins. C68920 553629 duloxetine hydrochloride The hydrochloride salt of duloxetine, a fluoxetine derivative belonging to the class of selective serotonin (5-HT) and norepinephrine (NE) reuptake inhibitors (SSNRIs) and exhibiting antidepressant activity. Duloxetine selectively prevents the reuptake of 5-HT and NE via transporter complexes on the pre-synaptic membrane, thereby increasing the level of these neurotransmitters within the synaptic cleft. As a result, this agent potentiates serotonergic and noradrenergic activities in the central nervous system, and alleviates depression and neuropathy sensations, such as pain and tingling. Furthermore, duloxetine does not show significant affinity for dopaminergic, adrenergic, cholinergic, histaminergic, opioid, glutamate, and gamma-aminobutyric acid (GABA) receptors. 554706 Se-methyl-seleno-L-cysteine A naturally occurring organoselenium compound found in many plants, including garlic, onions, and broccoli, with potential antioxidant and chemopreventive activities. Se-Methyl-seleno-L-cysteine (MSC) is an amino acid analogue of cysteine in which a methylselenium moiety replaces the sulphur atom of cysteine. This agent acts as an antioxidant when incorporated into glutathione peroxidase and has been shown to exhibit potent chemopreventive activity in animal models. C68823 554979 lipsomal cytarabine-daunorubicin CPX-351 A liposomal formulation containing a fixed combination of the antineoplastic agents cytarabine and daunorubicin in a 5:1 molar ratio. Liposomal cytarabine-daunorubicin CPX-351 has been designed to provide optimal delivery of a specific ratio of cytarabine to daunorubicin, one that has been shown to be synergistic in vitro. The antimetabolite cytarabine competes with cytidine for incorporation into DNA, inhibiting DNA synthesis. This agent also inhibits DNA polymerase, resulting in a decrease in DNA replication and repair. Daunorubicin, an intercalator and a topoisomerase II inhibitor, prevents DNA replication and inhibits protein synthesis. This agent also generates oxygen free radicals, resulting in the cytotoxic lipid peroxidation of cell membrane lipids. C67504 555065 petrolatum-mineral oil-lanolin-ceresin ointment A petrolatum-based ointment absorbed by dry and moist skin, petrolatum-mineral oil-lanolin-ceresin ointment is non-comedogenic, non-irritating, and non-sensitizing. It can reduce healing time of cracked, dry skin on hands, elbows, and knees, and helps prevent diaper rash. The original ointment also contained mineral oil, ceresin, lanolin alcohol. Its use is indicated in atopic dermatitis, eczema, and psoriasis when extra protection from a heavier base is needed. C28832 555067 sodium hyaluronate topical hydrogel A proprietary topical gel formulation containing sodium hyaluronate with wound repair and skin moisturizing properties. Upon application, sodium hyaluronate topical hydrogel adheres to injured tissues, hydrates skin, and provides protection from further chemical or mechanical irritation. Hyaluronate, a non-sulfated glucosaminoglycan, is a chief component of the extracellular matrix in connective, epithelial, and neural tissues and contributes significantly to cell proliferation and migration. C68822 555445 PGLA/PEG copolymer-based paclitaxel A controlled-release, intratumoral paclitaxel formulation in which paclitaxel is incorporated into a thermosensitive, biodegradable triblock copolymer consisting of poly(lactide-co-glycolide) (PLGA) and polyethylene glycol (PEG). Upon intratumoral injection, paclitaxel is released slowly and continuously into tumor tissues from the gelled thermosensitive triblock copolymer over a period of 4 to 6 weeks; in tumor cells, paclitaxel binds to tubulin and inhibits the disassembly-assembly dynamics of microtubules, resulting in cell cycle arrest and cell death. The thermosensitive triblock copolymer component of this formulation transforms from a water-soluble polymer at room temperature to a water-insoluble, biodegradable gel depot at body temperature; intratumoral controlled-release of paclitaxel from the gel minimizes systemic exposure to paclitaxel and the paclitaxel toxicity profile. C71692 555507 apomab A fully human monoclonal antibody directed against human death receptor 5 (DR5; TRAIL-R2; TNFRSF10B) with potential proapoptotic and antineoplastic activities. Mimicking the natural ligand TRAIL (tumor necrosis factor-related apoptosis inducing ligand), apomab binds to DR5, which may directly activate the extrinsic apoptosis pathway and indirectly induce the intrinsic apoptosis pathway in tumor cells. DR5 is a cell surface receptor of the TNF-receptor superfamily and is expressed in a broad range of cancers. C71693 555692 anti-EpCAM antibody fragment-bouganin fusion protein A fusion protein immunotoxin consisting of a humanized, single-chain monoclonal antibody Fab fragment specific for the epithelial cell adhesion molecule (EpCAM) conjugated with a modified bouganin cytotoxin with potential antineoplastic activity. Anti-EpCAM antibody fragment-bouganin fusion protein binds to EpCAM, delivering modified bouganin cytotoxin directly to EpCam-positive tumor cells, which may result in the inhibition of tumor cell protein synthesis and tumor cell death. EpCAM, a cell surface protein, is expressed by a variety of tumor cells and is frequently found in head and neck cancers. Bouganin is a plant-derived ribosome-inactivating protein (RIP), a toxic plant N-glycosidase that depurinates the universally conserved alpha-sarcin loop of ribosomal rRNA, inactivating the ribosome and preventing protein synthesis. Compared to unmodified bouganins, modified bouganins may have a reduced propensity to activate human T cells. 557106 serine protease inhibitor WX-671 An orally bioavailable, 3-amidinophenylalanine-derived, second generation serine protease inhibitor prodrug targeting the human urokinase plasminogen activator (uPA) system with potential antineoplastic and antimetastatic activities. After oral administration, serine protease inhibitor WX-671 is converted to the active Nα-(2,4,6-triisopropylphenylsulfonyl)-3-amidino-(L)-phenyla lanine-4-ethoxycarbonylpiperazide (WX-UK1), which inhibits several serine proteases, particularly uPA; inhibition of uPA may result in the inhibition of tumor growth and metastasis. uPA is a serine protease involved in degradation of the extracellular matrix and tumor cell migration and proliferation. C73985 557567 nanoparticle albumin-bound docetaxel ABI-008 A nanoparticle albumin-bound formulation of the taxane docetaxel with antineoplastic activity. Docetaxel is a semi-synthetic, second-generation taxane derived from a compound found in the European yew tree Taxus baccata. Docetaxel binds to and stabilizes tubulin, thereby inhibiting microtubule disassembly which results in cell-cycle arrest at the G2/M phase and cell death. This agent also inhibits pro-angiogenic factors such as vascular endothelial growth factor (VEGF) and displays immunomodulatory and pro-inflammatory properties by inducing various mediators of the inflammatory response. In nanoparticle albumin-bound docetaxel ABI-008 docetaxel is solubilized without the use of the nonionic solubilizer Cremophor ELP, permitting the administration of larger doses of docetaxel while avoiding Cremophor ELP-associated toxicity. C71696 557569 anti-IGF-1 receptor human monoclonal antibody R1507 A recombinant, fully human monoclonal antibody directed against the insulin-like growth factor-1 receptor (IGF-1R) with potential antineoplastic activity. Anti-IGF-1R human monoclonal antibody R1507 binds to membrane-bound IGF-1R, preventing the binding of the natural ligand IGF-1 and the activation of PI3K/AKT signal transduction; downregulation of the PI3K/AKT survival pathway may result in the induction of apoptosis and decreased cellular proliferation. The activation of IGF-1R, a receptor tyrosine kinase of the insulin receptor superfamily, stimulates cell proliferation, enables oncogenic transformation, and suppresses apoptosis; IGF-1R signaling has been implicated in tumorigenesis and metastasis. C71697 557721 DC-OVA vaccine An autologous, multivalent dendritic cell vaccine targeting ovarian cancer with potential immunostimulating and antineoplastic activities. DC-OVA vaccine is produced in vitro by pulsing autologous dendritic cells with killed autologous primary ovarian tumors as a source of tumor-associated antigens (TAAs); the pulsed DCs are then matured using various cytokines. Upon administration, DC-OVA vaccine may stimulate a cytotoxic T lymphocyte (CTL) response against ovarian cancer TAA-expressing ovarian cancer cells. 558123 cytokine-induced killer cells A preparation of autologous lymphocytes with potential immunopotentiating and antineoplastic activities. Cytokine-induced killer (CIK) cells are CD3-and CD56-positive, non-major histocompatibility complex (MHC)-restricted, natural killer (NK)-like T lymphocytes, generated ex-vivo by incubation of peripheral blood lymphocytes (PBLs) with anti-CD3 monoclonal antibody, interleukin (IL)-2, IL-1, and interferon gamma (IFN-gamma) and then expanded. When reintroduced back to patients after autologous stem cell transplantation, CIK cells may recognize and kill tumor cells associated with minimal residual disease (MRD). \nCIK cells may have enhanced cytotoxic activity compared to lymphokine-activated killer (LAK) cells. C71757 558131 indium In 111 pentetate A sterile, non-pyrogenic, isotonic solution of radioactive indium In 111 diethylenetriamine pentaacetate (DTPA). When administered intrathecally, indium In 111 pentetate percolates up the spinal canal with the cerebrospinal fluid (CSF) to the basal cisterns of the posterior and middle cranial fossas. This agent is used in radionuclide cisternography to image the flow of CSF, for the identification of abnormalities in CSF circulation, for location of sites of CSF leakage, and for evaluation of CSF shunt patency. Normally, this agent does not penetrate into the brain ventricles. C71725 558132 gallium citrate Ga 67 The citrate salt of the radioisotope gallium Ga 67. Although the mechanism is unknown, gallium Ga 67 concentrates in lysosomes and is bound to a soluble intracellular protein in certain viable primary and metastatic tumors and focal sites of inflammation, allowing scintigraphic localization. Ga-67 scintigraphy (GS) cannot differentiate between tumor and acute inflammation. 558806 modified vaccinia Ankara (Bavarian Nordic)-HER2 vaccine A cancer vaccine consisting of a proprietary, recombinant modified vaccinia Ankara (MVA) viral vector encoding an epitope of human epidermal growth factor receptor 2 (HER2) with potential antineoplastic activity. Upon administration, modified vaccinia Ankara (Bavarian Nordic)-HER2 vaccine may stimulate the host immune system to mount humoral and cytotoxic T lymphocyte responses against HER2-expressing tumor cells, resulting in tumor cell lysis. HER2, also known as ErbB-2, is a tyrosine kinase growth factor receptor and a member of the epidermal growth factor receptor family; it plays a significant role in the pathogenesis of some breast cancers. C71758 558903 quarfloxacin A fluoroquinolone derivative with antineoplastic activity. Quarfloxin disrupts the interaction between the nucleolin protein and a G-quadruplex DNA structure in the ribosomal DNA (rDNA) template, a critical interaction for rRNA biogenesis that is overexpressed in cancer cells; disruption of this G-quadruplex DNA:protein interaction in aberrant rRNA biogenesis may result in the inhibition of ribosome synthesis and tumor cell apoptosis. C71726 558906 phosphatidylcholine-bound silybin An oral preparation of the flavonoid silybin with potential antioxidant and chemopreventive activities. Silybin, also known as silibinin, is a mixture of two stereoisomers, denoted silybin A and silybin B, and is the major active constituent of silymarin, a mixture of flavonolignans extracted from blessed milk thistle (Silybum marianum). Silybin modulates P-glycoprotein (P-gp)-mediated cellular efflux; has oxygen radical-scavenging effects; inhibits the arachidonic acid pathway; and inhibits various cytochrome P450 enzymes. This agent may also exhibit anti-angiogenic activity, possibly by inducing endothelial cell apoptosis via modulation of\nthe transcription factor NF-kB, the Bcl-2 family of proteins, and caspases. Complexing silybin with phosphatidylcholine increases its bioavailability. C71883 558907 PI3K/mTOR dual kinase inhibitor XL765 An orally bioavailable small molecule targeting the phosphatidylinositol 3 kinase (PI3K) and mammalian target of rapamycin (mTOR) kinases in the PI3K/mTOR signaling pathway, with potential antineoplastic activity. PI3K/mTOR dual kinase inhibitor XL765 inhibits both PI3K kinase and mTOR kinase, which may result in tumor cell apoptosis and growth inhibition in susceptible tumor cell populations. Activation of the PI3K/mTOR pathway promotes cell growth, survival, and resistance to chemotherapy and radiotherapy; mTOR, a serine/threonine kinase downstream of PI3K, may also be activated in a PI3K-independent fashion in response to nutrient and energy deprivation. Accordingly, this agent maybe more potent compared to an agent that inhibits either PI3K kinase or mTOR kinase alone. C71704 558909 Class 1 PI3K kinase family inhibitor XL147 An orally bioavailable small molecule, targeting the class I phosphatidylinositol 3 kinase (PI3K) family of lipid kinases, with potential antineoplastic activity. Class 1 PI3K kinase family inhibitor XL147 reversibly binds to class 1 PI3Ks in an ATP-competitive manner, inhibiting the production of the secondary messenger phosphatidylinositol-3,4,5-trisphosphate (PIP3) and activation of the PI3K signaling pathway; this may result in inhibition of tumor cell growth and survival in susceptible tumor cell populations. Activation of the PI3K signaling pathway is frequently associated with tumorigenesis. Dysregulated PI3K signaling may contribute to tumor resistance to a variety of antineoplastic agents including genotoxic agents and receptor tyrosine kinase inhibitors. C71705 558911 nifurtimox A nitrofuran derivative with antiprotozoal and potential antineoplastic activities. Nifurtimox is reduced by cytosol enzymes or flavin-containing microsomal enzymes to a highly reactive nitro anion free radical; autooxidation of the nitro anion free radical generates cytotoxic superoxide anion (02-). In addition, nifurtimox-derived nitro anion free radicals may alkylate macromolecules such as nucleic acids and proteins, resulting in the disruption of their structure and function. C71734 558913 linifanib An orally bioavailable, small-molecule receptor tyrosine kinase (RTK) inhibitor with potential antineoplastic activity. Linifanib inhibits members of the vascular endothelial growth factor (VEGF) and platelet-derived growth factor (PDGF) receptor families; it exhibits much less activity against unrelated RTKs, soluble tyrosine kinases, or serine/threonine kinases. This agent does not have a general antiproliferative effect due to its high dose requirement. However, linifanib may exhibit potent antiproliferative and apoptotic effects on tumor cells whose proliferation is dependent on mutant kinases, such as fms-related tyrosine kinase receptor-3 (FLT3). C71759 559159 hTERT I540/R572Y/D988Y multipeptide vaccine A peptide vaccine consisting of multiple epitopes derived from the human telomerase reverse transcriptase (hTERT), the catalytic subunit of human telomerase, with potential immunostimulating and antineoplastic activities. hTERT I540/R572Y/D988Y multipeptide vaccine contains strongly antigenic peptide epitopes I540 (9-mer), R572Y (9-mer) and D988Y (10-mer). Vaccination with this agent may elicit a cytotoxic T cell (CTL) response against telomerase-expressing tumor cells. Directly linked to tumorigenesis, telomerase is expressed in the majority of human cancer cells but is infrequently expressed in normal cells. C71761 559164 survivin Sur1M2 peptide vaccine A modified recombinant nonapeptide (LMLGEFLKL) derived from the anti-apoptosis protein survivin with potential immunopotentiating and antineoplastic activities. Upon administration, survivin Sur1M2 peptide vaccine may elicit humoral and cellular immune responses against survivin-expressing cancers, resulting in decreased tumor cell proliferation and tumor cell death. The survivin protein inhibits caspase activation and apoptosis; it is undetectable in normal adult tissues but is expressed by several human cancers including lung, colon, breast, pancreas, and prostate cancer as well as hematopoietic malignancies and skin cancers. C71741 559165 CMV N495 peptide A nonapeptide consisting of amino acid residues 495-503 of the cytomegalovirus (CMV) internal matrix protein pp65 with immunostimulating activity. CMV N495 peptide may used as a control to gauge immunocompetence in individuals receiving cancer vaccines. C26640 559200 Hsp27 antisense oligonucleotide OGX-427 A second-generation antisense oligonucleotide targeting heat shock protein 27 (Hsp27) with potential antitumor and chemosensitizing activities. Hsp27 antisense oligonucleotide OGX-427 suppresses tumor cell expression of Hsp27, which may induce tumor cell apoptosis and enhance tumor cell sensitivity to cytotoxic agents. Hsp27, a chaperone belonging to the small heat shock protein (sHsp) group of proteins, is a cytoprotective protein that supports cell survival under conditions of stress; it has been found to be over-expressed in a variety of human cancers. C71740 559298 mirtazapine A synthetic tetracyclic derivative of the piperazino-azepines with antidepressant activity. Although its mechanism of action is unknown, mirtazapine enhances central adrenergic and serotonergic transmission, possibly by acting as an antagonist at central presynaptic alpha 2 adrenergic inhibitory autoreceptors and heteroreceptors. This agent is a potent antagonist of 5-hydroxytryptamine type 2 (5-HT2), 5-HT3, and histamine 1 (H1) receptors, and a moderate anatgonist of peripheral alpha 1 adrenergic and muscarinic receptors. 559320 multitargeted receptor tyrosine kinase inhibitor MP470 An orally bioavailable synthetic carbothioamide with potential antineoplastic activity. Multitargeted receptor tyrosine kinase inhibitor MP470 binds to mutant forms of the stem cell factor receptor (c-Kit; SCFR), inhibiting clinically relevant mutants of this receptor tyrosine kinase that may be associated with resistance to therapy. In addition, MP470 inhibits activities of other receptor tyrosine kinases, such as c-Met, Ret oncoprotein, and mutant forms of Flt3 and PDGFR alpha, which are frequently dysregulated in variety of tumors. This agent also suppresses the induction of DNA repair protein Rad51, thereby potentiating the activities of DNA damage-inducing agents.\nMutant forms of c-Kit are often associated with tumor chemoresistance. C71750 559621 dendritic cell-idiotype-keyhole limpet hemocyanin vaccine A cell-based vaccine composed of allogeneic dendritic cells (DC), pulsed with patient-specific non-Hodgkin's lymphoma idiotype (Id) determinants conjugated to keyhole limpet hemocyanin (KLH), with potential antitumor activity. Upon administration, this vaccine may stimulate the host immune system to mount a specific cytotoxic T-lymphocyte (CTL) response against Id-expressing lymphoma cells, resulting in tumor cell lysis. C71760 559644 HDAC inhibitor SB939 An orally bioavailable, small-molecule histone deacetylase (HDAC) inhibitor with potential antineoplastic activity. HDAC inhibitor SB939 inhibits HDACs, which may result in the accumulation of highly acetylated histones, followed by the induction of chromatin remodeling; the selective transcription of tumor suppressor genes; the tumor suppressor protein-mediated inhibition of tumor cell division; and, finally, the induction of tumor cell apoptosis. This agent may possess improved metabolic, pharmacokinetic and pharmacological properties compared to other HDAC inhibitors. C71708 560167 intranasal ketamine An intranasal formualtion of the synthetic cyclohexanone ketamine with analgesic and anesthetic activities. Although its mechanism of action is not well understood, ketamine appears to non-competitively block N-methyl-D-aspartate (NMDA) receptors and agonistically bind to and activate opiod mu and sigma receptors, thereby reducing pain perception, inducing sedation, and producing dissociative anesthesia. C71709 560174 anti-denatured collagen recombinant monoclonal antibody TRC093 A humanized, affinity-matured IgG1k antibody directed against denatured collagens (I-IV) with potential antiangiogenic and antineoplastic activities. Anti-denatured collagen recombinant monoclonal antibody TRC093 binds to multiple epitopes on denatured collagens, inhibiting proteolytic collagen-mediated signaling in the extracellular matrix (ECM) that is important to tumor angiogenesis, tumor growth, and metastasis. The epitopes on denatured collagen bound by this antibody are considered "cryptic" because, in vivo, they are accessible only on the subendothelial basement membrane of tumors or in normal tissues undergoing neovascularization. C71749 560180 mitosis-angiogenesis inhibitor R1530 A pyrazolobenzodiazepine small molecule with potential antiangiogenesis and antineoplastic activities. Mitosis-angiogenesis inhibitor (MAI) R1530 inhibits multiple receptor tyrosine kinases involved in angiogenesis, such as vascular endothelial growth factor receptor (VEGFR)-1, -2, -3, platelet-derived growth factor receptor (PDGFR) beta‚ FMS-like tyrosine kinase (Flt)-3, and fibroblast growth factor receptor (FGFR) -1, -2. In addition, this agents exhibits anti-proliferative activity by initiating mitotic arrest and inducing apoptosis. C71710 560189 pan-AKT kinase inhibitor GSK690693 An aminofurazan-derived inhibitor of Akt kinases with potential antineoplastic activity. Pan-AKT kinase inhibitor GSK-690693 binds to and inhibits Akt kinases 1, 2, and 3, which may result in the inhibition of protein phosphorylation events downstream from Akt kinases in the PI3K/Akt signaling pathway, and, subsequently, the inhibition of tumor cell proliferation and the induction of tumor cell apoptosis. In addition, this agent may inhibit other protein kinases including protein kinase C (PKC) and protein kinase A (PKA). As serine/threonine protein kinases which are involved in a number of biological processes, AKT kinases promote cell survival by inhibiting apoptosis and are required for glucose transport. C71711 560190 autologous anti-gp100:154-162 T-cell receptor gene-engineered peripheral blood lymphocytes Human autologous peripheral blood lymphocytes (PBLs) transduced with a glycoprotein 100 (gp100) epitope-determined T cell receptor (TCR) gene, with potential antineoplastic activity. PBLs are isolated from a melanoma patient and pulsed with a viral vector encoding the TCR specific for amino acid residues 154-162 of gp100 (KTWGQYWQV). After expansion ex vivo, the transduced autologous PBLs, expressing this specific TCR, are reintroduced into the patient and bind to melanoma cells expressing the gp100 protein, which may result in specific cytotoxic T-lymphocyte (CTL) killing of gp100-expressing melanoma cells. gp100 is a melanocyte lineage-specific antigen overexpressed in melanomas. C71748 560191 olaparib A small molecule inhibitor of the nuclear enzyme poly(ADP-ribose) polymerase (PARP) with potential chemosensitizing, radiosensitizing, and antineoplastic activities. Olaparib selectively binds to and inhibits PARP, inhibiting PARP-mediated repair of single strand DNA breaks; PARP inhibition may enhance the cytotoxicity of DNA-damaging agents and may reverse tumor cell chemoresistance and radioresistance.\nPARP catalyzes post-translational ADP-ribosylation of nuclear proteins and can be activated by single-stranded DNA breaks. C71721 560192 autologous anti-MART-1 F5 T-cell receptor gene-engineered peripheral blood lymphocytes Human autologous peripheral blood lymphocytes (PBLs) transduced with a melanoma antigen MART-1 epitope-determined T cell receptor (TCR) gene, with potential antineoplastic activity. PBLs are isolated from a melanoma patient and pulsed with a viral vector that encodes the TCR specific for an epitope of MART-1 (F5 TCR). After expansion ex vivo, the transduced autologous PBLs, expressing this specific TCR, are reintroduced into the patient, and bind to melanoma cells expressing the MART-1 antigen, which may result in specific cytotoxic T-lymphocyte (CTL) killing of MART-1-expressing melanoma cells. MART-1 (melanoma antigen recognized by T cells 1), also known as Melan-A, is a melanocyte lineage-specific transmembrane protein. C38587 560194 hypoxia-activated prodrug TH-302 A hypoxia-activated prodrug consisting of a 2-nitroimidazole phosphoramidate conjugate with potential antineoplastic activity. The 2-nitroimidazole moiety of hypoxia-activated prodrug TH-302 acts as a hypoxic trigger, releasing the DNA-alkylating dibromo isophosphoramide mustard moiety within hypoxic regions of tumors. Normoxic tissues may be spared due to the hypoxia-specific activity of this agent, potentially reducing systemic toxicity. C71722 560207 cytomegalovirus pp65-specific cytotoxic T lymphocytes Cytotoxic T lymphocytes (CTLs) specifically reactive to the cytomegalovirus (CMV) phosphoprotein pp65 with potential antiviral activity. To prepare CMV pp65-specific cytotoxic T lymphocytes in vitro, dendritic cells (DCs) are pulsed with CMV pp65 epitopes and then used to stimulate and propagate CMV pp65-specific cytotoxic T lymphocytes from peripheral blood mononuclear cells (PBMNCs); the CMV pp65-specific cytotoxic T lymphocyte population is then expanded so as to be sufficient for use in adoptive T lymphocyte therapy. When administered into a patient post-allogeneic hematopoietic stem cell transplantation, this agent may elicit a specific CTL response against CMV-infected host cells, which may result in the resolution of CMV infection. The CMV pp65 protein (65 kDa lower matrix phosphoprotein), the primary component of the enveloped subviral particle, is an immunodominant target for helper and cytotoxic T lymphocyte responses to CMV. C71747 560209 glycosylated recombinant human G-CSF AVI-014 A glycosylated form of a recombinant agent that is chemically identical to or similar to endogenous human granulocyte colony-stimulating factor (G-CSF) and is produced using transgenic biotechnology. Transgenic hens carrying recombinant human G-CSF cDNA express the naturally glycosylated recombinant human protein in egg albumen from which glycosylated recombinant human G-CSF AVI-014 is isolated. Produced endogenously by monocytes, fibroblasts, and endothelial cells, G-CSF binds to and activates specific cell surface receptors, stimulating neutrophil progenitor proliferation and differentiation and selected neutrophil functions. C74520 560733 S-adenosyl-L-methionine disulfate p-toluene-sulfonate The disulfate salt of the stable p-toluene-sulfonate complex of s-adenosyl-L-methionine (SAMe) with chemopreventive activity. SAMe disulfate p-toluene-sulfonate undergoes hydrolytic conversion to its active compound SAMe within cells. Although the mechanism of action is largely unknown, SAMe attenuates experimental liver damage and prevents experimental hepatocarcinogenesis. In addition, SAMe may reduce mitochondrial cytochrome C release, caspase 3 activation, and poly(ADP-ribose) polymerase cleavage, and attenuate okadaic acid-mediated hepatocyte apoptosis in a dose-dependent manner. SAMe is an essential compound in cellular transmethylation reactions and a precursor of polyamine and glutathione synthesis in the liver; SAMe deficiency is associated with chronic liver disease-associated decreases in the activity of methionine adenosyltransferase 1A (MAT1A), the enzyme that catalyzes the production of SAMe as the first step in methionine catabolism. C71745 560749 IL-2 recombinant fusion protein ALT-801 A recombinant protein consisting of the cytokine interleukin-2 (IL-2) fused to a humanized soluble T-cell receptor (TCR) directed against a tumor suppressor p53-derived antigen with potential immunopotentiating and antineoplastic activities. The TCR moiety of IL-2 recombinant fusion protein ALT-801 binds to tumor cells displaying p53 epitope/MHC complexes; subsequently, the tumor cell-localized IL-2 moiety may stimulate natural killer (NK) cell and T cell cytotoxic immune responses against p53-expressing tumor cells. C71743 560751 gavinostat An orally bioavailable hydroxymate inhibitor of histone deacetylase (HDAC) with potential anti-inflammatory, anti-angiogenic, and antineoplastic activities. Gavinostat inhibits class I and class II HDACs, resulting in an accumulation of highly acetylated histones, followed by the induction of chromatin remodeling and an altered pattern of gene expression. At low, nonapoptotic concentrations, this agent inhibits the production of pro-inflammatory cytokines such as tumor necrosis factor- (TNF-), interleukin-1 (IL-1), IL-6 and interferon-gamma. \nHDAC inhibitor ITF2357 has also been shown to activate the intrinsic apoptotic pathway, inducing apoptosis in hepatoma cells and leukemic cells. This agent may also exhibit anti-angiogenic activity, inhibiting the production of angiogenic factors such as IL-6 and vascular endothelial cell growth factor (VEGF) by bone marrow stromal cells. C71716 560774 selective androgen receptor modulator MDV3100 An orally bioavailable, organic, non-steroidal small molecule targeting the androgen receptor (AR) with potential antineoplastic activity. Through a mechanism that is reported to be different from other approved AR antagonists, selective androgen receptor modulator MDV3100 inhibits the activity of prostate cancer cell ARs, which may result in a reduction in prostate cancer cell proliferation and, correspondingly, a reduction in the serum prostate specific antigen (PSA) level. AR over-expression in prostate cancer represents a key mechanism associated with prostate cancer hormone resistance. C71744 560777 baclofen A synthetic chlorophenyl-butanoic acid derivative with muscle relaxant activity. Baclofen acts as a gamma-aminobutyric acid (GABA) agonist specific for GABA-B receptors in the central nervous system (CNS). At spinal and supraspinal sites, this agent reduces excitatory transmission. 560932 nucleotide analogue GS 9219 A prodrug of the acyclic nucleoside phosphonate analogue 9-(2-phosphonylmethoxyethyl)guanine (PMEG) with potential antineoplastic activity. Formulated to selectively accumulate in lymphocytes, nucleotide analogue GS 9219 is converted to its active metabolite, PMEG diphosphate (PMEGpp), via enzymatic hydrolysis, deamination, and phosphorylation; subsequently, PMEGpp is incorporated into nascent DNA chains by DNA polymerases, which may result in the termination of DNA synthesis, S-phase cell cycle arrest, and the induction of apoptosis in susceptible lymphoma cell populations. C71742 561025 pegylated granulocyte colony stimulating factor MAXY-G34 A long-acting, pegylated recombinant variant of human granulocyte colony-stimulating factor (G-CSF) with immunomodulating activity. Pegylated granulocyte colony stimulating factor MAXY-G34 contains multiple non-naturally occurring lysines that have been introduced into\nalpha helixes of wild type human G-CSF as pegylation sites; other naturally occurring lysine residues have been removed to prevent pegylation and the variant G-CSF is pegylated with methoxypolyethylene glycol succinimidyl propionate (mPEG SPA) at three amino acid residues. Similar to endogenous G-CSF, this agent binds to and activates specific cell surface receptors, stimulating neutrophil progenitor proliferation and differentiation and selected neutrophil functions. A difference in the degree of pegylation may account for the extended half-life of this agent compared to pegfilgrastim which is pegylated at only one amino acid residue. C71718 561135 prostate cancer vaccine ONY-P1 A cell-based vaccine derived from prostate cancer with potential immunopotentiating and antineoplastic activities. Prostate cancer vaccine ONY-P1 is derived from three irradiated allogeneic prostate cancer cell lines that represent different stages of prostate cancer and express a broad range of prostate and prostate cancer antigens. Upon administration, this vaccine may stimulate a host immune response against prostate cancer cells; in the vaccination schedule, the first two vaccinations are co-administered with bacillus Calmette-Guerin (BCG) as an adjuvant. C71723 561286 Aurora A kinase inhibitor MLN8237 A second-generation, orally bioavailable, highly selective small molecule inhibitor of the serine/threonine protein kinase Aurora A kinase with potential antineoplastic activity. Aurora kinase inhibitor MLN8237 binds to and inhibits Aurora A kinase, which may result in disruption of the assembly of the mitotic spindle apparatus, disruption of chromosome segregation, and inhibition of cell proliferation. Aurora A kinase localizes to the spindle poles and to spindle microtubules during mitosis, and is thought to regulate spindle assembly. Aberrant expression of Aurora kinases occurs in a wide variety of cancers, including colon and breast cancers. C71717 561306 insulin aspart recombinant A recombinant human insulin analog with rapid-acting, blood glucose-lowering activity. Insulin aspart, acting faster than regular human insulin, regulates glucose metabolism by binding to insulin receptors on muscle and fat cells, thereby facilitating the cellular uptake of glucose. This lowers blood glucose levels. At the same time, insulin aspart inhibits the liver's conversion of stored glycogen into glucose, which also contributes to lower blood glucose levels. Insulin aspart also inhibits lipolysis in adipose tissue, inhibits proteolysis, and enhances protein synthesis. 561310 insulin glargine recombinant A recombinant human insulin analog with long-acting, blood glucose-lowering activity. Insulin glargine, like regular types of human insulin, regulates glucose metabolism by binding to insulin receptors on muscle and fat cells, thereby facilitating the cellular uptake of glucose. This lowers blood glucose levels. At the same time, insulin glargine inhibits the liver's conversion of stored glycogen into glucose, which also contributes to lower blood glucose levels. Insulin glargine also inhibits lipolysis in adipose tissue, inhibits proteolysis, and enhances protein synthesis. 561347 baclofen/amitriptyline/ketamine gel A topical preparation of baclofen, amitriptyline, and ketamine compounded in a penetration-enhancing polaxamer-lecithin organogel (PLO) with potential antineuralgic activity. The gamma-aminobutyric acid (GABA) analogue baclofen appears to activate the inhibitory GABA(B) receptor, a G protein-coupled receptor, which may result in hyperpolarization of the neuronal cell membrane and inhibition of neurotransmitter release. Amitriptyline likely produces antineuralgic effects via modulation of multiple subtypes of glutamate (Glu) receptors, independent of its antidepressant actions. Ketamine displays complex pharmacologic actions including biogenic amine uptake inhibition, interaction with opioid receptors, and inhibition of N-methyl D-aspartate (NMDA) receptors. Stimulation of GABA(B) receptor activity, modulation of Glu receptor activity, and inhibition of NMDA receptor activity may be of benefit in managing neuropathic pain. 561498 propranolol hydrochloride The hydrochloride form of propranolol, a synthetic beta-adrenergic receptor blocker with antianginal, antiarrhythmic, and antihypertensive properties. Propranolol competitively antagonizes beta-adrenergic receptors, thereby inhibiting beta-adrenergic reactions, such as vasodilation, and negative chronotropic and inotropic effects. 561499 etodolac A pyranocarboxylic acid and non-steroidal anti-inflammatory drug (NSAID) with antipyretic and analgesic activities. Etodolac inhibits the activity of cyclooxygenase I and II, thereby preventing the formation of prostaglandin which is involved in the induction of pain, fever, and inflammation. It also inhibits platelet aggregation by blocking platelet cyclooxygenase and the subsequent formation of thromboxane A2. 561575 cixutumumab A fully human IgG1 monoclonal antibody directed against the human insulin-like growth factor-1 receptor (IGF-1R) with potential antineoplastic activity. Cixutumumab selectively binds to membrane-bound IGF-1R, thereby preventing the binding of the natural ligand IGF-1 and the subsequent activation of PI3K/AKT signaling pathway. Downregulation of the PI3K/AKT survival pathway may result in the induction of cancer cell apoptosis and may decrease cancer cellular proliferation. IGF-1R, a receptor tyrosine kinase of the insulin receptor superfamily overexpressed by many cancer cell types, stimulates cell proliferation, enables oncogenic transformation, and suppresses apoptosis; IGF-1R signaling has been implicated in tumorigenesis and metastasis. C79828 561728 tivozanib An orally bioavailable inhibitor of vascular endothelial growth factor receptors (VEGFRs) 1, 2 and 3 with potential antiangiogenic and antineoplastic activities. Tivozanib binds to and inhibits VEGFRs 1, 2 and 3, which may result in the inhibition of endothelial cell migration and proliferation, inhibition of tumor angiogenesis and tumor cell death. VEGFR tyrosine kinases, frequently overexpressed by a variety of tumor cell types, play a key role in angiogenesis. 563224 wild-type reovirus A serotype 3 Dearing strain (T3D) of reovirus (Respiratory Enteric Orphan virus) with potential oncolytic activity. Reovirus, a dsRNA virus, is able to replicate specifically in cancer cells bearing an activated Ras pathway. In contrast to normal cells, two-thirds of human cancer cells are Ras-activated. Unlike normal cells, Ras-activated tumor cells are deficient in host cellular protein kinase R (PKR) activity and so are unable to mount an antiviral response. In Ras-activated tumor cells, reovirus freely replicates and induces apoptosis; tumor cell lysis frees progeny viral particles to infect surrounding tumor cells. A cycle of infection, replication and cell death may continue until Ras-activated tumor cells are eradicated. PKR (eukaryotic translation initiation factor 2-alpha kinase 2) is activated by viral synthesis of double-stranded RNA and is an important component of innate immunity in vertebrates, protecting against viral infection. C60774 564398 dulanermin A recombinant human soluble protein corresponding to amino acids 114-281 of the Apo2 ligand/tumor necrosis factor-related apoptosis-inducing ligand (RhApo2L/TRAIL) with potential antineoplastic activity. Dulanermin binds to and activates TRAIL receptors 1 and 2 (TRAIL-R1/R2), which may activate caspases and induce p53-independent apoptosis in TRAIL-R1/R2-expressing tumor cells. The pro-apoptotic cell surface receptors TRAIL-R1 and -R2, also known as DR4 (death receptor 4) and DR5 (death receptor 5), are members of the TNF receptor family and are overexpressed by a variety of cancer cell types. C1685 564399 trastuzumab-MCC-DM1 antibody-drug conjugate An antibody-drug conjugate (ADC) consisting of the recombinant anti-epidermal growth factor receptor 2 (HER2) monoclonal antibody trastuzumab conjugated to the maytansinoid DM1 via a nonreducible thioether linkage (MCC) with potential antineoplastic activity. The trastuzumab moiety of this ADC binds to HER2 on tumor cell surface surfaces; upon internalization, the DM1 moiety is released and binds to tubulin, thereby disrupting microtubule assembly/disassembly dynamics and inhibiting cell division and the proliferation of cancer cells that overexpress HER2. Linkage of antibody and drug through a nonreducible linker has been reported to contribute to the improved efficacy and reduced toxicity of this ADC compared to similar ADCs constructed with reducible linkers. C82492 564415 cefmetazole sodium The sodium salt of the second-generation, semi-synthetic, beta-lactam cephalosporin cefmetazole with antibacterial activity. Cefmetazole binds to penicillin-binding proteins (PBPs) and prevents the crosslinking of peptidoglycan, which may result in the inhibition of cell wall synthesis, the loss of cell wall integrity, and bacterial cell wall rupture. PBPs are transpeptidases that are responsible for peptidoglycan crosslinking. 564417 kanamycin sulfate The sulfate salt of kanamycin, a naturally occurring aminoglycoside antibiotic with antimicrobial property. Derived from Streptomyces kanamyceticus, kanamycin is an antibiotic complex consisting of three components: kanamycin A, the major component (also usually designated as kanamycin), and kanamycins B and C, the minor components. This agent irreversibly binds to the bacterial 30S ribosomal subunit. Specifically, this antibiotic is lodged between 16S rRNA and S12 protein within the 30S subunit. This leads to interference with translational initiation complex, misreading of mRNA, thereby hampering protein synthesis and resulting in bactericidal effect. Aminoglycosides are mostly ineffective against anaerobic bacteria, fungi and viruses. C65998 566102 selenomethionine A selenium (Se) analogue of methionine in which sulfur is replaced with the trace element selenium. Selenomethionine (SeMet) can incorporate into proteins in place of methionine with no effects on protein structure and function, providing a mechanism for reversible Se storage in organs and tissues. Free selenium is incorporated into selenocysteine, an amino acid found in more than thirty selenoproteins including the glutathione peroxidases (GPx) enzymes, thioredoxin reductase (TR) and the iodothyronine deiodinase enzymes. C826 566188 tyrosine kinase inhibitor OSI-930 A selective thiophene-derived tyrosine kinase inhibitor with potential antineoplastic activity. Tyrosine kinase inhibitor OSI-930 inhibits stem cell factor receptor (c-Kit) and the vascular endothelial growth factor receptor 2 (VEGFR2), which may result in the inhibition of both tumor cell proliferation and tumor angiogenesis.\nBoth c-Kit and VEGFR2 are overexpressed in a variety of cancers. C70981 566191 IGF-1R inhibitor OSI-906 An orally bioavailable small molecule inhibitor of the insulin-like growth factor 1 receptor (IGF-1R) with potential antineoplastic activity. IGF-1R inhibitor OSI-906 selectively inhibits IGF-1R, which may result in the inhibition of tumor cell proliferation and the induction of tumor cell apoptosis. Overexpressed in a variety of human cancers, IGFR-1 stimulates cell proliferation, enables oncogenic transformation, and suppresses apoptosis. C70982 566437 allogeneic B7.1/HLA-A1 transfected tumor cell vaccine An allogeneic whole cell vaccine, derived from irradiated allogenic tumor cells manipulated to express human B7.1 (CD80 antigen) and human leukocyte antigen (HLA) A1, with potential antitumor activity. Vaccination with allogeneic B7.1/HLA-A1 transfected tumor cell vaccine may elicit a cytotoxic T lymphocyte (CTL) response against similar host tumor cells, resulting in decreased tumor cell proliferation. C70985 566443 Aurora kinase/VEGFR2 inhibitor CYC116 An orally bioavailable small molecule multi-kinase inhibitor with antineoplastic activity. Aurora kinase/VEGFR 2 inhibitor CYC116 inhibits Aurora kinases A and B and vascular endothelial growth factor receptor 2 (VEGFR2), resulting in disruption of the cell cycle, rapid cell death, and the inhibition of angiogenesis. Aurora kinases are serine/threonine protein kinases that are only expressed in actively dividing cells and are critical in division or mitosis. VEGFR2 is a receptor tyrosine kinase that appears to account for most of the mitogenic and chemotactic effects of vascular endothelial growth factor (VEGF) on adult endothelial cells. C70983 567705 apoptosis inducer GCS-100 A galectin-binding polysaccharide derived from citrus pectin with potential antineoplastic activity. Apoptosis inducer GCS-100 binds to the carbohydrate-binding domain of the lectin galectin-3, which may result in apoptosis mediated through mitochondria/caspase activation cascades; this agent may overcome tumor growth mediated through anti-apoptotic protein Bcl-2, heat shock protein-27 (Hsp-27), and nuclear factor-kappa B (NF-kB). Galectin-3, a chimeric molecule consisting of both\ncarbohydrate recognition and collagen-like domains, interacts with a variety of carbohydrate and\nprotein ligands to form pentamers with unique\ncrosslinking abilities; this lectin also exhibits anti-apoptotic properties, perhaps, in part, through the regulation of intracellular signaling pathways. C70984 570107 recombinant human EGF-rP64K/Montanide ISA 51 vaccine A peptide vaccine preparation, containing recombinant human epidermal growth factor (rEGF) linked to the Neisseria meningitidis-derived recombinant immunogenic carrier protein P64k (rP64k) and mixed with the immunoadjuvant Montanide ISA 51, with potential active immunotherapy activity. Recombinant human EGF-rP64K/Montanide ISA 51 vaccine may trigger a humoral immune response against vaccine rEGF and rP64K and, so, against endogenous EGF. Antibody-mediated inhibition of endogenous EGF binding to its receptor, epithelial growth factor receptor (EGFR), may result in the inhibition of tumor cell proliferation. C70674 570123 dornase alfa inhalation solution A highly purified solution of recombinant human deoxyribonuclease I (rhDNAse) with selective DNA cleaving activity. Administrated through inhalation of the nebulized solution, dornase alpha catalyzes DNA degradation in viscous airway secretions, which may render airway secretions less viscous, thus promoting the clearing of airway mucous plugging and improvement in pulmonary function. C70980 570192 autologous LMP1-/LMP2- specific cytotoxic T-lymphocytes A preparation of cytotoxic T-lymphocytes (CTL), specifically reactive to the Epstein-Barr virus (EBV) latent membrane proteins (LMP) 1 and 2, with potential antineoplastic activity. Autologous dendritic cells and EBV-infected lymphoblastoid cell lines (LCL) from patients with EBV-positive nasopharyngeal carcinoma (NPC) are transduced with an LMP1/LMP2-expressing adenoviral vector, are irradiated, and then are used to stimulate and expand autologous CTL to produce autologous LMP1-/LMP2-specific CTL ex vivo. Administration of autologous LMP1-/LMP2- specific cytotoxic T-lymphocytes may result in a specific CTL response against tumor cells expressing LMP1 and LMP2, resulting in cell lysis and inhibition of tumor cell proliferation in vivo. Among a limited set of viral antigens expressed by NPC cells, LMP1 and LMP2 are weak immunogens which, nevertheless, are capable of inducing a T-lymphocyte response. C70836 570198 anti-CD45 monoclonal antibody A monoclonal antibody directed against the receptor-like leukocyte cell surface glycoprotein CD45 with leukocyte-depleting activity. Upon administration, anti-CD45 monoclonal antibody binds to leukocyte surface-expressed CD45, which may result in the transient depletion of circulating leukocytes including circulating T cell depletion (TCD). CD45, a receptor-like protein-tyrosine phosphatase that consists of several isoforms, is present on all differentiated hematopoietic cells except erythrocytes and plasma cells and is essential for T cell development and lymphocyte activation. C70798 570533 CD20-targeted polypeptide TRU-015 A proprietary antibody-based single-chain polypeptide with B cell-depleting activity. Significantly smaller than a whole antibody, CD20-targeted polypeptide TRU-015 binds specifically to the B cell-specific cell surface antigen CD20 with full immunoglobulin Fv fragment-type target binding activity and full immunoglobulin Fc fragment-type effector function. This agent transiently depletes CD20-bearing B cells by inducing B cell -directed complement dependent cytotoxicity (CDC) and antibody-dependent cell-mediated cytotoxicity (ADCC) and B cell apoptosis. C70797 570535 ramucirumab A recombinant, fully human monoclonal antibody directed against human vascular endothelial growth factor receptor 2 (VEGFR-2) with antiangiogenesis activity. Ramucirumab specifically binds to and inhibits VEGFR-2, which may result in an in inhibition of tumor angiogenesis and a decrease in tumor nutrient supply. VEGFR-2 is a pro-angiogenic growth factor receptor tyrosine kinase expressed by endothelial cells. C70792 570599 Aurora kinase inhibitor SNS-314 A synthetic small molecule Aurora kinase (AK) inhibitor with potential antineoplastic activity. Aurora kinase inhibitor SNS-314 selectively binds to and inhibits AKs A and B, which may result in the inhibition of cellular division and proliferation in tumor cells that overexpress AKs.\nAKs are serine-threonine kinases that play essential roles in mitotic checkpoint control during mitosis. C70655 570641 gadobutrol A gadolinium-based, hydrophilic, macrocyclic, electrically\nneutral contrast agent used in contrast-enhanced MRI (CE-MRI). Gadobutrol is a non-ionic, paramagnetic complex consisting of gadolinium (Gd3+) chelated with the macrocyclic compound dihydroxy-hydroxymethylpropyl-tetraazacyclododecane-triacetic acid (butrol). Following intravenous administration, gadobutrol may increase MRI sensitivity for the detection of tumors and inflammatory and demyelinating diseases of the central nervous system (CNS) which are associated with areas with blood-brain\nbarrier defects due to altered perfusion or an enlarged extracellular space. This agent is eliminated in an unchanged form via the kidneys; extra-renal elimination is negligible. C70675 570643 anti-CD20 monoclonal antibody R7159 A glycoengineered, fully humanized IgG1 monoclonal antibody with potential antineoplastic activity. Anti-CD20 monoclonal antibody R7159, a third generation type II anti-CD20 antibody, selectivity binds to the extracellular domain of the human CD20 antigen on malignant human B cells. The Fc region carbohydrates of the antibody, enriched in bisected non-fucosylated glycosylation variants, contribute to its higher binding affinity for human FcgammaRIII receptors compared to non-glycoengineered antibodies, resulting in enhanced antibody-dependent cellular cytotoxicity (ADCC) and caspase-independent apoptosis. In addition, modification of elbow hinge sequences within the antibody variable framework regions may account for the strong apoptosis-inducing activity of R7159 upon binding to CD20 on target cells. C70741 570645 polyethyleneglycol-7-ethyl-10-hydroxycamptothecin A polyethylene glycol (PEG) conjugate of 7-ethyl-10-hydroxycamptothecin with potential antineoplastic activity. After hydrolysis in vivo, 7-ethyl-10-hydroxycamptothecin (SN38), an active metabolite of irinotecan, is released from polyethyleneglycol-7-ethyl-10-hydroxycamptothecin (PEG-SN38); 7-ethyl-10-hydroxycamptothecin selectively stabilizes topoisomerase I-DNA covalent complexes, resulting in single-stranded and double-stranded DNA breaks, the inhibition of DNA replication, and the induction of apoptosis. This agent is designed to deliver the active metabolite to tumor cells without the need for conversion as is the case with irinotecan. Compared to unPEGylated 7-ethyl-10-hydroxycamptothecin, PEGylation improves solubility and allows for parental delivery, and may result in a longer half-life and higher exposure for tumor cells. C70651 570670 aminopeptidase inhibitor CHR-2797 A proprietary orally bioavailable inhibitor of the M1 family of aminopeptidases with potential antineoplastic activity. Aminopeptidase inhibitor CHR-2797 is converted intracellularly into a poorly membrane-permeable active metabolite (CHR-79888) which inhibits the M1 family of aminopeptidases, particularly puromycin-sensitive aminopeptidase (PuSA), and leukotriene A4 (LTA4) hydrolase; inhibition of these aminopeptidases in tumor cells may result in amino acid deprivation, inhibition of protein synthesis due to a decrease in the intracellular free amino acid pool, an increase in the level of the proapoptotic protein Noxa, and cell death. Noxa is a member of the BH3 (Bcl-2 homology 3)-only subgroup of the proapoptotic Bcl-2 (B-cell CLL/lymphoma 2) protein family. C70650 570688 micronutrient-fortified probiotic yogurt An micronutrient-fortified fermented dairy product with potential positive immunomodulatory activity. Micronutrient-fortified probiotic yogurt contains various micronutrients in addition to beneficial microorganisms, such as strains of Lactobacillus. Probiotic Lactobacillus strains have been shown to protect against gastrointestinal and urogenital infections, to moderate diarrheal episodes, and to increase CD4 T-lymphocyte counts. In immunocompromised subjects, micronutrient supplementation may also increase CD4 T-lymphocyte counts. C70677 570689 carcinoembryonic antigen peptide 1-6D virus-like replicon particles vaccine A cancer vaccine, consisting of alphavirus vector-derived virus-like replicon particles expressing the 9-amino-acid carcinoembryonic antigen peptide (CAP) 1-6D, with potential antineoplastic activity. Vaccination with this agent may elicit a cytotoxic T lymphocyte (CTL) immune response against CEA-expressing tumor cells. C70644 570726 plant-derived hematopoiesis enhancer PG2 A proprietary botanical formulation derived from a traditional Chinese medicinal (TCM) plant with hematopoietic activity. Although the mechanism of action has yet to be fully elucidated, plant-derived hematopoiesis enhancer PG2 appears to stimulate multi-lineage progenitor cells that may be closely related to the hematopoietic stem cell. In both chemotherapy- and radiation therapy-induced animal models of myelosuppression, this agent has been shown to restore granulocyte, erythrocyte, and platelet counts to normal levels. Plant-derived hematopoiesis enhancer PG2 stimulates the production of numerous cytokines such as granulocyte-colony stimulating factor (G-CSF) and may stimulate the production of neuroendocrine hormones. C70640 570728 erastin analogue PRLX 93936 A structural analogue of erastin with potential antineoplastic activity. Erastin analogue PRLX 93936 appears to inhibit mitochondrial outer membrane protein VDACs (voltage-dependent anion channels) 2 and 3, resulting in an oxidative, non-apoptotic cell death. Erastin analogue PRLX 93936 exhibits greater lethality in cell lines harboring mutations in the GTPase protein oncogenes HRAS and KRAS or the serine-threonine protein kinase oncogene BRAF than in non-tumorigenic cell lines. VDACs 2 and 3 are up-regulated in a wide variety of tumor cell lines. C70625 570759 L-gossypol The levo-enantiomer of an orally bioavailable polyphenolic aldehyde, derived primarily from unrefined cottonseed oil, with potential antineoplastic activity. Mimicking the\ninhibitory BH3 (Bcl-2 homology 3) domain of endogenous antagonists of Bcl-2, L-gossypol binds to and inhibits various anti-apoptotic Bcl-2 proteins, which may result in the inhibition of tumor cell proliferation and the induction of tumor cell apoptosis. This agent has greater affinity for Bcl-2 proteins than racemic gossypol. C62178 570766 broad-spectrum human papillomavirus vaccine V505 A non-infectious recombinant cancer vaccine prepared from the human papillomavirus (HPV) with potential immunoprophylactic activity. Vaccination with broad-spectrum human papillomavirus vaccine V505 may stimulate the host immune system to mount humoral and cytotoxic T lymphocyte (CTL) responses against HPV-infected cells.\nHPV infection, the cause of genital warts, is a risk factor for the development of cancers of the cervix, vagina, vulva, anus, and penis. C70598 570770 fluorine F 18 fluoroethylcholine Ethylcholine labeled with fluorine F 18, a positron-emitting isotope. Fluorine F 18 fluoroethylcholine incorporates into tumor cells through an active, carrier-mediated transport mechanism for choline and then is phosphorylated intracellularly by choline kinase, yielding a phosphoryl derivative, and finally is integrated into cellular phospholipids, probably primarily into a phosphatidyl derivative; concentration of this agent in tumor cells as various fluorine F 18 fluoroethylcholine derivatives enables tumor imaging using positron emission tomography (PET). Choline kinase, the enzyme responsible for the phosphorylation of choline, is frequently up-regulated in human tumor cell lines. C70594 570771 ceftobiprole medocaril A water-soluble prodrug of ceftobiprole, a pyrrolidinone cephalosporin antibiotic, with bactericidal activity. Ceftobiprole binds to and inactivates penicillin-binding proteins (PBPs), enzymes involved in the terminal stages of bacterial cell wall assembly and cell wall reshaping during bacterial growth and division. This agent exhibits a broad spectrum of activity against gram-negative and gram-positive pathogens including methicillin-resistant S. aureus (MRSA), vancomycin-intermediate S. aureus (VISA) and vancomycin-resistant S. aureus (VRSA). Ceftobiprole is refractory to hydrolysis by class A and class C lactamases. C70597 570895 HIF-1alpha inhibitor PX-478 An orally active small molecule with potential antineoplastic activity. Although its mechanism of action has yet to be fully elucidated, HIF1-alpha inhibitor PX-478 appears to inhibit hypoxia-inducible factor 1-alpha (HIF1A) expression, which may result in decreased expression of HIF1A downstream target genes important to tumor growth and survival, a reduction in tumor cell proliferation, and the induction of tumor cell apoptosis. The inhibitory effect of this agent is independent of the tumor suppressor genes VHL and p53 and may be related to derangements in glucose uptake and metabolism due to inhibition of glucose transporter-1 (Glut-1). C70953 570963 renal cell carcinoma peptides vaccine IMA901 A multipeptide cancer vaccine targeting renal cell carcinoma with potential immunopotentiating activity. Renal cell carcinoma peptides vaccine IMA901 consists of 10 different synthetic tumor-associated peptide (TUMAP) antigens (9 HLA-class I-binding and 1 HLA class II-binding); endogenously, these TUMAPs are expressed by the majority of renal cell carcinomas. Vaccination with this agent may significantly increase host cytotoxic T-lymphocyte (CTL) immune responses against tumor cells expressing these peptide antigens. C70968 570981 anti-PSCA fully human monoclonal antibody AGS-1C4D4 An IgG1k fully human monoclonal antibody directed against the human prostate stem cell antigen (PSCA) with potential antineoplastic activity. Anti-PSCA fully human monoclonal antibody AGS-1C4D4 selectively targets and binds to PSCA, triggering complement-dependent cell lysis and antibody-dependent cell-mediated cytotoxicity in tumor cells expressing PSCA. PSCA is a glycosyl-phosphatidylinositol (GPI)-linked cell surface antigen found in cancers of the bladder, pancreas, and prostate. C71157 570982 Hsp90 inhibitor AUY922 A derivative of 4,5-diarylisoxazole and a third-generation heat shock protein 90 (Hsp90) inhibitor with potential antineoplastic activity. Hsp90 inhibitor AUY922 has been shown to bind with high affinity to and inhibit Hsp90, resulting in the proteasomal degradation of oncogenic client proteins; the inhibition of cell proliferation; and the elevation of heat shock protein 72 (Hsp72) in a wide range of human tumor cell lines. Hsp90, a 90 kDa molecular chaperone, plays a key role in the conformational maturation, stability and function of other\nsubstrate or "client" proteins within the cell, many of which are involved in signal transduction, cell cycle regulation and apoptosis, including kinases, transcription factors and hormone receptors. Hsp72 exhibits anti-apoptotic functions; its up-regulation may be used as a surrogate marker for Hsp90 inhibition. C71467 571076 Mycobacterium w An attenuated strain of Mycobacterium w, a non-pathogenic, rapidly growing, atypical mycobacterium, with non-specific immunopotentiating properties. In addition to sharing a number of common B and T cell determinants with Mycobacterium leprae and Mycobacterium tuberculosis, Mycobacterium w (Mw) also shares an immunogenic determinant with prostate specific antigen (PSA). In vitro and in vivo studies have shown that heat-killed Mw can induce significant T-cell responses. This agent may induce host T-cell responses against tumor cells expressing PSA. PSA is a glycoprotein secreted by prostatic epithelial and ductal cells and may be overexpressed in prostate cancer cells. C70969 571184 PP14 derivative-treated HLA-matched donor mononuclear cell-enriched leukocytes A preparation of allogeneic HLA-matched leukocytes treated with a derivative of placental protein 14 (PP14) with potential immunomodulating activity. PP14 derivative-treated HLA-matched donor mononuclear cell-enriched leukocytes contain at least fifty-five percent early-apoptotic T cells; after infusion and when processed by recipient dendritic cells, early-apoptotic T cells may help induce a decrease in the donor effector T-cell responses against the recipient of an allogeneic hematopoietic stem cell (HSC) transplant, thereby minimizing allogeneic HSC transplant-related graft-versus-host disease (GVHD). PP14, a 162 amino acid\nglycosylated protein secreted by the late secretory phase endometrium, binds to T cells in a carbohydrate fashion and has been shown to induce T-cell apoptosis; maternal immune tolerance to the fetus and pregnancy-related remissions of autoimmune disease may involve PP14-induced T cell apoptosis. C71162 571791 tamibarotene An orally active, synthetic retinoid, developed to overcome all-trans retinoic acid (ATRA) resistance, with potential antineoplastic activity. As a specific retinoic acid receptor (RAR) alpha/beta agonist, tamibarotene is approximately ten times more potent than ATRA in inducing cell differentiation and apoptosis in HL-60 (human promyelocytic leukemia) cell lines in vitro. Due to a lower affinity for cellular retinoic acid binding protein (CRABP), tamibarotene may show sustained plasma levels compared to ATRA.\nIn addition, this agent may exhibit a lower toxicity profile than ATRA, in part, due to the lack of affinity for the RAR-gamma receptor, the major retinoic acid receptor in the dermal epithelium. C71025 571792 natural human interferon alpha OPC-18 A proprietary preparation of natural human interferon alpha (IFN alpha) with potential immunomodulatory and antineoplastic activities. Natural human interferon alpha OPC-18 binds to cell-surface IFN alpha receptors (IFNARs), resulting in the transcription and translation of genes whose products mediate antiviral, antiproliferative, and immune-modulating effects.\nIFN alpha is a type I interferon produced by peripheral blood leukocytes or lymphoblastoid cells when exposed to live or inactivated virus, double-stranded RNA, or bacterial products and is the primary interferon produced by virus-induced leukocyte cultures. In addition to its pronounced antiviral activity, it activates NK cells. C71159 572211 patient-specific follicular lymphoma-derived anti-idiotype vaccine A patient-specific cancer vaccine directed against the soluble protein idiotype of an individual follicular lymphoma with potential antineoplastic activity. A patient-specific follicular lymphoma-derived anti-idiotype vaccine may be composed of a patient-specific, synthetic idiotype-related peptide (such as one corresponding to a hypervariable region of an IgG heavy chain) conjugated to the immunostimulant carrier protein keyhole limpet hemocyanin (KLH). Upon administration, this vaccine may induce an idiotype-specific cytotoxic T-lymphocyte (CTL) response against follicular lymphoma cells expressing the idiotype, resulting in tumor cell lysis. C71036 572214 cannabis-based oromucosal spray GW-1000-02 An herbal preparation containing a defined quantity of specific cannabinoids formulated for oromucosal spray administration with potential analgesic activity. Cannabis-based oromucosal spray GW-1000-02 contains a standardized extract of tetrahydrocannabinol (THC), the non-psychoactive cannabinoid cannabidiol (CBD), other minor cannabinoids, flavonoids, and terpenes from two cannabis plant varieties. Cannabinoids interact with G protein-coupled cannabinoid 1 (CB1) receptors in the central nervous system, resulting in analgesic, euphoric, and anticonvulsive effects. C71037 573071 formoterol fumarate/roxithromycin A combination preparation of the fumarate salt of a beta2-adrenergic receptor agonist and a macrolide antibiotic, with muscle-sparing and anti-cachexia effects. Formoterol appears to antagonize cachexia by reducing proteolysis mediated through the ubiquitin-protease pathway. Roxithromycin strongly inhibits inflammatory cytokine production and secretion from T cells and macrophages in vitro and in vivo. The combination exhibits a greater muscle sparing effect than either drug given individually at comparable doses. C71161 573083 conatumumab A fully human monoclonal agonist antibody directed against the extracellular domain of human TRAIL (tumor necrosis factor-related apoptosis-inducing ligand) receptor 2 (TR-2) with potential antineoplastic activity. Conatumumab mimics the activity of native TRAIL, binding to and activating TR-2, thereby activating caspase cascades and inducing tumor cell apoptosis. TR-2 is expressed by a variety of solid tumors and cancers of hematopoietic origin. C71015 573226 salirasib A salicylic acid derivative with potential antineoplastic activity. Salirasib dislodges all Ras isoforms from their membrane-anchoring sites, thereby preventing activation of RAS signaling cascades that mediated cell proliferation, differentiation, and senescence. RAS signaling is believed to be abnormally activated in one-third of human cancers, including cancers of the pancreas, colon, lung and breast. C71146 573227 anti-PD-1 monoclonal antibody CT-011 A humanized monoclonal antibody directed against human PD-1 (programmed cell death 1; PDCD1), with immunomodulating and antitumor activities. Anti-PD-1 monoclonal antibody CT-011 blocks interaction between the receptor PD-1 with its ligands, PD-1 ligand 1 (PD-1L1) and PD-1 ligand 2 (PD-1L2), resulting in the attenuation of apoptotic processes in lymphocytes, primarily effector/memory T cells, and the augmentation of the anti-tumor activities of NK cells. PD-1 is an inhibitory receptor belonging to the B7-receptor family that is expressed on lymphocytes and myeloid cells; its ligands, PD-1L1 and PD-1L2, are expressed not only by hematopoietic cells but also by cells in non-lymphoid tissues. C71014 573267 acridine carboxamide A tricyclic acridine-based (or carboxamide-based) drug with dual topoisomerase inhibitor and potential antineoplastic activities. Acridine carboxamide inhibits both topoisomerases I and II and intercalates into DNA, resulting in DNA damage, the disruption of DNA repair and replication, the inhibition of RNA and protein synthesis, and cell death. C2203 573371 Polo-like kinase 1 inhibitor ON 01910.Na A synthetic benzyl styryl sulfone analogue with potential antineoplastic activity. Polo-like kinase 1 inhibitor ON 01910.Na inhibits polo-like kinase1 (Plk1), inducing selective G2/M arrest followed by apoptosis in a variety of tumor cells while causing reversible cell arrest at the G1 and G2 stage without apoptosis in normal cells. This agent may exhibit synergistic antitumor activity in combination with other chemotherapeutic agents. Plk1, named after the polo gene of Drosophila melanogaster, is a serine/threonine protein kinase involved in regulating mitotic spindle function in a non-ATP competitive manner. C71355 573418 magnesium valproate The magnesium salt of valproic acid (2-propylpentanoic acid) with antiepileptic and potential antineoplastic activities. Magnesium valproate dissociates in the gastrointestinal tract and is absorbed into the circulation as magnesium ions and valproic acid ions; valproic acid may inhibit histone deacetylases, inducing tumor cell differentiation, apoptosis, and growth arrest. In addition, valproic acid exerts an antiepileptic effect, likely by inhibiting enzymes that catabolize the inhibitory neurotransmitter gamma-aminobutyric acid (GABA) catabolism and so increasing concentrations of GABA in the central nervous system (CNS). \nThe presence of the magnesium in this agent may contribute to its anticonvulsant activity and sedative properties. C71156 573427 high-selenium Brassica juncea A formulation of the mustard plant Brassica juncea grown in a medium that has been enriched with the trace element selenium with potential chemopreventive and chemopotentiating activities. Brassica juncea hyperaccumulates trace elements in soil. Selenium amino acid species found in selenized Brassica juncea include methylselenomethionine (MeSeMet) and methylselenocysteine (MeSeCys); both may be incorporated into selenoproteins in vivo. Selenium functions as a cofactor for antioxidant enzymes such as glutathione peroxidases and thioredoxin reductase, which protect cells from the free radical damage. In addition, in vitro MeSeCys has been shown to potentiate the antitumor effects of the irinotecan metabolite SN-38, by inducing phosphorylation of checkpoint kinase 2 (chk2) at threonine 68, which results in poly(ADP-ribose) polymerase cleavage, caspase 3 activation, and DNA fragmentation. C71154 573502 ertapenem sodium The sodium salt of ertapenem, a 1-beta-methyl carbapenem and a broad-spectrum beta-lactam antibiotic with bactericidal activity. Ertapenem binds to penicillin binding proteins (PBPs) located on the bacterial cell wall, in particular PBPs 2 and 3, thereby inhibiting the final transpeptidation step in the synthesis of peptidoglycan, an essential component of the bacterial cell wall. Inhibition of peptidoglycan synthesis results in weakening and lysis of the cell wall and cell death. In vitro, this agent has shown activity against Gram-positive and Gram-negative aerobic and anaerobic bacteria. Erapenem is resistant to hydrolysis by a variety of beta-lactamases, including penicillinases, cephalosporinases and extended-spectrum beta-lactamases. 573537 [18F]-labeled substance P antagonist receptor quantifier A radioconjugate consisting of the positron emitting radioisotope fluorine F 18 conjugated to the substance P antagonist receptor quantifier (SPA-RQ) used in radioimaging. [18F]-labeled substance P antagonist receptor quantifier is an antagonist of the neurokinin 1 (substance P) receptor (NK1R) and can function as a positron emission tomography (PET) imaging agent for detecting NK1R-expressing cells and tissues. NK1Rs are frequently expressed on the plasma membranes of tumor cells from glioblastoma and breast and pancreatic carcinomas. C71071 573538 recombinant adenovirus-interferon SCH 721015 A replication-deficient recombinant adenovirus encoding human interferon alpha-2b with potential antineoplastic activity. Upon intravesical administration, recombinant adenovirus-interferon SCH 721015 infects nearby tumor cells and expresses INF alpha-2b intracellularly which activates the transcription and translation of genes whose products mediate antiviral, antiproliferative, antitumor, and immune-modulating effects. C71011 573587 Polo-like kinase 1 inhibitor GSK-461364 A small molecule Polo-like kinase 1 (PLK1) inhibitor with potential antineoplastic activity. Polo-like kinase 1 inhibitor GSK461364 selectively inhibits Plk1, inducing selective G2/M arrest followed by apoptosis in a variety of tumor cells while causing reversible cell arrest at the G1 and G2 stage without apoptosis in normal cells. Plk1, named after the polo gene of Drosophila melanogaster, is a serine/threonine protein kinase involved in regulating mitotic spindle function in a non-ATP competitive manner. C70948 573742 anti-CCL-2 human monoclonal antibody CNTO 888 A recombinant monoclonal antibody directed against human CC chemokine ligand 2 (CCL2) with potential antineoplastic activity. Anti-CLL2 human monoclonal antibody CNTO 888 binds to and inhibits CLL2, which may result in inhibition of angiogenesis and, so, tumor cell proliferation. Endothelium-derived CLL2 (monocyte chemoattractant protein; MCP1) is a member of the beta-chemokine family, can stimulate monocyte/macrophage migration and smooth muscle cell (SMC) proliferation, and plays a role in angiogenesis and tumor cell migration; CCL2 induction of angiogenesis may involve the upregulation of hypoxia-inducible factor 1 alpha (HIF-1 alpha) gene expression which, in turn, induces vascular endothelial growth factor-A (VEGF-A) gene expression. C71010 574044 PVA microporous hydrospheres An embolic material composed of microspheres of polyvinyl alcohol (PVA) polymers. These water-soluble, compressible microspheres may be used to encapsulate various therapeutic agents; drug-loaded microspheres can then be used as a drug delivery vehicle during embolization of tumor vasculature. C71149 574045 PVA microporous hydrospheres/doxorubicin hydrochloride An embolic material composed of microspheres of polyvinyl alcohol (PVA) polymers loaded with doxorubicin hydrochloride with antineoplastic activity. Doxorubicin hydrochloride-loaded microspheres may be used as a drug delivery vehicle during embolization of tumor vasculature. Doxorubicin intercalates DNA, interferes with catalytic activity of topoisomerase II, and causes DNA adducts and other DNA damage, resulting in tumor cell growth inhibition and apoptosis. When used in tumor vasculature embolization, this preparation may provide more tumor-specific treatment with doxorubicin compared to the systemic administration of doxorubicin, thereby reducing the systemic toxicity of doxorubicin. C71149 574047 vector-peptide conjugated paclitaxel A proprietary conjugate of paclitaxel with antineoplastic activity. Similar to the free drug, the paclitaxel moiety in vector-peptide conjugated paclitaxel binds to and stabilizes tubulin molecules, promoting assembly of microtubules and inhibiting tubulin disassembly which results in the inhibition of cell division. The Kunitz domain-derived vector-peptide carries the conjugated paclitaxel through the blood brain barrier (BBB), bypassing the transmembrane p-glycoprotein (P-gp) efflux pump, which may result in higher concentrations of paclitaxel in the brain parenchyma. C70971 574048 anti-CD19-DM4 immunoconjugate SAR3419 An immunoconjugate consisting of an anti-CD19 monoclonal antibody conjugated to the maytansinoid DM4, a derivative of the cytotoxic agent maytansine (DM1), with potential antineoplastic activity. Anti-CD19-DM4 conjugate SAR3419 targets the cell surface antigen CD19, found on a number of B-cell-derived cancers. Upon antibody/antigen binding and internalization, the immunoconjugate releases DM4, which binds to tubulin and disrupts microtubule assembly/disassembly dynamics, resulting in inhibition of cell division and cell growth of CD19-expressing tumor cells. C71009 574264 desflurane A fluorinated ether with general anesthetic and muscle relaxant activities. Although the exact mechanism of action has not been established, desflurane, administered by inhalation, appears to act on the lipid matirx of the neuronal membrane, resulting in disruption of neuronal transmission in the brain. This agent may also enhance the synaptic activity of the inhibitory neurotransmitter gamma-aminobutyric acid (GABA). 574268 famotidine A propanimidamide and histamine H2-receptor antagonist with antacid activity. As a competitive inhibitor of histamine H2-receptors located on the basolateral membrane of the parietal cell, famotidine reduces basal and nocturnal gastric acid secretion, resulting in a reduction in gastric volume, acidity, and amount of gastric acid released in response to various stimuli. 574280 hydromorphone hydrochloride The hydrochloride salt of the semi-synthetic opioid hydromorphone with analgesic activity. Hydromorphone, the hydrogenated ketone of morphine, selectively binds the mu-opioid receptor, a G protein-coupled receptor. Binding stimulates the exchange of guanosine triphosphate (GTP) for guanosine diphosphate (GDP) on the G-protein complex, resulting in inhibition of plasma membrane-associated adenylate cyclase (AC) and a reduction in intracellular cyclic 3',5'-adenosine monophosphate (cAMP) levels. Due to a reduction in cAMP levels, voltage-gated potassium channels are activated, resulting in neuronal hyperpolarization and a reduction in neuronal excitability. In addition, this agent inhibits the opening of voltage-gated calcium channels, resulting in inhibition of calcium entry into neuronal cells and a reduction in the release of nociceptive neurotransmitters such as substance P and glutamate. 574480 Salvia officinalis extract tablet An oral tablet containing an extract of the plant Salvia officinalis (common sage) with reported antihydrotic, antibiotic, antihypertensive, anti-inflammatory, antioxidant, astringent, antispasmodic, estrogenic, and hypoglycemic properties. The primary biologically active component of common sage appears to be its essential oil which contains mainly cineol, borneol, and alpha- and beta-thujone. In addition, sage leaf contains numerous other substances including tannic acid; resins with oleic, ursonic, and ursolic acids; bitter substances with cornsole and cornsolic acid; fumaric, chlorogenic, caffeic and nicotinic acids; nicotinamide; flavones; flavone glycosides; and estrogenic substances. However, the mechanism(s) of action of common sage in the treatment of various disorders is unclear. C71519 574615 SN-38-loaded polymeric micelles NK012 A formulation consisting of polymeric micelles loaded with the irinotecan metabolite SN-38 with potential antineoplastic activity. SN-38-loaded polymeric micelles NK012 is an SN-38-releasing nanodevice constructed by covalently attaching SN-38 to the block copolymer PEG-PGlu, followed by self-assembly of amphiphilic block copolymers in an aqueous milieu. SN-38 (7-ethyl-10-hydroxy-camptothecin), a biological active metabolite of the prodrug irinotecan (CPT-11), binds to and inhibits topoisomerase I by stabilizing the cleavable complex between topoisomerase I and DNA, resulting in DNA breaks, inhibition of DNA replication, and apoptosis. SN-38 has been reported to exhibit up to 1,000-fold more cytotoxic activity against various cancer cells in vitro than irinotecan. This formulation increases the water-solubility of SN-38 and allows the delivery of higher doses of SN-38 than those achievable with SN-38 alone. C71521 575320 tanezumab A humanized monoclonal antibody directed against nerve growth factor (NGF), a modulator of nociceptor function, with potential analgesic activity. Tanezumab binds to NGF and prevents NGF binding to its high affinity, membrane-bound, catalytic receptor tropomyosin-related kinase A (TrkA), which is present on sympathetic and sensory neurons; reduced stimulation of TrkA by NGF inhibits the pain-transmission activities of these neurons. NGF, a neurotrophin, is critical to the growth and maintenance of sympathetic and sensory neurons. In addition, NGF may induce mast cells to release inflammatory proteins and may induce the upregulation of substance P and other pain-related peptides in sympathetic and sensory neurons. Upon neurotrophin binding, TrkA phosphorylates itself and members of the MAPK pathway, mediating the multiple neuronal effects of NGF. C71522 575516 VEGFR-2 inhibitor peptide CT-322 A highly specific, synthetic peptide vascular endothelial growth factor receptor-2 (VEGFR-2) antagonist with potential antiangiogenic activity. Derived from human fibronectin with a proprietary protein engineering process, VEGFR-2 inhibitor peptide CT-322 may block the activation of VEGFR-2 by all known activating ligands, thereby inhibiting the growth of new tumor blood vessels. C62791 575732 anti-CD33 monoclonal antibody-DM4 conjugate AVE9633 An immunoconjugate consisting of the humanized monoclonal antibody huMy9-6 conjugated to the cytotoxic maytansinoid DM4 with potential antineoplastic activity. The monoclonal antibody portion of anti-CD33 monoclonal antibody-DM4 conjugate AVE9633 specifically binds to the cell surface antigen CD33 expressed on myeloid leukemia cells; upon internalization, the DM4 moiety is released, binds tubulin, and disrupts microtubule assembly/disassembly dynamics, resulting in the inhibition of cell division and cell growth in myeloid leukemia cells that express CD33. CD33 is expressed on normal non-pluripotent hematopoietic stem cells as well as on myeloid leukemia cells. C71523 575735 folate receptor-targeted epothilone BMS753493 A folate receptor-targeting antimitotic agent with potential antineoplastic activity. Folate receptor-targeted epothilone BMS753493 contains an epothilone moiety linked to a single folate molecule. Mediated through the folate moiety, this agent delivers the antimitotic epothilone component into cells expressing folic acid receptors, frequently upregulated in many types of tumor cells. After ligand-receptor internalization, the epothilone moiety induces microtubule polymerization and stabilizes microtubules against depolymerization, resulting in the inhibition of mitosis and cellular proliferation. C71524 576686 tubulin-binding agent SSR97225 An antimitotic tubulin-binding agent with potential antineoplastic activity. Tubulin-binding agent SSR97225 binds to tubulin, arresting the cell cycle at the G2/M checkpoint and preventing mitosis. C71525 577331 oral microencapsulated diindolylmethane An orally bioavailable microencapsulated formulation of diindolylmethane, an indole phytonutrient found in cruciferous vegetables, with estrogen-modulating, antiandrogenic, and potential antineoplastic activities. As a dimer of indole-3-carbinol, diindolylmethane (DIM) modulates estrogen balance by reducing the levels of 16-hydroxy estrogen metabolites and increasing the formation of beneficial 2-hydroxy estrogen metabolites. DIM also antagonizes androgen receptor activity, which may result in diminished cell proliferation and apoptosis in susceptible tumor cell populations. Pure DIM, which is relatively hydrophobic, is poorly absorbed after oral administration. This oral formulation, which consists of DIM, d-alpha-tocopheryl acid succinate, phosphatidylcholine, and silica microencapsulated in starch, significantly improves the gastrointestinal absorption of DIM. C71132 577353 HPV L1 VLP vaccine V504 A vaccine formulation consisting of several types of human papillomavirus (HPV)-derived noninfectious virus-like particles (VLPs) with potential immunoprophylactic activity. Upon administration, HPV L1 VLP vaccine V504 may generate humoral immunity against various HPV L1 major capsid proteins, thereby preventing cervical infection upon exposure to the associated HPV types. VLPs are composed of self-assembling L1 major capsid proteins or functional L1 major capsid protein derivatives. C71526 577364 anti-IGF-1R recombinant monoclonal antibody SCH 717454 A recombinant, fully human monoclonal antibody directed against the insulin-like growth factor 1 receptor (IGF-1R) with potential antineoplastic activity. Anti-IGF-1R fully human monoclonal antibody SCH 717454 binds to membrane-bound IGF-1R, preventing binding of the ligand IGF-1 and the subsequent triggering of the PI3K/Akt signaling pathway; downregulation of this survival pathway may result in the induction of apoptosis and decreased cellular proliferation. The activation of IGF-1R, a tyrosine kinase and a member of the insulin receptor family, stimulates cell proliferation, enables oncogenic transformation, and suppresses apoptosis; IGF-1R signaling has been highly implicated in tumorigenesis and metastasis. C71527 577369 bromovinyl-deoxyuridine A uridine derivative and nucleoside analog with pro-apoptotic and chemosensitizing properties. In vitro, bromovinyl-deoxyuridine (BVDU) has been shown to downregulate the multifunctional DNA repair enzyme APEX nuclease 1, resulting in the inhibition of DNA repair and the induction of apoptosis. In addition, this agent may inhibit the expression of STAT3 (signal transducer and activator of transcription 3), which may result in the downregulation of vascular endothelial growth factor (VEGF). BVDU has also been found to inhibit the upregulation of chemoresistance genes (Mdr1 and DHFR) during chemotherapy. Overall, the gene expression changes associated with BVDU treatment result in the decrease or prevention of chemoresistance. In addition, this agent has been shown to enhance the cytolytic activity of NK-92 natural killer cells towards a pancreatic cancer cell line in vitro. C71528 577391 chlorzoxazone A benzoxazolone derivative with mild sedative and centrally-acting muscle relaxant activities. Although its exact mechanism of action is unknown, chlorzoxazone (CZ) appears to act at the spinal cord and subcortical levels of the brain to inhibit multisynaptic reflex arcs involved in producing and maintaining muscle spasms. This agent is extensively hydroxylated by cytochrome P450 2E1 (CYP2E1) to 6-hydroxychlorzoxazone (HCZ),11,12 which is subsequently glucuronidated and eliminated renally. Highly selective for CYP2E1, CZ may be used as a selective probe for phenotyping CYP2E1 in humans; the ratio of HCZ-to-CZ plasma concentrations obtained 2 to 4 hours after oral administration of CZ may be used as a phenotypic measure of CYP2E1 enzymatic activity. 577812 G2 checkpoint inhibitor CBP501 A peptide with G2 checkpoint-abrogating activity. G2 checkpoint inhibitor CBP501 inhibits multiple serine/threonine kinases, including MAPKAP-K2, C-Tak1, and CHK1, that phosphorylate serine 216 of the dual-specific phosphatase Cdc25C (cell division checkpoint 25 C); disruption of Cdc25C activity results in the inhibition of Cdc25C dephosphorylation of the mitotic cyclin-dependent kinase complex Cdc2/cyclin B, preventing entry into the mitotic phase of the cell cycle. C71529 578040 ganitumab A recombinant, fully human monoclonal antibody directed against the insulin-like growth factor 1 receptor (IGF-1R) with potential antineoplastic activity. Ganitumab binds to membrane-bound IGF-1R, preventing binding of the ligand IGF-1 and the subsequent triggering of the PI3K/Akt signaling pathway; inhibition of this survival signaling pathway may result in the inhibition of tumor cell proliferation and the induction of tumor cell apoptosis. IGF-1R is a tyrosine kinase and a member of the insulin receptor family. IGF-1R activation stimulates cell proliferation, enables oncogenic transformation, and suppresses apoptosis; IGF-1R signaling has been highly implicated in tumorigenesis and metastasis. C71531 579227 anti-IGF-1R recombinant monoclonal antibody BIIB022 A recombinant, human monoclonal antibody directed against the insulin-like growth factor 1 receptor (IGF-1R) with potential antineoplastic activity. Anti-IGF-1R recombinant monoclonal antibody BIIB022 binds to membrane-bound IGF-1R, preventing binding of the ligand IGF-1 and the subsequent triggering of the PI3K/Akt signaling pathway; inhibition of this survival signaling pathway may result in the inhibition of tumor cell proliferation and the induction of tumor cell apoptosis. The activation of IGF-1R, a tyrosine kinase and a member of the insulin receptor family, stimulates cell proliferation, enables oncogenic transformation, and suppresses apoptosis; IGF-1R signaling has been highly implicated in tumorigenesis and metastasis. C71530 579241 lonaprisan An orally bioavailable pentafluoroethyl derivative of a mifepristone-related steroid with antiprogestagenic activity. Lonaprisan is a pure, highly receptor-selective progesterone receptor (PR) antagonist; binding of this agent to PRs inhibits PR activation and the associated proliferative effects. Unlike many other antiprogestins such as mifepristone, this agent does not appear to convert to an agonist in the presence of protein kinase A (PKA) activators and shows high antiprogestagenic activity on both progesterone receptor (PR) isoforms PR-A and PR-B. C71532 579292 thymidine kinase-deleted vaccinia-hGM-CSF JX-594 A thymidine kinase-deleted vaccinia virus expressing human GM-CSF (hGM-CSF) with oncolytic activity. Upon intratumoral or intravenous administration, thymidine kinase-deleted vaccinia-hGM-CSF JX-594 may selectively infect and lyse tumor cells. While vaccinia displays a natural tumor cell tropism, deletion of the thymidine kinase gene increases the tumor selectivity of vaccinia by limiting viral replication to transformed cells. hGM-CSF expression by this agent may help recruit antigen processing cells (APCs), such as denritic cells and macrophages, to virally infected tumor cells, initiating a systemic antitumoral immune response. C71533 579574 budesonide/formoterol fumarate dihydrate inhalation aerosol An inhalation aerosol formulation containing budesonide and the fumarate dihydrate salt of formoterol with anti-inflammatory and bronchial smooth muscle-relaxing activities. The synthetic corticosteroid steroid budesonide binds to intracellular glucocorticosteroid receptors (GRs), exhibiting inhibitory activities against multiple cell types and mediators associated with allergic inflammation. The long-acting beta-adrenergic receptor agonist formoterol selectively binds to beta-2 adrenergic receptors in bronchial smooth muscle, activating intracellular adenyl cyclase, an enzyme that catalyzes the conversion of adenosine triphosphate (ATP) to cyclic-3',5'-adenosine monophosphate (cAMP); increased intracellular cAMP result in the relaxation of bronchial smooth muscle and inhibition of the cellular release of mediators of immediate hypersensitivity, especially from mast cells. C71534 579596 memantine hydrochloride The hydrochloride salt of memantine, a low-affinity, voltage-dependent, noncompetitive N-methyl-D-aspartate (NMDA) receptor antagonist. Memantine binds to and inhibits cation channels of glutamanergic NMDA receptors located in the central nervous system (CNS), preventing the prolonged influx of calcium ions and the associated neuronal excitotoxicity, and thereby potentially enhancing cognitive function. Memantine is also a 5-hydroxytryptamine type 3 (5HT3) receptor and nicotinic receptor antagonist. 579646 1-methyl-d-tryptophan A methylated tryptophan with anti-immunosuppressive activity. 1-methyl-d-tryptophan inhibits the enzyme indoleamine 2,3-dioxygenase (IDO), which degrades the essential amino acid tryptophan, and may increase or maintain tryptophan levels important to T cell function. Tryptophan depletion is associated with immunosuppression involving T cell arrest and anergy. C71535 579877 EGFRBi-armed autologous activated T cells Autologous activated T cells, loaded with a bispecific antibody produced by heteroconjugation of anti-CD3 and anti-epidermal growth factor receptor (EGFR) monoclonal antibodies, with potential antineoplastic activity. Binding of EGFRBi-armed autologous activated T cells to EGFR-positive tumor cells may result in increased T cell-mediated cytotoxicity towards tumor cells expressing EGFR. Arming activated T cells with this bispecific antibody may significantly increase T cell secretion of anti-tumor associated cytokines such as IL2, RANTES, IFN-gamma, and TNF-alpha. C71536 580835 allogeneic CD4+ memory Th1-like T cells/microparticle-bound anti-CD3/anti-CD28 A preparation consisting of allogeneic, differentiated Th1-like T cells bound to T cell-stimulating monoclonal antibodies with potential antitumor activity. More specifically, allogeneic CD4+ memory Th1-like T cells/microparticle-bound anti-CD3/anti-CD28 are composed of a proprietary preparation of mismatched, allogeneic differentiated CD4+ memory Th1-like T cells bound to paramagnetic, epoxy-covered 4.5 micron microparticles with covalently bound anti-CD3/anti-CD28 monoclonal antibodies at a 2:1 bead:cell ratio. The CD4+ memory Th1-like T cells are derived from precursors found in the circulation of a normal donor. Stimulated by the microparticle-bound monoclonal antibodies, the infused T cells produce pro-inflammatory, anti-tumor cytokines such as like IFN-gamma, TNF-beta, and IL-2, disabling tumor immune avoidance mechanisms and stimulating the host immune system to both reject the infused T cells and kill tumor cells. C71540 580837 fermented soybean protein beverage A fermented soybean-derived phytochemical beverage with potential antineoplastic activity. Fermented soybean protein beverage is reported to exhibit immunostimulatory, anti-viral, pro-apoptotic, anti-angiogenic, anti-proliferative, and anti-inflammatory activities and to enhance the cytotoxic effects of natural killer (NK) cells. The fermentation process is reported to hydrolyze many soybean proteins into amino acids and nitrogen-rich compounds and to protect and enhance the activities of isoflavones such as genistein, protease inhibitors, saponins, phytosterols, inositol hexaphosphate, and other beneficial dietary nutrients and micronutrients found in soybeans. C71541 580838 acadesine A 5-aminoimidazole-4-carboxamide (AICA) riboside, a purine nucleoside analog, and a nucleotide biosynthesis precursor with B cell pro-apoptotic activity. Following cellular uptake, acadesine is phosphorylated to AICA ribotide (ZMP), which mimics 5'-adenosine monophosphate (AMP). Both AMP-activated protein kinase (AMPK) and AMPK kinase (AMPKK) are activated by ZMP, which appears to be necessary for the induction of apoptosis. Acadesine-induced apoptosis also appears to require cytochrome c release from mitochondria and caspase activation and is p53-independent. However, the exact mechanism of acadesine-induced apoptosis is unknown. T cells are significantly less susceptible than B cells to acadesine-induced apoptosis. AMPK regulates several cellular systems including the cellular uptake of glucose, the beta-oxidation of fatty acids, protein synthesis, and the biogenesis of glucose transporter 4 (GLUT4) and mitochondria. C71537 580840 aziridinylbenzoquinone RH1 A water-soluble, synthetic aziridinylbenzoquinone with potential antineoplastic activity. Bioactivation of aziridinylbenzoquinone RH1 occurs through the two-electron reduction of the quinone to the hydroquinone by the two-electron quinone reductase DT-diaphorase (DTD). The resultant hydroquinone selectively alkylates and cross-links DNA at the 5'-GNC-3' sequence, inihibiting DNA replication, inducing apoptosis, and inhibiting tumor cell proliferation. DTD is over-expressed in many tumors relative to normal tissue, including lung, colon, breast and liver tumors. C29404 580988 angiogenesis inhibitor GT-111 An adenovirus encoding an endothelial cell-specific, murine pre-proendothelin-1 (PPE-1) promoter and a Fas-based chimeric death receptor with potential anti-angiogenic activity. Endothelial cell-specific transcriptional control of the adenoviral vector is achieved by the use of a modified murine PPE-1 promoter that is specifically activated in PPE-1-expressing angiogenic endothelial cells residing in the tumor microvasculature. Subsequently, the Fas-c (Fas-chimeric) death receptor, containing Fas and tumor necrosis factor (TNF) receptor 1 (TNFR1) moieties, is expressed in angiogenic endothelial cells; endothelial cell-specific Fas-mediated apoptosis is initiated by the binding of TNF-alpha, abundant in the tumor microenvironment, to the TNFR1 moiety of the expressed Fas-c death receptor. C71539 581226 gold sodium thiomalate The sodium salt of gold thiomalic acid, an organogold compound with antirheumatic and potential antineoplastic activities. Gold sodium thiomalate (GST) appears to inhibit the activity of atypical protein kinase C iota (PKCiota) by forming a cysteinyl-aurothiomalate adduct with the cysteine residue Cys-69 within the PB1 binding domain of PKCiota. This prevents the binding of Par6 (Partitioning defective protein 6) to PKCiota, thereby inhibiting PKCiota-mediated oncogenic signaling, which may result in the inhibition of tumor cell proliferation, the promotion of tumor cell differentiation, and the induction of tumor cell apoptosis. Atypical PKCiota, a serine/threonine kinase overexpressed in numerous cancer cell types, plays an important role in cancer proliferation, invasion, and survival; Par6 is a scaffold protein that facilitates atypical PKC-mediated phosphorylation of cytoplasmic proteins involved in epithelial and neuronal cell polarization. C74037 581229 tasquinimod A quinoline-3-carboxamide linomide analogue with antiangiogenic and potential antineoplastic activities. Tasquinimod has been shown to decrease blood vessel density but the exact mechanism of action is not known. This agent has also been shown to augment the antineoplastic effects of docetaxel and androgen ablation in a murine model of prostate cancer involving human prostate cancer xenografts. C74080 581379 LY6K/VEGFR1/VEGFR2 multipeptide vaccine A multipeptide vaccine consisting of peptides derived from lymphocyte antigen 6 complex locus K (LY6K) and type I and II vascular endothelial growth factor receptors (VEGFRs) with potential antineoplastic activity. Upon administration, LY6K/VEGFR1/VEGFR2 multipeptide vaccine may elicit an antitumor cytotoxic T-lymphocyte (CTL) immune response against LY6K-expressing tumor cells and/or VEGFR-expressing vascular endothelial cells involved in tumor angiogenesis. LY6K is a tumor-associated antigen (TAA) that occurs singly in glycosylphosphatidyl-inositol (GPI)-linked cell-surface glycoproteins or as three-fold repeated domain in the urokinase-type plasminogen activator receptor; VEGFRs are cell surface receptors that stimulate endothelial cell proliferation, invasion, angiogenesis, and vasculogenesis upon ligand binding and receptor activation. C74056 581382 anti-1-amino-3-[18F ]fluorocyclobutane-1-carboxylic acid A radiotracer containing a synthetic amino acid analogue of L-leucine radiolabeled with fluorine F 18 with potential diagnostic imaging use. Similar to most amino acids, anti-1-amino-3-[18F]fluorocyclobutane-1-carboxylic acid ([18]FACBC) appears to enter cells through the energy-independent L-type amino acid transporter (LAT) system. As an amino acid analogue, this agent is preferentially accumulated by tumor cells due to their increased metabolic needs; however, unlike naturally occuring amino acids, this non-natural amino acid-analogue radiotracer is not metabolized. Accordingly, [18]FACBC accumulates in tumor cells and can potentially be used to image tumors using positron emission tomography (PET). C74002 581399 standardized freeze-dried table grape powder A standardized freeze-dried preparation of desiccated table grapes containing polyphenols (including flavanols, anthocyanins, flavonols, and stilbenes such as resveratrol) and other unidentified compounds with antioxidant activity. Standardized freeze-dried table grape powder increases serum antioxidant activity and reduces the macrophage-mediated oxidation and uptake of low-density lipoprotein (LDL). \nThis agent has been shown to inhibit genes linked to the development of sporadic colorectal cancer and may exhibit chemopreventive activity for other human cancers. C74078 581584 adenoviral vector encoding HSV thymidine kinase An adenoviral vector engineered to express the herpes simplex virus thymidine kinase (HSV-tk) gene, which, when administered in conjunction with a synthetic acyclic guanosine analogue, possesses potential antineoplastic activity. Adenoviral vector encoding HSV thymidine kinase is transduced into tumor cells, sensitizing tumor cells that overexpress HSV-tk to synthetic acyclic guanosine analogues. Subsequently, a low dose of a synthetic acyclic guanosine analogue such as valacyclovir (VCV) or ganciclovir (GCV) is given, which may preferentially kill tumor cells containing the adenoviral vector and overexpressing HSV-tk. Release of tumor-associated antigens (TAAs) by dying tumor cells may then stimulate an antitumor cytotoxic T lymphocyte (CTL) response. C73996 582534 fluorine F 18 RGD-based integrin peptide-polymer AH111585 A small synthetic peptide containing an RGD-sequence (Arg-Gly-Asp) attached to the positron-emitting isotope fluorine F 18 that may be used to selectively image tumor cells and tumor vasculature by PET imaging. The RGD motif of fluorine F 18 RGD-based integrin peptide-polymer AH111585 selectively binds to the alphaVbeta3 integrin receptor, commonly upregulated on the surfaces of tumor cells and tumor vasculature endothelial cells. This agent may be of use in visualizing and quantifying a decrease in tumor vascularity in response to antiangiogenic agents. C74031 582893 sodium dichloroacetate The sodium salt of dichloroacetic acid with potential antineoplastic activity. Dichloroacetate ion inhibits pyruvate dehydrogenase kinase, resulting in the inhibition of glycolysis and a decrease in lactate production. This agent may stimulate apoptosis in cancer cells by restoring normal mitochondrial-induced apoptotic signaling. C73591 582896 Ad5F35-LMP1/LMP2-transduced autologous dendritic cells Autologous dendritic cells (DCs) transduced with the replication-deficient adenoviral vector Ad5F53 encoding the Epstein-Barr virus (EBV) transmembrane latent membrane proteins 1 and 2 (LMP1/LMP2) with potential immunostimulatory activity. Vaccination with Ad5F35-LMP1/LMP2-transduced autologous dendritic cells may stimulate a specific cytotoxic T-lymphocyte (CTL) response against LMP1- and LMP2-expressing tumor positive cells, resulting in tumor cell lysis and inhibition of tumor cell proliferation. LMP1 and LMP2 are expressed in various malignancies including nasopharyngeal cancer and EBV-positive Hodgkin disease. C73995 582989 fentanyl sublingual spray A sublingual preparation of a short-acting, synthetic anilidopiperidine opioid with analgesic activity. After rapid sublingual transmucosal absorption, the active ingredient fentanyl selectively binds to and activates mu-opioid receptors in the central nervous system (CNS), mimicking the effects of endogenous opiates. C74029 583257 doxorubicin-GnRH agonist conjugate AEZS-108 A peptide agonist of the gonadotropin releasing hormone-1 receptor (GnRH-1R) that is conjugated to the anthracycline antibiotic doxorubicin with potential antineoplastic activity. Doxorubicin-GnRH agonist conjugate AEZS-108 binds to GnRH-1Rs, which may be highly expressed on endometrial and ovarian tumor cell membrane surfaces, and is internalized. Once inside the cell, the doxorubicin moiety of this agent intercalates into DNA and inhibits the topoisomerase II activity, which may result in the inhibition of tumor cell DNA replication and tumor cell proliferation. C74025 583260 IGF-1R antagonist BMS-754807 An orally bioavailable antagonist of human insulin-like growth factor type I receptor (IGF-1R) with potential antineoplastic activity. IGF-1R antagonist BMS-7548077 binds to IGF-1R, preventing IGF-1 ligand binding and activation of IGF-1R-mediated signaling pathways; inhibition of IGF-1R-mediated signaling pathways may result in the inhibition of tumor cell proliferation and the induction of tumor cell apoptosis. IGF-1R is a receptor tyrosine kinase expressed on most tumor cells and is involved in mitogenesis, angiogenesis, and tumor cell survival. C74043 583270 gallium Ga 68-DOTANOC A gallium Ga 68-radiolabeled analogue of somatostatin that may be used in conjunction with positron emission tomography (PET) to image neuroendocrine tumors and metastases. Gallium Ga 68-DOTANOC is a conjugate of the somatostatin analogue 1-Nal3-octreotide (NOC) and gallium Ga 68-labeled 1,4,7,10-tetraazacyclododecane-N,N',N'',N'''-tetraacetic acid (DOTA). The somatostatin analogue NOC has a high affinity for somatostatin receptor subtypes 2, 3, and 5; these receptor subtypes have been shown to be present in large numbers on neuroendocrine tumors and their metastases, while most other normal tissues express low levels of these somatostatin receptor subtypes. C74034 583418 autologous dendritic cell-adenovirus CCL21 vaccine A cancer vaccine comprised of autologous dendritic cells (DCs) that have been transduced ex vivo with an adenoviral vector containing the CCL21 gene with potential immunostimulatory and antineoplastic activities. Upon intratumoral administration, autologous dendritic cell-adenovirus CCL21 vaccine expresses the chemokine CCL21, which may induce an antitumoral cytotoxic immune response in the tumor microenvironment. CCL21 [chemokine (C-C motif) ligand 21] has been shown to attract antigen presenting cells (APCs), like leukocytes and DCs, and natural killer (NK) cells and their T-cell effectors to induce a cytotoxic immune response. C74015 583540 proteasome inhibitor CEP 18770 An orally bioavailable synthetic P2 threonine boronic acid inhibitor of the chymotrypsin-like activity of the proteasome, with potential antineoplastic activity. Proteasome inhibitor CEP 18770 represses the proteasomal degradation of a variety of proteins, including inhibitory kappaBalpha (IkappaBalpha), resulting in the cytoplasmic sequestration of the transcription factor NF-kappaB; inhibition of NF-kappaB nuclear translocation and transcriptional up-regulation of a variety of cell growth-promoting factors; and apoptotic cell death in susceptible tumor cell populations. In vitro studies indicate that this agent exhibits a favorable cytotoxicity profile toward normal human epithelial cells, bone marrow progenitors, and bone marrow-derived stromal cells relative to the proteasome inhibitor bortezomib. The intracellular protein IkappaBalpha functions as a primary inhibitor of the proinflammatory transcription factor NF-kappaB. C74075 583541 nanoparticle albumin-bound rapamycin The macrolide antibiotic rapamycin bound to nanoparticle albumin with immunosuppressant (see sirolimus) and potential antiangiogenic and antineoplastic activities. Rapamycin binds to the immunophilin FK Binding Protein-12 (FKBP-12) to generate a complex that binds to and inhibits the activation of the mammalian Target Of Rapamycin (mTOR), a key regulatory kinase. In turn, inhibition of mTOR may result in the inhibition of the phosphatidylinositol 3 (PI-3) kinase/Akt pathway and vascular endothelial cell growth factor (VEGF) secretion, which may result in decreased tumor cell proliferation and tumor angiogenesis. The binding of water-insoluble rapamycin to nanoparticle albumin permits the albumin-mediated endocytosis of rapamycin by tumor cells and endothelial cells. C74065 583564 anti-CD38 monoclonal antibody A fully human monoclonal antibody directed against the cell surface glycoprotein CD-38 with potential antineoplastic activity. The binding of anti-CD38 monoclonal antibody to natural killer (NK) cells mimics the normal CD38-CD31 interaction on the NK cell surface. CD38 is also present on multiple myeloma (MM) cells and plasma leukemia cells; this agent may preferentially bind these cells, triggering antitumoral antibody-dependent\ncellular cytotoxicity (ADCC) and complement-dependent cytotoxicity (CDC). \nCD38, a cell surface glycoprotein, is present on various immune cells and has been shown to regulate the cytotoxic response of activated NK cells. C74007 583632 NY-ESO-1/LAGE-1 HLA class I/II peptide vaccine A cancer vaccine containing HLA class I- and II-binding peptides derived from the NY-ESO-1/LAGE-1 cancer/testis antigen with potential immunostimulatory and antineoplastic activities. Upon administration, NY-ESO-1/LAGE-1 HLA class I/II peptide vaccine may induce a cytotoxic immune response against tumor cells that over-express NY-ESO-1/LAGE-1. \n Rarely expressed by normal cells, the NY-ESO-1/LAGE-1 cancer/testis antigen has been shown to be preferentially expressed on the surface of some cancer cell types. C74066 583659 vaccinia virus (vvDD-CDSR) A highly tumor-selective vaccinia virus (vv) with an engineered double deletion (DD) of the thymidine kinase (tk) and vaccinia growth factor genes and additions of both a cytosine deaminase (CD) gene and a somatostatin receptor (SR) gene with potential oncolytic viral activity. The tk and vaccinia growth factor gene deletions in intratumorally administered vaccinia virus (vvDD-CDSR) help to restrict its replication and cytolytic activity to tumor cells with large nucleotide pools and tumor cells with activation of the EGFR-Ras pathway. Addition of the CD gene to the viral genome allows control of oncolytic viral infection through the administration of the prodrug 5-fluorocytosine (5-FC), converted by CD to the antimetabolite 5-fluorouracil (5-FU) in cells infected with this agent. Addition of the SR gene allows anatomical localization of vaccinia virus (vvDD-CDSR) through the use of octreotide scintigraphy. C74089 584170 gadolinium-chelate A coordination complex consisting of a gadolinium ion bound to a hexadentate organic chelating agent such as diethylenetriaminepentaacetic acid. Chelates of gadolinium are frequently utilized as magnetic resonance imaging (MRI) contrast agents and can be used to track nanoparticle-mediated drug delivery. 584589 malignant glioma tumor lysate-pulsed autologous dendritic cell vaccine A cell-based cancer vaccine composed of autologous dendritic cells (DCs) pulsed with lysates from malignant glioma cells with potential immunostimulatory and antineoplastic activities. Upon administration, malignant glioma tumor lysate-pulsed autologous dendritic cell vaccine exposes the immune system to undefined malignant glioma tumor-associated antigens (TAAs), which may result in anti-tumoral cytotoxic T lymphocyte (CTL) and antibody responses against glioma cells and glioma cell lysis. C74057 584599 synthetic brain tumor peptides-pulsed autologous dendritic cell vaccine A cell-based cancer vaccine composed of autologous dendritic cells (DCs) pulsed with synthetic brain tumor peptides with potential immunostimulatory and antineoplastic activities. Upon administration, synthetic brain tumor peptides-pulsed autologous dendritic cell vaccine may stimulate anti-tumoral cytotoxic T lymphocyte (CTL)l and antibody responses against glioma tumor cells, resulting in glioma tumor cell lysis. C74079 584706 varenicline A partial agonist of the nicotinic acetylcholine receptor (nAChR) subtype alpha4beta2. Nicotine stimulation of central alpha4beta2 nAChRs located at presynaptic terminals in the nucleus accumbens causes the release of the neurotransmitter dopamine, which may be associated with the experience of pleasure; nicotine addiction constitutes a physiologic dependence related to this dopaminergic reward system. As an AChR partial agonist, varenicline attenuates the craving and withdrawal symptoms that occur with abstinence from nicotine but is not habit-forming itself. C73609 584952 anti-endoglin monoclonal antibody TRC105 A human/murine chimeric monoclonal antibody directed against endoglin (CD105) with potential antiangiogenic and antineoplastic activities. Anti-endoglin monoclonal antibody TRC105 binds to endoglin, which may result in inhibition of tumor angiogenesis and decreased tumor cell proliferation. The glycoprotein endoglin is a transforming growth factor beta-1 (TGF beta-1) accessory receptor that is highly expressed on tumor vessel endothelial cells and appears to be essential for angiogenesis. C74010 584999 idiotype-pulsed autologous dendritic cell vaccine APC8020 A cell-based cancer vaccine composed of autologous dendritic cells (DCs) pulsed with tumor-derived clonal immunoglobulin (Ig) with potential immunostimulatory and antineoplastic activities. Upon administration, idiotype-pulsed autologous dendritic cell vaccine APC8020, containing idiotype (Id) protein structures that can be recognized by antibodies and by CD41 T lymphocytes and CD81 T lymphocytes, may stimulate antitumoral cytotoxic T lymphocyte (CTL) and antibody responses against Id-expressing tumor cells. The Id represents the unique antigenic determinants in the variable regions of the clonal Ig. C74042 585556 parathyroid hormone-related protein (1-36) A recombinant form of a mature, N-terminal secretory peptide derived from a parathyroid hormone-related protein (PTHrP) preprohormone through posttranslational endoproteolytic processing with vasodilating, myorelaxant, and parathyroid hormone (PTH)-like calciotropic activities. Expressed throughout the cardiovascular system, parathyroid hormone-related protein (1-36) [PTHrP (1-36)] was first identified as the PTH-like hypercalcemic factor of humoral hypercalcemia of malignancy; however, its sequence differs significantly from that of PTH (1-34) although both proteins share the same N-terminal end which accounts for the calciotropic activity. Both PTHrP (1-36) and PTH (1-34) bind to the type 1 parathyroid hormone receptor (PTH1R), a specific seven-transmembrane-helix-containing G protein-coupled receptor mainly located in bone and kidney cells. C74068 585656 eflornithine hydrochloride ointment An ointment formulation of the hydrochloride salt of an ornithine decarboxylase (ODC) inhibitor with hair-growth inhibitory and potential chemopreventive activities. When administered topically, eflornithine irreversibly inhibits skin ODC activity, thereby inhibiting the synthesis of polyamines; inhibition of polyamine synthesis may result in diminished hair growth and epidermal cell turnover. C74026 585657 diclofenac sodium gel A gel formulation of the sodium salt of diclofenac, a nonsteroidal benzeneacetic acid derivative with analgesic, antipyretic and anti-inflammatory activities. Diclofenac binds to and chelates both isoforms of cyclooxygenase (COX-1 and-2), thereby blocking the conversion of arachidonic acid (AA) to pro-inflammatory prostaglandins. This agent may also inhibit lipoxygenases, resulting in the inhibition of pro-inflammatory leukotriene synthesis from AA. C74024 586080 MET tyrosine kinase inhibitor PF-02341066 An orally bioavailable agent belonging to the class of c-met/hepatocyte growth factor receptor (HGFR) tyrosine kinase inhibitors with potential antineoplastic activity. MET tyrosine kinase inhibitor PF-02341066 inhibits the membrane receptor MET and activation of the MET signaling pathway, which may block tumor cell growth, migration and invasion, and tumor angiogenesis in susceptible tumor cell populations. C74061 586104 live-attenuated Listeria encoding human mesothelin vaccine CRS-207 A recombinant Listeria-based cancer vaccine containing a live-attenuated strain of the facultative intracellular bacterium Listeria monocytogenes (Lm) expressing human mesothelin with potential immunostimulatory and antineoplastic activities. Upon administration of this vaccine, Listeria invade professional phagocytes within the immune system and express mesothelin, which may activate a cytotoxic T-lymphocyte (CTL) response against mesothelin-expressing tumor cells, resulting in tumor cell lysis. In addition, the Listeria vector itself may induce a potent innate and adaptive immunity unrelated to mesothelin expression. Mesothelin is a cell surface glycoprotein involved in cell adhesion and is overexpressed in many epithelial-derived cancers, including pancreatic, ovarian and lung cancers, and malignant mesotheliomas. C74055 586115 perflutren lipid microspheres An injectable suspension of liposome-encapsuled microspheres containing the fluorocarbon gas perflutren for contrast enhancement in ultrasound procedures. Because the acoustic impedance of perflutren lipid microspheres is much lower than that of blood, impinging ultrasound waves are scattered and reflected at the microsphere-blood interface and may be visualized with ultrasound imaging. C74071 586119 (61)Cu-ATSM A lipophilic copper(II)bis(thiosemicarbazone) labeled with the positron-emitting isotope (61)Cu with hypoxia-selective and radioisotopic activities. With a high membrane permeability and redox potential, (61)Cu-ATSM easily enters and selectively resides in hypoxic cells. The extent of (61)Cu-ATSM retention in tissue is inversely related to the state of tissue oxygenation allowing the quantitation of tissue hypoxia with positron emission tomography (PET). C74019 586304 iodine I 125 anti-EGFR-425 monoclonal antibody A radioimmunoconjugate consisting of a murine IgG2a monoclonal antibody directed against the human epidermal growth factor receptor (EGFR) labeled with iodine I 125 with potential antineoplastic activity. Iodine I 125 anti-EGFR-425 monoclonal antibody binds specifically to the epidermal growth factor receptor (EGFR). Upon binding to EGFR-expressing tumor cells, this agent is internalized, selectively delivering a potentially cytotoxic dose of gamma radiation. EGFR is a receptor tyrosine kinase that may be overexpressed on the cell surfaces of various solid tumors. C74051 586372 iodine 131-6-beta-iodomethyl-19-norcholesterol A radioiodine-labeled cholesterol analogue with radioisotopic activity. Iodine 131-l-6-beta-iodomethyl-19-norcholesterol accumulates in tissues where steroid hormones are produced, including the adrenal cortex and, to a lesser extent, the ovaries and the testes. After binding to low-density lipoprotein (LDL) receptors in the adrenal cortex, this agent is internalized, permitting scintigraphic localization of areas of adrenocortical glucocorticoid, mineralocorticoid and androgen secretion, and the scintigraphic assessment of adrenocortical function. C74052 586417 Hedgehog antagonist GDC-0449 An orally bioavailable small molecule with potential antineoplastic activity. Hedgehog antagonist GDC-0449 targets the Hedgehog signaling pathway, blocking the activities of the Hedgehog-ligand cell surface receptors PTCH and/or SMO and suppressing Hedgehog signaling. The Hedgehog signaling pathway plays an important role in tissue growth and repair; aberrant constitutive activation of Hedgehog pathway signaling and uncontrolled cellular proliferation may be associated with mutations in the Hedgehog-ligand cell surface receptors PTCH and SMO. C74038 586439 anti-CD19 fully human monoclonal antibody MDX-1342 A fully human anti-CD19 monoclonal antibody directed against the B-cell-specific membrane protein CD-19 with potential antineoplastic activity. Anti-CD19 monoclonal antibody MDX-1342 binds to CD19, depleting and eliminating CD19-expressing B-cells. CD19 is widely expressed during B-cell development, from pro-B-cell to early plasma cell stages. C74003 586491 CXCR4 inhibitor MSX-122 An orally bioavailable inhibitor of CXCR4 with potential antineoplastic and antiviral activities. CXCR4 inhibitor MSX-122 binds to the chemokine receptor CXCR4, preventing the binding of stromal derived factor-1 (SDF-1) to the CXCR4 receptor and receptor activation, which may result in decreased tumor cell proliferation and migration. CXCR4, a chemokine receptor belonging to the GPCR (G protein-coupled receptor) gene family, plays an important role in chemotaxis and angiogenesis and is upregulated in several tumor cell types; it is also a co-receptor for HIV entry into T cells. C74022 586659 Brassica vegetable A vegetable belonging to the Brassica genus of plants in the mustard family with potential chemopreventive activity. Brassica vegetables, including broccoli, cabbage, kale, Brussel sprouts, turnip and cauliflower, contain a significant amount of glucosinolates. Glucosinolate metabolites, such as sulforaphane and indole-3-carbinol, act as antioxidants and may stimulate endogenous phase II detoxifying enzymes, including glutathione S-transferase and quinone reductase. These biotransformation enzymes play major roles in the detoxification of carcinogenic agents. C73795 586660 fentanyl citrate pectin-based nasal spray A pectin-based, aqueous nasal spray containing the citrate salt of fentanyl, a synthetic lipophilic phenylpiperidine opioid, with analgesic activity. Fentanyl binds to and stimulates mu-opioid receptors in the central nervous system (CNS), mimicking the analgesic effect of endogenous opiates. Upon intranasal administration of this agent and contact with the nasal mucosa, pectin in low-viscosity aqueous solution gels in the presence of mucosal calcium ions; from this intranasal gel delivery platform, fentanyl is released into the systemic circulation in a relatively rapid but controlled and sustained manner. C74028 586662 iodine-123 metaiodobenzylguanidine The neurotransmitter analogue 3-nitrobenzylguanidine conjugated to iodine I 123 and used as a gamma-emitting imaging agent. The adrenergic tissue uptake and storage of I-123 metaiodobenzylguanidine (I-123 MIBG) mimics that of norepinephrine (NE). The distribution of this agent enables the scintigraphic imaging of neural crest tumors, such as neuroblastoma and pheochromocytoma. C74049 586949 pegylated irinotecan NKTR 102 A formulation of polyethylene glycol (PEG)-encapsulated irinotecan with antineoplastic activity. The prodrug irinotecan, a semisynthetic derivative of camptothecin, is converted to the biologically active metabolite 7-ethyl-10-hydroxy-camptothecin by a carboxylesterase-converting enzyme. One thousand-fold more potent than its parent compound irinotecan, 7-ethyl-10-hydroxy-camptothecin inhibits topoisomerase I activity by stabilizing the cleavable complex of topoisomerase I and DNA, resulting in DNA breaks that inhibit DNA replication and trigger apoptosis. Pegylation provides improved drug penetration into tumors and decreases drug clearance, thereby increasing the duration of therapeutic effects while lowering the toxicity profile. C74069 587041 topical gemcitabine hydrochloride A topical preparation of gemcitabine hydrochloride with antineoplastic activity. Gemcitabine, an analogue of the antimetabolite nucleoside deoxycytidine, is converted intracellularly to the active metabolites difluorodeoxycytidine di- and triphosphate (dFdCDP, dFdCTP). dFdCDP inhibits ribonucleotide reductase, thereby decreasing the deoxynucleotide pool available for DNA synthesis; dFdCTP is incorporated into DNA, resulting in DNA strand termination and apoptosis. C74085 587179 glioma-associated antigen peptide-pulsed autologous dendritic cell vaccine A cancer vaccine comprised of autologous dendritic cells pulsed with synthetic glioma-associated antigen (GAA) peptides with potential antineoplastic activity. Upon administration, this vaccine may stimulate anti-tumoral cytotoxic T lymphocyte (CTL) and antibody responses against GAA peptide-expressing glioma cells, resulting in tumor cell lysis. C74036 587196 iodine I 124 iodo-azomycin galactopyranoside A diagnostic radiopharmaceutical comprised of iodo-azomycin galactopyranoside (IAZGP) labeled with the positron-emitting radioisotope iodine I 124 and used as an imaging agent. Iodine I 124 iodo-azomycin galactopyranoside (I-124 IAZGP) is reduced under hypoxic conditions, covalently binding to macromolecules in hypoxic cells. After incorporation into hypoxic tumor cell DNA, I-124 IAZGP can be localized and quantified using positron emission tomography (PET), allowing a quantitative assessment of hypoxic tumor burden. IAZGP appears to have a higher water solubility and faster clearance from normal tissue than traditional imidazole tracers. C74050 587251 ALVAC-MART-1 vaccine A cancer vaccine containing a replication-defective recombinant canarypox virus (ALVAC), encoding an epitope of MART-1 (melanoma antigen recognized by T-cells), with potential immunostimulatory and antineoplastic activities. Upon administration, the MART-1 epitope is expressed by the ALVAC vector in ALVAC-MART-1 vaccine; a host cytotoxic T lymphocyte (CTL) response against MART-1-expressing tumor cells may follow, resulting in tumor cell lysis and decreased tumor cell proliferation. C73999 587341 indibulin A synthetic small molecule with antimitotic and potential antineoplastic activities. Indibulin binds to a site on tubulin that is different from taxane- or Vinca alkaloid-binding sites, destabilizing tubulin polymerization and inducing tumor cell cycle arrest and apoptosis. This agent has been shown to be active against multidrug-resistant (MDR) and taxane- resistant tumor cell lines. C74045 587478 PI3K inhibitor BGT226 A phosphatidylinositol 3-kinase (PI3K) inhibitor with potential antineoplastic activity. PI3K inhibitor BGT226 specifically inhibits PIK3 in the PI3K/AKT kinase (or protein kinase B) signaling pathway, which may trigger the translocation of cytosolic Bax to the mitochondrial outer membrane, increasing mitochondrial membrane permeability; apoptotic cell death may ensue. Bax is a member of the proapoptotic Bcl2 family of proteins. C74073 587501 CD3/CD28 costimulated vaccine-primed autologous T-cells A population of T cells that have been sensitized to vaccine tumor antigen(s) in vivo; collected from the patient; co-stimulated with antibodies to the T-cell cell surface proteins CD3 and CD28 and expanded ex vivo; and then infused into the same patient. CD3, part of the T cell receptor complex, and CD28, a T-cell surface-associated co-stimulatory molecule, are both required for full T-cell activation. Adoptive transfer of CD3/CD28 costimulated vaccine-primed autologous T-cells may induce the production of interferon-gamma (IFN-gamma) and granulocyte-macrophage colony-stimulating factor (GM-CSF) and associated antitumor effects and a graft-versus-tumor (GVT) response. C74017 587505 nitroglycerin An organic nitrate with vasodilator activity. Nitroglycerin is converted into nitric oxide (NO) in smooth muscle and activates guanylyl cyclase, thereby increasing cGMP concentration, and resulting in smooth muscle relaxation. Dilatation of the veins results in decreased venous return to the heart, thereby decreasing left ventricular volume (reduced preload) and decreasing myocardial oxygen requirements. Arteriolar relaxation reduces arteriolar resistance (reduced afterload), thereby decreasing myocardial oxygen demands. In addition, nitroglycerin causes coronary artery dilatation, thereby improving myocardial blood distribution. 587979 yttrium Y 90 anti-CD45 monoclonal antibody AHN-12 A radioimmunoconjugate comprised of the monoclonal antibody AHN-12 conjugated to the radioisotope yttrium 90 with potential radioimmunotherapeutic activity. Yttrium Y 90 monoclonal antibody AHN-12 binds to the tyrosine phosphatase CD45, expressed on the surface of normal and malignant hematopoietic cells. After binding and internalization by CD45-expressing tumor cells, this agent may deliver a cytotoxic dose of beta radiation. C74093 587980 anti-CD45 monoclonal antibody AHN-12 A high affinity IgG1 monoclonal antibody with potential immunotherapeutic activity. Anti-CD45 monoclonal antibody AHN-12 recognizes CD45, a transmembrane protein tyrosine phosphatase that is expressed on the surface of normal and malignant hematopoietic cells. C74009 587999 Met tyrosine kinase inhibitor BMS-777607 An inhibitor of MET tyrosine kinase with potential antineoplastic activity. MET tyrosine kinase inhibitor BMS-777607 binds to c-Met protein, or hepatocyte growth factor receptor (HGFR), preventing binding of hepatocyte growth factor (HGF) and disrupting the MET signaling pathway; this agent may induce cell death in tumor cells expressing c-Met. c-Met, a receptor tyrosine kinase overexpressed or mutated in many tumor cell types, plays an important role in tumor cell proliferation, survival, invasion, and metastasis, and in tumor angiogenesis. C74060 588002 GD2 lactone/GD3 lactone-KLH conjugate bivalent vaccine A cancer vaccine, containing epitopes of the gangliosides GD2 and GD3 conjugated with the immunostimulant keyhole limpet hemocyanin (KLH), with potential antineoplastic activity. Vaccination with GD2 lactone/GD3 lactone-KLH conjugate bivalent vaccine may elicit antibodies against tumor cells expressing either epitope, resulting in complement-mediated cytotoxicity (CMC) and antibody-dependent cell-mediated cytotoxicity (ADCC). Located primarily in the nervous system, gangliosides, such as GD2 and GD3, are cell membrane components involved in cellular recognition and cell-cell communication. C74035 588003 immunoadjuvant QS-DG A synthetic saponin, chemically identical to the natural saponin QS-21, with immunoadjuvant activity. When co-administered with vaccine antigens, immunoadjuvant QS-DG may increase total antitumoral vaccine-specific antibody responses and cytotoxic T-lymphocyte (CTL) responses. C74044 588355 indium I 111 chimeric monoclonal antibody G250 A radioimmunoconjugate comprised of the chimeric monoclonal antibody G250 conjugated with the gamma-emitting radioisotope indium In 111. Indium I 111 chimeric monoclonal antibody G250 binds to G250, allowing the localization of G250-expressing tumor cells using gamma scintigraphy.\nFound in the majority of renal cell carcinomas (RCCs), G250 or carbonic anhydrase isozyme IX (CA IX) is a cell surface tumor-associated antigen (TAA). C74047 588356 indium I 111 bevacizumab A radioimmunoconjugate comprised of the recombinant humanized monoclonal antibody bevacizumab conjugated with the gamma-emitting radioisotope indium In 111. Indium I 111 bevacizumab binds to vascular endothelial growth factor (VEGF), allowing the detection of VEGF distribution using gamma scintigraphy. C74046 588359 copper Cu 64 trastuzumab A diagnostic radioimmunoconjugate comprised of the recombinant humanized monoclonal antibody trastuzumab conjugated with the positron-emitting radioisotope copper Cu 64. Copper Cu 64 trastuzumab binds to the extracellular domain of human epidermal growth factor receptor 2 (HER2), allowing the detection of HER2 distribution using positron emission tomography (PET). C74020 588681 flavonoid tablet A tablet formulation of flavonoids with antioxidant and potential chemopreventive activities. Polyphenolic, soluble plant pigment flavonoids inactivate oxygen radicals, prevent lipid peroxidation, and inhibit DNA oxidation. In vitro, these agents have been shown to increase the rate of apoptosis, and inhibit cell proliferation and angiogenesis. Furthermore, flavonoids can induce conjugating enzymes, such as glutathione transferases and glucuronosyltransferases. C74030 588881 tositumomab and iodine I 131 tositumomab A murine IgG2a lambda monoclonal antibody, both unradiolabeled and radiolabeled with iodine I 131, directed against the human B cell-specific surface antigen CD20. Tositumomab binds to CD20, resulting in complement-dependent cytotoxicity (CDC), antibody-dependent cellular cytotoxicity (ADCC), and apoptosis in B cells expressing CD20; in addition to the antibody-mediated cytotoxicity, iodine I 131 tositumomab delivers cytotoxic ionizing radiation specifically to CD20-expressing B cells. In a two-step therapeutic regimen, a predose of unradiolabeled tositumomab is administered first followed by the administration of a dosimetric dose of iodine I 131 tositumomab; 7-14 days later, a therapeutic dose of iodine I 131 tositumomab is administered. The predose of unradiolabeled tositumomab binds to nontumor B cells, increasing the terminal half-life of radiolabeled antibody while protecting nontumor B cells from radiolabeled antibody-mediated radiocytotoxicity. C72672 588895 anti-CD3 immunotoxin A-dmDT390-bisFv(UCHT1) A bivalent recombinant fusion protein immunotoxin derived from the anti-CD3 monoclonal antibody UCHT1 with potential antineoplastic activity. Anti-CD3 immunotoxin A-dmDT390-bisFv(UCHT1) consists of 1-390 amino acid residues of chain A diphtheria toxin (DT) joined via a spacer to the Fv fragment of UCHT1, which is connected to a second UCHT1 Fv fragment via a disulfide bond (hence the "bisFv" designation); the addition of the second Fv fragment overcomes the steric hindrance of immunotoxin binding due to the large N-terminal DT domain. Once inside target T cells, the DT moiety catalyzes the transfer of the ADP-ribose moiety of NAD to diphthamide, a posttranslationally modified histidine residue found in elongation factor 2 (EF-2); inactivation of EF-2, disruption of polypeptide chain elongation, and cell death ensue. CD3 is a complex of five cell-surface polypeptides associated with the T cell receptor (TCR) complex. C74004 588896 udenafil A benzenesulfonamide derivative with vasodilatory activity. Udenafil selectively inhibits phosphodiesterase type 5 (PDE5), thus inhibiting the degradation of cyclic guanosine monophosphate (cGMP) found in the smooth muscle of the corpus cavernosa and corpus spongiosum of the penis; inhibition of cGMP degradation results in prolonged muscle relaxation, vasodilation, and blood engorgement of the corpus cavernosa, and, so, prolonged penile erection. This agent does not significantly inhibit the PDE11 isozyme; PDE11 inhibition may be associated with significant myalgia. C74086 588950 Clino-San vaginal lubricant A vaginal lubricant formulated as a topical gel used to prevent and treat vaginal dryness. With a pH similar to that of normal vaginal discharge, Clino-San vaginal lubricant may reduce dryness, pain and irritation often caused by insufficient vaginal discharge due to atrophy of the vulvovaginal mucosa. C74018 588952 Manuka honey A monofloral honey with potential wound repair and antibacterial activities. Manuka honey is produced by bees fed on the flowers of the New Zealand Manuka bush (Leptospermum scoparium). Manuka honey contains a significant higher concentration of the 1,2-dicarbonyl compound methylglyoxal, which may account for its antibacterial activity; this agent may release small amounts of hydrogen peroxide which may also contribute to its antibacterial activity. Manuka honey has been reported to stimulate the formation of new blood capillaries and the growth of fibroblasts and epithelial cells when applied topically to wounds. C74058 588972 MET receptor tyrosine kinase inhibitor SGX523 An orally bioavailable small molecule, belonging to the class of c-Met/hepatocyte growth factor receptor (HGFR) tyrosine kinase inhibitors, with potential antineoplastic activity. MET receptor tyrosine kinase inhibitor SGX523 specifically binds to c-Met protein, or hepatocyte growth factor receptor (HGFR), preventing binding of hepatocyte growth factor (HGF) and disrupting the MET signaling pathway; this agent may induce cell death in tumor cells expressing c-Met. c-Met, a receptor tyrosine kinase overexpressed or mutated in many tumor cell types, plays an important role in tumor cell proliferation, survival, invasion, and metastasis, and in tumor angiogenesis. C74062 588974 CD40 agonist monoclonal antibody CP-870,893 A fully human monoclonal antibody (mAb) agonist of the cell surface receptor CD40 with potential immunostimulatory and antineoplastic activities. Similar to the CD40 ligand (CD40L or CD154), CD40 agonist monoclonal antibody CP-870,893 binds to CD40 on a variety of immune cell types, triggering the cellular proliferation and activation of antigen-presenting cells (APCs), activating B cells and T cells, and enhancing the immune response; in addition, this agent may activate CD40 present on the surfaces of some solid tumor cells, resulting in apoptosis and decreased tumor growth. CD40, a member of the tumor necrosis factor (TNF) receptor superfamily, is expressed on various immune cells, many B-cell malignancies, and some solid tumors, mediating both indirect tumor cell killing through the activation of the immune system and direct tumor cell apoptosis. C74008 588978 ALVAC(2) melanoma multi-antigen therapeutic vaccine A therapeutic cancer vaccine, based on a replication-defective recombinant canarypox virus (ALVAC) encoding multiple melanoma antigens, with potential immunostimulatory and antineoplastic activities. Vaccination with ALVAC(2) melanoma multi-antigen therapeutic vaccine may stimulate the host immune system to mount an immune response against antigen-expressing melanoma cells, resulting in inhibition of tumor growth and/or metastasis. C73998 589128 MEK inhibitor RDEA119 An orally bioavailable selective MEK inhibitor with potential antineoplastic activity. MEK inhibitor RDEA119 specifically inhibits mitogen-activated protein kinase kinase 1 (MAP2K1 or MAPK/ERK kinase 1), resulting in inhibition of growth factor-mediated cell signaling and tumor cell proliferation. MEK, a dual specificity threonine/tyrosine kinase, is a key component of the RAS/RAF/MEK/ERK signaling pathway that regulates cell growth; constitutive activation of this pathway has been implicated in many cancers. C74059 589135 adipose-derived regenerative cells A population of cells derived from adipose tissue with stem cell and wound repair activities. Adipose-derived regenerative cells (ADRC) consists of several cell types, such as adult stem cells, vascular endothelial cells, and vascular smooth muscle cells, among others. These cells contribute to wound repair through a variety of mechanisms by promoting blood vessel growth and blocking apoptosis. In addition, ADRC can differentiate into several tissue types, such as bone, cartilage, fat, skeletal muscle, smooth muscle and cardiac muscle. C73997 589188 lactobacillus fermented extract A proprietary dietary supplement. Lactobacillus fermented extract is made from soymilk fermented by several strains of lactobacillus and yeast via a symbiotic co-culturing technology. The composition of the agent includes amino acids, vitamins, minerals, fatty acids, isoflavones, and saponins. Lactobacillus fermented extract may support healthy intestinal function. C74053 589197 testosterone gel A topical gel preparation of synthetic testosterone. In vivo, testosterone is irreversibly converted to dihydrotestosterone (DHT) in target tissues by the enzyme 5-alpha reductase. Testosterone or DHT ligand-androgen receptor complexes act as transcription factor complexes, stimulating the expression of various responsive genes, resulting in an increase in protein anabolism, a decrease in amino acid catabolism, and retention of nitrogen, potassium, and phosphorus; DHT binds with higher affinity to nuclear androgen receptors than testosterone. In addition, testosterone is irreversibly converted to estradiol by the enzyme complex aromatase, particularly in the liver and adipose tissue. Testosterone and DHT promote the development and maintenance of male sex characteristics related to the internal and external genitalia, skeletal muscle, and hair follicles; estradiol promotes epiphyseal maturation and bone mineralization. C74081 589292 PI3K inhibitor BEZ235 An orally bioavailable phosphatidylinositol 3-kinase (PI3K) inhibitor with potential antineoplastic activity. PI3K inhibitor BEZ235 specifically inhibits PIK3 in the PI3K/AKT kinase (or protein kinase B) signaling pathway, which may trigger the translocation of cytosolic Bax to the mitochondrial outer membrane, increasing mitochondrial membrane permeability; apoptotic cell death may ensue. Bax is a member of the proapoptotic Bcl2 family of proteins. C74072 589299 anti-CD30 monoclonal antibody XmAb2513 A humanized monoclonal antibody directed against the cell surface receptor CD30 with potential immunotherapeutic activity. Anti-CD30 monoclonal antibody XmAb2513 specifically binds to the CD30 antigen, which may result in a cytotoxic T lymphocyte (CTL) response against CD30-expressing tumor cells. CD30, a member of the tumor necrosis factor (TNF) receptor superfamily, is expressed on activated lymphocytes transiently and is constitutively expressed in hematologic malignancies including Hodgkin's disease and some T-cell non-Hodgkin's lymphomas. C74005 589309 [F-18]HX4 A 2-nitroimidazole labeled with the positron-emitting radioisotope fluorine F 18. HX4, the 2-nitroimidazole moiety of [F-18]HX4, is selectively bioreduced and bound in hypoxic tumor cells, permitting the imaging of hypoxic tumor cells with positron emission tomography (PET). C74032 589315 hydrocodone/acetaminophen A combination preparation of the analgesic acetaminophen and the semisynthetic opioid agonist hydrocodone with analgesic and antitussive activities. Acetaminophen exerts its analgesic activity by inhibiting prostaglandin synthesis while hydrocodone exerts its analgesic activity by binding to the mu-receptors in the central nervous system (CNS), thereby mimicking the effects of endogenous opioids. 589317 WT1-sensitized T cells A population of allogeneic T-cells sensitized with Wilms tumor 1 (WT1) antigen with potential immunostimulatory and antineoplastic activities. Upon administration, WT1-sensitized T cells may bind to and lyse WT1-expressing tumor cells. WT1 antigen, a zinc finger DNA-binding protein acting as a transcriptional activator or repressor depending on the cellular or chromosomal context, is overexpressed in leukemic cells and in a vast number of nonhematological solid tumors. C74091 589323 autologous dendritic cell-tumor fusion vaccine A therapeutic cancer vaccine consisting of autologous dendritic cells (DCs) fused with autologous tumor cells with potential immunostimulatory and antineoplastic activities. Autologous dendritic cell-tumor fusion vaccine is generated in vitro by mixing DCs and irradiated tumor cells harvested from individual patients and treating them with polyethylene glycol (PEG) to produce DC-tumor cell fusion hybrid cells. Upon administration, autologous dendritic cell-tumor fusion vaccine may elicit antitumor humoral and cellular immune responses. C74016 589327 VEGFR2-169 peptide vaccine A peptide vaccine containing an HLA-A*2402-restricted epitope of vascular endothelial growth factor receptor (VEGFR) 2 with potential immunostimulatory and antineoplastic activities. Upon administration, VEGFR2-169 peptide vaccine may stimulate a cytotoxic T lymphocyte (CTL) response against VEGFR2-expressing tumor cells. VEGFR2, a receptor tyrosine kinase, is overexpressed by a variety of tumor types; overexpression is associated with tumor cell proliferation and tumor angiogenesis. HLA-A*2402 is an MHC class I molecule that presents antigenic peptides to CD8+ T cells; epitope design restricted to epitopes that bind most efficiently to HLA-A*2402 may improve antigenic peptide immunogenicity. C74090 589518 Arnebia Indigo Jade Pearl topical cream A proprietary multiherbal topical cream based on Chinese herbal medicine with potential antineoplastic, antiviral, antibacterial and immunostimulatory activities. Arnebia Indigo Jade Pearl topical cream contains 12 ingredients including 9 herbs infused in sesame oil, with an additional three powdered ingredients and beeswax added to the infused oil to create the salve. The purported mechanism(s) of action is unclear due to the complexity of the herbal mixture. C74013 589519 endothelin B receptor agonist SPI-1620 A highly selective peptide agonist of the endothelin-B receptor. Endothelin B receptor agonist SPI-1620 binds to endothelin-B receptors on endothelial cells in tumor blood vessels, which, unlike the angioarchitecture of normal blood vessels, are relatively devoid of smooth muscle. This agent may induce a transient, selective increase in blood flow to a tumor, which may result in an increase in the delivery of anticancer agents to the tumor and, so, an increase in anticancer agent efficacy. C74027 589521 anti-CD37 single-chain polypeptide TRU-016 A recombinant single-chain polypeptide engineered to exhibit the full binding and activity of an anti-CD37 monoclonal antibody with potential immunostimulatory and antineoplastic activities. Anti-CD37 single-chain polypeptide TRU-016 binds to CD37 on B-cells, which may result in antibody-dependent cell-mediated cytotoxicity (ADCC) and apoptosis. CD37 is a transmembrane glycoprotein expressed at high-levels on B cells and to a lesser extent on T cells and myeloid cells. This agent may have a longer half-life in vivo than conventional monoclonal antibodies. C74006 589811 MnSOD-plasmid liposomes A plasmid DNA encoding human manganese superoxide dismutase (MnSOD) and liposomally encapsulated with potential chemoprotective activity. When administered orally and localizing in the esophagus, MnSOD-plasmid liposomes express MnSOD, which scavenges reactive oxygen species (ROS); MnSOD scavenging of ROS may result in a reduction in ROS-mediated lipid peroxidation, apoptosis, and micro-ulceration in the epithelial lining of the esophagus. C74054 589887 URLC10 peptide/Montanide ISA51 vaccine A cancer vaccine containing URLC10 (up-regulated lung cancer 10) epitopes with potential immunostimulatory and antineoplastic activities. Upon administration, URL peptide vaccine may stimulate a cytotoxic T lymphocyte (CTL) response against URLC10-expressing tumor cells. Up-regulated in lung and esophageal cancers, the function of URLC10 is unknown. C74087 589964 yttrium Y 90 anti-CD66 monoclonal antibody BW 250/183 A radioimmunoconjugate consisting of the murine IgG1 monoclonal antibody BW250/183 labeled with yttrium Y 90 with potential radioimmunotherapeutic activity. Yttrium Y 90 anti-CD66 monoclonal antibody BW 250/183 binds to a 95 kD nonspecific cross-reacting antigen (CD66b or NCA-95) on granulocytes, selectively delivering a cytotoxic dose of Y 90 beta radiation to CD66b-expressing cells. CD66b, a member of the carcinoembryonic antigen (CEA) family with an unknown function, appears early in the differentiation of granulopoietic cells and is expressed on the cell surface of almost all human granulocytes and their more mature precursors. C74094 590146 mixed bacteria vaccine A cancer vaccine containing a mixture of killed bacteria with potential immunostimulatory and antineoplastic activities. Mixed bacteria vaccine (MBV or Coley’s toxins) consists of a pyrogenic bacterial lysate derived from Serratia marcescens and Streptococcus pyogenes; the active components in the lysate may be lipopolysaccharide (LPS), a component of the Gram-negative bacterial cell wall of Serratia, and streptokinase, an enzyme produced by Streptococcus pyogenes. LPS has been shown to stimulate the host humoral immune response and induce the release of various antitumor cytokines such as tumor necrosis factor (TNF) and interleukin-12 (IL-12). C74063 590609 PNP-expressing ovine atadenovirus FP253 An ovine atadenovirus encoding E. coli purine nucleoside phosphorylase (PNP) with prodrug activating activity. Under the control of a prostate-directed promoter, PNP-expressing atadenovirus vaccine FP253 expresses PNP in prostate tissue only after intraprostatic administration; this enzyme catalyzes systemically administered fludarabine prodrug into the active agent, 2-fluoroadenine. Localized prodrug activation provides prostate-targeted chemotherapy, potentially reducing systemic side effects. C74074 590612 huBC1-huIL12 fusion protein AS1409 An immunoconjugate consisting of the anti-tumor cytokine interleukin-12 (IL-12) fused to the tumor-targeting antibody BC1 with potential immunostimulatory and antineoplastic activities. The antibody moiety of huBC1-huIL12 fusion protein AS1409 binds to the human fibronectin splice variant ED-B, delivering IL-12 directly to the tumor vasculature; tumor vasculature-targeted IL-12 initiates localized immune cascade responses and exhibits cytotoxic and anti-angiogenic activity while minimizing the systemic side effects of IL-12. The human fibronectin splice variant ED-B is over-expressed in the extracellular matrix and blood vessels of tumor tissues. C74041 590620 MVA-PSA-PAP prostate cancer vaccine A cancer vaccine consisting of a recombinant modified vaccinia Ankara (MVA) viral vector encoding genes for prostate specific antigen (PSA) and prostate acid phosphatase (PAP) with potential immunostimulatory and antineoplastic activities. Upon administration, MVA-PSA-PAP prostate cancer vaccine\nexpresses PSA and PAP peptides, which may elicit humoral and cellular immune responses against prostate cancer cells expressing PSA and PAP. Multi-antigen vaccine therapy may be more efficacious than single-antigen therapy vaccine therapy. C74064 590631 Ga-68-labeled F(ab') 2- trastuzumab A radioimmunoconjugate consisting of a trastuzumab fragment labeled with the positron-emitting radioisotope gallium Ga 68 with radioisotopic and antibody activities. Upon administration, Ga-68-labeled F(ab')2-trastuzumab may bind to HER2-positive tumor cells, allowing radioimmunolocalization with positron emission tomography (PET). Trastuzumab is a recombinant humanized monoclonal antibody that selectively binds to the extracellular domain of human epidermal growth factor receptor 2 (HER2), overexpressed by many adenocarcinomas, particularly breast adenocarcinomas. C74033 590640 Aurora kinase inhibitor BI 811283 A small molecule inhibitor of the serine/threonine protein kinase Aurora kinase with potential antineoplastic activity. Aurora kinase inhibitor BI 811283 binds to and inhibits Aurora kinases, resulting in disruption of the assembly of the mitotic spindle apparatus, disruption of chromosome segregation, and inhibition of cell proliferation. Match C74014 590644 brostallicin A synthetic, alpha-bromoacrylic, second-generation minor groove binder (MGB), related to distamycin A, with potential antineoplastic activity. Brostallicin binds to DNA minor groove DNA, after having formed a highly reactive glutathione (GSH)-brostallicin complex in the presence of the enzyme glutathione S-transferase (GST), which is overexpressed in cancer cells; DNA replication and cell division are inhibited, resulting in tumor cell death. Compared to typical MGBs, this agent appears to bind covalently to DNA in a different manner and its activity does not depend on a functional DNA mismatch repair (MMR) mechanism. Accordingly, brostallicin may be effective against MMR-defective tumors that are refractory to various anticancer agents. C1889 590656 thioredoxin-1 inhibitor PX-12 An orally bioavailable small molecule with potential antineoplastic activity. Thioredoxin-1 inhibitor PX-12 irreversibly binds to thioredoxin-1 (Trx-1) and inhibits its activity, which may result in growth inhibition and the induction of apoptosis. Overexpressed in many cancer cell types, the low molecular weight redox protein Trx-1 regulates transcription factor activity and inhibits apoptosis, promoting cell growth and survival; it also interacts with growth factors extracellularly to stimulate cell growth. C74082 590657 atenolol A synthetic isopropylamino-propanol derivative used as an antihypertensive, hypotensive and antiarrhythmic. Atenolol acts as a peripheral, cardioselective beta blocker specific for beta-1 adrenergic receptors, without intrinsic sympathomimetic effects. It reduces exercise heart rates and delays atrioventricular conduction, with overall oxygen requirements decreasing. 590659 DEPDC1/MPHOSH1 peptide vaccine A cancer vaccine containing HLA-A*2402-restricted epitopes derived from DEP domain containing 1 (DEPDC1) and M phase phosphoprotein 1 (MPHOSPH1) with potential immunostimulatory and antineoplastic activities. Upon administration, DEPDC1/MPHOSH1 peptide vaccine may elicit a specific cytotoxic T lymphocyte (CTL) response against tumor cells expressing DEPDC1 and MPHOSPH1, tumor antigens that are overexpressed in bladder cancer cells.\nHLA-A*2402 is an MHC class I molecule that presents antigenic peptides to CD8+ T cells; epitope design restricted to epitopes that bind most efficiently to HLA-A*2402 may improve antigenic peptide immunogenicity. C74023 590662 belagenpumatucel-L A transforming growth factor beta2 (TGF-beta2) antisense gene-modified allogeneic tumor cell vaccine with potential immunostimulatory and antineoplastic activities. Belagenpumatucel-L is prepared by transfecting allogeneic non-small cell lung cancer (NSCLC) cells with a plasmid containing a TGF-beta2 antisense transgene, expanding the cells, and then irradiating and freezing them. Upon administration, this agent may elicit a cytotoxic T lymphocyte (CTL) response against host NSCLC cells, resulting in decreased tumor cell proliferation; vaccine immunogenicity may be potentiated by suppression of tumor TGF-beta2 production by antisense RNA expressed by the vaccine plasmid TGF-beta2 antisense transgene. Elevated levels of TGF-beta2 are frequently linked to immunosuppression in cancer patients and may be inversely correlated with prognosis in patients with NSCLC. C73438 590687 Src kinase inhibitor KX2-391 An orally bioavailable small molecule Src kinase inhibitor with potential antineoplastic activity. Unlike other Src kinase inhibitors which bind to the ATP-binding site, Src kinase inhibitor KX2-391 specifically binds to the peptide substrate binding site of Src kinase; inhibition of kinase activity may result in the inhibition of primary tumor growth and the suppression of metastasis. Src tyrosine kinases are upregulated in many tumor cells and play important roles in tumor cell proliferation and metastasis. C74077 590705 indium In 111 monoclonal antibody huPAM4 The humanized monoclonal antibody huPAM4, directed against the pancreatic cancer antigen MUC-1 and radiolabled with the gamma-emitting radioisotope indium I 111, with radioisotopic and antibody activities. Upon administration, indium In 111 monoclonal antibody huPAM4 may bind to MUC-1-positive tumor cells, allowing radioimmunolocalization with gamma scintigraphy. Overexpressed by many tumor cell types, MUC-1 antigen, a mammary-type apomucin, is a high-molecular-weight transmembrane glycoprotein. C74048 590709 AML mRNA plus lysate loaded autologous dendritic cell vaccine A cancer vaccine consisting of autologous dendritic cells loaded with separate preparations of acute myelogenous leukemia (AML) cell lysate and AML-specific messenger RNA (mRNA) with potential immunostimulatory and antineoplastic activities. Upon administration, AML mRNA plus lysate loaded autologous dendritic cell vaccine may elicit a potent cytotoxic T-cell (CTL) response against AML cells, resulting in tumor cell death.\nAutologous dendritic cells doubly-loaded with AML cell lysate and AML-specific mRNA may elicit superior primary, recall, and effector lytic immune responses compared to autologous dendritic cells loaded with tumor lysate or tumor mRNA alone. C74000 590711 oncolytic adenovirus Ad5-Delta 24RGD An adenovirus serotype 5 strain, selectively replication competent in cells defective in the Rb/p16 tumor suppressor pathway, with potential oncolytic activity. Oncolytic adenovirus Ad5-Delta 24RGD contains an integrin binding RGD-4C motif, allowing Coxsackie adenovirus receptor-independent infection of tumor cells, which are often deficient for Coxsackie and adenovirus receptors (CARs). Selectively replication competent in cells that are defective in retinoblastoma gene (Rb) or cyclin-dependent kinase inhibitor-2A (p16), active replication of oncolytic adenovirus Ad5-Delta 24RGD in tumor cells may induce oncolysis or cell lysis. As integral components of the late G1 restriction point, the Rb gene product and p16 are negative regulators of the cell cycle; ovarian cancer cells and non-small cell lung cancer cells may be defective in the Rb/p16 pathway. C74067 590712 Hsp90 inhibitor SNX-5422 mesylate The orally bioavailable mesylate salt of a synthetic prodrug targeting the human heat-shock protein 90 (Hsp90) with potential antineoplastic activity. Although the mechanism of action remains to be fully elucidated, Hsp90 inhibitor SNX-5542 is rapidly converted to SNX-2112, which accumulates in tumors relative to normal tissues. SNX-2112 inhibits Hsp90, which may result in the proteasomal degradation of oncogenic client proteins, including HER2/ERBB2, and the inhibition of tumor cell proliferation. Hsp90 is a molecular chaperone that plays a key role in the conformational maturation of oncogenic signaling proteins, such as HER2/ERBB2, AKT, RAF1, BCR-ABL, and mutated p53, as well as many other molecules that are important in cell cycle regulation or immune responses. C74040 590716 URLC10-TTK-KOC1-VEGFR1-VEGFR2 multipeptide vaccine A cancer vaccine containing five peptide epitopes with potential immunostimulatory and antitumor activity. Peptide epitopes in this vaccine are derived from: URLC10 (up-regulated lung cancer 10), TTK (TTK protein kinase), KOC1 (IGF II mRNA Binding Protein 3) and VEGFRs (vascular endothelial growth factor receptors) 1 and 2. Upon administration, URLC10-TTK-KOC1-VEGFR1-VEGFR2 multipeptide vaccine may stimulate a cytotoxic T lymphocyte (CTL) response against tumor cells expressing URLC10, TTK, KCO1, VEGFR 1 and 2 peptides, resulting in cell lysis and decreased tumor growth. C74088 592353 rexinoid NRX194204 An orally bioavailable synthetic retinoid X receptor (RXR) agonist with potential antineoplastic and anti-inflammatory activities. Rexinoid NRX 194204 selectively binds to and activates RXRs. Because RXRs can form heterodimers with several nuclear receptors (NRs), RXR activation by this agent may result in a broad range of gene expression depending on the effector DNA response elements activated. Rexinoid NRX 194204 may inhibit the tumor-necrosis factor (TNF)-mediated release of nitric oxide (NO) and interleukin 6 (IL6) and may inhibit tumor cell proliferation. This agent appears to be less toxic than RAR-selective ligands. C74076 592508 apatinib An orally bioavailable, small-molecule receptor tyrosine kinase inhibitor with potential antiangiogenic and antineoplastic activities. Apatinib selectively binds to and inhibits vascular endothelial growth factor receptor 2, which may inhibit VEGF-stimulated endothelial cell migration and proliferation and decrease tumor microvessel density. In addition, this agent mildly inhibits c-Kit and c-SRC tyrosine kinases. C74012 592510 TLR9 agonist IMO-2055 A synthetic oligonucleotide containing unmethylated CpG dinucleotides with potential immunopotentiating activity. Mimicking unmethylated CpG sequences in bacterial DNA, TLR9 agonist IMO-2055 binds to and activates intracellular Toll-like receptors (TLR) 9 in monocytes/macrophages, plasmacytoid dendritic cells (DCs) and B cells, initiating immune signaling pathways and activating B cells and DCs and inducing T-helper cell cytokine production. TLR9 is a member of the TLR family, which plays a fundamental role in pathogen recognition and activation of innate immunity. C74083 592511 HLA-A*2402-restricted URLC10-TTK-VEGFR1-VEGFR2 multipeptide vaccine A cancer vacine containing four HLA-A*2402-restricted peptide epitopes with potential immunostimulatory and antitumor activities. Peptide epitopes in this vaccine are derived from: URLC10 (up-regulated lung cancer 10), TTK (TTK protein kinase), and VEGFRs (vascular endothelial growth factor receptors) 1 and 2. Upon administration, URLC10-TTK-KOC1-VEGFR1-VEGFR2 multipeptide vaccine may stimulate a cytotoxic T lymphocyte (CTL) response against tumor cells expressing URLC10, TTK, VEGFR 1 and 2 peptides, resulting in cell lysis and decreased tumor growth. HLA-A*2402 is an MHC class I molecule that presents antigenic peptides to CD8+ T cells; epitope design restricted to epitopes that bind most efficiently to HLA-A*2402 may improve antigenic peptide immunogenicity. C74039 592567 yttrium Y 90 anti-CD19 monoclonal antibody BU12 A radioimmunoconjugate consisting of the murine IgG1 anti-CD19 monoclonal antibody (MoAb) BU12 labeled with the beta-emitting radioisotope yttrium Y 90 with radioisotopic and antibody activities. Yttrium Y 90 anti-CD19 monoclonal antibody BU12 binds to the CD19 molecule, specifically delivering cytotoxic beta radiation to CD19-expressing B cells. CD19 is a membrane antigen that is widely expressed during B-cell development, from pro-B-cell to early plasma cell stages. C74092 592693 yttrium Y 90 DOTA anti-CEA monoclonal antibody M5A A radioimmunoconjugate consisting of a monoclonal antibody directed against the human carcinoembryonic antigen (CEA) conjugated with the radioisotope yttrium 90 (Y-90) via the chelator tetra-azacyclododecanetetra-acetic acid (DOTA) with potential antineoplastic activity. The antibody moiety of yttrium Y 90 DOTA anti-CEA monoclonal antibody M5A binds to cells expressing the CEA antigen. Upon cellular internalization, this agent selectively delivers a cytotoxic dose of beta radiation. CEA, a tumor associated antigen, is overexpressed in many cancer types, including gastrointestinal, breast, non-small cell lung, and thyroid cancers. C77853 592860 yttrium Y 90 anti-CEA monoclonal antibody cT84.66 A radioimmunoconjugate comprised of a chimeric monoclonal antibody against human carcinoembryonic antigen (CEA) conjugated with the radioisotope yttrium 90 (Y-90) via the chelator tetra-azacyclododecanetetra-acetic acid (DOTA) with potential antineoplastic activity. The antibody moiety of yttrium Y90 DOTA anti-CEA monoclonal antibody cT84.66 binds to cells expressing the CEA antigen. Upon cellular internalization, this agent selectively delivers a cytotoxic dose of beta radiation. CEA, a tumor associated antigen, is overexpressed in many cancer types, including gastrointestinal, breast, non-small cell lung, and thyroid cancers. C77885 592863 anti-EpCAM/anti-CD3 recombinant bispecific monoclonal antibody MT110 A recombinant bispecific monoclonal antibody directed against both CD3 and epithelial cell adhesion molecule (EpCAM) with potential immunomodulating and antineoplastic activities. Anti-EpCAM/anti-CD3 recombinant bispecific monoclonal antibody MT110 attaches to both CD3-expressing T lymphocytes and EpCAM-expressing tumor cells, thereby selectively cross-linking tumor and T lymphocytes; this may result in the recruitment of cytotoxic T lymphocytes (CTL) to T lymphocyte/tumor cell aggregates and the CTL-mediated death of EpCAM-expressing tumor cells. CD3 is an antigen expressed on mature T cells; EpCAM, a cell surface protein, is expressed by a variety of tumor cells and is frequently found in head and neck cancers. C77854 592881 iodine I 123 anti-CEA recombinant diabody T84.66 A radioimmunoconjugate comprised of a recombinant scFv dimer diabody of a monoclonal antibody against human carcinoembryonic antigen (CEA) labeled with iodine I 123 (I-123) with potential radioimmunolocalization applications. The antibody moiety of iodine I 123 anti-CEA recombinant diabody T84.66 binds to cells expressing CEA, selectively delivering I-123 upon cellular internalization and allowing the scintigraphic imaging of CEA-expressing tumor cells. CEA, a tumor associated antigen, is overexpressed in many cancer types, including gastrointestinal, breast, non-small cell lung, and thyroid cancers. Compared to whole monoclonal antibodies, diabody fragments offer the advantages of rapid tumor targeting, rapid blood clearance, more uniform tumor distribution, and a lower potential for eliciting an immune response. C77911 592901 enteric-coated zoledronic acid tablet MER-101 An oral tablet formulation containing zoledronic acid combined with a proprietary absorption enhancer for improved zoledronic acid gastrointestinal absorption with anti-bone-resorption activity. The third-generation bisphosphonate zoledronic acid binds to hydroxyapatite crystals in the bone matrix, slowing their dissolution and inhibiting the formation and aggregation of these crystals. This agent also inhibits farnesyl pyrophosphate synthase, an enzyme involved in terpenoid biosynthesis. Inhibition of this enzyme prevents the biosynthesis of isoprenoid lipids, donor substrates of farnesylation and geranylgeranylation during the post-translational modification of small GTPase signalling proteins, which are important in the process of osteoclast turnover. The proprietary absorption enhancer is a GRAS (generally-recognized-as-safe) food additive. C77855 592962 anti-CD30 monoclonal antibody MDX-1401 A fully human, second-generation, nonfucosylated monoclonal antibody directed against the cell surface receptor CD30 with potential immunomodulating and antineoplastic activities. Anti-CD30 monoclonal antibody MDX-1401 specifically binds to the CD30 antigen, which may result in a cytotoxic T lymphocyte (CTL) response against CD30-expressing tumor cells. CD30, a member of the tumor necrosis factor (TNF) receptor superfamily, is expressed on activated lymphocytes transiently and is constitutively expressed in hematologic malignancies including Hodgkin's disease and some T-cell non-Hodgkin's lymphomas. Compared to conventional antibodies, deletion of fucose molecules on the antibody backbone, as is done in MDX-1401, may result in an increased affinity for Fc receptors and an enhanced antibody-dependent cellular cytotoxicity (ADCC). C77886 593099 erbB kinase inhibitor AZD8931 An erbB receptor tyrosine kinase inhibitor with potential antineoplastic activity. erbB kinase inhibitor AZD8931 binds to and inhibits erbB tyrosine receptor kinases, which may result in the inhibition of cellular proliferation and angiogenesis in tumors expressing erbB. The erbB protein family, also called the epidermal growth factor receptor (EGFR) family, plays major roles in tumor cell proliferation and tumor vascularization. C77887 593257 aerosol sargramostim An aerosol inhalation formulation containing a yeast-derived glycosylated recombinant form of human granulocyte macrophage colony stimulating factor (GM-CSF) with potential immunostimulating activity. Sargramostim binds to specific cell surface receptors, modulating the proliferation and differentiation of a variety of hematopoietic progenitor cells with some specificity towards stimulation of leukocyte production. This agent also activates neutrophils, monocytes, macrophages, and dendritic cells and promotes antigen presentation, upregulates antibody-dependent cellular cytotoxicity (ADCC), and increases interleukin-2-mediated, lymphokine-activated killer cell function. Aerosol inhalation may help achieve high concentrations of sargramostim in the lung. C77915 593430 tyroserleutide A tripeptide consisting of tyrosine, serine, and leucine with potential antineoplastic activity. Although the mechanism of its antitumor activity has yet to be fully elucidated, tyroserleutide appears to inhibit the expression of ICAM-1 (CD54), a cell adhesion factor of the immunoglobulin (Ig) superfamily that plays an important role in the invasion, adhesion, and metastasis of tumor cells. In addition, this agent may influence the Ca2+/calmodulin pathway, inhibiting phosphatidylinositol 3 kinase (PI3K); PI3K is upregulated in tumor cells and is involved in cellular proliferation. C77856 593437 oral JAK inhibitor INCB18424 An orally bioavailable Janus-associated kinase (JAK) inhibitor with potential antineoplastic and immunomodulating activities. Oral JAK inhibitor INCB18424 specifically binds to and inhibits protein tyrosine kinases JAK 1 and 2, which may lead to a reduction in inflammation and an inhibition of cellular proliferation. The JAK-STAT (signal transducer and activator of transcription) pathway plays a key role in the signaling of many cytokines and growth factors and is involved in cellular proliferation, growth, hematopoiesis, and the immune response; JAK kinases may be upregulated in inflammatory diseases, myeloproliferative disorders, and various malignancies. C77888 593502 montelukast sodium The orally bioavailable monosodium salt of montelukast, a selective cysteinyl leukotriene receptor antagonist with anti-inflammatory and bronchodilating activities. Montelukast selectively and competitively blocks the cysteinyl leukotriene 1 (CysLT1) receptor, preventing binding of the inflammatory mediator leukotriene D4 (LTD4). Inhibition of LTD4 activity results in inhibition of leukotriene-mediated inflammatory events including: migration of eosinophils and neutrophils; adhesion of leukocytes to vascular endothelium, monocyte and neutrophil aggregation; increased airway edema; increased capillary permeability; and bronchoconstriction. The CysLT1 receptor is found in a number of tissues including spleen, lung, placenta, small intestine, and nasal mucosa, and in a variety of cell types including monocyte/macrophages, mast cells, eosinophils,\n CD34-positive hemopoietic progenitor cells,\nneutrophils and endothelial cells. C47625 593616 sodium glycididazole The sodium salt of glycididazole with potential radiosensitizing activity. Due to its low redox potential, glycididazole is selectively activated via bioreduction in hypoxic tumor cells and may sensitize hypoxic tumor cells to the cytotoxic effects of ionizing radiation. C77889 593641 metformin hydrochloride The hydrochloride salt of the biguanide metformin with antihyperglycemic activity. Metformin decreases hepatic gluconeogenesis and intestinal absorption of glucose. This agent also increases the number and/or affinity of insulin receptors on muscle and adipose cells, increasing the sensitivity to insulin at receptor and post-receptor binding sites and increasing glucose uptake peripherally. 593681 B7-DC cross-linking antibody rHIgM12B7 A recombinant form of the monoclonal IgM antibody M12 isolated from a Waldenstrom macroglobulinaemia patient (rHIgM12) with potential immunomodulating activity. B7-DC cross-linking antibody rHIgM12B7 binds and crosslinks the B7 co-stimulatory family member B7-DC (PD-L2) on dendritic cells (DCs), antigen presenting cells (APCs) that play a crucial role in the human immune response. This results in enhanced activation of DCs; enhanced antigen-presenting activity; and increased production of immunomodulatory cytokines (especially interleukin 12); and may potentiate a specific cytotoxic T lymphocyte (CTL) response against Waldenstrom macroglobulinaemia B cells. C77857 593687 50% oxygen/50% nitrous oxide premix An equimolar gas mixture of oxygen (O2) and nitrous oxide (N2O) with potential analgesic activity. Upon inhalation, 50% oxygen/50% nitrous oxide premix produces rapidly reversible analgesia. The exact mechanism through which nitrous oxide exerts its analgesic effect has yet to be fully elucidated, but it appears to be associated with the neuronal release of endogenous opioid peptides. C77890 593933 anti-CD200 monoclonal antibody ALXN6000 A humanized monoclonal antibody directed against the human immunosuppressive molecule CD200 (OX-2) with potential immunomodulating and antineoplastic activities. Anti-CD200 monoclonal antibody ALXN6000 binds to CD200, blocking the binding of CD200 to its receptor, CD200R, present on cells of the macrophage lineage; inhibition of CD200 may augment the cytotoxic T-lymphocyte (CTL) mediated immune response against CD200-expressing tumor cells. CD200 is a type 1a transmembrane protein, related to the B7 family of co-stimulatory receptors, and is upregulated on the surface of multiple hematologic malignant cells; this transmembrane protein appears to be involved in the downregulation of a Th1 (helper T cell) immune response. C77891 593942 human monoclonal antibody B11-hCG beta fusion protein CDX-1307 A human monoclonal antibody (B11) directed against the mannose receptor and linked to the beta-subunit of human chorionic gonadotropin (hCG beta) with potential immunostimulating and antineoplastic activities. The monoclonal antibody moiety of human monoclonal antibody B11-hCG beta fusion protein CDX-1307 binds to mannose receptors on antigen presenting cells (APCs), including human dendritic cells (DCs) and macrophages. Upon internalization and processing, APCs present the processed hCG beta antigen on their cell surfaces, which may initiate an antibody-dependent cell-mediated cytotoxicity (ADCC) response against hCG beta-expressing tumor cells.\n The tumor-associated antigen (TAA) hCG beta is selectively overexpressed by a number of tumors including breast, colorectal, pancreatic, bladder and ovarian tumors; its expression may correlate with the stage of disease. C77858 594152 epothilone KOS-1584 A second-generation epothilone with potential antineoplastic activity. Epothilone KOS-1584 binds to tubulin and induces microtubule polymerization and stabilizes microtubules against depolymerization, which may result in the inhibition of cell division, the induction of G2/M arrest, and apoptosis. Compared to first-generation epothilones, this agent exhibits greater safety and efficacy with an enhanced pharmaceutical profile, including enhanced water solubility and tumor penetration, and reduced CNS exposure. In addition, epothilone KOS-1584 is a poor substrate for the P-glycoprotein (P-gp) drug efflux pump. C77892 594157 c-Met inhibitor JNJ-38877605 An orally bioavailable, small-molecule receptor tyrosine kinase inhibitor with potential antineoplastic activity. c-Met inhibitor JNJ-38877605 selectively inhibits c-Met (mesenchymal-epithelial transition), a receptor tyrosine kinase (RTK) involved in cancer cell survival and invasiveness, and tumor angiogenesis.\nc-Met is also known as hepatocyte growth factor receptor (HGFR). C77893 594363 apricoxib An orally bioavailable nonsteroidal anti-inflammatory agent (NSAID) with potential antiangiogenic and antineoplastic activities. Apricoxib binds to and inhibits the enzyme cyclooxygenase-2 (COX-2), thereby inhibiting the conversion of arachidonic acid into prostaglandins. Apricoxib-mediated inhibition of COX-2 may induce tumor cell apoptosis and inhibit tumor cell proliferation and tumor angiogenesis. COX-related metabolic pathways may represent crucial regulators of cellular proliferation and angiogenesis. C74021 594364 VEGFR1-1084 peptide vaccine A peptide vaccine containing an HLA-A*2402-restricted epitope of vascular endothelial growth factor receptor 1 (VEGFR1 or Flt-1) with potential immunostimulating, antiangiogenic, and antineoplastic activities. Upon vaccination, VEGFR1-1084 peptide vaccine may stimulate a cytotoxic T lymphocyte (CTL) response against VEGFR1-expressing endothelial cells of the tumor microvasculature, which may inhibit tumor angiogenesis and tumor cell proliferation. VEGFR1, a receptor tyrosine kinase, may be overexpressed on endothelial cells of the tumor microvasculature and is associated with tumor cell proliferation, invasion and tumor angiogenesis. HLA-A*2402 is an MHC class I molecule that presents antigenic peptides to CD8+ T cells; epitope design restricted to epitopes that bind most efficiently to HLA-A*2402 may improve antigenicity. C77895 594366 ErbB-2 inhibitor ARRY-380 An orally bioavailable inhibitor of the human epidermal growth factor receptor tyrosine kinase ErbB-2 (also called HER2) with potential antineoplastic activity. ErbB-2 inhibitor ARRY-380 selectively binds to and inhibits the phosphorylation of ErbB-2, which may prevent the activation of ErbB-2 signal transduction pathways, resulting in growth inhibition and death of ErbB-2-expressing tumor cells.\nErbB-2 is overexpressed in a variety of cancers and plays an important role in cellular proliferation and differentiation. C77896 594403 Coriolus versicolor extract An extract derived from the mushroom Coriolus versicolor, containing polysaccharide K (PSK) and polysaccharide-peptide (PSP), with potential immunomodulating and antineoplastic activities. Coriolus versicolor extract has been shown to stimulate the production of lymphocytes and cytokines, such as interferons and interleukins, and may exhibit antioxidant activities. However, the precise mechanism of action(s) of this agent is unknown. C78184 594404 sodium ferric gluconate complex in sucrose A compound containing elemental iron as the sodium salt of a ferric ion carbohydrate complex in an alkaline aqueous solution with approximately 20% sucrose w/v in water for injection, used to replete the total body content of iron. Iron is critical for normal hemoglobin and myoglobin syntheses to maintain\noxygen transport and various enzymatic processes, including the biosynthesis of deoxyribonucleotides catalyzed by ribonucleotide reductase (RNR). C78185 594405 PARP1 inhibitor PF-01367338 A tricyclic indole poly(ADP-Ribose) polymerase (PARP1) inhibitor with potential chemosensitizing, radiosensitizing, and antineoplastic activities. PARP-1 inhibitor PF-01367338 selectively binds to PARP1 and inhibits PARP1-mediated DNA repair, thereby enhancing the accumulation of DNA strand breaks and promoting genomic instability and apoptosis. This may enhance the cytotoxicity of DNA-damaging agents and reverse tumor cell resistance to chemotherapy and radiation therapy. PARP1 catalyzes post-translational ADP-ribosylation of nuclear proteins and is activated by single-strand DNA (ssDNA) breaks. C78186 594769 anti-CD70 monoclonal antibody MDX-1411 A glycoengineered, fully humanized IgG1 monoclonal antibody directed against the extracellular domain of the human CD70 molecule with potential antineoplastic activity. Anti-CD70 fully human monoclonal antibody MDX-1411 selectivity binds to the extracellular domain of CD70, which may induce an antibody-dependent cellular cytotoxicity (ADCC) response against CD70-expressing tumor cells. CD70, the ligand for the costimulatory receptor CD27 and a member of the tumor necrosis factor (TNF) family, is found on renal cell carcinoma (RCC) cells among other cancer cell types. C78187 594770 ribosome-inactivating protein CY503 A recombinant protein that inactivates the ribosome with potential antineoplastic and immunomodulating activities. Ribosome-inactivating protein CY503 binds to the cell surface sialyltransferase CD75 and is internalized; intracellularly, CY503 cleaves an adenine-specific N-glycosidic bond on the 28S ribosomal subunit, which may result in tumor cell apoptosis. This agent has also been shown to activate natural killer (NK) cells, induce cytokine receptor expression, and stimulate the release of cytokines. CD75 is expressed on mature B-cells and subsets of T-cells and erythrocytes. C78188 594863 Aurora A kinase/tyrosine kinase inhibitor ENMD-2076 An orally bioavailable synthetic small molecule with potential antiangiogenic and antineoplastic activities. Aurora A kinase/tyrosine kinase inhibitor ENMD-2076 selectively binds to and inhibits non-specified tyrosine kinases and Aurora kinases (AKs). The inhibition of AKs may result in the inhibition of cell division and proliferation and may induce apoptosis in tumor cells that overexpress AKs; antiangiogenic activity is related to the inhibition of angiogenic tyrosine kinases. AKs are serine-threonine kinases that play an essential role in mitotic checkpoint control during mitosis and are important regulators of cell division and proliferation. C78190 594869 R-(-)-gossypol acetic acid The orally bioavailable solvate of the R-(-) enantiomer of gossypol and acetic acid with potential antineoplastic activity. As a BH3 mimetic, R-(-)-gossypol binds to the hydrophobic surface binding groove BH3 of the anti-apoptotic proteins Bcl-2 and Bcl-xL, blocking their heterodimerization with pro-apoptotic members of the Bcl-2 family of proteins such as Bad, Bid, and Bim; this may result in the inhibition of tumor cell proliferation and the induction of tumor cell apoptosis. Racemic gossypol is a polyphenolic compound isolated from cottonseed. C78348 594943 riluzole A benzothiazole derivative with neuroprotective and potential anti-depressant and anxiolytic activities. While the mechanism of action of riluzole is unknown, its pharmacological activities in motor neurons include the following, some of which may be related to its effect: 1) an inhibitory effect on glutamate release, 2) inactivation of voltage-dependent sodium channels, and 3) interference with intracellular events that follow transmitter binding at excitatory amino acid receptors.\nIn animal models, this agent has been shown to exhibit myorelaxant and sedative activities, apparently due to the blockade of glutamatergic neurotransmission. C47704 595043 autologous dinitrophenyl-modified ovarian cancer vaccine A cancer vaccine consisting of autologous ovarian cancer cell peptide antigens conjugated to the hapten 2,4-dinitrophenol (DNP) with potential immunostimulating and antineoplastic activities. Administration of autologous dinitrophenyl-modified ovarian cancer vaccine may induce a cytotoxic T-lymphocyte (CTL) response against ovarian cancer cells. DNP conjugation may enhance the immunogenicity of weakly immunogenic antigens. C78193 595060 multitargeted tyrosine kinase inhibitor AP24534 An orally bioavailable multitargeted receptor tyrosine kinase (RTK) inhibitor with potential antiangiogenic and antineoplastic activities. Multitargeted tyrosine kinase inhibitor AP24534 inhibits unmutated and all mutated forms of Bcr-Abl, including T315I, the highly drug therapy-resistant missense mutation of Bcr-Abl. This agent also inhibits other tyrosine kinases including those associated with vascular endothelial growth factor receptors (VEGFRs) and fibroblast growth factor receptors (FGFRs); in addition, it inhibits the tyrosine kinase receptor TIE2 and FMS-related tyrosine kinase receptor-3 (Flt3). RTK inhibition by AP24534 may result in the inhibition of cellular proliferation and angiogenesis and may induce cell death. Bcr-Abl is a fusion tyrosine kinase encoded by the Philadelphia chromosome. C78194 595131 8-hydroxyquinoline sulfate ointment An ointment formulation containing the sulfate salt of 8-hydroxyquinoline in a petrolatum and lanolin base with skin-protecting activity. Upon topical application, 8-hydroxyquinoline sulfate exhibits antiseptic activity while lanolin moisturizes and softens skin. C78202 595163 sonepcizumab A humanized monoclonal antibody directed against sphingosine 1-phosphate (S1P) with potential antiangiogenic and antineoplastic activities. Upon administration, sonepcizumab binds S1P, which may result in the inhibition of tumor angiogenesis. S1P is the extracellular ligand for the G protein-coupled lysophospholipid receptor EDG-1 (endothelial differentiation gene-1). C78195 595181 5-[18F]fluorouracil The fluorine-18 (18F)-radiolabeled pyrimidine analog 5-fluorouracil (5-FU) with positron-emitting activity. Upon administration, 5-[18F]fluorouracil distribution in tumor tissue may be measured with positron emission tomography (PET). The degree of 5-[18F]fluorouracil uptake in tumor tissue may help to predict the response to 5-fluorouracil-based chemotherapy or to determine the response to other therapeutic agents used to treat 5-FU-sensitive tumors. C78203 595192 regorafenib An orally bioavailable small molecule with potential antiangiogenic and antineoplastic activities. Regorafenib binds to and inhibits vascular endothelial growth factor receptors (VEGFRs) 2 and 3, and Ret, Kit, PDGFR and Raf kinases, which may result in the inhibition of tumor angiogenesis and tumor cell proliferation. VEGFRs are receptor tyrosine kinases that play important roles in tumor angiogenesis; the receptor tyrosine kinases RET, KIT, and PDGFR, and the serine/threonine-specific Raf kinase are involved in tumor cell signaling. C78204 595290 docetaxel emulsion ANX-514 An injectable emulsion formulation containing the taxane docetaxel, a semisynthetic analogue of paclitaxel, with antineoplastic activity. Docetaxel binds specifically to the beta-tubulin subunit of the microtubule, stabilizing tubulin and inhibiting microtubule disassembly, which results in cell-cycle arrest at the G2/M phase and cell death. This agent also inhibits pro-angiogenic factors such as vascular endothelial growth factor (VEGF) and induces various mediators of the inflammatory response. Docetaxel emulsion ANX-514 is formulated without polysorbate 80 or other detergents in order to reduce the incidence and severity of hypersensitivity reactions. In addition, the exclusion of polysorbate 80 in this formulation precludes foaming during the preparation process, thus facilitating preparation and administration. C78196 595296 autologous anti-PSMA gene-modified T-cells Autologous prostate specific membrane antigen (PSMA) gene-modified T lymphocytes with potential antineoplastic activity. Human autologous T-lymphocytes are isolated and transduced ex vivo with a retrovirus encoding a chimeric immune receptor (CIR) consisting of an antibody fragment against PSMA fused with signaling domains of the T cell. Upon reintroduction into the patient, autologous anti-PSMA gene-modified T-cells bind to PSMA-expressing prostate cancer cells, which may result in specific cytotoxic T-lymphocyte (CTL) tumor cell killing. C78197 595298 SC-PEG E. coli L-asparaginase An intravenous formulation containing E. coli-derived L-asparaginase II conjugated with succinimidyl carbonate monomethoxypolyethylene glycol (SC-PEG), with potential antineoplastic activity. L-asparaginase hydrolyzes L-asparagine to L-aspartic acid and ammonia, thereby depleting cells of asparagine; asparagine depletion blocks protein synthesis and tumor cell proliferation, especially in the G1 phase of the cell cycle and ultimately induces tumor cell death. Asparagine is critical to protein synthesis in acute lymphoblastic leukemia (ALL) cells which, unlike normal cells, cannot synthesize this amino acid due to the absence of the enzyme asparagine synthase. Pegylation decreases enzyme antigenicity and increases its half life. SC is used as a PEG linker to facilitate attachment to asparaginase and enhances the stability of the formulation. C78198 595342 allogeneic LMP1-/LMP2- specific cytotoxic T-lymphocytes A preparation of cytotoxic T-lymphocytes (CTL), specifically reactive to the Epstein-Barr virus (EBV) latent membrane proteins (LMP) 1 and 2, with potential antineoplastic activity. Peripheral blood mononuclear cells (PBMC) are collected from a donor and are exposed ex vivo to dendritic cells (DCs) transfected with a replication-deficient adenovirus encoding EBV LMP1/2 to generate LMP1/2-specific CTL which are subsequently expanded. Administration of allogeneic LMP1-/LMP2- specific CTL to patients with LMP1/2-positive tumors may result in a specific CTL response against tumor cells expressing LMP1 and LMP2, resulting in cell lysis and inhibition of tumor cell proliferation. As tumor associated antigens (TAAs), LMP1 and LMP2 are expressed in various malignancies including nasopharyngeal cancer and EBV-positive Hodgkin lymphoma. C78201 595536 FAK inhibitor PF-00562271 An orally bioavailable small molecule and ATP-competitive focal adhesion kinase (FAK) inhibitor with potential antineoplastic and antiangiogenic activities. FAK inhibitor PF-00562271 inhibits the tyrosine kinase FAK, and to a lesser extent, proline-rich tyrosine kinase (PYK2), which may inhibit tumor cell migration, proliferation, and survival.\n As FAK is a signal transducer for integrins, inhibition of FAK by this agent may prevent integrin-mediated activation of several downstream signals including ERK, JNK/MAPK and PI3K/Akt. FAK and PYK2, upregulated in many tumor cell types, are involved in tumor cell invasion, migration and proliferation. C78199 595679 alpha-Gal glycosphingolipids A preparation of glycosphingolipids (GSL), containing the disaccharide epitope galactose-alpha-1,3-galactose (alpha-Gal), with potential antineoplastic activity. Upon intratumoral injection, alpha-Gal glycosphingolipids may stimulate the immune system to mount complement-mediated cytotoxicity (CMC) and antibody-dependent cell-mediated cytotoxicity (ADCC) responses against alpha-Gal GSL, which may result in tumor cell death; these responses involve natural anti-alpha-Gal immunoglobulins (Igs). As antibodies that occur naturally due to sensitization to alpha-Gal present on symbiotic bacterial flora, anti-alpha-Gal Igs are present in unusually high amounts in human sera. GSL represent a glycolipid subtype containing the amino alcohol sphingosine; tumor-associated GSL antigens contain various oligosaccharide residues. C78200 595701 TGF-beta-resistant LMP-specific cytotoxic T-lymphocytes A preparation of transforming growth factor-beta (TGF-beta)-resistant cytotoxic T-lymphocytes (CTL) reactive to Epstein-Barr virus (EBV) latent membrane proteins 1 and 2 (LMP 1 and 2) with potential antineoplastic activity. T lymphocytes are transduced with a retroviral vector expressing the dominant-negative mutant type II TGF-beta receptor, which blocks signaling by all three TGF-beta isoforms. These TGF-beta-resistant T-lymphocytes are exposed ex-vivo to dendritic cells (DCs) transfected with a replication-deficient adenovirus encoding EBV LMP; subsequent exposure to LMP1- or LMP2-expressing lymphoblastoid cell lines is used to expand the CTL. Administered to patients with EBV-positive tumors, TGF-beta-resistant LMP-specific CTL target LMP-positive cells, which may result in a specific CTL response, followed by cell lysis and inhibition of tumor cell proliferation. Tumor-expressed TGF-beta inhibits T lymphocyte activation and expansion. C77859 596155 cholecalciferol/d-alpha tocopherol/L-selenomethionine/green tea extract/saw palmetto berry extract/daidzein/genistein/lycopene prostate health supplement A dietary supplement consisting of a blend of 8 natural ingredients with potential antineoplastic and chemopreventive activities. This dietary supplement contains vitamin D3 (as cholecalciferol), vitamin E (as d-alpha tocopherol), selenium (as L-selenomethionine), epigallocatechin (green tea extract), saw palmetto (berry extract), lycopene, and the isoflavonoids daidzein and genistein. This combination preparation may decrease prostate cell growth and inhibit prostate carcinogenesis. C77860 596304 SMO antagonist BMS 833923 An orally bioavailable small-molecule SMO (Smoothened) inhibitor with potential antineoplastic activity. SMO antagonist BMS-833923 inhibits the sonic hedgehog (SHH) pathway protein SMO, which may result in a suppression of the SHH signaling pathway. SMO is a G-protein coupled receptor that lies just downstream of the SHH ligand cell surface receptor Patched-1 in the SHH pathway; in the absence of ligand Patched-1 inhibits SMO and ligand binding to Patched-1 results in increased levels of SMO. The SHH signaling pathway plays an important role in cellular growth, differentiation and repair; constitutive activation of this pathway is associated with uncontrolled cellular proliferation and has been observed in a variety of cancers. C77861 596456 99mTc-DTPA-mannosyl-dextran A radiolabeled macromolecule consisting of the chelating agent diethylenetriamine pentaacetic acid (DTPA) and mannose each attached to a dextran backbone and labeled with metastable technetiumTc-99 (Tc-99m), with mannose binding and radioisotopic activities. Upon injection, the mannose moiety of 99mTc-DTPA-mannosyl-dextran binds to mannose-binding protein (MBP). As MBPs reside on the surface of dendritic cells and macrophages, this gamma-emitting macromolecule tends to accumulate in lymphatic tissue where it may be imaged using gamma scintigraphy. This agent exhibits rapid clearance from the injection site, rapid uptake and high retention within the first draining lymph node, and low uptake by the remaining lymph nodes. MBP is a C-type lectin that binds mannose or fucose carbohydrate residues, such as those found on the surfaces of many pathiogens, and once bound activates the complement system. C77898 596487 mangafodipir trisodium The trisodium salt of mangafodipir with potential antioxidant and chemoprotective activities. Consisting of manganese (II) ions chelated to fodipir (dipyridoxyl diphosphate or DPDP), mangafodipir scavenges oxygen free radicals such as superoxide anion, hydrogen peroxide, and hydroxyl radical, potentially preventing oxygen free radical damage to macromolecules such as DNA and minimizing oxygen free radical-related chemotoxicity in normal tissues. However, this agent may potentiate the chemotherapy-induced generation of oxygen free radicals in tumor cells, resulting in the potentiation of chemotherapy-induced cytotoxicity; tumor cells, with higher levels of reactive oxygen species than normal cells, possess a lower threshold for oxygen free radical-mediated cytotoxicity. Mangafodipir is traditionally used as an imaging agent in magnetic resonance imaging (MRI). C66053 596513 natalizumab A humanized recombinant IgG4 monoclonal antibody directed against the alpha4 subunit of the integrins alpha4beta1 and alpha4beta7 with immunomodulating, anti-inflammatory, and potential antineoplastic activities. Natalizumab binds to the apha4-subunit of alpha4beta1 and alpha4beta7 integrins expressed on the surface of all leukocytes except neutrophils, inhibiting the alpha4-mediated adhesion of leukocytes to counter-receptor(s) such as vascular cell adhesion molecule-1 (VCAM-1); natalizumab –mediated disruption of VCAM-1 binding by these integrins may prevent the transmigration of leukocytes across the endothelium into inflamed parenchymal tissue. Integrins are cellular adhesion molecules (CAMs) that are upregulated in various types of cancer and some autoimmune diseases; alpha4beta1 integrin (VLA4) has been implicated in the survival of myeloma cells, possibly by mediating their adhesion to stromal cells. C77862 596530 retinoid analogue NRX 195183 An orally bioavailable retinoid acid receptor (RAR) alpha agonist with potential antineoplastic activity. Retinoid analogue NRX 195183 binds to and activates RAR alpha, modulating the transcription of genes responsible for cell differentiation and proliferation, which may result in cell differentiation, decreased cell proliferation, and the inhibition of tumorigenesis. Encoded by the RARA gene, RAR alpha is a nuclear receptor and a member of the steroid receptor superfamily. C77899 596541 IMT-1012 immunotherapeutic vaccine A multi-peptide cancer vaccine with potential immunostimulating and antineoplastic activities. IMT-1012 immunotherapeutic vaccine contains twelve different synthetic peptides or tumor associated antigens (TAAs), including cyclin I (CCNI), cyclin-dependent kinase CDC2, EDDRI and TACE/ADAM17, each of which is involved in a different pathway associated with tumor growth, survival, and metastasis. Each antigen in the vaccine elicits a specific cytotoxic T-lymphocyte (CTL) immune response against tumor cells expressing that antigen. This multi-antigen/multi-pathway targeting strategy provides broad immunotherapeutic coverage with respect to tumor complexity and heterogeneity and may result in enhanced vaccine efficacy. C77863 596550 DM4-conjugated anti-Cripto monoclonal antibody BIIB015 A humanized IgG1 monoclonal antibody directed against the cell surface-associated protein Cripto and conjugated to the maytansinoid DM4 with potential antineoplastic activity. The monoclonal antibody moiety of DM4-conjugated anti-Cripto monoclonal antibody BIIB015 binds to the tumor associated antigen (TAA) Cripto; upon internalization, the DM4 moiety binds to tubulin and disrupts microtubule assembly/disassembly dynamics, resulting in inhibition of cell division and cell growth of Cripto-expressing tumor cells. Constitutively expressed during embryogenesis, Cripto belongs to the EGF-CFC family of \ngrowth factor-like molecules and plays a key role in signaling pathways of certain transforming growth factor-beta superfamily members; as a TAA, Cripto is overexpressed in carcinomas such as those of the breast, ovary, stomach, lung, and pancreas while its expression is absent in normal tissues. C77864 596649 HLA-A*0201-restricted URLC10-VEGFR1-VEGFR2 multipeptide vaccine A cancer vaccine containing three HLA-A*2402-restricted peptide epitopes with potential immunostimulatory, antiangiogenic, and antitumor activities. Vaccine peptide epitopes are derived from the tumor associated antigen (TAA) URLC (up-regulated in lung cancer 10) and vascular endothelial growth factor receptors (VEGFR) 1 and 2. Upon administration, HLA-A*0201-restricted URLC10-VEGFR1-VEGFR2 multipeptide vaccine may stimulate a cytotoxic T lymphocyte (CTL) response against URLC10-expressing tumor cells and the tumor microvasculature expressing VEGFR 1 and 2 peptides; this may result in tumor cell lysis, the inhibition of tumor angiogenesis, and decreased tumor growth. HLA-A*0201 is an MHC class I molecule that presents antigenic peptides to CD8+ T cells; epitope design restricted to epitopes that bind most efficiently to HLA-A*0201 may improve antigenic peptide immunogenicity. C77900 596690 anti-CEA IgCD28TCR-transduced autologous T cells A population of autologous tumor infiltrating lymphocytes (TIL) transduced with a retroviral vector encoding the chimeric gene IgCD28TCR with potential immunostimulating and antineoplastic activities. The chimeric IgCD28TCR gene consists of portions of CD28, the zeta chain of the T-cell receptor (TCRzeta), and a single chain antibody domain (sFv) specific for the tumor-associated antigen CEA. Upon administration, these gene-modified TIL bind to tumor cells expressing CEA, which may result in activation and proliferation of TIL and an enhanced cytotoxic T-lymphocyte (CTL) response against CEA-expressing tumor cells. CEA may be overexpressed in various gastrointestinal and breast cancers. CD28, a T-cell surface-associated co-stimulatory molecule, is required for full T-cell activation, proliferation, and survival; expression of the CD28 fragment in this chimeric gene construct may impede activation-induced cell death (AICD) of TIL. C77865 596693 multitargeted tyrosine kinase inhibitor JNJ-26483327 An orally bioavailable, small-molecule, multitargeted reversible tyrosine kinase inhibitor with potential antineoplastic activity. Multitargeted tyrosine kinase inhibitor JNJ-26483327 binds to and inhibits several members of the epidermal growth factor receptor (EGFR) family, including EGFR, HER2 and HER4; Src family kinases (Lyn, Yes, Fyn, Lck and Src); and vascular endothelial growth factor receptor type 3 (VEGFR3). By inhibiting several different signaling molecules that play crucial roles at various stages in tumorigenesis, this agent may inhibit tumor growth, invasion, migration and metastasis. In addition, JNJ-26483327 crosses the blood-brain barrier (BBB). C77866 596702 HLA-A*2402-restricted URLC10-TTK-KOC1 multipeptide vaccine A cancer vaccine containing three HLA-A*2402-restricted peptide epitopes with potential immunostimulatory and antitumor activities. Peptide epitopes in this vaccine are derived from URLC10 (up-regulated lung cancer 10); TTK (TTK protein kinase); and KOC1 (IGF II mRNA Binding Protein 3). Upon administration, URLC10-TTK-KOC1 multipeptide vaccine may stimulate a cytotoxic T lymphocyte (CTL) response against tumor cells expressing URLC10, TTK and KOC1 peptides, resulting in tumor cell lysis and decreased tumor growth. HLA-A*2402 is an MHC class I molecule that presents antigenic peptides to CD8+ T cells; epitope design restricted to epitopes that bind most efficiently to HLA-A*2402 may improve antigenic peptide immunogenicity. C77897 596704 HDAC inhibitor JNJ-26481585 An orally bioavailable, second-generation, hydroxamic acid-based inhibitor of histone deacetylase (HDAC) with potential antineoplastic activity. HDAC inhibitor JNJ-26481585 inhibits HDAC leading to an accumulation of highly acetylated histones, which may result in an induction of chromatin remodeling; inhibition of the transcription of tumor suppressor genes; inhibition of tumor cell division; and the induction of tumor cell apoptosis. HDAC, an enzyme upregulated in many tumor types, deacetylates chromatin histone proteins. Compared to some first generation HDAC inhibitors, JNJ-26481585 may induce superior HSP70 upregulation and bcl-2 downregulation. C77912 596734 HDM2 antagonist JNJ-26854165 An orally bioavailable, small-molecule HDM2 antagonist with potential antineoplastic activity. HDM2 antagonist JNJ-26854165 inhibits the binding of the\nHDM2–p53 complex to the proteasome, blocking the degradation of p53; p53 signaling and p53-mediated induction of tumor cell apoptosis may thus be restored. In addition to p53, degradation of other HDM2 client proteins may be inhibited. HDM2 (human homolog of double minute 2), a zinc finger protein, is a negative regulator of the p53 pathway; often overexpressed in cancer cells, this oncoprotein has been implicated in cancer cell proliferation and survival. C77904 596744 HLA-A*2404-restricted RNF43-TOMM34-VEGFR1-VEGFR2 multipeptide vaccine A cancer vaccine containing four HLA-A*2402-restricted peptide epitopes with potential immunostimulatory and antitumor activities. Peptide epitopes in this vaccine are derived from ring finger protein 43 (RNF43); translocase of outer mitochondrial membrane 34 (TOMM34); and vascular endothelial growth factor receptors (VEGFR) 1 and 2. Upon administration, HLA-A*2404-restricted RNF43-TOMM34-VEGFR1-VEGFR2 multipeptide vaccine may stimulate a cytotoxic T lymphocyte (CTL) response against tumor cells expressing RNF43, TOMM34, and VEGFR 1 and 2 peptides, resulting in tumor cell lysis and decreased tumor growth. HLA-A*2402 is an MHC class I molecule that presents antigenic peptides to CD8+ T cells; epitope design restricted to epitopes that bind most efficiently to HLA-A*2402 may improve antigenic peptide immunogenicity. C77867 596748 HLA-A*0201-restricted VEGFR1-VEGFR2 multipeptide vaccine A cancer vaccine containing two HLA-A*0201-restricted peptide epitopes with potential immunostimulatory and antitumor activities. Peptide epitopes in this vaccine are derived from: vascular endothelial growth factor receptors (VEGFR) 1 and 2. Upon administration, HLA-A*0201-restricted VEGFR1-VEGFR2 multipeptide vaccine may stimulate a cytotoxic T lymphocyte (CTL) response against tumor cells expressing VEGFR 1 and 2 peptides, resulting in tumor cell lysis and decreased tumor growth. HLA-A*0201 is an MHC class I molecule that presents antigenic peptides to CD8+ T cells; epitope design restricted to epitopes that bind most efficiently to HLA-A*0201 may improve antigenic peptide immunogenicity. C77905 596764 black tea Black tea is an infusion of dried leaves from plants of the Theaceae family. Due to the alkaloid caffeine, its main effect is stimulation. Black teas also contain other phytochemicals such as flavonoid and flavonoid-related compounds with strong antioxidant effects. They also attenuate atherosclerotic inflammation, reduce thrombosis, promote normal endothelial function, and block expression of cellular adhesion molecules. Black tea may reduce the risk of cancer, heart diseases, infectious diseases, and degenerative diseases. C29871 596765 HLA-A*2402-restricted KOC1-TTK-CO16-DEPDC1-MPHOSPH1 multipeptide vaccine A cancer vaccine containing five HLA-A*2402-restricted peptide epitopes with potential immunostimulatory and antitumor activities. Peptide epitopes in this vaccine are derived from IGF II mRNA binding protein 3 (KOC1); TTK protein kinase (TTK); URLC10 (up-regulated lung cancer 10); DEP domain containing 1 (DEPDC1); and M phase phosphoprotein 1 (MPHOSPH1). Upon administration, HLA-A*2404-restricted KOC1-TTK-CO16-DEPDC1-MPHOSPH1 multipeptide vaccine may stimulate a cytotoxic T lymphocyte (CTL) response against tumor cells expressing KOC1, TTK, CO16, DEPDC1 and MPHOSPH1 peptides, resulting in tumor cell lysis and decreased tumor growth. HLA-A*2402 is an MHC class I molecule that presents antigenic peptides to CD8+ T cells; epitope design restricted to epitopes that bind most efficiently to HLA-A*2402 may improve antigenic peptide immunogenicity. C77868 596795 NAE inhibitor MLN4924 A small molecule inhibitor of Nedd8 activating enzyme (NAE) with potential antineoplastic activity. NAE inhibitor MLN4924 binds to and inhibits NAE, which may result in the inhibition of tumor cell proliferation and survival. NAE activates Nedd8 (Neural precursor cell expressed, developmentally down-regulated 8), an ubiquitin-like (UBL) protein that modifies cellular targets in a pathway that is parallel to but distinct from the ubiquitin-proteasome pathway (UPP). Functioning in diverse regulatory activities, proteins conjugated to UBLs like Nedd8 typically are not targeted for proteasomal degradation. C77906 597298 allogeneic multipotent adult progenitor cells A biologic product that consists of undifferentiated stem cells, obtained from adult bone marrow or other non-embryonic tissue sources, that are expanded in vitro and deposited in master cell banks for "off-the-shelf" use, with potential hematopoiesis-inducing and immunomodulating activities. Allogeneic multipotent adult progenitor cells (MAPCs) are non-immunogenic due to the lack of major histocompatibility (MHC) molecule expression, and so elicit no immune response upon administration. In vivo, bone marrow-derived adult stem cells are capable of maturing into a broad range of cell types and may help restore the immune system by producing multiple therapeutic molecules in response to inflammation and tissue damage. C77874 597304 HLA-A*2402-restricted URLC10-KOC1-VEGFR1-VEGFR2 multipeptide vaccine A cancer vaccine containing four HLA-A*2402-restricted peptide epitopes with potential immunostimulatory and antitumor activities. Peptide epitopes in this vaccine are derived from URLC10 (up-regulated lung cancer 10 or CO16); KOC1 (IGF II mRNA Binding Protein 3); and vascular endothelial growth factor receptors (VEGFRs) 1 and 2. Upon administration, this multipeptide vaccine may stimulate a cytotoxic T lymphocyte (CTL) response against URL10-, KOC1-, VEGFR1- and VEGFR2-expressing tumor cells, resulting in tumor cell lysis and decreased tumor growth. HLA-A*2402 is an MHC class I molecule that presents antigenic peptides to CD8+ T cells; epitope design restricted to epitopes that bind most efficiently to HLA-A*2402 may improve antigenic peptide immunogenicity. C77875 597305 multitargeted tyrosine kinase inhibitor MGCD265 An orally bioavailable, small-molecule, multitargeted tyrosine kinase inhibitor with potential antineoplastic activity. Multitargeted tyrosine kinase inhibitor MGCD265 binds to and inhibits the phosphorylation of several receptor tyrosine kinases (RTKs), including the c-Met receptor (hepatocyte growth factor receptor); the Tek/Tie-2 receptor; vascular endothelial growth factor receptor (VEGFR) types 1, 2, and 3; and the macrophage-stimulating 1 receptor (MST1R or RON). Inhibition of these RTKs and their downstream signaling pathways may result in the inhibition of tumor angiogenesis and tumor cell proliferation in tumors overexpressing these RTKs. C77876 597306 murine TYRP2 plasmid DNA vaccine A plasmid DNA vaccine encoding the mouse tumor associated antigen tyrosinase-related protein-2 (TYRP2) with potential immunostimulating and antineoplastic activities. Upon administration, murine TYRP2 plasmid DNA vaccine may stimulate the host immune system to mount a cytotoxic T lymphocyte (CTL) response against tumor cells expressing TYRP2; this vaccine may also induce an immune response against tyrosinase-related protein-1 (TYRP1).\n TYRP2 and TYRP1, melanosomal membrane glycoproteins upregulated in melanoma cells, are involved in melanin synthesis. C77877 597657 HLA-A*0201-restricted VEGFR1 peptide vaccine A cancer vaccine containing an HLA-A*0201-restricted vascular endothelial growth factor receptor 1 (VEGFR1) peptide (sequence: TLFWLLLTL) with potential immunostimulatory and antitumor activities. Upon administration, HLA-A*0201-restricted VEGFR1-derived peptide vaccine may stimulate a cytotoxic T lymphocyte (CTL) response against tumor cells expressing VEGFR1, resulting in tumor cell lysis and decreased tumor growth. HLA-A*0201 is an MHC class I molecule that presents antigenic peptides to CD8+ T cells; epitope design restricted to epitopes that bind most efficiently to HLA-A*0201 may improve antigenic peptide immunogenicity. C77878 597662 HLA-A*2402-restricted VEGFR1 peptide vaccine A cancer vaccine containing the HLA-A*2402-restricted vascular endothelial growth factor receptor 1 (VEGFR1) peptide epitope with potential immunostimulatory and antitumor activities. Upon administration, HLA-A*2402-restricted VEGFR1 peptide vaccine may stimulate a cytotoxic T lymphocyte (CTL) response against tumor cells expressing VEGFR 1 peptide, resulting in tumor cell lysis and decreased tumor growth. HLA-A*2402 is an MHC class I molecule that presents antigenic peptides to CD8+ T cells; epitope design restricted to epitopes that bind most efficiently to HLA-A*2402 may improve antigenic peptide immunogenicity. C77869 597722 glycosylated recombinant human interleukin-7 A glycosylated recombinant protein which is chemically identical to or similar to endogenous human interleukin-7 (IL-7) with hematopoietic and immunopotentiating activities. Naturally produced by bone marrow, thymic stromal, and spleen cells, the cytokine interleukin-7 is a hematopoietic growth factor for progenitor B cells and T cells, stimulating proliferation and differentiation of mature T-cells and natural killer (NK) cells. As with glycosylated endogenous proteins, glycosylation of recombinant proteins \nmay fundamentally affect their biological activity, function, clearance from circulation, and antigenicity; glycosylation of recombinant proteins that are chemically identical to similar to endogenous proteins may render protein structures and biological activities that are more similar to those of glycosylated endogenous proteins. C77879 597742 oral milataxel An orally bioavailable taxane with potential antineoplastic activity. Upon oral administration, milataxel and its major active metabolite M-10 bind to and stabilize tubulin, resulting in the inhibition of microtubule depolymerization and cell division, cell cycle arrest in the G2/M phase, and the inhibition of tumor cell proliferation. Unlike other taxane compounds, milataxel appears to be a poor substrate for the multidrug resistance (MDR) membrane-associated P-glycoprotein (P-gp) efflux pump and may be useful for treating multidrug-resistant tumors. C77880 597757 polyvalent antigen-KLH conjugate vaccine A multivalent cancer vaccine comprised of the five tumor-associated antigens (TAAs) globo H, GM2 ganglioside, Tn-MUC1, TF, and sTn conjugated with the immunoadjuvant keyhole limpet hemocyanin (KLH), with potential antineoplastic activity. Upon administration, polyvalent antigen-KLH conjugate vaccine may induce production of IgG and IgM antibodies and antibody-dependent cell-mediated cytotoxicity (ADCC) against tumor cells expressing these TAAs, resulting in tumor cell death and tumor growth inhibition. Globo H (globo H hexasaccharide 1); GM2 ganglioside; Tn-MUC1 (human tumor-associated epithelial mucin 1 carrying the tumor-specific glycan Tn); TF (Thompson-Friedreich); and sTn (sialyl-Tn) are overexpressed in a variety of cancer cells. KLH is a hapten carrier and serves as an immunostimulant to improve immune recognition of antigens. C77870 598079 lidocaine patch 5% A transdermal patch containing a 5 percent aqueous base solution of the synthetic amide-type anesthetic lidocaine with analgesic activity. Upon topical application and transdermal delivery, the active ingredient lidocaine binds to and blocks voltage-gated sodium channels in the neuronal cell membrane; lidocaine-mediated stabilization of neuronal membranes inhibits the initiation and conduction of nerve impulses and produces a reversible local anesthesia. C29988 598296 polyethylene glycol 3350-based laxative A polyethylene glycol-based solution containing polyethylene glycol (PEG) 3350 (macrogol 3350) and electrolytes with laxative activity. As an orally administered nonabsorbable osmotic agent, PEG 3350 increases fecal water content and decreases gastrointestinal transit time. C77958 598301 milk protein-based energy drink An oral milk protein-based nutritional supplement. Milk protein-based energy drink is a flavored liquid that consists of milk protein, rapeseed and sunflower oils, carbohydrates, vitamins, minerals and trace-elements, providing 1.5kcal and 10 mg of protein per ml. C77871 598363 ramelteon A synthetic melatonin analogue with hypnotic and circadian rhythm-modulating activities. Ramelteon binds to and activates melatonin receptors 1 and 2 in the suprachiasmatic nucleus (SCN) of the brain, thereby promoting the onset of sleep. Unlike the nonbenzodiazepine sedative hypnotics zolpidem and zaleplon, this agent does not activate GABA receptors and, so, produces no GABA receptor-mediated anxiolytic, myorelaxant, and amnesic effects. C66504 598379 Hsp90 inhibitor STA-9090 A synthetic small-molecule inhibitor of heat shock protein 90 (Hsp90) with potential antineoplastic activity. Hsp90 inhibitor STA-9090 binds to and inhibits Hsp90, resulting in the proteasomal degradation of oncogenic client proteins, the inhibition of cell proliferation and the elevation of heat shock protein 72 (Hsp72); it may inhibit the activity of multiple kinases, such as c-Kit, EGFR, and Bcr-Abl, which as client proteins depend on functional HsP90 for maintenance. Hsp90, a 90 kDa molecular chaperone upregulated in a variety of tumor cells, plays a key role in the conformational maturation, stability and function of "client" proteins within the cell, many of which are involved in signal transduction, cell cycle regulation and apoptosis, including kinases, transcription factors and hormone receptors. Hsp72 exhibits anti-apoptotic functions; its up-regulation may be used as a surrogate marker for Hsp90 inhibition. C77872 598417 immunotherapy regimen MKC-1106-MT An immunotherapy regimen containing three components: a plasmid encoding portions of the two melanoma-associated antigens Melan A (also called MART-1) and tyrosinase and two synthetic analogs of Melan-A and tyrosinase antigen epitopes with potential immunostimulating and antitumor activities. First, the plasmid is injected directly into lymph nodes in order to sensitize or prime antigen-presenting cells (APCs) and central memory T cells in lymph nodes to plasmid-expressed Melan A and tyrosinase. After several priming injections with plasmids, the Melan A and tyrosinase synthetic epitope analogs are injected directly into lymph nodes; upon binding to major histocompatibility complex (MHC) molecules on APC cell surfaces, these synthetic epitope analogs may stimulate a "primed" cytotoxic T lymphocyte (CTL) response against melanoma tumor cells, resulting in tumor cell lysis. Melan-A and tyrosinase are overexpressed by melanoma tumor cells. C77971 598429 strawberry-blackberry-black raspberry-blueberry berry mixture A dietary supplement consisting of a mixture of strawberries, blackberries, black raspberries and blueberries with potential antineoplastic activity. Although the exact mechanism of action through which berries may exert their anti-tumor effect has yet to be elucidated, in vivo studies suggest that the ingestion of a mixture of berries seems to result in a reduction in tumor growth and tumor development. As berries are rich in phytonutrients, such as anthocyanins, flavonols, ellagitannins, galltannins, proanthocyanidins, and phenolic acids, the antineoplastic effects of strawberry-blackberry-black raspberry-blueberry berry mixture on cancer cells may be attributable to phytonutrient antioxidant and apoptotic activities. In addition, phytoestrogens in berries may be protective against estrogen-sensitive tumors. C77873 598794 glucosamine sulfate/chondroitin sulfate tablet An oral tablet formulation of a dietary supplement containing the sulfate salts of the amino sugar glucosamine and the glucosaminoglycan chondroitin with potential analgesic, anti-inflammatory, and anti-arthritic activities. Both glucosamine and chondroitin are naturally occurring substances that play a key role in cartilage formation and repair. Glucosamine is an essential substrate for glycosaminoglycans and hyaluronic acid, needed for formation of the joint proteoglycan structural matrix, and may prevent chondrocytic catabolic activity and inhibit production of inflammatory mediators. Chondroitin is the major glycosaminoglycan in cartilage, responsible for the elasticity of cartilage; it may reduce the IL-1beta-induced nuclear factor-kappaB (NF-kB) translocation in chondrocytes, inhibiting NF-kB-mediated inflammatory processes. C77881 598799 vascular disrupting agent CYT997 An orally bioavailable small-molecule with tubulin-inhibiting, vascular-disrupting, and potential antineoplastic activities. Vascular disrupting agent (VDA) CYT997 inhibits tubulin polymerization in tumor blood vessel endothelial cells and tumor cells, blocking the formation of the mitotic spindle and leading to cell cycle arrest at the G2/M phase; this may result in disruption of the tumor vasculature and tumor blood flow, and tumor cell death. C77882 598859 ashwagandha root powder extract A dietary supplement containing an extract powder derived from the root of the ashwagandha shrub with potential antineoplastic, antioxidant, immunostimulating and anti-angiogenic activities. Ashwagandha root powder extract contains numerous alkaloids, including withanine as the primary alkaloid, and steroidal lactone withanolides. The withanolides in this agent may suppress nuclear factor-kappaB activation and nuclear factor-kappaB-regulated gene expression, potentiating apoptosis and inhibiting tumor cell invasion. Cultivated in India and North America, ashwagandha (Withania somnifera Dunal or Indian ginseng) belongs to the Solanaceae (nightshade) family. C77883 598873 poly-TLR agonist polyantigenic vaccine CADI-05 A poly-Toll-like receptor (TLR) agonist polyantigenic vaccine containing heat killed Mycobacterium indicus pranii (Mycobacterium w or Mw) with potential immunostimulating and antineoplastic activities. Upon administration, poly-TLR agonist polyantigenic vaccine activates a number of TLRs, which may result in macrophage and plasmacytoid dendritic cell (pDC) stimulation; secretion of interferon alpha; production of pro-inflammatory cytokines; upregulation of co-stimulatory molecules, enhanced T and B-cell stimulatory responses; T cell proliferation, and a Th1 immune response. TLRs are transmembrane receptors that recognize structurally conserved microbial molecules such as bacterial cell-surface lipopolysaccharides (LPS), lipoproteins, lipopeptides, lipoarabinomannan and flagellin, among others; immune responses stimulated by TLR activation may result in antineoplastic effects. C77884 599024 renal cell carcinoma/CD40L RNA-transfected autologous dendritic cell vaccine AGS-003 A cancer vaccine in which autologous dendritic cells are transfected with patient-specific renal cell carcinoma (RCC) RNA and a synthetic, truncated human CD40 ligand (CD40L) RNA with potential immunostimulatory and antineoplastic activities. Individual RCC-specific RNA, encoding a unique repertoire of tumor-associated antigens (TAAs) (including telomerase reverse transcriptase, G250, and oncofetal antigen) is electroporated into autologous dencritic cells (DCs), transfected with synthetic RNA that encodes a truncated version of the T-cell protein CD40L; the transfected autlogous DCs express and process both patient-specific RCC TAAs and the truncated CD40L protein. When reintroduced back to the patient, renal cell carcinoma/CD40L RNA-transfected autologous dendritic cell vaccine AGS-003 may elicit a highly specific cytotoxic T-cell (CTL) response against RCC cells expressing the patient-specific RCC TAA repertoire. The signal cascade initiated by stimulation of the truncated, ectopically expressed co-stimulatory molecule CD40L results in the secretion of the inflammatory cytokine IL-12 downstream. C77907 599034 MEK inhibitor GSK1120212 An orally bioavailable inhibitor of mitogen-activated protein kinase kinase (MEK MAPK/ERK kinase) with potential antineoplastic activity. MEK inhibitor GSK1120212 specifically binds to and inhibits MEK 1 and 2, resulting in an inhibition of growth factor-mediated cell signaling and cellular proliferation in various cancers. MEK 1 and 2, dual specificity threonine/tyrosine kinases often upregulated in various cancer cell types, play a key role in the activation of the RAS/RAF/MEK/ERK signaling pathway that regulates cell growth. C77908 599037 FGFR1 receptor antagonist FP-1039 A soluble fusion protein consisting of the extracellular domain of human fibroblast growth factor receptor 1 (FGFR1) fused to the Fc portion of human immunoglobulin G1 (IgG1) with potential antineoplastic and anti-angiogenic activities. FGFR1 receptor antagonist FP-1039 prevents FGFR ligands, such as FGF1, FGF2, FGF4, from binding to their cognate receptors, thereby inhibiting the activation of the related FGFR tyrosine kinases. Inhibition of FGFR1 by this agent may retard tumor cell proliferation and induce tumor cell death. FP-1039 may also inhibit vascular endothelial growth factor (VEGF)-induced angiogenesis. FGFR1 is a receptor tyrosine kinase upregulated in certain tumor cells and involved in tumor cellular proliferation, differentiation, angiogenesis, and survival; most ligands that bind to FGFR1 also bind to\nthe related receptors FGFR3 and FGFR4. C77970 599041 HPV DNA plasmids therapeutic vaccine VGX-3100 A DNA vaccine consisting of plasmids encoding the E6 and E7 genes of human papilloma virus (HPV) subtypes 16 and 18, respectively, with potential immunostimulating and antineoplastic activities. Administered via intramuscular electroporation, HPV DNA plasmids therapeutic vaccine VGX-3100 expresses E6 and E7 proteins, which may elicit a cytotoxic T-lymphocyte (CTL) response against cervical cancer cells expressing E6 and E7 proteins, resulting in tumor cell lysis. HPV type 16 and HPV type 18 are the most common HPV types involved in cervical carcinogenesis. C77909 599246 Ad-sig-hMUC-1/ecdCD40L vaccine A cancer vaccine consisting of a recombinant adenoviral vector encoding the tumor-associated antigen (TAA) human MUC-1 (hMUC-1) linked to the extracellular domain (ecd) of the co-stimulatory molecule CD40 ligand (CD40L) and an adenovirus signal sequence that encodes a secretory signal peptide (Ad-sig) with potential immunostimulating and antineoplastic activities. Due to the presence of the secretory signal peptide expressed by Ad-sig in the vaccine construct, transfected cells may secrete a fusion protein composed of hMUC-1 and the CD40L ecd. The CD40L moiety part of the fusion protein binds to CD40 receptors on dendritic cells (DCs). Subsequently, DCs may be activated and migrate, T-cells may expand, and a cytotoxic T lymphocyte (CTL) response against tumor cells that overexpress hMUC-1 may follow. MUC-1 is a hypoglycosylated TAA overexpressed by epithelial cancer cells. C77910 599247 ultralow-molecular-weight heparin AVE5026 An ultralow-molecular-weight heparin (ULMWH) (Mw: 2000-3000 daltons) consisting of a polydisperse mixture of oligomeric heparin fragments with potential anticoagulant activity. Ultralow-molecular-weight heparin AVE5026 binds to and activates antithrombin III (ATIII), which may result in the inhibition of activated factor Xa and, to a much lesser extent, factor IIa (thrombin) and so the inhibition of fibrin formation. Compared to low-molecular-weight heparins (LMWHs), AVE5026 exhibits an even higher ratio of anti-Factor Xa to anti-Factor IIa activity (>30:1). Compared to unfractionated heparins, the use of LMWHs is associated with lower incidences of major bleeding, osteoporosis and heparin-induced thrombocytopenia. Like LMWHs, this agent may inhibit tumor growth by regulating angiogenesis and apoptosis. AVE5026 is prepared by partial depolymerization of unfractionated porcine mucosal heparin. C78447 599454 mesothelioma tumor lysate-pulsed autologous dendritic cell vaccine A cell-based cancer vaccine consisting of autologous dendritic cells (DCs) pulsed with mesothelioma tumor lysate with potential immunostimulating and antineoplastic activities. Upon administration, mesothelioma tumor lysate-pulsed autologous dendritic cell vaccine may stimulate the host immune system to mount a specific cytotoxic T lymphocyte (CTL) response against mesothelioma tumor cells, resulting in tumor cell lysis. C78448 599455 TLR8 agonist VTX-2337 A small-molecule Toll-like receptor 8 (TLR8) agonist with potential immunostimulating and antineoplastic activities. TLR8 agonist VTX-2337 binds to TLR8, present in cutaneous dendritic cells, monocytes/macrophages, and mast cells, which may result in the activation of the central transcription factor nuclear factor-B, the secretion of proinflammatory cytokines and other mediators, and a Th1-weighted antitumoral cellular immune response. Primarily localized to endosomal membranes intracellularly, TLR8, like other TLRs, recognizes pathogen-associated molecular patterns (PAMPs) and plays a key role in the innate immune system. C80521 599456 glembatumumab vedotin An antibody-drug conjugate, consisting of the fully human monoclonal antibody CR011 directed against glycoprotein NMB (GPNMB) and conjugated via a cathepsin B-sensitive valine-citrulline (vc) linkage to the cytotoxic agent monomethyl auristatin E (MMAE), with potential antineoplastic activity. Upon administration, the monoclonal antibody CR011 moiety binds to glycoprotein nmb (GPNMB), expressed on the surfaces of a variety of cancer cell types; upon endocytosis, the synthetic dolastin analogue MMAE is released via enzymatic cleavage into the tumor cell cytosol, where it binds to tubulin and inhibits tubulin polymerization, which may result in G2/M phase arrest and apoptosis. The vc linkage system is highly stable in serum, rendering the cytotoxicity of glembatumumab vedotin specific for GPNMB-positive cells. GPNMB is a transmembrane protein overexpressed on the surfaces of various cancer cell types, including melanoma, breast, and prostate cancer cells. C78449 599463 transferrin receptor-targeted anti-RRM2 siRNA CALAA-01 A proprietary transferrin receptor-targeted nanoparticle preparation of a non-chemically modified small-interfering RNA (siRNA) directed against the M2 subunit of ribonucleotide reductase (RRM2) with potential antineoplastic activity. Upon administration, transferrin receptor-targeted anti-RRM2 siRNA CALAA-01 binds to transferrin receptors (TfRs), releasing anti-RRM2 siRNA after endocytosis; anti-RRM2 siRNA silences the expression of RRM2 via the RNAi pathway, impeding the assembly of the holoenzyme ribonucleotide reductase (RR) which catalyzes the production of deoxyribonucleotides. As a result, inhibition of cellular proliferation may occur in cells expressing TfR, a cell surface protein overexpressed on various cancer cell types. C78450 599668 DI-Leu16-IL2 immunocytokine A recombinant fusion protein consisting of de-immunized and humanized anti-CD20 monoclonal antibody Leu16 fused to human cytokine interleukin-2 (IL2) with potential antineoplastic activity. The antibody moiety of DI-Leu16-IL2 immunocytokine binds to tumor cells expressing the CD20 antigen, which may result in an antibody-dependent cell-mediated cytotoxicity (ADCC) towards CD20-expressing tumor cells; the localized IL2 moiety of this fusion protein may stimulate natural killer (NK) and T-lymphocyte mediated immune responses, enhancing the ADCC response. De-immunization involves the modification of potential helper T cell epitopes that bind to MHC class II molecules; humanization involves combining recombinant murine variable (V) regions with human immunoglobulin light and heavy chain constant regions. CD20 antigen, a hydrophobic transmembrane protein located on normal pre-B and mature B lymphocytes, is overexpressed by various cancer cell types. C78451 599670 MART-1:26-35(27L) peptide vaccine A peptide-based cancer vaccine consisting of amino acid residues 26 through 35 of MART-1 (melanoma antigen recognized by T-cells-1) with a leucine substitution at amino acid position 27 to improve immunogenicity. Upon administration, MART-1:26-35(27L) peptide vaccine may induce a cytotoxic T-lymphocyte (CTL) response against MART-1-expressing tumor cells, resulting in decreased tumor growth. The tumor-associated antigen (TAA) MART-1 may be overexpressed on melanoma cancer cells. C2772 599759 white button mushroom extract A heat-stable extract of white button mushrooms (Agaricus bisporus) with potential chemopreventive and immunomodulating activities. Phytochemicals, such as polysaccharides and especially beta-D-glucans found in the white button mushroom extract, bind to and inhibit the activity of aromatase, an enzyme responsible for the conversion of androgens to estrogens and which is often upregulated in breast cancer cells. The consequent decrease in estrogen production may result in the suppression of estrogen-dependent cellular proliferation. In addition, this extract may promote dendritic cell (DC) maturation, increase interferon gamma (IFN-gamma) and tumor necrosis factor alpha (TNF-alpha) production, and may enhance natural killer (NK) cell activity, thus amplifying both innate and T cell-mediated immune responses against cancer cells. C78490 599760 fentanyl buccal soluble film A transmucosal formulation consisting of a small, mucoadhesive, bioerodible polymer disc formulated with the citrate salt of fentanyl, a synthetic anilidopiperidine opioid with analgesic activity. Upon application, fentanyl buccal soluble film rapidly releases fentanyl which is quickly absorbed into the systemic circulation. Fentanyl selectively binds to and activates mu-opioid receptors in the central nervous system (CNS), thereby mimicking the effects of endogenous opiates. C78461 599816 PGG beta-glucan An injectable formulation of the polysaccharide beta 1,3/1,6 glucan derived from the cell wall of the yeast Saccharomyces cerevisiae with potential immunomodulating and antineoplastic activities. PGG beta-glucan binds to an alternate site on the neutrophil complement receptor 3 (CR3), priming the neutrophil to become cytotoxic when binding to complement on tumor cells via CR3. This agent has been reported to selectively activate immune cells without inducing pro-inflammatory cytokines, potentially reducing potential side effects observed with the induction of broad innate immune responses. In addition, PGG beta-glucan may induce hematopoietic progenitor cell (HPC) mobilization. C78463 599832 anti-KIR monoclonal antibody IHP 2101 A human monoclonal antibody directed against the human inhibitory killer IgG-like receptor (KIR) with potential immunostimulating and antineoplastic activities. Anti-KIR monoclonal antibody IPH 2101 binds to the KIR receptor expressed on human natural killer (NK) cells, which may prevent KIR-mediated inhibition of NK cells and permit NK cell-mediated anti-tumor cytotoxicity. KIRs are surface glycoproteins that bind to major histocompatibility complex (MHC)/human leukocyte antigen (HLA) class I subtypes on target cells; binding of KIRs inhibits NK cell-mediated cytotoxicity. C78464 599836 methoxyamine An orally bioavailable small molecule inhibitor with potential adjuvant activity. Methoxyamine covalently binds to apurinic/apyrimidinic (AP) DNA damage sites and inhibits base excision repair (BER), which may result in an increase in DNA strand breaks and apoptosis. This agent may potentiate the anti-tumor activity of alkylating agents. C78084 599841 aldehyde dehydrogenase-bright cells A specific population of stem and progenitor cells that expresses aldehyde dehydrogenase (ALDH) with hematopoietic activity. Isolated from umbilical cord blood and primed in culture with cytokines before infusion to patients, aldehyde dehydrogenase-bright cells may restore progenitor cell function and may reconstitute immune cell function and reconstituting, repairing and regenerating tissue. C78466 599982 CMVpp65-A*0201 peptide vaccine A peptide-based cancer vaccine containing a mutated form of the HLA-A*0201-restricted cytomegaloviral epitope CMVpp65(495-503) with potential immunostimulatory and antitumor activities. Upon subcutaneous administration, CMVpp65-A*0201 peptide vaccine may stimulate a cytotoxic T lymphocyte (CTL) response against CMV-positive cells, resulting in cell lysis. HLA-A*0201 is an MHC class I molecule that presents antigenic peptides to CD8+ T cells; epitope design restricted to epitopes that bind most efficiently to HLA-A*0201 may improve antigenic peptide immunogenicity. CMVpp65, a tegument protein of the herpes virus CMV, is the main viral antigen found in peripheral blood mononuclear cells (PBMCs) after viral infection and may activate cell-mediated immunity. C78467 599996 [18F]-ML-10 A small molecular-weight, malonic acid-based probe [(2-(5-fluoro-pentyl)-2-methyl-malonic acid or ML-10] labeled with the radioactive isotope fluorine F 18 with potential apoptosis radioimaging use. Upon administration, [F18]-ML-10 binds selectively to apoptotic cells due to apoptotic cell membrane features that differ from those of normal, healthy and necrotic cell membranes. Upon entering the apoptotic cell, this agent accumulates within the cytoplasm where it can be imaged using positron emission tomography (PET). Detection of apoptotic cells using this imaging technology may be useful in monitoring tumor responses to cytotoxic therapies. ML-10 appears to mimic the alkyl-malonic acid motif present in gamma -carboxyglutamic (Gla), an amino acid that plays a crucial role in the binding of clotting factors to negatively-charged phospholipids exposed on the surfaces of apoptotic cells. C78468 599997 topical myristyl nicotinate cream A topical cream containing the ester prodrug myristyl nicotinate (MN), a lipophilic nicotinic acid derivative with potential chemopreventive activity. Upon topical application, myristyl nicotinate penetrates into the epidermis where the agent is cleaved and is converted into nicotinic acid (niacin); nicotinic acid then diffuses into cells where it is converted to nicotinamide adenine dinucleotide (NAD). NAD may stimulate poly(ADP-ribose) polymerase-1 (PARP-1); enhance skin cell turnover and epidermal differentiation; and strengthen skin barrier function. NAD is a coenzyme that plays a crucial role in many redox reactions; PARP-1 is an enzyme that plays an important role in DNA repair. C78469 600075 alpha-galactosylceramide-pulsed autologous dendritic cells A cancer vaccine comprised of autologous dendritic cells (DCs) pulsed with the marine sponge glycolipid alpha-galactosylceramide (alpha-GalCer) with potential immunostimulatory and antimetastatic activities. Upon administration, alpha-galactosylceramide-pulsed autologous dendritic cells may result in the activation and proliferation of a subset of endogenous natural killer T ( NKT) cells, B cells, and CD4+ and CD8+ T cells, and the production of interferon-gamma and interleukin-12; these cascade events may result in a T helper-1 cell-biased proinflammatory antitumor immune response. The NKT cell ligand alpha-GalCer was originally isolated from the marine sponge Agelas mauritianusis. C78489 600076 PI3K inhibitor GSK1059615 A phosphoinositide 3-kinase (PI3K) inhibitor with potential antineoplastic activity. PI3K inhibitor GSK1059615 inhibits PI3K in the PI3K/AKT kinase signaling pathway, which may trigger the translocation of cytosolic Bax to the mitochondrial outer membrane and an increase in mitochondrial membrane permeability, followed by apoptosis. Bax is a member of the proapoptotic Bcl-2 family of proteins. PIK3, an enzyme often overexpressed in cancer cells, plays a crucial role in tumor cell regulation and survival. C78470 600083 estradiol vaginal ring A flexible elastomer ring containing 17 beta-estradiol used for estrogen replacement. Upon vaginal insertion, estradiol vaginal ring releases a consistent low-dose of estrogen which binds to and activates nuclear receptors in estrogen-responsive tissues. By increasing the amount of estradiol locally, symptoms of vaginal dryness or decreased sexual interest may improve. 17 beta-estradiol is the major naturally occurring estrogen produced in the ovaries of premenopausal women. C78471 600085 testosterone vaginal cream A topical cream containing a synthetic form of the endogenous androgenic steroid testosterone. Upon vaginal application, testosterone is irreversibly converted to dihydrotestosterone (DHT) in target tissues by the enzyme 5-alpha reductase. Testosterone or DHT ligand-androgen receptor complexes act as transcription factor complexes, stimulating the expression of various responsive genes. DHT binds with higher affinity to androgen receptors than testosterone, activating gene expression more efficiently. In addition, testosterone is irreversibly converted to estradiol by the enzyme complex aromatase, particularly in the liver and adipose tissue. Topical application of testosterone may improve symptoms of vaginal dryness. C78472 600183 zirconium Zr 89 cetuximab A radioimmunoconjugate comprised of the recombinant chimeric monoclonal antibody cetuximab labeled with the radioisotope zirconium Z 89 (Zr 89) with radioisotopic activity and potential imaging use. The antibody moiety of zirconium Zr 89 cetuximab binds to the extracellular domain of the epidermal growth factor receptor (EGFR). Upon binding, the radioisotope moiety may be detected using positron emission tomography (PET), allowing the imaging and quantification of EGFR-expressing tumor cells. EGFR is a tyrosine kinase that may be overexpressed on the cell surfaces of various tumor cell types. C78473 600185 PSP-94-derived peptide PCK3145 A synthetic 15-mer peptide corresponding to amino acids 31-45 of the 94-amino acid isoform of human prostate secretory protein (PSP-94) with potential anti-metastasis and anti-angiogenesis activities. PSP-94-derived peptide PCK3145 may inhibit the secretion of the metastasis-related protein matrix metalloproteinase-9 (MMP-9) and its potential binding to its cell surface receptor CD44; may interfere with the vascular endothelial growth factor (VEGF) signaling pathway, resulting in an anti-angiogenesis effect; and may reduce the levels of parathyroid hormone-related protein (PTHrP), decreasing plasma calcium levels. PSP-94, one of three predominant proteins found in seminal fluid, may be down-regulated in prostate cancer, representing a potential survival mechanism for prostate cancer cells. MMP-9 is implicated in the invasion and metastasis of cancer. PTHrP may be expressed by various tumor cell types, resulting in the hypercalcemia of malignancy. C78474 600512 HDAC inhibitor CHR-3996 An orally bioavailable, second-generation hydroxamic acid-based inhibitor of histone deacetylase (HDAC) with potential antineoplastic activity. HDAC inhibitor CHR-3996 inhibits HDAC, resulting in an accumulation of highly acetylated histones, the induction of chromatin remodeling, and the selective transcription of tumor suppressor genes; these events may result in the inhibition of tumor cell division and the induction of tumor cell apoptosis. This agent may upregulate HSP70 and downregulate anti-apoptotic Bcl-2 proteins more substantially than some first-generation HDAC inhibitors. HDACs, upregulated in many tumor cell types, are a family of metalloenzymes responsible for the deacetylation of chromatin histone proteins. C78475 600513 mTOR kinase inhibitor OSI-027 An orally bioavailable mammalian target of rapamycin (mTOR) kinase inhibitor with potential antineoplastic activity. mTOR kinase inhibitor OSI-027 binds to and inhibits both the raptor-mTOR (TOR complex 1 or TORC1) and the rictor-mTOR (TOR complex 2 or TORC2) complexes of mTOR, which may result in tumor cell apoptosis and a decrease in tumor cell proliferation. mTOR is a serine/threonine kinase that is upregulated in some tumors and plays an important role downstream in the PI3K/Akt/mTOR signaling pathway. C78476 600544 topical betulinic acid A topical formulation of a pentacyclic lupane-type triterpene derivative of betulin (isolated from the bark of Betula alba, the common white birch) with antiinflammatory, anti-HIV and antineoplastic activities. Betulinic acid induces apoptosis through induction of changes in mitochondrial membrane potential, production of reactive oxygen species, and opening of mitochondrial permeability transition pores, resulting in the release of mitochondrial factors involved in apoptosis, activation of caspases, and DNA fragmentation. Although originally thought to exhibit specific cytotoxicity against melanoma cells, this agent has been found to be cytotoxic against non-melanoma tumor cell types including neuroectodermal and brain tumor cells. C78477 600553 astuprotimut-R A cancer vaccine consisting of a recombinant form of human melanoma antigen A3 (MAGE-A3) combined with a proprietary adjuvant with potential immunostimulatory and antineoplastic activities. Upon administration, astuprotimut-R may stimulate a cytotoxic T lymphocyte (CTL) response against tumor cells expressing the MAGE-A3 antigen, resulting in tumor cell death. MAGE-A3, a tumor-associated antigen (TAA) originally discovered in melanoma cells, is expressed by various tumor types. The proprietary immunostimulating adjuvant in this agent is composed of a specific combination of immunostimulating compounds selected to increase the anti-tumor immune response to MAGE-A3. C78478 600630 18F-fluoromethylcholine A radiotracer consisting of methylcholine labeled with the positron-emitting radioisotope fluorine F 18 (18F-FMCH) with potential imaging use. Upon administration, 18F-fluoromethylcholine incorporates into tumor cells through an active, carrier-mediated transport mechanism for choline and then is phosphorylated intracellularly by choline kinase, an enzyme frequently upregulated in human tumors, yielding phosphoryl 18F-fluoromethylcholine. In turn, phosphoryl 18F-fluoromethylcholine is integrated into phospholipids in the cell membrane as part of phosphatidylcholine. As the proliferation of cancer cells is much higher than normal cells, tumor cells exhibit an increased rate of 18F-FMCH uptake and incorporation, allowing tumor imaging with positron emission tomography (PET). C78479 600816 ombrabulin A synthetic water-soluble analogue of combretastatin A4, derived from the South African willow bush (Combretum caffrum), with potential vascular-disrupting and antineoplastic activities. Ombrabulin binds to the colchicine binding site of endothelial cell tubulin, inhibiting tubulin polymerization and inducing mitotic arrest and apoptosis in endothelial cells. As apoptotic endothelial cells detach from their substrata, tumor blood vessels collapse; the acute disruption of tumor blood flow may result in tumor necrosis. C78480 600817 padeliporfin A vascular-acting photosensitizer consisting of a water-soluble, palladium-substituted bacteriochlorophyll derivative with potential antineoplastic activity. Upon administration, paldeliporfin is activated locally when the tumor bed is exposed to low-power laser light; reactive oxygen species (ROS) are formed upon activation and ROS-mediated necrosis may occur at the site of interaction between the photosensitizer, light and oxygen. Vascular-targeted photodynamic therapy (VTP) with padeliporfin may allow tumor-site specific cytotoxicity while sparing adjacent normal tissues. C78481 600855 hyperimmune bovine colostrum A dietary supplement consisting of bovine colostrum, containing high titers of immunoglobulins (Igs), with immunostimulating and anti-infective activities. Hyperimmune bovine colostrum is harvested during the first days after calving from cows that have been inoculated repeatedly with specific pathogens during pregnancy. In addition to high titers of anti-pathogen specific antibodies, hyperimmune colostrum is also rich in other immune factors, proline-rich polypeptides (PRP), lactoferrin, glycoproteins, lactalbumins, cytokines, growth factors, vitamins, and minerals. This dietary supplement may exhbit anti-infective activity in immunocompromised patients. C78491 600952 blue citrus-based herbal capsule An oral capsule formulation of a traditional Chinese herbal medicine with potential analgesic activity. In addition to other herbs, seeds and fruits, blue citrus-based herbal capsule contains the Chinese herb blue citrus (qing pi), which is produced from the dried immature green peel of the tangerine Citrus reticulata Blanco. Blue citrus contains large amounts of limonene, citral and synephrine, which may attribute to its analgesic activity. However, due to the complexity of its chemical components, the exact mechanism of action of this agent remains to be determined. C78482 600953 yttrium-90 polycarbonate brachytherapy plaque A polycarbonate-based semicylindrical plaque impregnated with yttrium Y 90 with radioisotopic and antineoplastic activities. An yttrium-90 polycarbonate brachytherapy plaque may be applied to a tumor site with a special brachytherapy applicator for a predetermined interval of time, selectively delivering a cytotoxic dose of beta-emitting yttrium Y 90. C80739 601032 MET tyrosine kinase inhibitor PF-04217903 An orally bioavailabe, small-molecule tyrosine kinase inhibitor with potential antineoplastic activity. MET tyrosine kinase inhibitor PF-04217903 selectively binds to and inhibits mesenchymal epithelial transition (MET or c-Met), disrupting the c-Met signaling pathway, which may result in the inhibition of tumor cell growth, migration and invasion of tumor cells, and the induction of death in tumor cells expressing c-Met. The receptor tyrosine kinase c-Met, also known as hepatocyte growth factor (HGF) receptor, is overexpressed or mutated in many tumor cell types, playing an important role in tumor cell proliferation, survival, invasion, and metastasis and angiogenesis. C78483 601033 IAP inhibitor HGS1029 The hydrochloride salt of a small-molecule inhibitor of IAP (Inhibitor of Apoptosis Protein) family proteins with potential antineoplastic activity. IAP inhibitor HGS1029 selectively inhibits the biological activity of IAP proteins, which may restore apoptotic signaling pathways; this agent may work synergistically with cytotoxic drugs to overcome tumor cell resistance to apoptosis. IAPs are overexpressed by many cancer cell types, suppressing apoptosis by binding and inhibiting active caspases-3, -7 and -9 via their BIR (baculoviral lAP repeat) domains. C78484 601044 asparaginase-Erwinia An enzyme isolated from the bacterium Erwinia chrysanthemi (E. carotovora). Asparagine is critical to protein synthesis in leukemic cells, which cannot synthesize this amino acid due to the absence of the enzyme asparagine synthase. Asparaginase hydrolyzes L-asparagine to L-aspartic acid and ammonia, thereby depleting leukemic cells of asparagine and blocking protein synthesis and tumor cell proliferation, especially in the G1 phase of the cell cycle. This agent also induces apoptosis in tumor cells. The Erwinia-derived product is often used for those patients who have experienced a hypersensitivity reaction to the E. Coli formulation. 601057 C-11 choline A radiotracer consisting of choline labeled with the positron-emitting isotope carbon C 11 with potential imaging use. Upon administration, C-11 choline incorporates into tumor cells through an active, carrier-mediated transport mechanism for choline and then is phosphorylated intracellularly by choline kinase, an enzyme frequently upregulated in human tumors, yielding phosphoryl C-11 choline. In turn, phosphoryl C-11 choline is integrated into phospholipids in the cell membrane as part of phosphatidylcholine. As the proliferation of cancer cells is much higher than normal cells, tumor cells exhibit an increased rate of C-11 choline uptake and incorporation, allowing tunor imaging with positron emission tomography (PET). C78485 601058 anti-PLGF monoclonal antibody TB-403 A humanized monoclonal antibody directed against placental growth factor (PLGF) with potential anti-angiogenic and antineoplastic acivities. Anti-PLGF monoclonal antibody TB-403 binds to PLGF, inhibiting the binding of PLGF to the vascular endothelial growth factor receptor, which may result in the inhibition of tumor angiogenesis and tumor cell proliferation. PLGF is a protein that belongs to the family of vascular endothelial growth factors (VEGFs). C78486 601127 IL-2/Lptn gene-modified allogeneic neuroblastoma tumor cell vaccine A cancer vaccine consisting of allogeneic neuroblastoma tumor cells have been genetically modified to secrete the human cytokine interleukin-2 (IL-2) and the human chemokine lymphotactin (Lptn) with potential immunostimulating and antineoplastic activities. Upon administration, IL-2 and Lptn are secreted by the IL-2/Lptn gene-modified allogeneic neuroblastoma tumor cell vaccine, potentially enhancing the cytotoxic T lymphocyte (CTL) response elicited by vaccine neuroblastoma tumor-associated antigens (TAAs) against host neuroblastoma tumor cells. Produced by activated progenitor T cells, Lptn belongs to the C chemokine subfamily and is a potent chemotactic factor for lymphocytes; IL-2 stimulates natural killer (NK) cells and may enhance a vaccine-elicited CTL immune response against tumor cells. C78487 601193 PSMA/TARP peptide vaccine A peptide-based cancer vaccine containing epitopes of T cell receptor gamma-chain alternate reading frame protein (TARP) and prostate-specific membrane antigen (PSMA) in combination with a Poly IC-LC immunoadjuvant, with potential antineoplastic activity. Upon administration, PSMA/TARP peptide vaccine may stimulate a host cytotoxic T-cell (CTL) response against TARP- and PSMA-expressing tumor cells, resulting in tumor cell cytotoxicity. The nuclear protein TARP and PSMA are commonly expressed in prostate cancer cells. C78819 601195 PADRE-CMV fusion peptide vaccine A peptide-based vaccine containing a pan HLA DR-binding epitope (PADRE) fused to a cytomegalovirus (CMV) peptide epitope, with potential anti-viral and immunomodulating activities. Upon administration, PADRE-CMV fusion peptide may stimulate a cytotoxic T-lymphocyte (CTL) response against CMV in the CMV-infected host. The synthetic peptide PADRE is a universal helper T cell epitope. C78820 601198 tetanus-CMV fusion peptide vaccine A vaccine containing an inactivated epitope of tetanus toxin fused to a cytomegalovirus (CMV) peptide epitope, with potential anti-viral and immunomodulating activities. Upon administration, tetanus-CMV fusion peptide may stimulate a cytotoxic T-lymphocyte (CTL) response against CMV in the CMV-infected host. Tetanus toxin contains universal T cell helper epitopes. C78821 601204 STAT3 decoy oligonucleotide A double-stranded 15-mer oligonucleotide, corresponding closely to the signal transducer and activator of transcription 3 (STAT3) response element within the c-fos promoter, with potential antineoplastic activity. STAT3 decoy oligonucleotide binds specifically to activated STAT3 and blocks binding of STAT3 to DNA sequences on a variety of STAT3-responsive promoters, which results in the inhibition of STAT3-mediated transcription and, potentially, the inhibition of tumor cell proliferation. STAT3 is constitutively activated in a variety of cancers including squamous cell carcinoma of the head and neck, contributing to the loss of cell growth control and neoplastic transformation. C78822 601215 autologous PBTL CD19CAR-28 zeta A preparation of autologous peripheral blood T-lymphocytes (PBTL) that have been genetically modified to express the chimeric antigen receptor (CAR) anti-CD19/CD3 zeta chain fusion protein coupled to the intracellular signal domain of CD28 antigen, with potential immunostimulating and antineoplastic activities. Upon administration, autologous PBTL CD19CAR-28 zeta may stimulate host cytotoxic T lymphocyte (CTL) and antibody responses against CD19-expressing tumor cells, resulting in tumor cell lysis. CD19 antigen is a B-cell specific cell surface antigen expressed in all B-cell lineage malignancies. CD3 zeta is one of several membrane-bound polypeptides found in the T-cell receptor (TCR)/CD3 complex and regulates the assembly of complete TCR complexes and their expression on the cell surface. CD28 is essential for CD4+ T-cell proliferation, interleukin-2 production, and T-helper type-2 (Th2) development. C78823 601216 autologous EBV-CTL CD19CAR zeta Autologous Epstein-Barr virus (EBV)-specific cytotoxic T-lymphocytes (CTL) that have been genetically modified to express a T-cell chimeric antigen receptor (CAR) targeting the CD19 antigen, with potential immunotherapeutic activity. The CAR consists of a single chain Fv of anti-CD19 IgG1 coupled with an intracellular signaling region of the zeta-chain of the TCR/CD3 complex (CD3 zeta). Autologous EBV-CTL CD19CAR zeta directs the T-lymphocytes to CD19-expressing tumor cells, stimulating a selective toxicity to tumor cells. CD19 antigen is a B-cell specific cell surface antigen expressed in all B-cell lineage malignancies. C78824 601485 anthracycline analogue GPX-150 A synthetic non-cardiotoxic analogue of the anthracycline antibiotic doxorubicin with potential antineoplastic activity. Anthracycline analogue GPX-150 intercalates DNA and impedes the activity of topoisomerase II, inducing single and double-stranded breaks in DNA; inhibiting DNA replication and/or repair, transcription, and protein synthesis; and activating tumor cell apoptosis. C78863 601486 PI3K delta inhibitor CAL-101 A small molecule inhibitor of the delta isoform of the 110 kDa catalytic subunit of class IA phosphoinositide-3 kinases (PI3K) with potential immunomodulating and antineoplastic activities. PI3K-delta inhibitor CAL-101 inhibits the production of the second messenger phosphatidylinositol-3,4,5-trisphosphate (PIP3), preventing the activation of the PI3K signaling pathway and thus inhibiting tumor cell proliferation, motility, and survival. Unlike other isoforms of PI3K, PI3K-delta is expressed primarily in hematopoietic lineages. The targeted inhibition of PI3K-delta is designed to preserve PI3K signaling in normal, non-neoplastic cells. C78825 601797 anti-DR5 agonist monoclonal antibody TRA-8 An agonist mouse monoclonal antibody directed against TRAIL death receptor type 5 (DR5) with potential antineoplastic activity. Anti-DR5 agonist monoclonal antibody TRA-8 binds DR5, which may induce apoptosis in DR5-expressing tumor cells. DR5 is a tumor cell surface ligand that crosslinks with death receptor type 4 (DR4) when bound by TRAIL [Tumor necrosis (TNF)-related apoptosis-inducing ligand], triggering apoptosis via a death receptor signaling pathway. The apoptotic activity of this antibody may not require DR4/DR5 crosslinking. C78826 601822 123-I-MIP-1072 An iodine 123-radiolabled small molecule that exhibits high affinity for prostate-specific membrane antigen (PSMA) with potential use in molecular imaging. 123-I-MIP-1072, a radiolabeled glutamate-urea-lysine analogue, selectively binds PSMA, which allows imaging of PSMA-expressing prostate cancer cells with gamma scintigraph. PSMA is a transmembrane glycoprotein highly expressed by malignant prostate epithelial cells and vascular endothelial cells of various solid tumors. C78827 601823 123-I-MIP-1095 An iodine 123-radiolabled small molecule that exhibits high affinity for prostate-specific membrane antigen (PSMA) with potential use in molecular imaging. 123-I-MIP-1095, a radiolabeled glutamate-urea-lysine analogue, selectively binds PSMA, which allows imaging of PSMA-expressing prostate cancer cells with gamma scintigraph. PSMA is a transmembrane glycoprotein highly expressed by malignant prostate epithelial cells and vascular endothelial cells of various solid tumors. C78828 601870 CD4+CD25+ regulatory T cells Regulatory T cells that express CD4 and CD25 (interleukin 2 receptor) antigens, with immunomodulating activity.. CD4+CD25+ T regulatory cells (Tregs), a subset of CD4+ T cells expressing high levels of CD25 and the transcription factor Foxp3, are essential in maintaining immunologic homeostasis, preventing autoimmunity by suppressing self-reactive T cells; CD4+CD25+ Tregs may induce tolerance to allogeneic organ transplants such as hematopoetic stem cell transplants (HSCTs). C78829 601895 autologous OFA-iLRP RNA-transfected dendritic cell vaccine A cancer vaccine consisting of autologous, mature monocyte-derived dendritic cells (DCs) transfected with oncofetal antigen immature laminin receptor protein (OFA-iLRP) RNA, with potential antineoplastic activity. Upon administration, DCs in the OFA-iLRP RNA-transfected autologous dendritic cell vaccine express, process, and present OFA-iLRP to the host immune system, which may mount a potent cytotoxic T-cell (CTL) response against OFA-iLRP-expressing tumor cells. As a highly conserved protein, OFA-iLRP is preferentially expressed in fetal tissues and in many types of cancer, including hematopoietic malignancies, but is not detectable in normal differentiated adult cells. C78830 601981 allogeneic melanoma vaccine AGI-101H A cancer vaccine derived from two gentically modified human melanoma cell lines with potential antineoplastic activity. Allogeneic melanoma vaccine AGI-101H consists of a 1:1 mixture of cells from two genetically modified human melanoma cell lines, designated as Mich1H6 and Mich2H6, that have been gamma-irradiated to render the cells non-proliferative. Upon administration, this vaccine may stimulate a cytotoxic immune response against melanoma tumor cells. C78861 601983 androstane steroid HE3235 An orally bioavailable adrenal steroid analogue with potential antineoplastic activity. Androstane steroid HE3235 appears to bind the androgen receptor (AR), down-regulating anti-apoptotic genes, such as Bcl-2, while increasing the expression of pro-apoptotic genes, such as caspases. In vitro and in vivo studies indicate that this agent\ninhibits androstenediol-dependent LNCaP cell tumor growth. In addition, HE3235 may potentiate chemotherapeutic agents by down-regulating ABCG2, the gene encoding the multi-drug resistant (MDR) protein MDR2. C78831 602166 allogeneic large multivalent immunogen melanoma vaccine LP2307 A cancer vaccine, containing human-specific large multivalent immunogen (LMI) isolated from plasma membrane fractions of the melanoma cell lines MSM-M1 and MSM-M2, with potential immunostimulating and antineoplastic activities. Upon administration, allogeneic large multivalent immunogen melanoma vaccine LP2307 may stimulate a CD8+ cytotoxic T lymphocyte (CTL) response against melanoma tumor cells that express melanoma-specific LMI. C78862 609860 LV.IL-2/B7.1-transduced AML blast vaccine A whole-cell cancer vaccine, containing human acute myeloid leukemic (AML) blasts that have been genetically engineered to express a B7.1/IIL-2 fusion protein encoded by a self-inactivating lentiviral vector (LV), with potential antineoplastic and immunomodulating activities. Upon administration, LV.IL-2/B7.1-transduced AML blast vaccine may stimulate a host cytotoxic T lymphocyte (CTL) response against AML cells. The single fusion protein encoded by the LV is postsynthetically cleaved to produce biologically active membrane-anchored B7.1 and secreted IL-2 in AML blasts; combined expression of IL-2 and the co-stimulatory molecule B7.1 by AML blasts may increase stimulation of both allogeneic and autologous cytotoxic T cells. C78832 609870 fusidic acid/betamethasome valerate topical cream A topical cream formulation of the bacteriostatic antibiotic fusidic acid and the synthetic, long-acting glucocorticoid betametasone valerate with potential anti-bacterial and immunomodulating activities. Fusidic acid/betamethasone valerate topical cream inhibits Gram-positive bacterial protein synthesis and replication and inhibits the inflammatory response by preventing phospholipid release, inhibiting eosinophil activity, and decreasing pro-inflammatory cytokine production. C78833 609874 erythromycin topical cream A topical cream formulation containing the broad-spectrum macrolide antibiotic erythromycin with anti-bacterial activity. Erythromycin interacts with the 50S subunit of the bacterial 70S ribosomal RNA complex resulting in the inhibition of protein synthesis and bacterial cell death. C78834 609877 derma-membrane-structure topical cream A topical cream formulation containing physiological lipids with potential anti-xerotic activity. Derma-membrane-structure topical cream contains ingredients that mirror the lipid component of the the skin, including hydrated phosphatidyl choline, but does not contain conventional emulsifiers that may disrupt the skin-lipid barrier. This cream can also be used as a vehicle or base for topically applied medications. C78835 609881 pomegranate-extract pill A pill formulation of polyphenol extracts derived from the fruit of the deciduous shrub Punica granatum with antioxidant and potential chemopreventive activities. By binding and neutralizing free-radical compounds, the polyphenol extracts contained in pomegranate-extract pill may prevent their genotoxic and carcinogenic effects. C78864 609888 oral JAK2 inhibitor SB1518 An orally bioavailable inhibitor of Janus kinase 2 (JAK2) and the JAK2 mutant JAK2V617F with potential antineoplastic activity. Oral JAK2 inhibitor SB1518 competes with JAK2 for ATP binding, which may result in inhibition of JAK2 activation, inhibition of the JAK-STAT signaling pathway, and so caspase-dependent apoptosis. JAK2 is the most common mutated gene in bcr-abl-negative myeloproliferative disorders; the JAK2V617F gain-of-function mutation involves a valine-to-phenylalanine modification at position 617. The JAK-STAT signaling pathway is a major mediator of cytokine activity. C78837 609889 anti-EGFR monoclonal antibody RO5083945 A glycoengineered monoclonal antibody directed against the epidermal growth factor receptor (EGFR) with potential antineoplastic activity. anti-EGFR monoclonal antibody RO5083945 binds to the extracellular domain of EGFR, preventing the activation and subsequent dimerization of the receptor; the decrease in receptor activation and dimerization may result in an inhibition of downstream ERK and JNK signaling pathways and so inhibition of EGFR-dependent tumor cell proliferation and metastasis. EGFR, a member of the epidermal growth factor family of extracellular protein ligands, may be overexpressed on the cell surfaces of various solid tumor cell types. C78838 609890 anti-integrin monoclonal antibody-DM4 immunoconjugate IMGN388 An immunoconjugate consisting of an anti-integrin monoclonal antibody covalently attached to the maytansinoid DM4, a derivative of the cytotoxic agent maytansine (DM1), with potential antineoplastic activity. Anti-integrin monoclonal antibody-DM4 immunoconjugate IMGN388 binds to tumor cell surface integrins; upon internalization, the DM4 moiety is released from the immunoconjugate, binding to tubulin and disrupting microtubule assembly/disassembly dynamics, which may result in inhibition of cell division and cell growth of integrin-expressing tumor cells. Integrins, a class of transmembrane cell surface receptors, link the extracellular matrix (ECM) to intracellular signaling pathways that control cell proliferation and differentiation. C78839 609930 anti-myeloma monoclonal antibody-DM4 immunoconjugate BT-062 An immunoconjugate consisting of a monoclonal antibody directed against a highly-expressed myleoma cell surface antigen covalently attached to the maytansinoid DM4, a derivative of the cytotoxic agent maytansine (DM1), with potential antineoplastic activity. Anti-myeloma monoclonal antibody-DM4 immunoconjugate BT-062 binds to an unspecified cell surface antigen highly expressed on myeloma cells; upon internaliization the DM4 moiety is released, binding to tubulin and disrupting microtubule assembly/disassembly dynamics, which may result in the inhibition of cell division and cell growth of myeloma tumor cells. C78840 610129 HDAC inhibitor PCI-24781 A broad-spectrum phenyl hydroxamic acid inhibitor of histone deacetylase (HDAC) with potential antineoplastic activity. HDAC inhibitor PCI-24781 inhibits several isoforms of HDAC, resulting in an accumulation of highly acetylated histones, followed by the induction of chromatin remodeling; the selective transcription of tumor suppressor genes; and the tumor suppressor protein-mediated inhibition of tumor cell division and induction of tumor cell apoptosis. In addition, this agent has been shown to inhibit homologous recombination (HR) activity by inhibiting the expression of RAD51. RAD51, a homologue of bacterial RecA, assists in the repair of DNA double-strand breaks (DSBs). C68920 610130 tubulin inhibitor ALB 109564(a) A semi-synthetic derivative of the vinka alkaloid vinblastine with potential antineoplastic activity. Tubulin inhibitor ALB 109564(a) binds to tubulin monomers and inhibits microtubule formation, resulting in disruption of mitotic spindle assembly and arrest of tumor cells in the G2/M phase of the cell cycle. C78842 610131 oral Hsp90 inhibitor IPI-493 An orally bioavailable formulation of the ansamycin derivative 17-amino-17-demethoxygeldanamycin (17-AG) with potential antineoplastic activity. Oral Hsp90 inhibitor IPI-493 binds to and inhibits Hsp90, which may result the in growth inhibition in sensitive tumor cell populations. Hsp90, a 90 kDa molecular chaperone, may be highly expressed in tumor cells, playing a key role in the conformational maturation, stability and function of other substrate or "client" proteins within the cell; many of these client proteins are involved in signal transduction, cell cycle regulation and apoptosis, and may include kinases, transcription factors and hormone receptors. C78843 610132 WT1-A10/AS01B immunotherapeutic GSK2130579A An immunotherapeutic consisting of the recombinant fusion protein WT1-A10 combined with the adjuvant ASO1B with potential immunostimulating and antineoplastic activities. Upon administration, WT1-A10/AS01B immunotherapeutic GSK2130579AWT1 may induce a WT1-specific cytotoxic T-lymphocyte (CTL) response against WT1-expressing tumor cells, resulting in cell lysis and the inhibition of cellular proliferation. The tumor-associated antigen WT1 (Wilms tumor protein-1) is overexpressed in most types of leukemia and in a variety of solid cancers. WT1-A10 is a 292 amino acid recombinant fusion protein consisting of a 12-mer truncated tat sequence (leader sequence) and amino acids number 2-281 of the WT1 sequence; ASO1B consists of a combination of the adjuvants monophosporyl lipd A (MPL) and Q21. C78865 610133 anti-HGF monoclonal antibody SCH900105 A monoclonal antibody directed against human hepatocyte growth factor (HGF) with potential antineoplastic activity. Anti-HGF monoclonal antibody SCH900105 binds to the soluble ligand HGF, preventing the binding of HGF to its receptor c-Met and activation of the HGF/c-Met signaling pathway, which may result in cell death in c-Met-expressing tumor cells. c-Met, a receptor tyrosine kinase overexpressed or mutated in many tumor cell types, plays a key role in cancer cell growth, survival, angiogenesis, invasion, and metastasis. C78844 611933 tetrodotoxin A neurotoxin with potential analgesic activity. Tetrodotoxin binds to the pores of fast voltage-gated fast sodium channels in nerve cell membranes, inhibiting nerve action potentials and blocking nerve transmission. Although found in various species of fish (such as the pufferfish), newts, frogs, flatworms, and crabs, tetrodotoxin, for which there is no known antidote, is actually produced by bacteria such as Vibrio alginolyticus, Pseudoalteromonas tetraodonis, and other vibrio and pseudomonas bacterial species. C78845 612037 Hsp90 inhibitor BIIB028 A small-molecule inhibitor of heat shock protein (Hsp) 90 with potential antineoplastic activity. Hsp90 inhibitor BIIB028 blocks the binding of oncogenic client proteins to Hsp90, which may result in the proteasomal degradation of these proteins and so the inhibition of tumor cell proliferation. Hsp90 is a molecular chaperone that plays a key role in the conformational maturation of oncogenic signaling proteins, such as Her2/Erbb2, Akt, Raf1, Bcr-Abl, and mutated p53, in addition to other molecules involved in cell cycle regulation and immune responses. C78846 612038 PI3K inhibitor PX-866 A small-molecule wortmannin analogue inhibitor of the alpha, gamma, and delta isoforms of phosphoinositide 3-kinase (PI3K) with potential antineoplastic activity. PI3K inhibitor PX-866 inhibits the production of the secondary messenger phosphatidylinositol-3,4,5-trisphosphate (PIP3) and activation of the PI3K/Akt signaling pathway, which may result in inhibition of tumor cell growth and survival in susceptible tumor cell populations. Activation of the PI3K/Akt signaling pathway is frequently associated with tumorigenesis and dysregulated PI3K/Akt signaling may contribute to tumor resistance to a variety of antineoplastic agents. C78848 612154 curcumin/green tea extract/Polygonum cuspidatum extract/soybean extract capsule An oral capsule containing curcumin, green tea extract, Polygonum cuspidatum extract, and soybean extract, with antioxidant and potential chemopreventive activities. The antioxidants in curcumin/green tea extract/Polygonum cuspidatum extract/soybean extract capsule bind to and neutraliize free-radicals, which may prevent their genotoxic and carcinogenic effects. C78849 612729 HDAC/EGFR/Her2 inhibitor CUDC-101 A multi-targeted, small-molecule inhibitor of histone deacetylase (HDAC), epidermal growth factor receptor tyrosine kinase (EGFR/ErbB1), and human epidermal growth factor receptor 2 tyrosine kinase (HER2/neu or ErbB2) with potential antineoplastic activity. HDAC/EGFR/HER2 inhibitor CUDC-101 inhibits the activity of these three enzymes but the exact mechanism of action is presently unknown. This agent may help overcome resistance to inhibition of EGFR and Her2 through a simultaneous, synergistic inhibition of EGFR, Her2, and HDAC. C78850 612730 anti-PD-L1 monoclonal antibody MDX-1105 A fully human monoclonal antibody directed against the protein ligand PD-L1 (Programmed Death-1 Ligand 1) with immunomodulating and potential antineoplastic activities. Anti-PD-L1 monoclonal antibody MDX-1105 binds to PD-L1, blocking its binding to and activation of its receptor, PD-1 (Programmed Death 1), which may enhance the T-cell-mediated immune response to neoplasms and reverse T-cell inactivation in chronic infectious disease. PD-L1 is expressed broadly on hematopoietic and parenchymal tissues; PD-1, a transmembrane protein, is a negative regulator of the immune system that limits the expansion and survival of CD8+ T cells. C78852 612849 anti-HER3 monoclonal antibody U3-1287 A fully human monoclonal antibody directed against the membrane-bound receptor HER3 (ERBB3) with potential antineoplastic activity. Anti-HER3 monoclonal antibody U3-1287 binds to and inhibits HER3 activation, which may result in inhibition of HER3-dependent PI3K/Akt signaling and so inhibition of cellular proliferation and differentiation. HER3, a member of the epidermal growth factor receptor (EGFR) family of receptor tyrosine kinases, is frequently overexpressed in solid tumors, including breast, lung, and colorectal tumors of epithelial origin; it has no active kinase domain itself but is activated through heterodimerization with other members of the EGFR receptor family that do. C78853 612855 dinaciclib A pyrazolo[1,5-a]pyrimidine with potential antineoplastic activity. Dinaciclib selectively inhibits cyclin dependent kinases CDK1, CDK2, CDK5, and CDK9; inhibition of CDK1 and CDK2 may result in cell cycle repression and tumor cell apoptosis. C78854 612860 mTOR kinase inhibitor AZD8055 An inhibitor of the mammalian target of rapamycin (mTOR) with potential antineoplastic activity. mTOR kinase inhibitor AZD8055 inhibits the serine/threonine kinase activity of mTOR, resulting in decreased expression of mRNAs necessary for cell cycle progression, which may induce cell cycle arrest and tumor cell apoptosis. mTOR phosphorylates transcription factors, such as S6K1 and 4E-BP1, which stimulate protein synthesis and regulate cell growth, proliferation, motility, and survival. C78856 613221 pomegranate liquid extract A liquid extract preparation derived from pomegranate (Punica granatum) seeds with antioxidant, and potential antineoplastic and chemopreventive activities. Pomegranate liquid extract contains flavonoids which may promote differentiation and apoptosis in tumor cells by down-regulating vascular endothelial growth factor (VEGF) and stimulating migration inhibitory factor (MIF), thus inhibiting angiogenesis.Pomegranate liquid extract flavanoids also scavenge reactive oxygen species (ROS) and, in some cell types, may prevent ROS-mediated cell injury and death. C78866 613506 calcium aluminosilicate anti-diarrheal A clay compound consisting of aluminosilicate and calcium ions with potential antidiarrheal activity. Calcium aluminosilicate anti-diarrheal consists of microscopically large flat plates of aluminosilicate separated by calcium ions that may sorb toxic chemotherapeutic drugs and their metabolites and inflammatory proteins such as TNF-alpha, which may help minimize chemotherapy-mediated or radiation therapy-mediated damage to the intestinal epithelium and so therapy-related diarrhea. C78858 613844 anti-ErbB3 receptor monoclonal antibody MM-121 A fully human monoclonal antibody directed against the human epidermal growth factor receptor ErbB3 (Her3) with potential antineoplastic activity. Anti-ErbB3 receptor monoclonal antibody MM-121 binds to binds to and inhibits ErbB3 activation, which may result in inhibition of ErbB3-dependent PI3K/Akt signaling and so inhibition of cellular proliferation and differentiation. ErbB3, a member of the epidermal growth factor receptor (EGFR) family of receptor tyrosine kinases, is frequently overexpressed in solid tumors, including breast, lung, and colorectal tumors of epithelial origin; it has no active kinase domain itself but is activated through heterodimerization with other members of the EGFR receptor family that do. C78859 613893 anti-TweakR monoclonal antibody PDL192 A humanized monoclonal antibody directed against the tumor necrosis factor-like weak inducer of apoptosis receptor (TWEAKR) with potential antineoplastic, immunomodulating and antiangiogenic activities. Anti-TWEAKR monoclonal antibody PDL192 binds to TWEAKR and inhibits TWEAK ligand binding and activation of NF-kappaB-mediated cytokine release, which may result in tumor cell apoptosis. TWEAKR is a cell-surface receptor with homology to tumor necrosis factor receptors. Upon binding with its ligand, TWEAKR has been shown to stimulate cytokine release and cell proliferation, migration, and survival; it may also promote apoptosis under some conditions. This receptor may be overexpressed in a variety of tumors including those of the pancreas, colon, lung, kidney, and breast. C80045 614024 3'-C-ethynylcytidine A synthetic cytidine nucleoside containing a covalently bound ethynyl group with potential antineoplastic and radiosensitizing activities. 3'-C-ethynylcytidine is metabolized in tumor cells to ethynylcytidine triphosphate (ECTP), which inhibits RNA synthesis by competitive inhibition of RNA polymerases I, II and III; subsequently, RNase L is activated, resulting in apoptosis. RNase L is a potent antiviral and antiproliferative endoribonuclease that cleaves singled stranded RNA, causes 28s rRNA fragmentation, and activates Janus Kinase (JAK), a mitochondrial-dependent apoptosis signaling molecule. C80037 614254 anti-DKK1 monoclonal antibody BHQ880 A humanized monoclonal antibody directed against Wnt antagonist Dickkopf-1 (DKK1) with potential anti-osteolytic activity. Anti-DKK1 monoclonal antibody BHQ880 binds to and inhibits DKK1, enhancing signaling through the Wnt pathway, which may result in osteoblast differentiation and activation within the bone matrix and the reversal of tumor-induced osteolytic disease. DKK! is a potent Wnt signaling pathway antagonist. C80040 614265 alpha-lipoic acid analogue CPI-613 A racemic mixture of the enantiomers of a synthetic alpha-lipoic lipoic acid analogue with potential chemopreventive and antineoplastic activities. Although the exact mechanism of action is unknown, alpha-lipoic acid analogue CPI-613 has been shown to inhibit metabolic and regulatory processes required for cell growth in solid tumors. Both enantiomers in the racemic mixture exhibit antineoplastic activity. C80039 614594 retinoid 9cUAB30 A synthetic analogue of 9-cis retinoic acid with potential antineoplastic and chemopreventive activities. Retinoid 9cUAB30 binds to and activates retinoid X receptor (RXR) homodimers and/or and retinoic acid receptor (RAR)/RXR heterodimers, which may result in the dissociation of corepressor protein and the recruitment of coactivator protein, followed by transcription of downstream target genes into mRNAs and protein translation. Gene transcription regulated by these transcription factors may result in inhibition of cell proliferation, induction of cell differentiation, and apoptosis of both normal cells and tumor cells. C80061 614606 copper gluconate The orally bioavailable copper salt of D-gluconic acid. In addition to its roles as an enzyme cofactor for cytochrome C oxidase and superoxide dismutase, copper forms complexes with the thiocarbamate disulfiram (DSF) forming DSF-copper complexes, which enhances the DSF-mediated inhibition of the 26S proteasome; proteasome inhibition may result in inhibition of cellular protein degradation, cessation of cell cycle progression, inhibition of cellular proliferation, and the induction of apoptosis in susceptible tumor cell populations. C80050 614649 amitriptyline hydrochloride The hydrochloride salt of the tricyclic dibenzocycloheptadiene amitriptyline with antidepressant and antinociceptive activities. Amitriptyline inhibits the re-uptake of norepinephrine and serotonin by the presynaptic neuronal membrane in the central nervous system (CNS), thereby increasing the synaptic concentration of norepinephrine and serotonin. Due to constant stimulation to these receptors, amitriptyline may produce a downregulation of adrenergic and serotonin receptors, which may contribute to the antidepressant activity. In the CNS the antinociceptive activity of this agent may involve high affinity binding to and inhibition of N-methyl-D-aspartate (NMDA) receptors and/or the enhancement of the action of serotonin at the spinal terminals of an opioid-mediated intrinsic analgesia system. 614666 anti-GD2 monoclonal antibody hu14.18K322A A monoclonal antibody directed against human glycosphingolipid GD2 with potential antineoplastic activity. Upon binding to the GD2 antigen, anti-GD2 monoclonal antibody hu14.18K322A triggers a host immune response against GD2-expressing tumor cells, which may result in tumor cell death. GD2, an O-acetylated disialoganglioside with expression in normal tissues restricted primarily to the cerebellum and peripheral nerves, is commonly expressed at high levels on tumors of neuroectodermal origins such as melanomas and neuroblastomas. C80042 614677 anti-DLL4 monoclonal antibody OMP-21M18 A humanized monoclonal antibody directed against the N-terminal epitope of Notch ligand DLL4 (delta-like 4) with potential antineoplastic activity. Anti-DLL4 monoclonal antibody OMP-21M18 binds to the membrane-binding portion of DLL4 and prevents its interaction with Notch-1 and Notch-4 receptors, thereby inhibiting Notch-mediated signaling and gene transcription, which may impede tumor angiogenesis. Activation of Notch receptors by DLL4 stimulates proteolytic cleavage of the Notch intracellular domain (NICD); after cleavage, NICD is translocated into the nucleus and mediates the transcriptional regulation of a variety of genes involved in vascular development. The expression of DLL4 is highly restricted to the vascular endothelium. C80041 614683 anti-GPC3 monoclonal antibody GC33 A humanized monoclonal antibody directed against the cell surface oncofetal protein glypican-3 (GPC3) with potential antineoplastic activity. Anti-GPC3 monoclonal antibody GC33 binds to GPC3 and triggers a host immune response against GPC3-expressing tumor cells, which may result in tumor cell death. GPC3, a heparin sulfate proteoglycan, is frequently upregulated in hepatocellular carcinoma and mesoderm-derived organs such as the liver, lungs, and kidney. C80043 614830 cyclosporine ophthalmic emulsion An topical ophthalmic formulation containing cyclosporine, an undecapeptide produced by the fungus Beauveria nivea, with immunosuppressant and anti-inflammatory activities. The exact therapeutic mechanism of action of cyclosporine is not known but may involve binding to the cellular protein cytophilin, resulting in inhibition of the enzyme calcineurin. This agent appears to specifically and reversibly inhibit immunocompetent lymphocytes in the G0-or G1-phase of the cell cycle. T-lymphocytes are preferentially inhibited with T-helper cells as the primary target. Cyclosporine also inhibits lymphokine production and release. C80051 615086 L-carnitine L-tartrate A dietary supplement containing the levo-enantiomers of carnitine and tartrate with potential chemoprotective and antioxidant activities. L-carnitine L-tartrate increases fatty acid oxidation and reduces purine catabolism and free radical formation, which may prevent exercise fatigue, muscle weakness, chemotherapy-induced peripheral neuropathy, and hyperlipoproteinemia. L-carnitine, the biologically active form of carnitine, is a carrier molecule that transports activated long-chain fatty acids (LCFAs)from the cytosol to mitochondria where fatty acids are oxidized, resulting in ATP production,. L-tartrate, a salt of tartaric acid, is a potent antioxidant. C80057 615096 camptothecin analogue TLC388 A synthetic analogue of camptothecin with potential antineoplastic and radio-sensitizing activities. Camptothecin analogue TLC388 selectively stabilizes topoisomerase I-DNA covalent complexes during S-phase, thereby inhibiting religation of topoisomerase I-mediated single-strand DNA breaks and producing potentially lethal double-strand DNA breaks when encountered by the DNA replication machinery. Topoisomerase I relaxes negative super-coiled DNA during replication and transcription. This agent has been chemically modified to enhance the potency and stability of camptothecin. C80047 615097 131-I-MIP-1145 An iodine 131-radiolabeled small-molecule benzamide compound with potential antineoplastic activity. The benzamide moiety of 131-I-MIP-1145 binds to melanin, selectively delivering a cyotoxic dose of gamma and beta radiation to melanin-expressing tumor cells. Melanin pigments, polymer derivatives of the amino acid tyrosine, are over-expressed in approximately 40% of melanomas. C80056 615142 caricotamide/tretazicar A combination therapy consisting of the prodrug tretazicar and the enzyme co-substrate caricotamide with potential antineoplastic activity. In the presence of separately and simultaneously administered caricotamide, tretazicar is converted to the short-lived cytotoxic DNA cross-linking agent dinitrobenzamide by NAD(P)H quinine oxidoreductase 2 (NQO2), resulting in the inhibition of DNA replication and the induction of apoptosis. NQO2 has been found to be elevated in certain cancers such as hepatocellular carcinoma (HCC). C80048 615145 B16alphaGal melanoma vaccine A whole cell melanoma cancer vaccine with potential immunostimulating and antineoplastic activities. B16alphaGal melanoma vaccine contains three types of human melanoma cell lines that are genetically engineered to express the alpha(1,3)-galactosyl (alphaGal) epitope on cell surfaces. The agent stimulates a hyperacute rejection of whole melanoma cancer cells expressing alphaGal epitopes, initiated by opsonization by anti-alphaGal antibodies and followed by antibody-dependent cell-mediated cytotoxicity (ADCC) and cell lysis. This results in the stimulation of a broader cytotoxic T-lymphocyte response (CTL) directed against tumor antigens on melanoma cells that do not express alphaGal. AlphaGal is not normally expressed in humans because alpha(1,3)-galactosyltransferase (Alpha-GT), the enzyme that catalyzes the synthesis of alphaGal epitopes on glycoproteins and glycolipids, is not naturally present in humans and other primates. C80046 615188 decoy activin receptor ACE-011 A soluble fusion protein composed of the extracellular domain of the activin receptor type IIA (ActRIIA) linked to the Fc portion of human IgG1 with anabolic bone activity. Decoy activin receptor ACE-011 selectively binds to activin, inhibiting its binding to ActRIIA and ActRIIA signaling, resulting in the stimulation of osteoblast activity and the inhibition of osteoclast activity and so normal bone formation and increased bone mineral density and strength. The Fc moiety of this fusion protein binds to the salvage receptor FcRN, preventing its lysosomal degradation and so extending its half-life in the circulatory system. C80038 615263 PARP inhibitor MK4827 An inhibitor of poly (ADP-ribose) polymerase (PARP) with potential antineoplastic activity. PARP Inhibitor MK4827 inhibits PARP activity, enhancing the accumulation of DNA strand breaks and promoting genomic instability and apoptosis. The PARP family of proteins detect and repair single strand DNA breaks by the base-excision repair (BER) pathway. The specific PARP family member target for PARP inhibitor MK4827 is unknown. C80059 615423 macrogol 3350-based oral osmotic laxative An isotonic solution containing macrogol 3350 and electrolytes with laxative activity. Macrogol 3350-based oral osmotic laxative promotes the retention of water in the bowel, thereby increasing the water content of stool, which results in increased gastrointestinal motility and stool transit time and evacuation of colonic contents. Macrogol 3350 is also known as polyethylene glycol (PEG) 3350. C29080 615425 sodium picosulfate/magnesium oxide/citric acid oral laxative An oral laxative formulation containing the stimulant cathartic sodium picosulfate as the primary active ingredient . Picosulfate acts on the enteric nerves in the intestinal wall to increase muscle contractions, thereby stimulating peristaltic action and promoting defecation. Other active ingredients are osmotic agents that increase stool water content. C80015 615498 sodium biphosphate/sodium phosphate oral laxative An oral hyperosmotic saline laxative containing sodium biphosphate and sodium phosphate. Sodium phosphate/sodium biphosphate oral laxative promotes retention of water in the bowel, thereby increasing stool water content and volume, which results in increased gastrointestinal motility and stool transit time and evacuation of colonic contents. C29052 615652 technetium Tc 99m mebrofenin A radioconjugate composed of the iminodiacetic acid derivative mebrofenin bound to an isotope of the synthetic element technetium (Tc). Upon administration and rapid clearance form the circulation, technetium Tc 99m mebrofenin is secreted into the hepatobiliary system, emitting gamma rays that are detectable with planar scintigraphy or single photon emission computer tomography (SPECT). Mebrofenin has no pharmacological effect at the recommended dosage for diagnostic imagining. C80064 615723 hTERT vaccine V934/V935 A cancer vaccine directed against human telomerase reverse transcriptase (hTERT), the catalytic subunit of human telomerase, with potential immunostimulating and antineoplastic activities. Upon administration, hTERT vaccine V934/V935 may elicit a cytotoxic T cell (CTL) response against telomerase-expressing tumor cells, which may result in tumor cell death. Telomerase is involved in the restoration and maintenance of telomere length and so the functional lifespan of cells. Abnormally reactivated in tumorigenesis, telomerase is expressed in the majority of human cancer cells but is not expressed or is expressed at very low levels in normal cells. C80055 615854 sagopilone A fully synthetic low-molecular-weight epothilone with potential antineoplastic activity. Sagopilone binds to tubulin and induces microtubule polymerization while stabilizing microtubules against depolymerization, which may result in the inhibition of cell division, the induction of G2/M arrest, and apoptosis. The agent is not a substrate for the P-glycoprotein (P-gp) efflux pump and so may exhibit activity in multidrug-resistant (MDR) tumors. The epothilone class of metabolites was originally isolated from the myxobacterium Solangium cellulosum. C80062 615911 cytomegalovirus IE-1-specific cytotoxic T lymphocytes Cytotoxic T-lymphocytes (CTLs), specifically reactive to the cytomegalovirus (CMV) immediate early-1 (IE-1) protein, with immunomodulating activity. Adoptive immunotherapy with cytomegalovirus IE-1-specific cytotoxic T lymphocytes may help reconstitute CD8+ cytomegalovirus-specific CTL responses in CMV-infected immunocompromised hosts. IE-1 is one of the first CMV antigens expressed by CMV-infected cells, predominantly inducing a CD8+ CTL response. C80052 616102 2'-F-ara-deoxyuridine A deoxyuridine prodrug with potential antineoplastic activity. Upon cellular uptake, 2’-F-ara-deoxyuridine (FAU) is phosphorylated by thymidine kinase to FAU monophosphate and subsequently methylated in the 5'-position by thymidylate synthase (TS) to its activated form, 1-(2-deoxy-2-fluoro-beta-D-arabinofuranosyl) 5-methyluracil monophosphate (FMAUMP). FMAUMP is incorporated into DNA leading to an inhibition of DNA synthesis and so cell growth. The catalytic activity of TS is critical to activation of FAU and subsequent incorporation into DNA. FAU may be beneficial in the case of tumors with high TS activity that are resistant to TS inhibitors. C80036 616656 eritoran tetrasodium The tetrasodium salt of a synthetic analogue of the lipid A portion of the endotoxin lipopolysaccharide (LPS) with potential immunomodulating activity. Eritoran binds to the Toll-like receptor (TLR)/CD14/MD2 receptor complex present on most cells of the immune system, inhibiting the activation of the receptor complex by LPS, which may result in the inhibition of pro-inflammatory cytokine secretion and a potentially fatal systemic inflammatory response syndrome (SIRS). LPS is found in the outer membrane of Gram-negative bacteria and binds to the TLR/CD14/MD2 receptor complex of immune cells, especially macrophages, resulting in the release of pro-inflammatory cytokines. C80053 616875 Hedgehog pathway inhibitor IPI-926 An orally bioavailable, cyclopamine-derived inhibitor of the Hedgehog (Hh) pathway with potential antineoplastic activity. Specifically, Hedgehog pathway inhibitor IPI-926 binds to and inhibits the cell membrane-spanning G-protein coupled receptor SMO, which may result in the suppression of Hh pathway signaling and a decrease in tumor cell proliferation and survival. SMO is activated upon binding of Hh ligand to the cell surface receptor Patched (PTCH); inappropriate activation of Hh signaling and uncontrolled cellular proliferation may be associated with SMO mutations. The Hh signaling pathway plays an important role in proliferation of neuronal precursor cells in the developing cerebellum and other tissues. C80063 617168 gadobenate dimeglumine A gadolinium-based paramagnetic contrast agent. When placed in a magnetic field, gadobenate dimeglumine produces a large magnetic moment and so a large local magnetic field, which can enhance the relaxation rate of nearby protons; as a result, the signal intensity of tissue images observed with magnetic resonance imaging (MRI) may be enhanced. Because this agent is preferentially taken up by normal functioning hepatocytes, normal hepatic tissue is enhanced with MRI while tumor tissue is unenhanced. In addition, because gadobenate dimeglumine is excreted in the bile, it may be used to visualize the biliary system using MRI. C77547 617169 BLI850 An oral laxative containing sodium sulfate, potassium sulfate, magnesium sulfate and sucralose. Oral sulfate-based laxative BLI850 exhibits osmotic activity, attracting water into the intestinal tract from tissues and increasing the volume and the water content of the stool; gastrointestinal motility is stimulated, resulting in defecation. Sucralose, an artificial sweetener, may contribute to the laxative effect. C80080 617182 gadoxate disodium A paramagnetic contrast agent consisting of the disodium salt of the gadolinium ion chelated with the lipophilic moiety ethoxybenzyl (EOB) bound to diethylenetriamine pentaacetic acid (DTPA). When placed in a magnetic field, gadolinium produces a large magnetic moment and so a large local magnetic field, which can enhance the relaxation rate of nearby protons; as a result, the signal intensity of tissue images observed with magnetic resonance imaging (MRI) may be enhanced. Because this agent is preferentially taken up by normal functioning hepatocytes, normal hepatic tissue is enhanced with MRI while tumor tissue is unenhanced. In addition, because this agent is excreted in the bile, it may be used to visualize the biliary system using MRI. C77548 617258 artesunate A water-soluble, semi-synthetic derivative of the sesquiterpine lactone artemisinin with anti-malarial, anti-shistosomiasis, antiviral, and potential anti-neoplastic activities. Upon hydrolysis of artesunate’s active endoperoxide bridge moiety by liberated heme in parasite-infected red blood cells, reactive oxygen species and carbon-centered radicals form, which have been shown to damage and kill parasitic organisms. Additionally, in vitro studies demonstrate that this agent induces DNA breakage in a dose-dependent manner. Artesunate has also been shown to stimulate cell differentiation, arrest the cell cycle in the G1 and G2/M phases, inhibit cell proliferation, and induce apoptosis through mitochondrial and caspase signaling pathways. Artemisinin is isolated form the plant Artemisia annua. C73005 617377 topotecan hydrochloride liposomes The hydrochloride salt of a semisynthetic derivative of camptothecin mixed with sphingomyelin/cholesterol and sonicated to form small unilamellar vesicles containing topotecan, with potential antineoplastic activity. Topotecan hydrochloride liposomes mediates efficient drug delivery of topotecan into the cytosol from the endosome compartment. During the S phase of the cell cycle, topotecan selectively stabilizes topoisomerase I-DNA covalent complexes, inhibiting religation of topoisomerase I-mediated single-strand DNA breaks and producing potentially lethal double-strand DNA breaks when complexes are encountered by the DNA replication machinery. C80065 617378 Anti-M-CSF monoclonal antibody MCS110 A humanized monoclonal antibody directed against macrophage colony-stimulating factor (M-CSF) with potential anti-osteolytic activity. Anti-M-CSF monoclonal antibody MCS110 binds to M-CSF and blocks M-CSF-mediated signaling through the M-CSF receptor CD116 expressed on osteoclasts, which may result in inhibition of M-CSF-induced osteoclast differentiation and so osteoclastic bone resorption. Osteoclasts are derived through the fusion of cells of the monocyte/macrophage lineage. Osteoblasts and stromal cells may react to bone metastases by producing M-CSF and its osteoclastogenic cofactor RANKL (receptor activator of NF-kappaB ligand). C80044 617379 gamma-D-glutamyl-L-tryptophan An orally bioavailable synthetic peptide containing the amino acids D-glutamine and L-tryptophan connected by a gamma-glutamyl linkage with potential immunostimulating, antimicrobial and antineoplastic activities. Although the exact mechanism of action is unknown, gamma-D-glutamyl-L-tryptophan this agent appears to inhibit the expression of STAT-3, reversing immunosuppression and stimulating an anti-tumor immune response. This agent may stimulate the production of T-lymphocytes, in particular the helper T (Th1) cells, activate macrophages, and increase levels of interleukin 2 and interferon gamma. STAT-3, a transcription factor upregulated in many cancer cell types, is involved in tumor cell growth and survival and immunosuppression. C80054 617455 trabedersen A transforming growth factor (TGF)-beta2 specific phosphorothioate antisense oligodeoxynucleotide with the sequence 5'-CGGCATGTCTATTTTGTA-3', with potential antineoplastic activity. Trebedersen binds to TGF-beta2 mRNA causing inhibition of protein translation, thereby decreasing TGF-beta2 protein levels; decreasing intratumoral TGF-beta2 levels may result in the inhibition of tumor cell growth and migration, and tumor angiogenesis. TGF-beta2, a cytokine often over-expressed in various malignancies, may play an important role in promoting the growth, progression, and migration of tumor cells. C80066 617902 armodafinil The R-enantiomer of the racemic synthetic agent modafinil with central nervous system (CNS) stimulant and wakefulness-promoting activities. Although the exact mechanism of action has yet to be fully elucidated, armodafinil appears to inhibit the reuptake of dopamine by binding to the dopamine-reuptake pump, which leads to an increase in extracellular dopamine levels in some brain regions. This agent does not bind to or inhibit several receptors and enzymes that may be involved in sleep/wake regulation and is not a direct- or indirect-acting dopamine receptor agonist. Armodafinil has a longer half-life than modafinil. C65241 617992 fentanyl matrix transdermal patch A transdermal formulation containing the synthetic phenylpiperidine opioid agonist fentanyl, with analgesic activity. Upon topical administration, fentanyl diffuses from the transdermal patch through the skin, is transported via the systemic circulation, and selectively binds to the mu-receptor in the central nervous system (CNS), mimicking the effects of endogenous opiates. Stimulation of the mu-receptor inhibits adenyl cyclase activity, induces opening of G-protein-coupled inwardly rectifying potassium (GIRK) channels, and blocks the opening of N-type voltage-gated calcium channels, resulting in hyperpolarization and reduced neuronal excitability; in addition, neuronal release of neurotransmitters such as substance P, GABA, dopamine, acetylcholine and noradrenaline may decrease. C80067 618206 gadoterate meglumine A gadolinium chelate paramagnetic contrast agent. When placed in a magnetic field, gadoterate meglumine produces a large magnetic moment and so a large local magnetic field, which can enhance the relaxation rate of nearby protons; as a result, the signal intensity of tissue images observed with magnetic resonance imaging (MRI) may be enhanced. Because this agent is preferentially taken up by normal functioning hepatocytes, normal hepatic tissue is enhanced with MRI while tumor tissue is unenhanced. In addition, because gadobenate dimeglumine is excreted in the bile, it may be used to visualize the biliary system using MRI. C80124 618682 CDK4 inhibitor P1446A-05 A protein kinase inhibitor specific for the cyclin-dependent kinase 4 (CDK4) with potential antineoplastic activity. CDK4 inhibitor P1446A-05 specifically inhibits CDK4-mediated G1-S phase transition, arresting cell cycling and inhibiting cancer cell growth. The serine/threonine kinase CDK4 is found in a complex with D-type G1 cyclins and is the first kinase to become activated upon mitogenic stimulation, releasing cells from a quiescent stage into the G1/S growth cycling stage; CDK-cyclin complexes have been shown to phosphorylate the retinoblastoma (Rb) transcription factor in early G1, displacing histone deacetylase (HDAC) and blocking transcriptional repression. C80049 618692 Raf/MEK dual kinase inhibitor RO5126766 A protein kinase inhibitor specific for the Raf and MEK mitogen-activated protein kinases (MAPKs) with potential anti-neoplastic activity. Raf/MEK dual kinase Inhibitor RO5126766 specifically inhibits the kinase activities of Raf and MEK, resulting in the inhibition of of target gene transcription that promotes malignant transformation of cells. Both Raf and MEK are serine/threonine-specific kinases that respond to extracellular stimuli, such as mitogens, and are involved in the regulation of cellular processes, such as gene expression, mitosis, differentiation, and apoptosis. C80060 618712 recombinant human granulocyte colony-stimulating factor A recombinant therapeutic agent which is chemically identical to or similar to the endogenous cytokine granulocyte colony-stimulating factor (G-CSF). Secreted by monocytes, macrophages and neutrophils and other cells after activation, G-CSF stimulates the proliferation and differentiation of hematopoietic progenitor cells committed to the neutrophil/ granulocyte lineage. C1287 618858 VEGFR/PDGFR dual kinase inhibitor TAK-593 An oral formulation containing a small-molecule receptor tyrosine kinase inhibitor of both vascular endothelial growth factor receptor (VEGFR) and platelet-derived growth factor receptor (PDGFR) with potential antineoplastic activity. TAK-593 selectively binds to and inhibits VEGFR and PDGFR, which may result in the inhibition of angiogenesis and tumor cell proliferation. C79794 618862 anti-ganglioside GM2 monoclonal antibody BIW-8962 A humanized anti-ganglioside GM2 (GM2) monoclonal antibody with potential antineoplastic and immunomodulating activities. Upon administration, anti-ganglioside GM2 monoclonal antibody BIW-8962 may activate an antibody dependent cellular cytotoxicity (ADCC) against GM2-expressing tumor cells. GM2 is a tumor associated antigen (TAA) overexpressed on the surface of many cancer cells, such as multiple myeloma (MM) cells and neuroblastoma cells. C79795 619042 Lactobacillus acidophilus probiotic A probiotic containing the bacterium Lactobacillus acidophilus with potential antimicrobial and immunomodulatory activities. As a dietary supplement, Lactobacillus acidophilus (L. acidophilus), a naturally-occurring bacteria, may improve digestion and help maintain adequate colonization of the gastrointestinal (GI) tract by modulating the composition of the normal microflora. Because it produces lactic acid and hydrogen peroxide and other substances during fermentation, this bacterium creates an acidic environment unfavorable to pathogens such as Candida albicans. In addition, during colonization of the GI tract, L. acidophilus may form a protective barrier, preventing attachment of pathogens. Dietary supplementation with this bacterium has been shown to enhance natural and acquired immunity in mice. C79797 619043 anti-IGF-1R monoclonal antibody AVE1642 A humanized monoclonal antibody directed against the human insulin-like growth factor-1 receptor (IGF-1R/CD221) with potential antineoplastic activity. Anti-IGF-1R monoclonal antibody AVE1642 specifically binds to and blocks membrane-bound IGF-1R, preventing the binding of the natural ligand IGF-1 and the subsequent activation of PI3K/AKT signal transduction, which may result in the induction of apoptosis and a decrease in cellular proliferation. Activation of IGF-1R , a receptor tyrosine kinase of the insulin receptor superfamily overexpressed by various cancer cell types, stimulates cell proliferation, promotes angiogenesis, enables oncogenic transformation, and suppresses apoptosis. C79798 619122 allogeneic large multivalent immunogen breast cancer vaccine A cancer vaccine, containing human-specific large multivalent immunogens (LMIs) isolated from the membrane fraction of cells from a breast cancer cell line, with potential immunostimulatory and antineoplastic activities. Upon administration, allogeneic large multivalent immunogen breast cancer vaccine may stimulate a cytotoxic T lymphocyte (CTL) immune response against tumor cells that express the breast cancer cell-specific LMIs. C79799 619354 Ad5-CMV-NIS A recombinant type 5 adenovirus (Ad5), encoding the gene for the human sodium-iodide symporter (NIS) linked to the cytomegalovirus (CMV) promoter, with potential gene transfection activity. Upon intratumoral injection, Ad5-CMV-NIS is taken up by tumor cells, resulting in the cellular expression of NIS. Subsequently, orally administered iodine 131 is taken up by NIS-expressing tumor cells, which may result in the selective accumulation of a cytotoxic dose of beta and gamma radiation in non-thyroidal tumor cells, sparing adjacent normal tissue. NIS, an intrinsic membrane glycoprotein, is an ion pump that actively transports iodide into cells which concentrate iodine; in addition to thyroid epithelial cells, it is found in non-thyroidal tissues including the salivary glands, the gastric mucosa, and lactating mammary glands. C79800 624375 gemcitabine 5'-elaidic acid ester A lipophilic, unsaturated fatty acid ester derivative of gemcitabine (dFdC), an antimetabolite deoxynucleoside analogue, with potential antineoplastic activity. Upon hydrolysis intracellularly by esterases, the prodrug gemcitabine is converted into the active metabolites difluorodeoxycytidine di- and tri-phosphate (dFdCDP and dFdCTP) by deoxycytidine kinase. dFdCDP inhibits ribonucleotide reductase, thereby decreasing the deoxynucleotide pool available for DNA synthesis; dFdCTP is incorporated into DNA, resulting in DNA strand termination and apoptosis. Due to its lipophilicity, gemcitabine 5'-elaidic acid ester exhibits an increased cellular uptake and accumulation, resulting in an increased conversion to active metabolites, compared to gemcitabine. In addition, this formulation of gemcitabine may be less susceptible to deamination and deactivation by deoxycytidine deaminase. C79803 624396 Chk1 inhibitor SCH 900776 An agent targeting cell cycle checkpoint kinase 1 (Chk1) with potential radiosensitization and chemosensitization activities. Chk1 inhibitor SCH 900776 specifically binds to and inhibits Chk1, which may result in tumor cells bypassing Chk1-dependent cell cycle arrest in the S and G2/M phases to undergo DNA repair prior to entry into mitosis; tumor cells may thus be sensitized to the DNA-damaging effects of ionizing radiation and alkylating chemotherapeutic agents. Chk1 is an ATP-dependent serine-threonine kinase that in response to DNA damage phosphorylates cdc25 phosphatases, resulting in inhibitory tyrosine phosphorylation of CDK-cyclin complexes and cell cycle arrest. C79867 625428 anti-VEGFR-1 monoclonal antibody IMC-18F1 A fully human IgG1 monoclonal antibody directed against human vascular endothelial growth factor receptor 1 (VEGFR-1/FLT-1) with potential antiangiogenesis and antineoplastic activities. Anti-VEGFR-1 monoclonal antibody IMC-18F1 specifically binds to and inhibits the activity of VEGFR-1, which may prevent the activation of downstream signaling pathways and so inhibit tumor angiogenesis; the subsequent reduction in tumor nutrient supply may inhibit tumor cell proliferation. Tumor cell overexpression of VEGFR-1 may be associated with tumor angiogenesis and tumor cell proliferation and invasion; VEGFR-1 may modulate VEGFR-2 signaling. C79808 626093 synthetic colorectal tumor-associated peptides vaccine IMA910 A synthetic tumor-associated peptide (TUMAP)-based cancer vaccine directed against colorectal cancer with potential immunostimulatory and antineoplastic activities. Synthetic colorectal tumor-associated peptides vaccine IMA910 contains 13 different synthetic tumor-associated peptides (TUMAPs), each of which represents a tumor associated antigen (TAA) specific for colorectal cancer. Upon administration, this agent may elicit a cytotoxic T-lymphocyte (CTL) response against colorectal tumors expressing these TAAs, which may result in a reduction in colorectal tumor cell proliferation. C79806 626159 FAK inhibitor PF-04554878 An orally bioavailable, small-molecule focal adhesion kinase (FAK) inhibitor with potential antiangiogenic and antineoplastic activities. FAK inhibitor PF-04554878 inhibits FAK, which may prevent the integrin-mediated activation of several downstream signal transduction pathways, including ERK, JNK/MAPK and PI3K/Akt, thus inhibiting tumor cell migration, proliferation and survival. The tyrosine kinase FAK is , a signal transducer for integrins that is upregulated in many tumor cell types and is involved in tumor cell invasion, migration and proliferation. C79809 626166 copper Cu 64-ATSM A radioconjugate consisting of a lipophilic copper(II)bis(thiosemicarbazone) labeled with the positron- and beta-emitting isotope (64)Cu with hypoxia-selective and antineoplastic activities. With a high membrane permeability and redox potential, copper Cu 64-ATSM is preferentially taken up by hypoxic cells compared to normoxic cells; the extent of retention in tissue is inversely related to the state of tissue oxygenation allowing the quantitation of tissue hypoxia by positron emission tomography (PET). In addition, the radioactive copper moiety of this agent may deliver a selective cytotoxic dose of beta radiation to hypoxic tumor cells. C79824 626630 anti-PDGFR alpha monoclonal antibody IMC-3G3 A fully human IgG1 monoclonal antibody directed against the platelet-derived growth factor receptor alpha (PDGFR alpha) with potential antineoplastic activity. Anti-PDGFR alpha monoclonal antibody IMC-3G3 selectively binds to PDGFR alpha, .blocking the binding of its ligand, PDGF; signal transduction downstream of PDGFR through the MAPK and PI3K pathways is inhibited, which may result in inhibition of angiogenesis and tumor cell proliferation. Overexpressed by various cancer cell types, PDGFR is a transmembrane protein tyrosine kinase receptor, consisting of isoforms A and B, that is important in regulating cellular growth and differentiation and angiogenesis. C79825 626663 adenosine A3 receptor agonist CF102 An orally bioavailable, synthetic, highly selective adenosine A3 receptor (A3AR) agonist with potential antineoplastic activity. Adenosine A3 receptor agonist CF102 selectively binds to and activates the cell surface-expressed A3AR, deregulating Wnt and NF-kB signal transduction pathways downstream, which may result in apoptosis of A3AR-expressing tumor cells. A3AR, a G protein-coupled receptor, is highly expressed on the cell surfaces of various solid tumor cell types, including hepatocellular carcinoma (HCC) cells, and plays an important role in cellular proliferation. C79826 626715 steroid sulfatase inhibitor BN 83495 An orally bioavailable tricyclic coumarin-based sulfamate with potential antineoplastic activity. Steroid sulfatase inhibitor BN 83495 selectively binds to and inhibits steroid sulfatase (STS), which may inhibit the production of locally active estrogens and so inhibit estrogen-dependent cell growth in tumor cells, such as those of the breast, ovary, and endometrium. STS is a cytoplasmic enzyme responsible for the conversion of circulating inactive estrone sulfate and estradiol sulfate to biologically active unconjugated estrone and estradiol, respectively. C79827 629060 taltirelin hydrate The hydrate of tatirelin, a thyrotropin releasing hormone (TRH) analogue with potential neuroprotective, analgesic and central nervous system-stimulating (CNS)/analeptic activities. Taltirelin mimics the physiological actions of TRH on the CNS while exerting a minimal effect on the release of thyrotrophin (TSH) from the anterior lobe of the pituitary. Like TRH, the mechanism of action of this agent in the CNS has not been fully elucidated mechanism, but may involve various cerebral monoamine pathways. Compared to TRH, taltirelin has a much longer half-life and duration of effects. C79830 629109 masitinib mesylate The orally bioavailable mesylate salt of masatinib, a multi-targeted protein tyrosine kinase inhibitor with potential antineoplastic activity. Masitinib selectively binds to and inhibits both the wild-type and mutated forms of the stem cell factor receptor (c-Kit; SCFR); platelet-derived growth factor receptor (PDGFR); fibroblast growth factor receptor 3 (FGFR3); and, to a lesser extent, focal adhesion kinase (FAK). As a consequence, tumor cell proliferation may be inhibited in cancer cell types that overexpress these receptor tyrosine kinases (RTKs). C79831 629375 ALVAC(2)-NY-ESO-1 (M)/TRICOM vaccine A cancer vaccine consisting of a replication-defective recombinant canarypox virus [ALVAC(2)] encoding the cancer-testis antigen NY-ESO and the TRIad of COstimulatory Molecules (B7-1, ICAM-1 and LFA-3; also called TRICOM), with potential immunostimulatory and antineoplastic activities. Upon administration, ALVAC(2)/NY-ESO (M)/TRICOM vaccine may stimulate the host immune system to mount a cytotoxic T lymphocyte (CTL) response against NY-ESO-expressing cancer cells, which may result in the inhibition of tumor cell proliferation. NY-ESO-1, a tumor associated antigen (TAA), is found in normal testis and on the surface of various tumor cells, including bladder, breast, hepatocellular, melanoma, and prostate tumor cells. TRICOM may enhance antigen presentation and activate cytotoxic T-cells. In addition, ALVAC(2) encodes the vaccinia virus (vv) E3L ad K3L genes, which may potentiate the translation of the NY-ESO and TRICOM genes. C79832 629379 light-emitting oncolytic vaccinia virus GL-ONC1 An attenuated oncolytic vaccinia virus encoding the light-emitting fusion protein Renilla luciferase-Aequorea green fluorescent protein (RUC-GFP) with potential bioluminescent and antineoplastic activities. Upon administration, light-emitting oncolytic vaccinia virus GL-ONC1 specifically enters tumor cells due to the permeable nature of the tumor vasculature. Once inside the cell, the virus replicates, resulting in tumor cell lysis and the release of mature viral particles into the tumor microenvironment. Released viral particles may then infect and destroy neighboring tumor cells. In addition, the release of tumor-associated antigens (TAAs) by lysed tumor cells into the bloodstream may activate the immune system to mount a cytotoxic T lymphocyte (CTL) response against the tumor. The expression of RUC-GFP by this agent allows for both detection and monitoring of virally infected tumor cells in vivo and vitro with luciferase-mediated bioluminescence imaging and fluorescence imaging techniques. C79833 629499 cold contaminant-free iodine I 131 metaiodobenzylguanidine An I 131 radioiodinated synthetic analogue of the neurotransmitter norepinephrine, manufactured with a proprietary process, with radioisotopic and potential antineoplastic activities. Cold contaminant-free iodine I 131 metaiodobenzylguanidineIobenguane (MIBG) localizes to adrenergic tissue and may be used to image or eradicate tumor cells that accumulate and metabolize norepinephrine. This agent is manufactured using a technology that avoids the production of unwanted "cold contaminants" (i.e., carrier molecules), which may cause undesirable side effects and compete with MIBG for binding on target receptor sites. C82344 629676 MEK-1/MEKK-1 inhibitor E6201 A synthetic, fungal metabolite analogue inhibitor of mitogen-activated protein kinase kinase 1 (MEK-1) and mitogen-activated protein kinase kinase kinase 1 (MEKK-1) with potential antipsoriatic and antineoplastic activities. MEK-1/MEKK-1 inhibitor E6201 specifically binds to and inhibits the activities of MEK-1 and MEKK-1, which may result in the inhibition of tumor cell proliferation. MEK-1 and MEKK-1 are key components in the RAS/RAF/MEK/MAPK signaling pathway, which regulates cell proliferation and is frequently activated in human cancers. C79848 629766 anti-Her-2-CAR retroviral vector-transduced autologous peripheral blood lymphocytes Autologous human peripheral blood lymphocytes (PBLs) transduced with a retroviral vector encoding an anti-Her-2 (epidermal growth factor receptor 2) chimeric T cell receptor (chimeric antigen receptor or CAR) gene with potential immunostimulatory and antineoplastic activities. Autologous PBLs from a patient with Her-2-positive cancer are pulsed with a retroviral vector that encodes the CAR gene specific for Her-2. After expansion in culture and reintroduction into the patient, anti-Her-2-CAR retroviral vector-transduced autologous peripheral blood lymphocytes, expressing anti-Her-2-CAR on their cell surfaces, bind to Her-2 antigen on tumor cell surfaces; subsequently, Her-2-expressing tumor cells may be lysed. Her-2 (ErbB-2), a receptor tyrosine kinase (RTK) overexpressed by a variety of cancer cell types, belongs to the EGFR superfamily and plays key roles in tumor cell proliferation and tumor angiogenesis. C79834 629922 Hsp90 inhibitor XL888 An orally bioavailable, ATP-competitive, small-molecule inhibitor of heat shock protein 90 (Hsp90) with potential antineoplastic activity. Hsp90 inhibitor XL888 specifically binds to Hsp90, inhibiting its chaperone function and promoting the proteasomal degradation of oncogenic signaling proteins involved in tumor cell proliferation and survival; inhibition of tumor cell proliferation may result. Hsp90, a chaperone complex protein upregulated in a variety of tumor cell types, regulates the folding and degradation of many oncogenic signaling proteins, including Her-2 and Met. C78935 629927 anti-EphA2 monoclonal antibody-MMAF immunoconjugate MEDI-547 An auristatin analogue immunoconjugate directed against Eph receptor A2 (EphA2)-positive cancer cells with potential antineoplastic activity. Anti-EphA2 monoclonal antibody-MMAF immunoconjugate MEDI-547 is generated by conjugating the fully human IgG1 anti-EphA2 monoclonal antibody (1C1) to the small-molecule microtubule inhibitor monomethyl auristatin phenylalanine (MMAF) via the stable linker maleimidocaproyl (mc) (1C1-mcMMAF). The monoclonal antibody moiety of this agent selectively binds to cells expressing the EphA2 receptor. After internalization and enzymatic cleavage of the immunoconjugate within the tumor cell cytosol, free MMAF binds to tubulin and inhibits its polymerization, which may result in G2/M phase arrest and tumor cell apoptosis. The cell-surface receptor EphA2, a member of the ephrin family of receptor tyrosine kinases (RTKs) involved in mammalian development, is overexpressed by a variety of different cancer cell types. C79836 629935 MCT/LCT lipid emulsion A nutritional lipid emulsion consisting of both coconut oil-derived medium chain triglycerides (MCTs) and soybean oil-derived long chain triglycerides (LCTs). The LCTs in the MCT/LCT lipid emulsion supply the body with essential omega-6 fatty acids, which are needed as components of phospholipids in cell membranes and as precursors of eicosanoids. The MCTs mainly provide calories for energy. In addition to LCTs and MCTs, this lipid emulsion contains egg yolk lecithin, glycerol, and the antioxidant alpha-tocopherol (vitamin E). C79837 629937 MCT/LCT/fish oil omega-3 fatty triglyceride lipid emulsion A nutritional lipid emulsion consisting of coconut oil-derived medium chain triglycerides (MCTs), soybean oil-derived long chain triglycerides (LCT), and the fish oil-derived polyunsaturated omega-3 fatty acids. This lipid emulsion supplies essential fatty acids and calories for energy. Omega-3 fatty acids may decrease the production of certain pro-inflammatory cytokines, including interleukin 1 (IL-1), Il-6 and tumor necrosis factor (TNF). The MCTs mainly provide calories for energy. In addition to LCTs, MCTs, and omega-3 fatty acids, this lipid emulsion contains egg yolk lecithin, glycerol, and the antioxidant alpha-tocopherol (vitamin E). C79839 630382 anti-CEA TCR retroviral vector-transduced autologous lymphocytes Autologous human peripheral blood lymphocytes (PBLs), transduced with a retroviral vector encoding both the alpha and beta chains of a T cell receptor (TCR) specific for the carcinoembryonic antigen (CEA), with potential immunostimulating and antineoplastic activities. After transduction, expansion in culture, and reintroduction into the patient, anti-CEA TCR retroviral vector-transduced autologous lymphocytes bind to tumor cells expressing CEA, which may result in cytokine expression, activation and proliferation of T-cells, and a specific cytotoxic T-lymphocyte (CTL) response against CEA-expressing tumor cells. The tumor-associated antigen (TAA) CEA is overexpressed by a variety of cancer cell types, including those of the gastrointestinal tract, lung , and breast. C79842 630596 gp100:154-162 peptide vaccine A peptide consisting of amino acid residues 154 through 162 of the melanoma-melanocyte antigen gp100. Vaccination with gp100:154-162 peptide may enhance tumor-specific T-cell immunity. gp100 antigen is a self-antigen expressed by melanocytes, pigmented retinal cells, and most melanoma lesions and is recognized via class I and II HLA-restricted mechanisms. C2764 630680 IL4-Pseudomonas exotoxin fusion protein PRX321 A fusion protein consisting of the cytokine interleukin-4 (IL-4) linked to a truncated form of Pseudomonas exotoxin with potential antineoplastic activity. Upon specific, high-affinity binding to IL-4 receptors (IL-4Rs) located on the tumor cell surface., IL4-Pseudomonas exotoxin fusion protein PRX321 is internalized; the exotoxin moiety then binds to translation elongation factor 2 (EF-2), which may result in ADP ribosylation, deactivation of EF-2, inhibition of protein synthesis, and tumor cell apoptosis. The Pseudomonas exotoxin moiety of this agent has been engineered to reduce non-specific binding to cells expressing its receptor, the multiligand cell surface receptor alpha 2-macroglobulin receptor/low-density lipoprotein receptor-related protein (alpha 2MR/LRP). IL-4R is a type I transmembrane protein that binds IL-4 and IL-13 and may be overexpressed by cancers such as renal cell carcinoma (RCC) and glioma. C79843 630756 Polo-like kinase 1 inhibitor BI 6727 A dihydropteridinone Polo-like kinase 1 (Plk1) inhibitor with potential antineoplastic activity. Polo-like kinase 1 inhibitor BI 6727 selectively inhibits Plk1, inducing selective G2/M arrest followed by apoptosis in a variety of tumor cells while causing reversible cell arrest at the G1 and G2 stage without apoptosis in normal cells. Plk1, named after the polo gene of Drosophila melanogaster, is a serine/threonine protein kinase involved in regulating mitotic spindle function in a non-ATP competitive manner. C79844 630943 PPE-expressing replication-defective HSV-1 vector NP2 A replication-defective (ICP4-deleted) herpes simplex virus type 1 (HSV-1) viral vector expressing the human preproenkephalin A (PPE) gene with potential antinociceptive activity. Upon intradermal administration, PPE-expressing replication-defective HSV-1 vector NP2 is transported by retrograde axonal transport to the dorsal root ganglion (DRG) and becomes dormant. In the DRG, the vector transduces sensory neurons with high efficiency, delivering the engineered PPE gene; transduced neurons then express the protein proenkephalin A, the precursor for Met- and Leu-enkephalin. After proteolytic cleavage from proenkephalin A in the DRG neuronal cytosol, transgene-mediated Met- and Leu-enkephalin bind to mu and gamma- opioid receptors, which may result in the inhibition of nociceptive neurotransmission. C79845 631444 AC-T regimen A chemotherapy regimen consisting of doxorubucin hydrochloride (Adriamycin) and cyclophosphamide, followed by paclitaxel (Taxol), administered on either a dose-dense or sequential schedule and used as an adjuvant treatment for breast cancer. C63427 631451 BEACOPP regimen A chemotherapy regimen consisting of bleomycin, etoposide, doxorubicin hydrochloride (Adriamycin), cyclophosphamide, vincristine (Oncovin), procarbazine and prednisone, used for the treatment of advanced-stage Hodgkin lymphoma. C63370 631615 elesclomol sodium The water soluble sodium salt of a small-molecule bis(thio-hydrazide amide) with oxidative stress induction, pro-apoptotic, and potential antineoplastic activities. Elesclomol induces oxidative stress, creating high levels of reactive oxygen species (ROS), such as hydrogen peroxide, in both cancer cells and normal cells. Because tumor cells have elevated levels of ROS compared to normal cells, the increase in oxidative stress beyond baseline levels elevates ROS beyond sustainable levels, exhausting tumor cell antioxidant capacity, which may result in the induction of the mitochondrial apoptosis pathway. Normal cells are spared because the increase in the level of oxidative stress induced by this agent is below the threshold at which apoptosis is induced. C79840 631940 gemcitabine-cisplatin regimen A chemotherapy regimen consisting of gemcitabine hydrochloride and cisplatin used in the treatment of advanced-stage non-small cell lung, advanced-stage bladder, advanced-stage cervical, pancreatic, and epithelial ovarian cancers; this regimen is also used in the treatment of malignant mesothelioma. C63406 631941 ICE regimen A chemotherapy regimen consisting of ifosfamide, carboplatin and etoposide used in the treatment of relapsed and refractory non-Hodgkin and Hodgkin lymphomas. 632130 R-CHOP regimen An immunochemotherapy regimen consisting of rituximab, cyclophosphamide, hydroxydaunorubicin hydrochloride (doxorubicin hydrochloride), vincristine (Oncovin) and prednisone used to treat both indolent and aggressive forms of non-Hodgkin lymphoma. 632219 Aurora B kinase inhibitor TAK-901 A small-molecule inhibitor of the serine-threonine kinase Aurora B with potential antineoplastic activity. Aurora B kinase inhibitor TAK-901 binds to and inhibits the activity of Aurora B, which may result in a decrease in the proliferation of tumor cells that overexpress Aurora B. Aurora B is a positive regulator of mitosis that functions in the attachment of the mitotic spindle to the centromere; the segregation of sister chromatids to each daughter cell; and the separation of daughter cells during cytokinesis. This serine/threonine kinase may be amplified and overexpressed by a variety of cancer cell types. C82674 632222 mammaglobin-A DNA vaccine A cancer vaccine containing a plasmid encoding the mammaglobin-A gene with potential immunostimulating and antineoplastic activities. Upon administration, mammaglobin-A DNA vaccine may induce both humoral and cytotoxic T lymphocyte (CTL) immune responses against tumor cells that express mammaglobin-A, which may result in decreased tumor growth. The 10 kiloDalton (kD) glycoprotein mammglobin-A is expressed in over 80% of human breast cancers. C82675 632436 liposome-encapsulated irinotecan hydrochloride PEP02 A liposomal formulation of the hydrochloride salt of the semisynthetic camptothecin analogue irinotecan with potential antineoplastic activity. During the S phase of the cell cycle, irinotecan selectively stabilizes topoisomerase I-DNA covalent complexes, inhibiting religation of topoisomerase I-mediated single-strand DNA breaks and producing lethal double-strand DNA breaks when complexes are encountered by the DNA replication machinery. Liposome encapsulation of this agent promotes efficient drug delivery into the cytosol from the endosome compartment of the cell. C82676 632465 BCG intravesical solution A solution containing an attenuated, live culture preparation of the\nBacillus Calmette Guerin (BCG) strain of Mycobacterium bovis with potential immunostimulating activity. Although the precise mechanism of action is unknown, upon intravesical administration, attenuated, live BCG bacteria in the solution come into direct contact with the bladder wall, inciting an antitumor granulomatous inflammatory reaction. C83496 632625 c-Met inhibitor AMG 208 A selective small-molecule inhibitor of the proto-oncogene c-Met with potential antineoplastic activity. c-Met inhibitor AMG 208 inhibits the ligand-dependent and ligand-independent activation of c-Met, inhibiting its tyrosine kinase activity, which may result in cell growth inhibition in tumors that overexpress c-Met. C-Met encodes the hepatocyte growth factor receptor tyrosine kinase, plays an important role in epithelial cell proliferation and has been shown to be overexpressed in a variety of cancers. C82677 632630 diphenhydramine hydrochloride/dexamethasone/nystatin magic mouthwash An oral suspension containing diphenydramine hydrochloride, dexamethasone and nystatin, with anithistaminic, antiinflammatory, and antifungal activities. Diphenhydramine hydrochloride/dexamethasone/nystatin magic mouthwash inhibits the cytokine-mediated inflammation and yeast colonization of the oral mucosa associated with chemotherapy and radiation therapy. C82678 632702 ionic silver-impregnated sodium carboxymethyl cellulose antimicrobial dressing A textile fiber dressing composed of ionic silver-impregnated sodium carboxymethylcellulose with potential wound-healing and antimicrobial activities. Ionic silver-impregnated sodium carboxymethylcellulose antimicrobial dressing inhibits microbial growth and promotes wound healing while protecting the wound site from external factors that may cause pain, promote infection, or slow the natural wound healing process. Ionic silver has a high affinity for negatively charged side groups on microbial cell proteins. Upon binding, ionic silver alters the molecular structure of proteins with a role in normal microbial cell functions thereby interfering with cell wall synthesis, transcription, translation, electron transport across membranes and protein folding, resulting in microbial cell death. C82679 632705 sodium carboxymethylcellulose dressing A textile fiber dressing composed of sodium carboxymethylcellulose with potential wound-healing activity. Sodium carboxymethylcellulose dressing protects the wound site from external factors that may cause pain, promote infection, or slow the natural wound healing process. Sodium carboxymethylcellulose is a non-toxic, non-allergenic, anionic water-soluble polymer derived from cellulose. C82680 632847 distilled water An ultra-pure form of water with potential antineoplastic activity. Derived by boiling impure water and condensing the resultant steam in a sterile container, distilled water has been shown to kill bladder cancer cells in vitro through osmotic lysis (cytolysis). C82681 632992 irinotecan-eluting beads Microporous hydrospheres of polyvinylalcohol (PVA) impregnated with irinotecan with potential antineoplastic activity. In transarterial chemoembolization (TACE), irinotecan-eluting beads are administered into blood vessels that feed the tumor, occluding tumor blood vessels and inducing ischemic tumor necrosis while simultaneously delivering high-dose chemotherapy locally. Irinotecan, a semisynthetic derivative of camptothecin, inhibits topoisomerase I activity by stabilizing the cleavable complex between topoisomerase I and DNA, resulting in DNA breaks that inhibit DNA replication and trigger apoptotic cell death. C82682 633311 anti-IGF1/2 monoclonal antibody MEDI-573 A humanized monoclonal antibody directed against insulin-like growth factors 1 and 2 (IGF-1/2) with potential antineoplastic activity. Anti-IGF1/2 monoclonal antibody MEDI-573 inhibits IGF1- and IGF2-stimulated activation of membrane-bound IGF receptors and the subsequent triggering of proliferation and survival signaling pathways. This may result in the inhibition of tumor cell proliferation and the induction of tumor cell apoptosis. IGF1/2 ligands stimulate cell proliferation, enable oncogenic transformation, and suppress apoptosis; IGF1/2 signaling has been highly implicated in tumorigenesis and metastasis. C82683 633312 anti-PDGFR alpha monoclonal antibody MEDI-575 A humanized monoclonal antibody directed against the platelet-derived growth factor receptor (PDGFR) alpha with potential antineoplastic activity. Anti-PDGFR alpha monoclonal antibody MEDI-575 inhibits activation of the cell-surface tyrosine kinase PDGFR alpha subunit and subsequent triggering of mitogenic signaling pathways, including the JAK/STAT, PI3K/Akt, and MAP kinase pathways. PDGFR alpha acts as a mitogenic signaling receptor for cells of mesenchymal origin and inhibition of receptor activity may inhibit tumor cell proliferation. C82684 633313 anti-AGS-16 monoclonal antibody AGS-16M18 A humanized monoclonal antibody directed against the activator of g-proteins signaling (AGS) cell surface protein AGS-16 with potential antineoplastic activity. Anti-AGS-16 monoclonal antibody AGS-16M18 selectively binds to AGS-16, triggering complement-dependent cell lysis (CDCL) and antibody-dependent cell-mediated cytotoxicity (ADCC) in tumor cells expressing AGS-16. While normally expressed at low levels in the proximal tubules of the kidney, AGS-16 has been found to be overexpressed in more than 95% of kidney and 40% of liver neoplasms. C82685 633505 anti-AGS-8 monoclonal antibody AGS-8M4 A humanized monoclonal antibody directed against the activator of g-proteins signaling (AGS) cell surface protein AGS-8 with potential antineoplastic activity. Anti-AGS-8 monoclonal antibody AGS-8M4 selectively binds to AGS-8, triggering complement-dependent cell lysis and antibody-dependent cell-mediated cytotoxicity in tumor cells expressing AGS-8. While normally expressed at low levels in the heart in response to ischemia, AGS-8 has been found to be expressed in more than 70% of ovarian neoplasms. C82686 633506 MEK inhibitor RO4987655 An orally active small molecule, targeting mitogen-activated protein kinase kinase 1 (MAP2K1 or MEK1), with potential antineoplastic activity. MEK inhibitor RO4987655 binds to and inhibits MEK, which may result in the inhibition of MEK-dependent cell signaling and the inhibition of tumor cell proliferation. MEK, a dual specificity threonine/tyrosine kinase, is a key component of the RAS/RAF/MEK/ERK signaling pathway that regulates cell growth; constitutive activation of this pathway has been implicated in many cancers. C82696 633588 3,4-diaminopyridine An organic compound derived from pyridine with potassium channel inhibition activity. 3,4-diaminopyridine inhibits potassium channel efflux, increasing the duration of the action potential, which results in an increase in the duration of calcium channel opening and enhanced acetylcholine (ACh) release. Increased ACh availability at the motor end plate allows muscles to contract. C82687 633689 umbilical cord blood-derived mesenchymal stem cells Multipotent stem cells of mesenchymal origin isolated from umbilical cord blood. Umbilical cord blood-derived mesenchymal stem cells can differentiate into a variety of cell types including fibroblasts, osteoblasts, chondrocytes, myocytes, adipocytes, and endothelial cells. C82688 633695 ribonuclease QBI-139 A nuclease of mammalian origin that cleaves the phosphodiester bond between nucleotides of ribonucleic acids with potential antineoplastic activity. Ribonuclease QBI-139 catalyzes the hydrolysis and degradation of RNA leading to the inhibition of protein synthesis and cell death. C82689 633696 HDAC inhibitor CHR-2845 A hydroxamic acid-derived histone deacetylase (HDAC) inhibitor with potential antineoplastic activity. CHR-2845 inhibits HDAC leading to an accumulation of highly acetylated histones, which may result in chromatin remodeling, inhibition of tumor oncogene transcription, inhibition of tumor cell division, and the induction of tumor cell apoptosis. HDAC, an enzyme upregulated in many tumor types, deacetylates chromatin histone proteins; this agent may specifically target HDACs in cells of the monocyte-macrophage lineage. C82690 633820 Hsp90 inhibitor AB-010 An orally bioavailable nanoparticle albumin-bound inhibitor of heat shock protein 90 (Hsp90) with potential antineoplastic activity. Hsp90 inhibitor AB-010 selectively binds to Hsp90, inhibiting its chaperone function and promoting the degradation of oncogenic signaling proteins involved in tumor cell proliferation and survival. This agent may inhibit the growth of a wide variety of cancer cell types; the incorporation of albumin into its formulation may facilitate its endothelial transcytosis through the gp60-regulated albumin transport pathway. Hsp90, a chaperone protein upregulated in a variety of tumor cells, regulates the folding and degradation of many oncogenic signaling proteins. C82691 633936 deoxycytidine analogue TAS-109 An analogue of the nucleoside deoxycytidine with potential antineoplastic activity. Nucleoside analogue TAS-109 is incorporated into DNA and directly inhibits the activity of DNA polymerase, which may result in inhibition of DNA replication and cell cycle arrest in the S and G2/M phases, DNA fragmentation, and tumor cell apoptosis. C82697 633945 sheddase inhibitor INCB007839 An orally bioavailable inhibitor of the ADAM (A Disintegrin And Metalloprotease) family of multifunctional membrane-bound proteins with potential antineoplastic activity. Sheddase inhibitor INCB007839 represses the metalloproteinase "sheddase" activities of ADAM10 and ADAM17, which may result in the inhibition of tumor cell proliferation. The metalloproteinase domains of ADAMs cleave cell surface proteins at extracellular sites proximal to the cell membrane, releasing or "shedding" soluble protein etcodomains from the cell surface; the disintegrin domains of these multifunctional proteins interact with various components of the extracellular matrix (ECM). ADAM10 processes particular epithelial growth factor receptor (EGFR) ligands and appears to regulate Notch signaling through the cleavage of Notch and its related ligand delta-like ligand-1 (Dll-1). ADAM17 (also known as Tumor necrosis factor-Converting Enzyme or TACE) is involved in processing tumor\nnecrosis factor (TNF) from its membrane bound precursor to its soluble circulating form and in processing ligands for the epidermal growth factor receptor (EGFR) family. C82692 633978 DHAP regimen A chemotherapy regimen consisting of dexamethasone, high-dose cytarabine (ARA-C) and cisplatin (Platinol), used for the treatment of relapsed and refractory Hodgkin and non-Hodgkin lymphomas. C63441 634547 multitargeted tyrosine kinase inhibitor DCC-2036 An orally bioavailable small-molecule inhibitor of multiple tyrosine kinases with potential antineoplastic activity. Multitargeted tyrosine kinase inhibitor DCC-2036 binds to and inhibits the Bcr-Abl fusion oncoprotein by changing the conformation of the folded protein to disallow ligand-dependent and ligand-independent activation; in addition, this agent binds to and inhibits Src family kinases LYN, HCK and FGR and the receptor tyrosine kinases TIE-2 and VEGFR-2. Multitargeted tyrosine kinase inhibitor DCC-2036 may exhibit more potent activity against T315I Bcr-Abl gatekeeper mutant kinases than other Bcr-Abl kinase inhibitors. The TIE-2 and VEGFR-2 receptor tyrosine kinases regulate angiogenesis, respectively, while the Src family kinases Abl, LYN, and HCK Src regulate a variety of cellular responses including differentiation, division, adhesion, and the stress response. C82693 634612 Eg5 kinesin-related motor protein inhibitor ARQ 621 A small-molecule inhibitor of the kinesin-related motor protein Eg5 with potential antineoplastic activity. Eg5 kinesin-related motor protein inhibitor ARQ 621 selectively inhibits the activity of Eg5, which may result in mitotic disruption, apoptosis and cell death. The ATP-dependent Eg5 kinesin-related motor protein (also known as KIF11 or kinesin spindle protein-5) is a plus-end directed kinesin motor protein involved in the regulation of spindle dynamics, including assembly and maintenance, during mitosis. C82694 634790 trans sodium crocetinate The sodium salt of the trans-isomer of the carotenoid crocetin with potential antihypoxic and radiosensitizing activities. Trans sodium crocetinate (TSC) increases the diffusion rate of oxygen in aqueous solutions such as from plasma to body tissue. The agent has been shown to increase available oxygen during hypoxic and ischemic conditions that may occur in hemorrhage, vascular and neurological disorders, and in the tumor microenvionment. C82695 634923 botulinum toxin type A An injectable formulation of a neurotoxin derived through the fermentation of the Hall strain of Clostridium botulinum type A with neuromuscular transmission inhibitory and analgesic activities. Upon injection into the affected muscle, the heavy chain portion of botulinum toxin type A (BTX-A) binds to the cell membrane of the motor nerve and is internalized via endocytosis. Upon entry, the light chain portion of the toxin is activated and cleaves the protein SNAP-25, thereby preventing the fusion of acetylcholine (ACh)-containing synaptic vesicles with the cell membrane and, so, the release\nof ACh into the neuromuscular\njunction; subsequent binding of ACH to motor end-plate nicotinic acid receptors and ACh-mediated muscle contraction are thus blocked. In addition to ACh, BTX-A may inhibit the release of neuropeptides, such as substance P and glutamate, which may contribute to its analgesic activity. C82623 634927 live attenuated measles virus vaccine A live, attenuated measles vaccine with potential antineoplastic activity. Upon subcutaneous administration, live attenuated measles virus vaccine may activate the immune system to mount a cytotoxic T-lymphocyte (CTL) response against measles-positive tumor cells. Measles virus has been shown to be present in some non-small cell lung cancers. C82651 635527 proteasome inhibitor MLN9708 An orally bioavailable second generation proteasome inhibitor (PI) with potential antineoplastic activity. Proteasome inhibitor MLN9708 inhibits the activity of the proteasome, blocking the targeted proteolysis normally performed by the proteasome, which results in an accumulation of unwanted or misfolded proteins; disruption of various cell signaling pathways may follow, resulting in the induction of apoptosis. Compared to first generation PIs, second generation PIs may have an improved pharmacokinetic profile with increased potency and less toxicity. Proteasomes are large protease complexes that degrade unneeded or damaged proteins that have been ubiquinated. C82653 636121 mRNA-derived prostate cancer vaccine CV9103 A prostate cancer vaccine containing mRNAs encoding prostate specific antigen (PSA), prostate specific membrane antigen (PSMA), prostate stem cell antigen (PSCA) and six-transmembrane epithelial antigen of the prostate (STEAP), with potential antitumor activity. Upon administration, mRNA-derived prostate cancer vaccine CV9103 may stimulate the immune system to mount a cytotoxic T lymphocyte response (CTL) against PSA-, PSMA-, PSCA- and STEAP-expressing prostate tumor cells. The mRNA used in this vaccine is modified and formulated to have enhanced translational potency and adjuvant activities. .PSA, PSMA, PSCA and STEAP may be upregulated in prostate cancer cells; their expression in prostate cancer has been correlated with disease progression. C82654 636135 afamelanotide A synthetic peptide analogue of the naturally occurring alpha-melanocyte stimulating hormone (a-MSH) with potential photoprotective activity. Mimicking the action of a-MSH, afamelanotide stimulates melanocytes to increase the production and release of melanin. Increased melanocyte melanin may protect against ultraviolet radiation (UVR)-initiated cellular DNA damage, oxidation of membrane proteins, and alterations in intracellular signaling processes in epidermal cells. Endogenously, a-MSH is released by skin cells in response to UVR exposure, stimulating melanocytes to produce and release melanin. C82655 636152 zirconium Zr 89 bevacizumab A radioimmunoconjugate comprised of the recombinant humanized monoclonal antibody bevacizumab labeled with the radioisotope zirconium Zr 89 (Zr 89) with radioisotopic activity and potential imaging use. The antibody moiety of zirconium Zr 89 bevacizumab targets and binds to the extracellular domain of the vascular endothelial growth factor receptor (VEGFR). Upon binding, the radioisotope moiety may be detected using positron emission tomography (PET), allowing the imaging and quantification of VEGFR-expressing tumor cells. VEGFR, a tyrosine kinase, is overexpressed on the cell surfaces of various tumor cell types. C82656 636186 beta-glucan MM-10-001 A powder formulation containing a triple helix beta-glucan, isolated from the cell walls of the shiitake mushroom (Lentinula edodes), with potential immunostimulating activity. The beta-glucan in beta-glucan MM-10-001 binds to a lectin site within the complement receptor 3 (CR3 or iC3b receptor) on leukocytes, priming the receptor to trigger cytotoxic degranulation of leukocytes when leukocyte CR3 binds to iC3b-opsonized tumor cells. iC3b is the proteolyticly inactive product of the complement cleavage fragment C3b. C82657 636193 oseltamivir phosphate The phosphate salt of oseltamivir, a synthetic derivative prodrug of ethyl ester with antiviral activity. By blocking neuraminidases on the surfaces of influenza viruses, oseltamivir interferes with host cell release of complete viral particles. 636195 zanamivir A sialic acid-analogue neuraminidase inhibitor with antiviral activity. Administered into the respiratory tract by aerosol inhalation, zanamivir selectively binds to and inhibits influenza A and B virus neuraminidase-mediated cleavage of sialic acid residues in host cell membrane-bound glycoprotein receptors for influenza viruses, preventing the release of progeny viruses from host cell surfaces and, so, further viral replication. C47786 636196 pegylated recombinant human hyaluronidase PH20 A pegylated formulation of a recombinant form of human hyaluronidase with potential antitumor activity. Upon intravenous administration, pegylated recombinant human PH20 degrades hyaluronic acid (HA) coating tumor cells, which may result in the inhibition of tumor cell growth. In addition, the degradation of HA may result in a lowering of the interstitial fluid pressure (IFP), allowing better penetration of chemotherapeutic agents into the tumor bed. HA is a glycosaminoglycan found in the extracellular matrix (ECM) that is frequently overproduced by various tumor cell types. The presence of HA in tumors correlates with increased tumor cell growth, metastatic potential, tumor progression, increased resistance to chemotherapeutic agents, and an elevation in tumor IFP. C82659 636649 enteric-coated TRPM8 agonist D-3263 hydrochloride An enteric-coated orally bioavailable formulation of the hydrochloride salt of a small-molecule agonist for transient receptor potential melastatin member 8 (TRPM8 or Trp-p8) with potential antineoplastic activity. The active ingredient in enteric-coated TRPM8 agonist D-3263 hydrochloride binds to and activates TRPM8, which may result in an increase in calcium and sodium entry; the disruption of calcium and sodium homeostasis; and the induction of cell death in TRPM8-expressing tumor cells. This agent may decrease dihydrotestosterone (DHT) levels, which may contribute to its inhibitory effects on prostate cancer and BPH. TRPM8 is a transmembrane calcium channel protein that is normally expressed in prostate cells and appears to be overexpressed in benign prostatic hyperplasia (BPH) and in prostate cancer. C82660 636663 HLA-A2-restricted synthetic glioma antigen peptides vaccine A synthetic peptide cancer vaccine consisting of HLA-A2-restricted peptides derived from glioma-associated antigens (GAA) with potential immunostimulating and antineoplastic activities. Upon administration, HLA-A2-restricted synthetic glioma antigen peptides vaccine may stimulate the host immune system to mount a cytotoxic T lymphocyte (CTL) response against tumor cells expressing the corresponding GAAs, resulting in glioma tumor cell lysis. HLA-A2 is an MHC class I molecule that presents antigenic peptides to CD8+ T cells; epitope design restricted to epitopes that bind most efficiently to HLA-A2 may improve antigenic peptide immunogenicity. C82661 636692 fentanyl citrate buccal tablet A tablet formulation containing the citrate salt of the synthetic anilidopiperidine opiate fentanyl with analgesic activity. Upon contact with the buccal mucosa, fentanyl citrate buccal tablet rapidly releases fentanyl which is quickly absorbed into the systemic circulation. Fentanyl selectively binds to and activates mu-opioid receptors in the central nervous system (CNS), mimicking the effects of endogenous opioids. C83012 637113 angiogenesis inhibitor JI-101 An orally active inhibitor of vascular endothelial growth factor receptor 2 (VEGFR2), platelet-derived growth factor receptor beta (PDGFRb), and the ephrin B4 receptor B4 (EphB4) with potential antiangiogenic and antineoplastic activities. Angiogenesis inhibitor JI-101 binds to and inhibits VEGFR2, PDGFRb and EphB4, which may inhibit tumor angiogenesis and, so, cellular proliferation in tumor cells overexpressing VEGFR2, PDGFRb and EphB4. \nThe receptor tyrosine kinases VEGFR2, PDGFRb and EphB4 may be overexpressed in a number of different cancer cell types and may play crucial roles in tumor angiogenesis. C82413 637163 actinium Ac 225 lintuzumab A radioimmunoconjugate consisting of the humanized monoclonal antibody lintuzumab conjugated to the alpha-emitting radioisotope actinium Ac 225 with potential antineoplastic activity. The monoclonal antibody moiety of actinium Ac 225 lintuzumab specifically binds to the cell surface antigen CD33 antigen, delivering a cytotoxic dose of alpha radiation to cells expressing CD33. CD33 is a cell surface antigen expressed on normal non-pluripotent hematopoietic stem cells and overexpressed on myeloid leukemia cells. C82414 637352 huachansu A traditional Chinese medicine (TCM) containing a water soluble Bufo toad skin extract that includes the cardiac glycosides bufalin, cinobufagin and resibufogenin with potential antineoplastic and antiangiogenic activities. Although the exact mechanism of action of this TCM has yet to be fully elucidated, huachansu, which may be administered in an injectable form, may induce cell cycle arrest and apoptosis by suppressing the expression of anti-apoptotic proteins, such as Bcl-2, while inducing the expression of pro-apoptotic proteins, such as BAX. C82415 637355 autologous NSCLC DNA-transfected semi-allogeneic fibroblasts MRC-5 vaccine A vaccine consisting of irradiated human fetal lung fibroblasts (Medical Research Council 5 or MRC-5) transfected with autologous non-small cell lung cancer (NSCLC)-derived DNA with potential immunostimulatory and antineoplastic activities. Upon administration, autologous NSCLC DNA-transfected semi-allogeneic fibroblasts MRC-5 vaccine expresses NSCLC tumor-associated antigens (TAAs) in addition to MHC class I-determinants and the co-stimulatory molecule B7.1, which may induce a cytotoxic T-lymphocyte (CTL) response against NSCLC cells. The MRC-5 cell line, established in 1966, is a human diploid lung fibroblast cell line that is permissive for infection by a wide range of human viruses including human cytomegalovirus (HCMV) and coxsackie B viruses. C82416 637356 MUC1 peptide-poly-ICLC adjuvant vaccine A vaccine preparation containing mucus 1 (MUC1) peptide and the adjuvant poly-ICLC with potential immunostimulatory and antineoplastic activities. Upon administration, MUC1 peptide-poly-ICLC adjuvant vaccine may induce the host immune system to mount a cytotoxic T cell response against MUC1-expressing tumor cells. MUC1, a tumor associated antigen normally present on the lining of the human colon, may be overexpressed and/or mutated in a variety of cancer cell types. The adjuvant poly-ICLC, a ligand for toll-like receptor-3, induces the release of cytokines which may help boost the immune response against MUC1. C82417 637546 recombinant human albumin-human granulocyte colony-stimulating factor A long-acting recombinant fusion protein incorporating human serum albumin (HSA)-derived and human granulocyte colony stimulating factor (G-CSF)-derived moieties with potential granulopoietic activity. G-CSF, a naturally occurring cytokine, stimulates the production of granulocytes and stem cells in the bone marrow and their release into the blood; it also stimulates the differentiation, function, and survival of neutrophil precursors and mature neutrophils. Albumin fusion may promote an increased serum half-life and bioavailability of the G-CSF moiety of this fusion protein. C81936 637599 CDC7 kinase inhibitor BMS-863233 An orally bioavailable cell division cycle 7 homolog (CDC7) kinase inhibitor with potential antineoplastic activity. CDC7 kinase inhibitor BMS-863233 binds to and inhibits the activity of CDC7, which may result in the inhibition of DNA replication and mitosis, the induction of tumor cell apoptosis, and the inhibition of tumor cell proliferation in CDC7-overexpressing tumor cells. CDC7, a serine-threonine kinase overexpressed in a variety of tumor cell types, plays an essential role in the initiation of DNA replication by activating origins of replication. C82418 637612 CHK2 inhibitor LY2603618 An inhibitor of the cell cycle checkpoint kinase 2 (chk2) with potential chemopotentiating activity. Chk2 inhibitor LY2603618 binds to and inhibits the activity of chk2, which may prevent the repair of DNA caused by DNA-damaging agents, thus potentiating the antitumor efficacies of various chemotherapeutic agents. Chk2, an ATP-dependent serine-threonine kinase, is a key component in the DNA replication-monitoring checkpoint system and is activated by double-stranded breaks (DSBs); activated chk2 is overexpressed by a variety of cancer cell types. C81937 637721 recombinant human epidermal growth factor A recombinant form of the naturally-occurring polypeptide human epidermal growth factor with potential epithelial regenerative and cytoprotective activities. Upon topical application, recombinant human epidermal growth factor (rhEGF) may stimulate epithelial proliferation, differentiation and migration, which may result in the acceleration of epithelial regeneration and wound healing. In addition, rhEGF may attenuate epithelial cytotoxicities related to chemotherapy and/or radiotherapy. C81938 637760 anti-HGF monoclonal antibody TAK-701 A humanized monoclonal antibody directed against human hepatocyte growth factor (HGF) with potential antineoplastic activity. Anti-HGF monoclonal antibody TAK-701 binds to the soluble ligand HGF, preventing HGF binding to and activation of the HGF receptor c-Met and so the activation of the c-Met signaling pathway; this may result in the induction of cell death in c-Met-expressing tumor cells. c-Met, a receptor tyrosine kinase overexpressed or mutated in a variety of tumor cell types, plays a key role in cancer cell growth, survival, angiogenesis, invasion, and metastasis. C81939 637761 doxorubicin-eluting beads A drug-device combination product consisting of small polymeric beads impregnated with the anthracycline antibiotic doxorubicin with potential antineoplastic activity. The beads consist of polyvinyl alcohol (PVA) microspheres modified with sulfonic acid groups and loaded with doxorubicin. During transarterial chemoembolization (TACE), doxorubicin-eluting beads embolize to the tumor vasculature and release cytotoxic doxorubicin, which may result in both ischemic necrosis of tumor tissue due to mechanical blockage of the tumor vasculature and doxorubicin-mediated inhibition of tumor cell proliferation. C82419 637762 HLA-A*2402-restricted URLC10 peptides vaccine A cancer vaccine containing HLA-A*2402-restricted epitope peptides URLC10 (up-regulated lung cancer 10) with potential immunostimulatory and antineoplastic activities. Upon administration, HLA-A*2402-restricted URLC10 peptides vaccine may stimulate a cytotoxic T lymphocyte (CTL) response against URLC10-expressing tumor cells. URLC10, a tumor associated antigen, is often overexpressed in lung, esophageal and gastric cancers. HLA-A*2402 is an MHC class I molecule that presents antigenic peptides to CD8+ T cells; epitope design restricted to epitopes that bind most efficiently to HLA-A*2402 may improve antigenic peptide immunogenicity. C82421 637782 p53 synthetic long peptide (70-251) vaccine A peptide vaccine consisting of 10 synthetic long peptides (SLPs), 25-30 amino acids in size and derived from the middle portion of p53 (amino acids 70-251), mixed with the adjuvant Montanide ISA-51 with potential immunostimulatory and antitumor activities. Upon administration, p53 synthetic long peptide (70-251) vaccine may stimulate the host immune system to mount a cytotoxic T-cell lymphocyte (CTL) response against p53-expressing tumor cells. p53, a tumor associated antigen (TAA), may be overexpressed in variety of cancer cell types. C82420 638087 anti-human integrin alpha v subunit monoclonal antibody EMD 525797 A humanized monoclonal antibody directed against the human alpha v integrin subunit with potential antiangiogenic and antineoplastic activities. Anti-human integrin alpha v subunit monoclonal antibody EMD 525797, a chimeric antibody which includes the antigen binding sites of the anti-integrin mouse antibody 17E6, binds to and inhibits the activity of alphavbeta3 integrin (vitronectin receptor); this may result in the inhibition of endothelial cell-cell interactions, endothelial cell-matrix interactions, and integrin-mediated tumor angiogenesis and metastasis in alphavbeta3-expressing tumor cells. Alphavbeta3 integrin, a cell adhesion and signaling receptor, is expressed on the surface of tumor vessel endothelial cells and plays a crucial role in endothelial cell adhesion and migration. C82422 638088 Pim kinase inhibitor SGI-1776 A small-molecule pan-Pim protein kinase inhibitor with potential antineoplastic activity. Pim kinase inhibitor SGI-1776 binds to and inhibits the activities of Pim-1, -2 and -3, serine-threonine kinases, which may result in the interruption of the G1/S phase cell cycle transition, the expression of pro-apoptotic Bcl2 proteins and tumor cell apoptosis. PIM kinases play key roles in cell cycle progression and apoptosis inhibition and may be overexpressed in various malignancies. C82404 638167 fluorescein sodium injection An injectable form of the sodium salt of the fluorophore fluorescein. Fluorescein responds to electromagnetic radiation between the wavelengths of 465-490 nm and fluoresces, emitting light at wavelengths of 520-530 nm that can be detected visually. C82405 638168 anti-endosialin/TEM1 monoclonal antibody MORAb-004 A humanized IgG1 monoclonal antibody directed against human endosialin/TEM1 (tumor endothelial marker;CD248) with potential anti-angiogenic and antineoplastic activities. Anti-endosialin/TEM1 monoclonal antibody MORAb-004 binds to and inhibits the activity of cell surface protein endosialin/TEM1, which may result in the inhibition of angiogenesis, tumor cell proliferation and metastasis. Endosialin/TEM1 plays a key role in angiogenesis and may be overexpressed on tumor stromal cells and endothelial cells. C82406 638423 pTVG-HP plasmid DNA vaccine A cancer vaccine containing plasmid DNA encoding human prostatic acid phosphatase (PAP) (pTVG-HP) with potential immunostimulatory and antineoplastic activities. Upon administration, pTVG-HP plasmid DNA vaccine may stimulate the host immune system to generate a cytotoxic T lymphocyte (CTL) response against PAP-expressing prostate cancer cells. PAP or prostatic specific acid phosphatase (PSAP) is a tumor associated antigen (TAA) that may be overexpressed in prostate cancer. C82407 638648 BTK inhibitor PCI-32765 An orally bioavailable small-molecule inhibitor of Bruton's tyrosine kinase (BTK) with potential antineoplastic activity. BTK inhibitor PCI-32765 binds to and inhibits BTK activity, preventing B-cell activation and B-cell-mediated signaling and inhibiting the growth of malignant B cells that overexpress BTK. BTK, a member of the src-related BTK/Tec family of cytoplasmic tyrosine kinases, is required for B cell receptor (BCR) signaling, plays a key role in B-cell maturation, and is overexpressed in a number of B-cell malignancies. C81934 638649 folate receptor-targeted vinca alkaloid EC0489 A folate receptor-targeting cytotoxic drug conjugate consisting of a folate vitamin analogue linked to a vinca alkaloid microtubule destabilizing agent with potential antineoplastic activity. Mediated through its folate moiety, folate receptor-targeted Vinca alkaloid EC0489 delivers the cytotoxic vinca alkaloid moiety directly to cells expressing folic acid receptors, frequently upregulated in many types of tumor cells. After ligand-receptor internalization, the vinca alkaloid moiety binds to tubulin and disrupts microtubule assembly-disassembly dynamics, resulting in cell cycle arrest and apoptosis. The relative tumor cell specificity of this agent reduces the toxicity profile of its Vinca alkaloid moiety. C81935 639514 TPH inhibitor LX1032 An orally bioavailable small-molecule inhibitor of tryptophan hydroxylase (TPH) with potential antiserotonergic activity. TPH inhibitor LX1032 binds to and blocks the activity of TPH, which may result in a reduction in peripheral serotonin (5-HT) production and improvement of serotonin-mediated gastrointestinal effects such as severe diarrhea. This agent does not cross the blood-brain barrier (BBB), thus CNS serotonin levels are unaffected. TPH, the rate-limiting enzyme in serotonin biosynthesis, is overexpressed in carcinoid tumor cells. C81941 639516 anti-MET monoclonal antibody MetMAb A humanized monovalent monoclonal antibody directed against the hepatocyte growth factor receptor (c-Met) with potential antineoplastic activity. Anti-MET monoclonal antibody MetMAb binds to the extracellular domain of c-Met, preventing the binding of its ligand, hepatocyte growth factor (HGF); the activation of the c-Met signaling pathway is thus inhibited, which may result in cell death in c-Met-expressing tumor cells. c-Met, a receptor tyrosine kinase, is overexpressed on the cell surfaces of a variety of cancer cell types and may play a key role in their proliferation, invasion and survival. C82348 639521 2G-1 TCR retroviral vector-transduced lymphocytes A preparation of autologous human T-lymphocytes isolated from renal cell cancer (RCC) patient and transduced with 2G-1 TCR, a retroviral vector encoding the alpha and beta chains of a T-cell receptor that recognizes TNF-related apoptosis inducing ligand (TRAIL) bound to death receptor 4 (DR4), with potential immunostimulating and antineoplastic activities. After transduction, expansion in culture, and introduction into the RCC patient, 2G-1 TCR retroviral vector-transduced lymphocytes may stimulate a cytotoxic T lymphocyte (CTL) response against RCC cells with TRAIL bound to DR4 on their surfaces. TRAIL, a member of the TNF superfamily, is a homotrimeric type II membrane protein that rapidly induces oligomerization of receptor intracellular death domains and apoptosis in a variety of tumor cells when bound to its receptors; DR4 (TRAIL receptor 1), a member of the TNF receptor family, is overexpressed by a variety of malignant cell types. C82408 639524 Aurora kinase inhibitor AMG 900 A small-molecule inhibitor of Aurora kinases A, B and C with potential antineoplastic activity. Aurora kinase inhibitor AMG 900 selectively binds to and inhibits the activities of Aurora kinases A, B and C, which may result in inhibition of cellular division and proliferation in tumor cells that overexpress these kinases. Aurora kinases are serine-threonine kinases that play essential roles in mitotic checkpoint control during mitosis and are overexpressed by a wide variety of cancer cell types. C82349 639530 autologous NY-ESO-1-melanoma-specific CD8+ T cells A preparation of autologous CD8+ (cytotoxic) T-lymphocytes sensitized to cancer-testis antigen NY-ESO-1 antigen with potential immunostimulating and antineoplastic activities. Autologous CD8+ T-lymphocytes, isolated from a melanoma patient, are exposed to an NY-ESO-1 peptide ex vivo, expanded, and reintroduced into the patient; these tumor-reactive T-cells may stimulate a host immune response against tumor cells expressing the NY-ESO-1 antigen, resulting in tumor cell lysis. NY-ESO-1, an antigen found in normal testis, may be upregulated in various cancers, including bladder, breast, hepatocellular, melanoma, and prostate cancers. C82350 639653 M87o-transduced CD34+ peripheral blood stem cells Peripheral blood stem cells (PBSCs) transduced with the retroviral vector M87o encoding for the HIV-1-entry inhibitor peptide membrane-anchored antiviral peptide C46 (maC46). Expression of C46 by M87o-transduced CD34+ peripheral blood stem cells may prevent the fusion of viral and cellular membranes, thereby inhibiting HIV-1 entry. C46 is a membrane-anchored peptide encoding amino acids 628 to 673 of the HIV-1 entry inhibitory transmembrane glycoprotein gp41. C82351 639654 pVAXrcPSAv53l vaccine A cancer vaccine containing xenogenic DNA from rhesus macaque (Macaca mulatta) that encodes prostate specific antigen (PSA) with potential immunostimulating and antineoplastic activities. Upon repeated intradermal administration via electroporation, pVAXrcPSAv53l vaccine may induce a cytotoxic T-lymphocyte (CTL) response against PSA-expressing prostate cancer cells. Rhesus PSA is 89% homologous to human PSA. C82352 639691 TLR-directed cationic lipid-DNA complex JVRS-100 A cationic lipid DNA complex (CLDC) consisting of DOTIM/cholesterol liposomes and plasmid DNA, containing immunostimulatory CpG and non-CpG motifs, with potential immunostimulating and antineoplastic activities. Upon systemic administration, TLR-directed cationic lipid-DNA complex JVRS-100 enters dendritic cells (DCs) and macrophages; immunostimulatory DNA binds to and activates Toll-like receptors (TLRs), which may result in the generation of anti-tumor natural killer (NK) cell and T-cell responses by the innate immune system. In addition, as a vaccine adjuvant, this agent may induce a strong cytotoxic T-lymphocyte (CTL) response to co-administered antigen. C82353 639752 Lu-177-labeled di-HSG-DOTA peptide IMP-288 A radiolabeled divalent histamine-succinyl-glycine (HSG) hapten-peptide linked with the macrocyclic chelator 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA) to the radionuclide lutetium (Lu) 177. After pretargeting with a bispecific monoclonal antibody (BiMoAB) directed against both a tumor associated antigen (TAA) and the HSG hapten-peptide, the HSG portion of administered Lu-177-labeled di-HSG-DOTA peptide IMP-288 binds the anti-HSG portion of the BiMoAB; Lu-177 radioisotopic activity localized to tumor cells bearing the TAA can then be visualized scintigraphically. C82354 639754 anti-CEA/anti-HSG bispecific monoclonal antibody TF2 A tri-Fab bispecific monoclonal antibody (BiMoAb) divalent for the carcinoembryonic antigen (CEA) and monovalent for histamine-succinyl-glycine (HSG) peptide-hapten. Anti-CEA/anti-HSG bispecific monoclonal antibody TF2 binds to the tumor associated antigen (TAA) CEA on CEA-expressing tumor cells. Subsequently, an HSG peptide-hapten carrying a radionuclide is administered, binding to the anti-HSG binding fragment on the BiMoAb. Depending on the characteristics of the radionuclide used, CEA-expressing tumor cells may then be radioimaged and/or treated radioimmunotherapeutically. C82355 639760 indium In-111-DOTA-di-HSG peptide IMP-288 A radiolabeled divalent histamine-succinyl-glycine (HSG) hapten-peptide linked with the macrocyclic chelator 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA) to the radionuclide indium (In) 111. After pretargeting with a bispecific monoclonal antibody (BiMoAB) directed against both a tumor associated antigen (TAA) and the HSG hapten-peptide, the HSG portion of administered indium-In-labeled di-HSG-DOTA peptide IMP-288 binds the anti-HSG portion of the BiMoAB; In-111 radioisotopic activity localized to tumor cells bearing the TAA can then be visualized scintigraphically. C82356 640180 cefazolin sodium The sodium salt of cefazolin, a beta-lactam antibiotic and first-generation cephalosporin with bactericidal activity. Cefazolin binds to and inactivates penicillin-binding proteins (PBP) located on the inner membrane of the bacterial cell wall. Inactivation of PBPs interferes with the cross-linkage of peptidoglycan chains necessary for bacterial cell wall strength and rigidity, which results in the weakening of the bacterial cell wall and cell lysis. 640231 leucine-enhanced essential amino acid dietary supplement An orally bioavailable leucine enriched essential amino acid dietary supplement with potential anti-cachexia activity. Leucine-enhanced essential amino acid nutritional supplement may stimulate the mammalian target of rapamycin (mTOR) signaling pathway, which may promote protein synthesis in muscle cells. Although the exact mechanism by which leucine and other essential amino acids stimulate mTOR has yet to be fully elucidated, leucine may stimulate mTOR by inhibiting adenosine monophosphate protein kinase (AMPK), which negatively controls mTOR signaling. C82357 640250 adecatumumab A recombinant human IgG1 monoclonal antibody (MoAb) directed against the tumor associated antigen (TAA) epithelial cell adhesion molecule (EpCAM) with potential antitumor activity. Adecatumumab binds to EpCAM, which may result in antibody-dependent cellular cytotoxicity (ADCC) directed against EpCAM-expressing tumor cells. EpCAM (CD326), a cell surface protein upregulated on many tumor cell types, promotes the proliferation, migration and invasiveness of tumor cells; for some cancers, overexpression has been correlated with decreased survival. C82358 640261 technetium Tc 99m ethylenedicysteine-deoxyglucose A radiopharmaceutical consisting of ethylenedicysteine-deoxyglucose (EC-DG) labeled with the metastable radioisotope technetium Tc-99 (99mTc). Upon administration, technetium Tc 99m ethylenedicysteine-deoxyglucose accumulates in cells with increased metabolic activity such as proliferating tumor cells; tumor tissue may then be imaged using gamma scintigraphy. C82377 640265 anti-interleukin 6 monoclonal antibody ALD518 A humanized monoclonal antibody directed against the pro-inflammatory cytokine interleukin-6 (Il-6) with potential immunomodulating activity. Upon administration, anti-interleukin 6 monoclonal antibody ALD518 binds to and blocks the activity of IL-6, which may mitigate the catabolic effects of IL-6. C82359 640421 milatuzumab A humanized monoclonal antibody directed against CD74 with potential immunostimulating and antineoplastic activities. Milatuzumab binds to and inhibits the activity of the tumor-associated antigen (TAA) CD74, which may result in the death of CD74-expressing tumor cells. CD74, a TAA which may be overexpressed by myeloma and malignant B cells, may promote survival in rapidly proliferating tumor cells. C82360 640422 iCD40 receptor-expressing autologous dendritic cell vaccine BP-GMAX-CD1 A genetically-modified autologous dendritic cell-based vaccine expressing a drug-inducible costimulatory CD40 receptor (iCD40) with potential immunomodulating and antineoplastic activities. Autologous dendritic cells (DCs) are genetically modified to express the iCD40 receptor and are pulsed with tumor antigen. Upon intradermal administration, these DCs accumulate in local draining lymph nodes. Twenty-four hours after vaccination, the dimerizer agent AP1903 is administered; AP1903 binds to and activates iCD40 receptors presented on DC cell surfaces, thus activating the DCs and stimulating a cytotoxic T-lymphocyte (CTL) response against host tumor cells that express the tumor antigen. This delayed activation strategy optimizes DC accumulation in local draining lymph nodes prior to DC activation. iCD40 contains a membrane-localized cytoplasmic CD40 domain fused to a drug-binding domain. C82361 640440 dimerizer drug AP1903 A lipid-permeable tacrolimus analogue with homodimerizing activity. Dimerizer drug AP1903 homodimerizes an analogue of human protein FKBP12 (Fv) which contains a single acid substitution (Phe36Val) so that AP1903 binds to wild-type FKBP12 with 1000-fold lower affinity. This agent is used to homodimerize the Fv-containing drug-binding domains of genetically engineered receptors such as the iCD40 receptor of the autologous dendritic cell vaccine BP-GMAX-CD1, resulting in receptor activation. C82412 640624 innate immunostimulator rBBX-01 A recombinant 19 kDa protein derived from the Apicomplexa protozoan Eimeria with potential immunostimulating and antitumor activities. Upon administration, innate immunostimulator rBBX-01 activates dendritic cells (DCs), stimulates the Toll-like receptor 11 (TLR-11)-mediated release of interleukin-12 (Il-12) from DCs, and induces a T-helper 1 (Th1) type immune response, which may induce an immune response against tumor cells. Infection with Eimeria, a coccidian commonly infecting the intestine, may be negatively correlated with tumorigenesis. C82362 640626 c-Met/VEGFR kinase inhibitor E7050 An orally bioavailable dual kinase inhibitor of c-Met (hepatocyte growth factor receptor) and VEGFR-2 (vascular endothelial growth factor receptor-2) tyrosine kinases with potential antineoplastic activity. c-Met/VEGFR kinase inhibitor E7050 binds to and inhibits the activities of both c-Met and VEGFR-2, which may inhibit tumor cell growth and survival of tumor cells that overexpress these receptor tyrosine kinases. c-Met and VEGFR-2 are upregulated in a variety of various tumor cell types and play important roles in tumor cell growth, migration and angiogenesis. C82363 640630 acelullar cadaveric dermal matrix A human dermis-derived allograft material. Acellular cadaveric dermal matrix (ACDM) is derived from human cadaveric dermis from which the epidermis, all viable cells and major histocompatibility class (MHC) II antigens have been removed to minimize alloimmunogenicity, while the dermal collagen matrix is preserved. ACDM may placed over wounds to aid as a substitute for skin when necessary such as for surgical reconstruction or for protection against wound exposure and breakdown and wound infection. C82364 640964 CEOP regimen A chemotherapy regimen consisting of cyclophosphamide, epirubicin, Oncovin (vincristine), and prednisone which may be used in the treatment of aggressive non-Hodgkin lymphomas. C82410 640973 anti-DLL4 monoclonal antibody REGN421 A human monoclonal antibody directed against Delta-like ligand-4 (DLL4) with potential antineoplastic activity. Anti-DLL4 monoclonal antibody REGN421 specifically binds to human DLL4, preventing its binding to Notch receptors and inhibiting Notch signaling, which may result in defective tumor vascularization and, so, the inhibition of tumor cell growth. DLL4 is the only Notch ligand selectively expressed on endothelial cells; DLL4/Notch signaling is required for the development of functional tumor blood vessels. C82367 640980 CD34/TK75-transduced donor lymphocytes A preparation of donor T-lymphocytes that are transfected with a retroviral vector encoding a chimeric suicide gene consisting of the extracellular and transmembrane domains of human CD34 and mutant 75 of the herpes simplex virus thymidine kinase (HSV-TK75) with potential controllable immunomodulating activity. Donor T cell therapy following allogeneic hematopoietic stem cell (HSC) transplantation may result in a graft-versus-leukemia (GVL) and help control transplant-related viral infections. In the event that graft-versus-host disease (GVHD) develops due to donor lymphocyte infusion, CD34/TK75-transduced donor lymphocytes may be selectively eliminated by administration of the prodrug antiviral agent ganciclovir GCV. In CD34/T75-transduced donor lymphocytes, GCV is phosphorylated by expressed HSV-TK75 to its monophosphate form and, subsequently, converted into its active triphosphate form, which specifically kills the donor lymphocytes. The expressed CD34 moiety of the chimeric suicide gene serves as a selection marker; mutant 75 of HSV-TK confers increased GCV sensitivity. C82409 640981 losartan potassium The potassium salt of losartan, a non-peptide angiotensin II receptor antagonist with antihypertensive activity. Losartan selectively and competitively binds to the angiotensin II receptor (type AT1) and blocks the binding of angiotensin II to the receptor, thus promoting vasodilatation and counteracting the effects of aldosterone. Coverted from angiotensin I by angiotensin-converting enzyme (ACE), angiotensin II stimulates the adrenal cortex to synthesize and secrete aldosterone, decreasing sodium excretion and increasing potassium excretion, and acts as a vasoconstrictor in vascular smooth muscle. 641009 rabeprazole sodium The sodium salt of the prodrug rabeprazole, a substituted benzimidazole proton pump inhibitor, with potential anti-ulcer activity. After protonation, accumulation, and transformation to the active sulfenamide within the acidic environment of gastric parietal cells, rabeprazole selectively and irreversibly binds to and inhibits the H+, K+ATPase (hydrogen-potassium adenosine triphosphatase) enzyme system located on the parietal cell secretory surface, inhibiting gastric acid secretion. C29410 641166 bone metastasis targeting peptide-11 A peptide that mimics naturally occurring interleukin-11 (IL-11) with interleukin receptor binding activity. Upon administration, bone metastasis targeting peptide-11 (BMTP-11) binds to interleukin-11 receptor alpha (IL-11Ra) BMTP-11. This agent might be used to deliver therapeutic agents specifically to IL-11Ra-expressing tumor cells while sparing normal cells. IL-11Ra is a cell surface receptor that may be overexpressed by osteosarcoma cells and by prostate cancer cells in prostate cancer bone metastases. C82370 641167 recombinant Saccharomyces cerevisia-CEA(610D) vaccine GI-6207 A whole, heat-killed, recombinant Saccharomyces cerevisiae yeast-based vaccine genetically altered to express the carcinoembryonic antigen (CEA) peptide 610D with potential immunostimulating and antineoplastic activities. Upon administration, recombinant Saccharomyces cerevisia-CEA(610D) vaccine GI-6207 may stimulate a host cytotoxic T-lymphocyte (CTL) response against CEA-expressing tumor cells, which may result in tumor cell lysis. CEA, a tumor associated antigen, is overexpressed on a wide variety of human cancer cells including colorectal, gastric, lung, breast and pancreatic cancer cells. CEA 610D encodes for 9 amino acids (605-613) in which aspartate is substituted for asparagine at position 610 (610D) in order to strengthen the induction of the CTL response against CEA-expressing tumor cells. C82371 641179 anti-CD19/CD22 bispecific ligand-directed toxin DT2219ARL An immunotoxin consisting of two scFv ligands recognizing human CD19 and CD22 linked to the first 389 amino acids of diphtheria toxin (DT), DT 390, with potential antineoplastic activity. The VH and VL regions of anti-CD22 (sFv) and anti-CD19 are reversed and linked by an aggregration stabilizing linker (ARL) consisting of a 20 amino acid segment of human muscle aldolase (hma) and an Xho1 -compatible restriction site; the CDR3 region of the VH of anti-CD22 sFv is mutated to enhance its affinity. The anti-CD19 and anti CD-22 portions of the immunotoxin specifically bind to CD19 and CD22 receptors on tumor B cells. Upon internalization, DT catalyzes ADP ribosylation of elongation factor 2 (EF-2) which may result in the irreversible inhibition of protein synthesis and cell death in CD19- and CD22-expressing tumor cells. CD19 and CD22 transmembrane proteins upregulated on malignant B cells. C82375 641461 pan-VEGFR/Tie2 tyrosine kinase inhibitor CEP-11981 An orally bioavailable inhibitor of vascular endothelial growth factor receptor (VEGFR) and Tie2 receptor tyrosine kinases with potential antiangiogenic and antineoplastic activities. Pan-VEGFR/Tie2 tyrosine kinase inhibitor CEP-11981 selectively binds to VEGFR and Tie2 receptor tyrosine kinases, which may result the inhibition of endothelial cell migration, proliferation and survival and the inhibition of tumor cell proliferation and tumor cell death. VEGFR and Tie2 are frequently overexpressed by a variety of tumor cell types and play crucial roles in the regulation of angiogenesis and the maintenance of tumor blood vessels. Tie2 (tyrosine kinase with immunoglobulin-like\nand EGF-like domains) is activated by angiopoietin-1 (Ang-1). c82379 641462 PI3K inhibitor GDC-0941 bismesylate The orally bioavailable bismesylate salt of a potent small-molecule thieno[3,2-d]pyrimidine inhibitor of the class I phosphatidylinositol 3 kinase (PI3K) isoforms p100alpha and p100delta with potential antineoplastic activity. PI3K inhibitor GDC-0941 selectively binds to PI3K isoforms in an ATP-competitive manner, inhibiting the production of the secondary messenger phosphatidylinositol-3,4,5-trisphosphate (PIP3) and activation of the PI3K/Akt signaling pathway; inhibition of tumor cell growth, motility and survival in susceptible tumor cell populations may result. Activation of the PI3K/Akt signaling pathway is frequently associated with tumorigenesis; dysregulated PI3K/Akt signaling may contribute to tumor resistance to a variety of antineoplastic agents. C82380 641467 human myeloid progenitor cells CLT-008 Early- to late-stage myeloid progenitor cells derived from adult human stem cells with potential hematopoietic activity. Upon infusion, human myeloid progenitor cells CLT-008 proliferate into mature myeloid cells, including granulocytes, macrophages, platelets, and erythrocytes. These myeloid progenitor cells die within forty-five days after a burst of hematopoiesis. This agent cannot create lymphoid cells, including T cells associated with graft-versus-host disease (GVHD). C82381 641468 DNA minor groove-binding agent PM01183 A synthetic tetrahydropyrrolo [4, 3, 2-de]quinolin-8(1H)-one alkaloid analogue with potential antineoplastic activity. DNA minor groove-binding agent PM01183 covalently binds to residues lying in the minor groove of DNA, which may result in delayed progression through S phase, cell cycle arrest in the G2/M phase and cell death. C82382 641472 gamma secretase inhibitor PF-03084014 A selective gamma secretase (GS) inhibitor with potential antitumor activity. Gamma secretase inhibitor PF-03084014 binds to GS, blocking proteolytic activation of Notch receptors; Notch signaling pathway inhibition may follow, which may result in the induction of apoptosis in tumor cells that overexpress Notch. The integral membrane protein GS is a multi-subunit protease complex that cleaves single-pass transmembrane proteins, such as Notch receptors, at residues within their transmembrane domains. Overexpression of the Notch signaling pathway has been correlated with increased tumor cell growth and survival. C82383 641917 TSP-1 mimetic fusion protein CVX-045 A fusion protein containing two thrombospondin (TSP-1)-derived nonamer peptides covalently attached, via a proprietary diketone linker, to a proprietary humanized catalytic monoclonal aldolase monoclonal antibody with potential antiangiogenic and antineoplastic activities. The TSP-1 mimetic peptide moieties of TSP-1 mimetic fusion protein CVX-045 bind to TSP-1 receptors, such as CD36, and inhibit tumor angiogenesis, which may result in the inhibition of tumor cell proliferation. The proprietary humanized catalytic monoclonal aldolase monoclonal antibody contains reactive lysine residues in its binding sites, which react covalently with compounds having a diketone function; the TSP-1 mimetic peptide moieties are then covalently attached to the diketone linkers via a proprietary spacer. C82384 641919 immunocytokine NHS-IL2-LT A fusion protein consisting of a mouse-human chimeric antibody directed against DNA released by necrotic tumor cells fused to two molecules of a genetically modified human interleukin-2 (IL-2) with potential antineoplastic activity. Upon administration, the antibody moiety of immunocytokine NHS-IL2-LT binds to DNA released by necrotic tumor cells located primarily at the core of necrotic solid tumors, delivering the IL-2 moiety. In turn, the IL-2 moiety of this agent activates the immune system to mount a cytotoxic T lymphocyte response against nearby tumor cells. C82411 641974 Smoothened antagonist LDE225 An orally bioavailable small-molecule Smoothened (Smo) antagonist with potential antineoplastic activity. Smoothened antagonist LDE225 selectively binds to the Hedgehog (Hh)-ligand cell surface receptor Smo, which may result in the suppression of the Hh signaling pathway and, so, the inhibition of tumor cells in which this pathway is abnormally activated. The Hh signaling pathway plays an important role in cellular growth, differentiation and repair. Inappropriate activation of Hh pathway signaling and uncontrolled cellular proliferation, as is observed in a variety of cancers, may be associated with mutations in the Hh-ligand cell surface receptor Smo. C82385 641977 BRAF inhibitor GSK2118436 An orally bioavailable inhibitor of B-raf (BRAF) protein with potential antineoplastic activity. BRAF inhibitor GSK2118436 selectively binds to and inhibits the activity of B-raf, which may inhibit the proliferation of tumor cells which contain a mutated BRAF gene. B-raf belongs to the the raf/mil family of serine/threonine protein kinases and plays a role in regulating the MAP kinase/ERKs signaling pathway, which may be constitutively activated due to BRAF gene mutations. C82386 641983 HSP90 inhibitor HSP990 An orally bioavailable inhibitor of human heat-shock protein 90 (Hsp90) with potential antineoplastic activity. Hsp90 inhibitor Hsp990 binds to and inhibits the activity of Hsp90, which may result in the proteasomal degradation of oncogenic client proteins, including HER2/ERBB2, and the inhibition of tumor cell proliferation. Hsp90, upregulated in a variety of tumor cells, is a molecular chaperone that plays a key role in the conformational maturation, stability and function of oncogenic signaling proteins, such as HER2/ERBB2, AKT, RAF1, BCR-ABL, and mutated p53, as well as many other molecules that are important in cell cycle regulation and/or immune responses. C82387 642215 autologous GM-CSF-secreting breast cancer vaccine An autologous tumor cell vaccine containing irradiated breast cancer cells transfected with the granulocyte macrophage-colony-stimulating factor (GM-CSF) gene with potential antineoplastic activity. Autologous breast cancer cells are transduced ex vivo with an adenovirus vector encoding the GM-CSF gene and irradiated and then reintroduced into the patient. Upon repeated subcutaneous administration of the vaccine, autologous GM-CSF-secreting breast cancer cells secrete GM-CSF, which may stimulate a tumor-specific cytotoxic T-lymphocyte (CTL) response. C82388 642286 Polo-like kinase 1 inhibitor MK1496 An orally bioavailable Polo-like kinase 1 (Plk1) inhibitor with potential antineoplastic activity. Polo-like kinase 1 inhibitor MK1496 selectively inhibits Plk1, inducing selective G2/M arrest followed by apoptosis in a variety of tumor cells while causing reversible cell arrest at the G1 and G2 stage without apoptosis in normal cells. Plk1, named after the polo gene of Drosophila melanogaster, is a serine/threonine protein kinase involved in regulating mitotic spindle function in a non-ATP competitive manner. C82389 642287 Akt inhibitor GSK2110183 An orally bioavailable inhibitor of the serine/threonine protein kinase Akt (protein kinase B) with potential antineoplastic activity. Akt inhibitor GSK2110183 binds to and inhibits the activity of Akt, which may result in inhibition of the PI3K/Akt signaling pathway and tumor cell proliferation and the induction of tumor cell apoptosis. Activation of the PI3K/Akt signaling pathway is frequently associated with tumorigenesis and dysregulated PI3K/Akt signaling may contribute to tumor resistance to a variety of antineoplastic agents. C82390 642288 KSP/VEGF siRNAs ALN-VSP02 A lipid nanoparticle formulation containing two small interfering RNAs (siRNAs) for kinesin spindle protein (KSP) and vascular endothelial growth factor (VEGF) with potential antitumor activity. Upon intravenous administration, the siRNAs in KSP/VEGF siRNAs ALN-VSP02ALN bind to both KSP and VEGF messenger RNAs (mRNAs), preventing translation of KSP and VEGF proteins; this may result in growth inhibition of tumor cells that overexpress KSP and VEGF. VEGF and KSP are upregulated in many tumor cells and play an important role in tumor proliferation and survival. C82391 642488 autologous CD133-positive BTSC mRNA-pulsed autologous dendritic cell vaccine A cancer vaccine consisting of autologous dendritic cells (DCs) loaded with CD133-positive autologous brain tumor stem cells (BTSCs) –derived mRNA with potential immunostimulatory and antineoplastic activities. Upon intradermal administration, autologous CD133-positive BTSC mRNA-pulsed autologous dendritic cell vaccine may elicit a cytotoxic T-lymphocyte (CTL) response against the CD133-positive BTSCs from which the autologous tumor mRNA is derived. CD133, a tumor-associated antigen (TAA) and neural stem cell marker, has been found on a specific subset of glioblastoma multiforme (GBM) stem cells; its presence has been correlated with resistance to conventional chemotherapy and radiotherapy. C85445 642493 iodine I 131-labeled anti-CEA/anti-HSG bispecific monoclonal antibody TF2 A tri-Fab bispecific monoclonal antibody (BiMoAb) divalent for the carcinoembryonic antigen (CEA) and monovalent for histamine-succinyl-glycine (HSG) peptide-hapten radiolabeled with iodine I 131 (I131) with antigen-binding and radioisotopic activities. Iodine I 131-labeled anti-CEA/anti-HSG bispecific monoclonal antibody TF2 binds to the tumor-associated antigen (TAA) CEA on CEA-expressing tumor cells; these cells may then be radioimaged scintigraphically. C85446 642531 recombinant human angiotensin converting enzyme 2 APN01 A recombinant, soluble glycosylated form of human angiotensin converting enzyme 2 (rhACE2) with antihypertensive and potential antineoplastic activities. Recombinant human angiotensin converting enzyme 2 APN01 may normalize ACE2 levels, cleaving angiotensin II to create angiotensin-(1-7) and restoring the function of the renin-angiotensin system (RAS). ACE2, a homolog of ACE1, appears to function as a negative regulator of the RAS system by converting angiotensin II to angiotensin-(1-7), a peptide with actions that counteract the cardiovascular actions of angiotensin II. In addition, angiotensin-(1-7) may inhibit cyclooxygenase 2 (COX-2) and the production of proinflammatory prostaglandins and may activate the angiotensin-(1-7) G protein-coupled receptor Mas, resulting in diminished tumor cell proliferation. ACE2 levels may be reduced in malignancy and diabetes and in liver, cardiovascular and lung diseases. C85447 642606 Akt inhibitor SR13668 An orally bioavailable indole-3-carbinol (I3C) analogue inhibitor of the serine/threonine protein kinase Akt (protein kinase B) with potential antineoplastic and antiangiogenic activities. Akt inhibitor SR13668 binds to and inhibits the activity of Akt, which may result in inhibition of the PI3K/Akt signaling pathway and tumor cell proliferation, and the induction of tumor cell apoptosis. Activation of the PI3K/Akt signaling pathway is frequently associated with tumorigenesis and dysregulated PI3K/Akt signaling may contribute to tumor resistance to a variety of antineoplastic agents. C85448 642612 [F18]VM4-037 A radiopharmaceutical consisting of a sulfonamide covalently attached to the positron-emitting isotope fluorine F 18 with CA-IX-binding and radioisotopic activities. Upon administration, the sulfonamide moiety of [F18]VM4-037 binds to the cell-surface tumor-associated antigen (TAA) carbonic anhydrase IX isoenzyme (CA-IX); CA-IX-expressing tumor cells can then be visualized using positron emission tomography (PET). CA-IX has been found to be elevated in a variety of hypoxic tumors; elevated CA-IX has been positively correlated with tumor growth, tumor invasion and poor prognosis. C85449 642644 autologous lymphoma cell/autologous dendritic cell electrofusion hybrid vaccine A cell-based cancer vaccine consisting of hybrid cells created by electrofusing autologous dendritic cells (DCs) and autologous lymphoma cells with potential immunostimulating and antitumor activities. Upon administration, autologous lymphoma cell/autologous dendritic cell electrofusion hybrid vaccine may stimulate the immune system to mount a specific cytotoxic T-lymphocyte (CTL) response against specific autologous lymphoma-associated antigens, resulting in lymphoma cell apoptosis. C85450 642645 autologous lymphoma cell/allogeneic dendritic cell electrofusion hybrid vaccine A cell-based cancer vaccine consisting of hybrid cells created by electrofusing autologous dendritic cells (DCs) and allogeneic lymphoma cells with potential immunostimulating and antitumor activities. Upon administration, autologous lymphoma cell/allogeneic dendritic cell electrofusion hybrid vaccine may stimulate the immune system to mount a specific cytotoxic T-lymphocyte (CTL) response against specific autologous lymphoma-associated antigens, resulting in lymphoma cell apoptosis. C85451 642647 autologous lymphoma cell lysate-pulsed autologous dendritic cell vaccine A cell-based cancer vaccine composed of autologous dendritic cells (DCs) pulsed with lysate from autologous lymphoma cells with potential immunostimulatory and antineoplastic activities. Upon intranodal administration, autologous lymphoma cell lysate-pulsed autologous DC vaccine may stimulate the immune system to mount anti-tumoral cytotoxic T lymphocyte (CTL) and antibody responses against lymphoma cells, which may result in lymphoma cell lysis. C85452 642753 Anti-FLT3 monoclonal antibody IMC-EB10 A fully human, IgG1 monoclonal antibody directed against the FLT3 tyrosine kinase receptor (CD135) with potential antineoplastic activity. Upon binding to FLT3, anti-FLT3 monoclonal antibody IMC-EB10 blocks FLT3 ligand binding to FLT3 and subsequent FLT3 phosphorylation, which may result in the inhibition of FLT3-mediated signal transduction pathways. In addition, this agent may stimulate an anti-FLT3 antibody-dependent cell-mediated cytotoxicity (ADCC) against FLT3-expressing tumor cells, which may result in the inhibition of cellular proliferation and survival in FLT3-expressing cells. FLT3 (FLK2), a class III tyrosine kinase receptor, is overexpressed or mutated in most B lineage and acute myeloid leukemias. C85453 642817 Hsp90 inhibitor AT13387 A synthetic, orally bioavailable, small-molecule inhibitor of heat shock protein 90 (Hsp90) with potential antineoplastic activity. Hsp90 inhibitor AT13387 selectively binds to Hsp90, thereby inhibiting its chaperone function and promoting the degradation of oncogenic signaling proteins involved in tumor cell proliferation and survival. Hsp90, a chaperone protein upregulated in a variety of tumor cells, regulates the folding, stability and degradation of many oncogenic signaling proteins. C85454 642819 HLA-A*2402-restricted URLC10-CDCA1-VEGFR1-VEGFR2 multipeptide vaccine A cancer vaccine containing four HLA-A*2402-restricted peptide epitopes with potential immunostimulatory and antitumor activities. The peptide epitopes are derived from URLC10 (up-regulated lung cancer 10); CDCA1 (cell division associated 1); and vascular endothelial growth factor receptors (VEGFRs) 1 and 2. Upon administration, HLA-A*2402-restricted URLC10-CDCA1-VEGFR1-VEGFR2 multipeptide vaccine may stimulate a cytotoxic T lymphocyte (CTL) response against URL10-, CDCA1-, VEGFR1- and VEGFR2-expressing tumor cells, resulting in tumor cell lysis and decreased tumor cell proliferation. HLA-A*2402 is an MHC class I molecule that presents antigenic peptides to CD8+ T cells; epitope design restricted to epitopes that bind most efficiently to HLA-A*2402 may improve antigenic peptide immunogenicity. C85455 642824 granisetron transdermal system A transdermal system containing the selective serotonin (5-HT) receptor antagonist granisetron with antinauseant and antiemetic activities. Upon application of the transdermal system (patch) to the skin and the subsequent sustained release of granisetron into the bloodstream, granisetron selectively binds to and inhibits 5-HT subtype 3 (5-HT3) receptors located peripherally on vagus nerve terminals and centrally in the chemoreceptor trigger zone (CTZ) of the area postrema, which may result in suppression of chemotherapy-induced nausea and vomiting. C80377 642968 DNP-modified autologous renal cell carcinoma tumor cell vaccine A cancer vaccine consisting of autologous renal cell carcinoma (RCC) tumor cells modified with the hapten 2,4-dinitrophenol (DNP) with potential immunostimulating and antineoplastic activities. Administration of DNP-modified autologous renal cell carcinoma tumor cell vaccine may induce a cytotoxic T-lymphocyte (CTL) response against renal cell carcinoma tumor cells. DNP conjugation may enhance the immunogenicity of weakly immunogenic antigens. C85456 642976 vinorelbine tartrate oral An orally bioavailable tartrate salt of vinorelbine, a semisynthetic vinca alkaloid with potential antineoplastic activity. Vinorelbine binds to tubulin, thereby inhibiting tubulin polymerization into microtubules and spindle formation and resulting in apoptosis of susceptible cancer cells. Inhibition of mitotic microtubules correlates with antitumor activity, whereas inhibition of axonal microtubules seems to correlate with vinorelbine's neurotoxicity. Compared to related vinca alkaloids, vinorelbine is more selective against mitotic than axonal microtubules in vitro, which may account for its decreased neurotoxicity. This agent is also a radiation-sensitizing agent. C85457 643465 technectium Tc 99m-NC100692 A synthetic Arg-Gly-Asp (RGD)-containing cyclic peptide radiolabeled with technetium Tc 99m with integrin-binding and radioisotopic activities. Upon administration, technectium Tc 99m-NC100692 binds to alpha5beta3 integrin and to a lesser extent alpha5beta5; subsequently, alpha5beta3-expressing tumor cells can be visualized using scintigraphy and the degree of tumor angiogenesis can be determined. Integrins, membrane-spanning protein receptors, may be upregulated on proliferating endothelial cells; their overexpression has been associated with neovascularization, differentiation, proliferation of tumor cells and poor prognosis. C85458 643475 autologous HER2 chimeric receptor/TGFbeta dominant negative receptor-expressing EBV-specific cytotoxic T lymphocytes A preparation of transforming growth factor-beta (TGF-beta)-resistant Epstein-Barr virus (EBV)-specific cytotoxic T-lymphocytes (CTLs) directed to EBV through their native receptor and HER2 through a retrovirally transduced HER2 chimeric antigen receptor (CAR) with potential antineoplastic activity. Autologous EBV-specific CTLs are produced by exposing autologous CTLs to "stimulator" autologous EBV-transformed lymphoblastoid cell lines (EBV-LCLs). Subsequently, autologous EBV-specific CTLs are transduced with retroviral vectors expressing the mutant type II TGF-beta dominant-negative receptor (DNR), which blocks signaling by all three TGF-beta isoforms, and the HER2 CAR. After transduction, transgenic EBV-CTLs are expanded on EBV-LCLs. Upon administration, autologous HER2 chimeric receptor/TGFbeta dominant negative receptor-expressing EBV-specific cytotoxic T lymphocytes may bind to HER2-expressing tumors cells, which may result in CTL-mediated cell lysis and inhibition of tumor cell proliferation. Tumor-expressed TGF-beta inhibits T lymphocyte activation and expansion. C85459 643477 CK2 inhibitor CX-4945 An orally bioavailable small-molecule inhibitor of CK2 with potential antineoplastic activity. CK2 inhibitor CX-4945 selectively binds to and inhibits the enzyme casein kinase II (CK2), which may lead to an inhibition of cellular proliferation. CK2, a protein kinase often overexpressed in a variety of cancer cell types, appears to be correlated with malignant transformation, tumor growth and survival. C85460 643573 iodine I 123 iodobenzamide A radiopharmaceutical containing the dopamine D2/D3 receptor agonist iodobenzamide (IBZM) labeled with the radionuclide iodine I 123 with dopamine receptor-binding and radioisotopic activities. Upon administration, iodine I 123 iodobenzamide binds to dopamine D2/D3 receptors; subsequently, tissues expressing these receptors can be visualized using single photon emission computed tomography (SPECT). Dopamine receptors are a class of metabotropic G protein-coupled receptors found in the central nervous system (CNS) and neuroendocrine tumors such as pheochromocytoma and paraganglioma. C85461 643625 TARP 27-35 peptide vaccine A peptide-based cancer vaccine, containing amino acid residues 27 through 35 of T cell receptor gamma alternate reading frame protein (TARP), with potential immunostimulatory and antineoplastic activities. Upon administration, TARP 27-35 peptide vaccine may stimulate a host cytotoxic T-cell (CTL) response against TARP-expressing tumor cells, resulting in tumor cell cytotoxicity. The nuclear protein TARP is commonly expressed on prostate and breast cancer cells and is highly immunogenic. C85462 643628 TARP 29-37-9V peptide vaccine A peptide-based cancer vaccine, consisting of amino acid residues 29 through 37 of T cell receptor gamma alternate reading frame protein (TARP) with a leucine-to-valine substitution at position 9, with potential immunostimulatory and antineoplastic activities. Upon administration, TARP 29-37-9V peptide vaccine may induce a cytotoxic T-lymphocyte (CTL) response against TARP-expressing tumor cells, which may result in decreased tumor cell proliferation. The leucine-to-valine substitution at position 9 of this peptide improves its immunogenicity. The nuclear protein TARP is commonly expressed on prostate and breast cancer cells and is highly immunogenic. C85463 643767 anti-GnRH vaccine PEP223 A peptide vaccine derived from the synthetic peptide pyroEHWSYGLRPG, corresponding to amino acids 22-31 of mouse gonadotropin releasing hormone (GnRH), with potential immunocastration activity. PEP223 is dimerized and contains a D-lysine (k) substitution at position 6 (pyroEHWSYkLRPG) to increase its immunogenicity. Anti-GnRH vaccine PEP223 may stimulate the immune system to mount a cytotoxic T-lymphocyte (CTL) response against GnRH, neutralizing its activity. In turn, testosterone production and tumor cell growth may be inhibited in testosterone-sensitive tumors. C85464 643796 p53 activator APR-246 A quinuclidinone derivative that targets the Wrap53 gene with potential antineoplastic activity. p53 activator APR-246 binds to and activates transcription of the Wrap53 gene, which results in an increase in WRAP53 p53 antisense transcript levels and, potentially, an increase in native p53 activity; in turn, increased p53 activity may lead to an induction of cell cycle arrest and apoptosis in tumor cells. This agent may work synergistically with other antineoplastic agents. p53, a tumor suppressor and transcription factor normally activated upon DNA damage, is mutated or absent in various cancer cell types and plays a key role in DNA repair and the induction of apoptosis. The Wrap53 transcript, a natural p53 antisense transcript, regulates endogenous p53 mRNA levels and additional induction of p53 protein by targeting the 5' untranslated region of p53 mRNA. C85465 643814 natural killer cells ZRx101 A population of activated, immortalized, interleukin-2 (IL-2)-dependent, cytotoxic natural killer (NK) cells with potential antitumor activity. Natural killer cells ZRx101 are derived from NK-92 cells, having been modified to target tumor-associated antigens (TAAs) upregulated in certain types of cancer. The NK-92 cell line was originally isolated from a patient with large granular lymphocytic (LGL) leukemia/lymphoma. C85466 644219 rAD-p53 A replication-defective, recombinant adenoviral vector encoding the wild-type human tumor-suppressor protein p53 gene with potential antineoplastic activity. Upon intratumoral administration, rAD-p53 binds to the coxsakie-and-adenovirus receptor (CAR) on tumor cells and enters cells selectively via receptor-mediated endocytosis, which may result in the overexpression of wild-type p53 intracellularly and p53-mediated tumor regression. In addition, this agent may stimulate the immune system to mount a cytotoxic T-lymphocyte (CTL) immune response against tumor cells, may activate natural killer (NK) cells to exert antitumor ‘bystander effects’ and may downregulate the expression of various oncogenes. The p53 protein blocks tumor cell cycle progression and directly initiates apoptosis; the p53 gene, a tumor suppressor gene, is deleted or mutated in a significant number of cancers. C85485 644381 formoterol fumarate oral The orally bioavailable fumarate salt of formoterol, a long-acting, selective beta2-adrenergic receptor agonist with bronchodilating and potential anti-cachexia and anabolic activities. In addition to formoterol’s bronchodilating activity, formoterol exhibits anti-cachexia activity through the inhibition of the ATP-ubiquitin-dependent proteolytic system, which may result in a decrease in protein degradation and muscle cell apoptosis. In addition, formoterol may also increase insulin-like growth factor (IGF) signaling, resulting in an increase in protein synthesis. This agent may also inhibit the calcium-dependent calpain system, resulting in the inhibition of muscle wasting. 644579 supersaturated calcium phosphate rinse An aqueous oral rinse composed of an electrolyte solution supersaturated with phosphate and calcium ions with antimucositis and analgesic activities. This solution may help relieve mucositis and mucositis-induced pain by restoring the natural electrolyte and pH balance of human saliva and lubricating mucosal tissues of the mouth, tongue and oropharynx. C84398 644818 pan-PI3K/mTOR inhibitor SF1126 A water soluble, small-molecule prodrug containing the pan-PI3K/mTOR inhibitor LY294002/SF1101 conjugated to the RGD-containing tetra-peptide SF1174 with potential antineoplastic and antiangiogenic activities. The targeting peptide SF1174 moiety of pan-PI3K/mTOR inhibitor SF1126 selectively binds to cell surface integrins and, upon cell entry, the agent is hydrolyzed to the active drug SF1101; SF1101 selectively inhibits all isoforms of phosphoinositide-3-kinase (PI3K) and other members of the PI3K superfamily, such as the mammalian target of rapamycin (mTOR) and DNA-PK. By inhibiting the PI3K signaling pathway, this agent may inhibit tumor cell and tumor endothelial cell proliferation and survival.\nIntegrins are transmembrane cell adhesion proteins expressed on the surfaces of endothelial and tumor cells. C85469 644896 autologous TARP peptide-pulsed dendritic cell vaccine A cell-based cancer vaccine comprised of autologous dendritic cells pulsed with autologous T cell receptor gamma-chain alternate reading frame protein (TARP) peptide with potential immunostimulatory and antineoplastic activities. Upon intradermal administration, autologous TARP peptide-pulsed dendritic cell vaccine may stimulate anti-tumoral cytotoxic T lymphocyte (CTL) and antibody responses against TARP-expressing cancer cells, resulting in tumor cell lysis. The highly immunogenic nuclear protein TARP is commonly expressed in breast and prostate cancer cells. C85470 646826 stabilized sulphur hexafluoride microbubble-based contrast agent An injectable ultrasound contrast media formulation composed of microbubbles of stabilized sulphur hexafluoride (SF6) in sodium chloride solution. With stabilized sulphur hexafluoride microbubble-based contrast agent, ultrasound waves are scattered and reflected at the microbubble-blood interface during ultrasound imaging, thereby enhancing blood vessel visualization and the contrast between blood vessels and adjacent tissues. C85471 646836 carbon C 14 eribulin acetate A radioconjugate containing the acetate salt of eribulin, labeled with the beta particle-emitting radioisotope carbon C 14 , with radioisotopic and potential antineoplastic activities. Upon administration, eribulin binds to the vinca domain of tubulin and inhibits the polymerization of tubulin and the assembly of microtubules, resulting in inhibition of mitotic spindle assembly, induction of cell cycle arrest at G2/M phase, and, potentially, tumor regression. The radioisotope moiety of this agent acts as a radioactive tracer. C85472 646997 calcium-41 chloride aqueous solution An orally bioavailable aqueous solution containing the chloride salt of the radioisotope calcium-41 (41Ca) with phosphate-binding and radioisotopic activities. Upon administration of calcium-41 chloride aqueous solution, calcium-41 is preferentially taken up by osteoblasts, which generate mineralized osteoid containing calcium. Calcium-41 accumulation and turnover in bone can be measured with bone scintigraphy and urinary isotope excretion testing. C85473 646998 calcium-46 chloride aqueous solution An orally bioavailable aqueous solution containing the chloride salt of the radioisotope calcium-46 (46Ca) with phosphate-binding and radioisotopic activities. Upon administration of calcium-46 chloride aqueous solution, calcium-46 is preferentially taken up by osteoblasts, which generate mineralized osteoid containing calcium. Calcium-46 accumulation and turnover in bone can be measured with bone scintigraphy and urinary isotope excretion testing. C85474 647103 claudiximab A monoclonal antibody directed against the antigen GC182 with potential immunostimulatory and antineoplastic activities. Upon administration, claudiximab specifically binds to GC128, which may stimulate the immune system to mount a cytotoxic T-lymphocyte (CTL) response against GC182-expressing tumor cells, resulting in decreased tumor cell proliferation. The CD20-like antigen GC182, a gastric differentiation protein, is often overexpressed on the cell surfaces of a variety of tumor cells, including gastric, pancreatic, esophageal cancer and non-small cell lung cancer (NSCLC) cells. C85475 647541 micellar nanoparticle-encapsulated cisplatin NC-6004 A nanoparticle-based prodrug formulation consisting of polymeric micelles incorporating the inorganic platinum agent cisplatin with potential antineoplastic activity. In micellar nanoparticle-encapsulated cisplatin NC-6004, cisplatin forms a polymer-metal complex with hydrophilic polyethylene glycol poly(glutamic acid) block copolymers by attaching to the micelle inner core consisting of the hydrophobic polymer polyamino acid. Upon cell entry and release from the polymer-metal complex, cisplatin forms highly reactive, charged platinum complexes that bind to nucleophilic groups such as GC-rich sites in DNA, inducing intrastrand and interstrand DNA cross-linking, DNA-protein cross-linking and, subsequently, tumor cell apoptosis and growth inhibition. Due to the hydrophilic nature of polyethylene glycol, this formulation increases the water-solubility of cisplatin and decreases the nephrotoxicity and neurotoxicity associated with the administration of cisplatin alone. C85476 647542 anti-ErbB2/anti-ErbB3 bispecific monoclonal antibody MM-111 A bispecific monoclonal antibody directed against the human epidermal growth factor receptors ErbB2 (Her2) and ErbB3 (Her3) with potential antineoplastic activity. The anti-ErB2 targeting arm of anti-ErbB2/anti-ErbB3 bispecific monoclonal antibody MM-111 binds to ErbB2 on tumor cells with high affinity while the anti-Erb3 therapeutic arm binds to ErbB3, which may result in the inhibition of cellular proliferation and differentiation in ErbB2-overexpressing tumor cells via inhibition of ErbB3-dependent signal transduction pathways. ErbB2 and ErB3 are members of the epidermal growth factor receptor (EGFR) family of receptor tyrosine kinases and are frequently overexpressed in solid tumors. C85486 647806 ferumoxides injectable solution An injectable, aqueous colloid solution containing a non-stoichiometric magnetite core of superparamagnetic iron oxide (SPIO) coated with dextran administered as a magnetic resonance imaging (MRI) contrast media. Upon intravenous administration, ferumoxides accumulates in phagocytic reticuloendothelial system (RES) cells of the liver (Kupffer cells). When exposed to a strong external magnetic field, ferumoxides exhibits enhanced T2 relaxation, resulting in signal loss in normal tissues (image darkening) on mid T1/T2 or strongly T2-weighted images. Tissues with decreased RES function such as metastases, primary liver cancer, cysts and various benign tumors, adenomas, and hyperplasia, retain their native signal intensity, consequently the contrast between normal tissue (with image darkening) and abnormal tissue is increased. C85477 647821 anti-A5B1 integrin monoclonal antibody PF-04605412 A monoclonal antibody directed against the human alpha5beta1 integrin with potential antiangiogenic and antineoplastic activities. Anti-alpha5beta1 integrin monoclonal antibody PF-04605412 selectively binds to alpha5beta1 integrin, preventing the binding of integrin ligands. This may result in the inhibition of endothelial cell-cell interactions, endothelial cell-matrix interactions, and integrin-mediated tumor angiogenesis and metastasis in alpha5beta1-expressing tumor cells. Alpha5beta1 integrin, a cell adhesion and signaling receptor, is often overexpressed on the surface of tumor vessel endothelial cells and plays a crucial role in endothelial cell adhesion and migration. C85478 647824 autologous renal cell carcinoma tumor lysate-dendritic cell vaccine A cell-based cancer vaccine composed of autologous dendritic cells (DCs) pulsed with renal cell carcinoma (RCC) tumor cell lysate containing tumor associated antigens (TAAs) with potential immunostimulatory and antineoplastic activities. Upon administration, autologous renal cell carcinoma tumor lysate-dendritic cell vaccine may stimulate anti-tumoral cytotoxic T-lymphocyte (CTL) and antibody responses against RCC tumor cells expressing RCC TAAs, resulting in RCC tumor cell lysis. C85479 647827 azurin-derived cell-penetrating peptide p28 A water-soluble, amphipathic, 28 amino acid (amino acids 50-77), 2.9 kD fragment peptide (p28) derived from the protein azurin with potential antineoplastic and antiangiogenic activities. Although the mechanism has yet to be fully elucidated, the preferential cellular uptake of azurin-derived cell-penetrating peptide p28 by tumor cells and endothelial cells is likely via caveolae-mediated endocytosis; the C-terminal 18 amino acid residues (50-67) appear to responsible for this preferential uptake. After cell entry, the first 12 amino acid residues interact with tumor suppressor p53 and form a p28:p53 complex, which may result in a reduction of proteasomal degradation of p53, increased p53 levels, and p53-mediated cell cycle inhibition and apoptosis.\nAzurin is a cupredoxin secreted by the bacterium Pseudomonas aeruginosa. Cell penetrating peptides (CPPs) are cationic and/or amphipathic peptides, typically less than 30 amino acids in length, that can penetrate cell membranes easily and may transport molecular cargo. C85480 647828 p38/Tie2 kinase inhibitor Arry-614 An orally bioavailable small-molecule inhibitor of p38 and Tie2 kinases with potential antineoplastic, anti-inflammatory and antiangiogenic activities. p38/Tie2 kinase inhibitor Arry-614 binds to and inhibits the activities of p38 and Tie2 kinases, which may inhibit the production of proinflammatory cytokines and may decrease tumor angiogenesis and tumor cell growth and survival. p38 is a MAP kinase that is often upregulated in cancer cells, playing a crucial part in the production of a variety of cytokines involved in inflammation and cellular proliferation such as tumor necrosis factor (TNF) and interleukin (IL)-1 and -6. Tie2 is an endothelial cell specific receptor that is activated by angiopoietins, growth factors required for angiogenesis. This agent has also been reported to inhibit other kinases including vascular endothelial growth factor receptor (VEGFR2) and Src tyrosine kinases. C85481 648122 2-hydroxyflutamide depot A depot formulation containing a bioresorbable, controlled-release, calcium sulphate-based paste of the nonsteroidal antiandrogen 2-hydroxyflutamide (2-HOF) with potential antineoplastic activity. Upon injection into the tumor site in the prostate, 2-hydroxyflutamide depot slowly releases 2-HOF, which competitively binds to androgen receptors (ARs), blocking the binding of dihydrotestosterone (DHT). This may inhibit androgen-dependent DNA and protein synthesis, resulting in tumor cell growth arrest and decreased cellular proliferation. In addition, 2-HOF inhibits nuclear uptake of androgen in androgen-responsive tissues. C85482 648124 buprenorphine transdermal matrix patch A transdermal matrix patch containing the synthetic opioid buprenorphine with analgesic and sedative activities. Buprenorphine binds to and activates the mu-opioid receptors in the central nervous system (CNS), thereby mimicking the effects of the endogenous opiates. Binding to opioid receptors stimulates exchange of GTP for GDP, inhibits adenylate cyclase, and decreases intracellular cAMP. This inhibits the release of various nociceptive neurotransmitters, such as substance P, gamma-aminobutyric acid (GABA), dopamine, acetylcholine, noradrenaline, vasopressin, and somatostatin. In addition, buprenorphine closes N-type voltage-gated calcium channels and opens calcium-dependent inwardly rectifying potassium channels, resulting in hyperpolarization, reduced neuronal excitability, analgesia and sedation. Buprenorphine is a partial agonist at the mu-opioid receptor and an antagonist at the kappa-opioid receptor in the CNS. C85483 648245 resveratrol formulation SRT501 A proprietary formulation of resveratrol, a polyphenolic phytoalexin derived from grapes and other food products with potential antioxidant, anti-obesity, antidiabetic and chemopreventive activities. Resveratrol may activate sirtuin subtype 1 (SIRT-1). SIRT1 activation has been reported to inhibit tumorigenesis and tumor cell proliferation.\nSIRT-1 is a member of the silent information regulator 2 (SIR2) (or sirtuin) family of enzymes that plays an important role in mitochondrial activity and acts as a protein deacetylase. SIRT1 appears to be involved in the regulation of numerous transcription factors such as Nf-kB and p53. C85484 648336 Akt inhibitor GSK2141795 An orally bioavailable inhibitor of the serine/threonine protein kinase Akt (protein kinase B) with potential antineoplastic activity. Akt inhibitor GSK2141795 binds to and inhibits the activity of Akt, which may result in inhibition of the PI3K/Akt signaling pathway and tumor cell proliferation and the induction of tumor cell apoptosis. Activation of the PI3K/Akt signaling pathway is frequently associated with tumorigenesis and dysregulated PI3K/Akt signaling may contribute to tumor resistance to a variety of antineoplastic agents. C84870 648543 IGF-1R/IR inhibitor KW-2450 An orally bioavailable inhibitor of insulin-like growth factor 1 receptor (IGF-1R) and insulin receptor (IR) tyrosine kinases with potential antineoplastic activity. IGF-1R/IR inhibitor KW-2450 selectively binds to and inhibits the activities of IGF-1R and IR, which may result in the inhibition of tumor cell proliferation and the induction of tumor cell apoptosis. IGF-R1 and IR tyrosine kinases, overexpressed in a variety of human cancers, play significant roles in the stimulation of cellular proliferation, oncogenic transformation, and suppression of apoptosis. C84871 648549 non-small cell lung cancer mRNA-derived vaccine CV9201 A non-small cell lung cancer (NSCLC) vaccine containing modified mRNAs encoding cancer-testis antigen NY-ESO-1, melanoma-associated antigens C1 (MAGE-C1/CT7) and C2 (MAGE-C2/CT10), survivin, and the oncofetal antigen 5T4 with potential antitumor and immunomodulatory activities. Upon subcutaneous administration, non-small cell lung cancer mRNA-derived vaccine CV9201 may stimulate the immune system to mount a cytotoxic, antigen-specific T lymphocyte response (CTL) against NSCLC cells. The modified mRNAs in this vaccine are taken up by cells after injection and exhibit enhanced translational potency. The five tumor-associated antigens (TAAs) encoded by these mRNAs are frequently expressed by NSCLC cells. C84872 648749 progesterone vaginal insert A tablet preparation formulated for vaginal administration containing a micronized synthetic form of the endogenous steroid hormone progesterone with progesterone activity. Upon vaginal insertion, progesterone binds to the progesterone receptor, resulting in dissociation of heat shock proteins, receptor phosphorylation, and transcription activation through direct or indirect interaction with transcription factors. This agent exerts inhibitory effects on estrogen by decreasing the number of estrogen receptors and increasing its metabolism to inactive metabolites. Progesterone induces secretory changes in the endometrium, decreases uterine contractility during pregnancy, and maintains pregnancy. C84874 648750 estradiol/norethindrone acetate tablet An orally bioavailable tablet formulation containing the semisynthetic estrogen estradiol in combination with the acetate form of the synthetic progestin norethindrone, with estrogenic and progesteronic activities. Estradiol binds to and activates intracellular estrogen receptors found in the reproductive tract and other estrogen-responsive tissues. The activated complex enters the nucleus, binds to the estrogen response elements on DNA, and activates the transcription of genes involved in the maintenance of the female reproductive system and secondary sexual characteristics, the proliferation of the endometrium, and bone metabolism. Norethindrone binds to the intracellular progesterone receptors in the reproductive system and the activated ligand/receptor complex interacts with specific DNA response elements, resulting in an alteration in protein synthesis; inhibition of luteinizing hormone (LH) and follicle stimulating hormone (FSH) release; inhibition of ovulation; an increase in cervical mucus production; and induction of the secretory phase of the endometrial cycle.\nAdministration of estradiol/norethindrone acetate may abrogate vasomotor symptoms associated with menopause and prevent bone loss associated with the postmenopause. Because chronic estrogen stimulation unopposed by progesterone may increase the risk of endometrial carcinoma, administration of a combination estrogen-progestin in postmenopause may reduce the risk for women who require estrogen replacement therapy. C84875 649012 anti-CD19-CAR retroviral vector-transduced autologous T cells A preparation of autologous peripheral blood T-lymphocytes (PBTL) that have been genetically modified to express a chimeric antigen receptor (CAR) consisting of an anti-CD19 scFv (single chain variable fragment); an extracellular portion of human CD28 and the entire transmembrane and cytoplasmic portion of human CD28; and the cytoplasmic portion of the human TCR-[zeta] molecule with potential immunostimulating and antineoplastic activities. Upon administration, anti-CD19-CAR retroviral vector-transduced autologous T cells may stimulate host cytotoxic T lymphocyte (CTL) and antibody responses against CD19-expressing tumor cells, resulting in tumor cell lysis. CD19 antigen is a B-cell specific cell surface antigen expressed in all B-cell lineage malignancies. CD3 zeta is one of several membrane-bound polypeptides found in the T-cell receptor (TCR)/CD3 complex and regulates the assembly of complete TCR complexes and their expression on the cell surface. CD28 is essential for CD4+ T-cell proliferation, interleukin-2 production, and T-helper type-2 (Th2) development. 649018 nutritional supplement drink A calorie-dense nutritional supplement drink containing a variety of vitamins and minerals. Nutritional supplement drink contains vitamin A, vitamin C, D, E and K, calcium, iron, thiamin, riboflavin, niacin, folate, vitamin B6, vitamin B12, pantothenic acid, biotin, phosphorus, iodine, magnesium, zinc, selenium, copper, manganese, chromium, molybdenum, chloride and choline. In addition, this drink contains protein, fiber and fa, including omega-3 fatty acids. C84876 649022 white wine An alcoholic beverage made from fermented white grapes with potential orexigenic activity. Although not well understood, the mechanism for white wine's potential orexigenic activity may be due, in part, to its alcohol content and may involve alterations in neurotransmitter and hormone activities related to appetite regulation. C84877 649061 melphalan hydrochloride/sulfobutyl ether beta-cyclodextrin complex A propylene glycol-free intravenous formulation containing the hydrochloride salt of the nitrogen mustard phenylalanine derivative melphalan complexed with polyanionic sulfobutyl ether beta-cyclodextrin (SBE-CD) with potential antineoplastic activity. Upon administration, melphalan is converted into highly reactive ethylenimmonium intermediates that induce covalent guanine N7-N7 intra- and inter-crosslinks and alkylation of adenine N3 of DNA; RNA and proteins may also be alkylated. Subsequently, RNA transcription and protein synthesis are inhibited, resulting in cell growth arrest. The addition of sulfobutyl ether beta-cyclodextrin to the formulation improves the solubility, stability and ease of use of melphalan; cyclodextrins are cyclic dextrins derived from starch. C84878 649140 iodine I 131 phospholipid ether analogue CLR1404 A small-molecule radiopharmaceutical consisting of the beta-emitting radioisotope iodine I 131 attached to a phospholipid ether (PLE) analogue, comprised of a linear 18 carbon backbone, with potential antineoplastic activity. Iodine I 131 phospholipid ether analogue CLR1404 selectively accumulates in tumor cells, thereby delivering a cytotoxic dose of radiation to cancer cells. Compared to normal cells, tumor cells are unable to metabolize and eliminate PLEs possibly due to deficiency of the enzyme phospholipase-D. In addition, the radioiodine moiety of this agent is resistant to de-iodination. C84879 649142 Hsp90 inhibitor MPC-3100 An orally bioavailable, synthetic, second-generation small-molecule inhibitor of heat shock protein 90 (Hsp90) with potential antineoplastic activity. Hsp90 inhibitor MPC-3100 selectively binds to Hsp90, thereby inhibiting its chaperone function and promoting the degradation of oncogenic signaling proteins involved in tumor cell proliferation and survival; this agent may inhibit the growth and survival of a wide variety of cancer cell types. Hsp90, a chaperone protein upregulated in a variety of tumor cells, regulates the folding, stability, and degradation of many oncogenic signaling proteins. C84836 649505 PARP inhibitor CEP-9722 A small-molecule prodrug of CEP-8983, a novel 4-methoxy-carbazole inhibitor of the nuclear enzymes poly(ADP-ribose) polymerase (PARP) 1 and 2, with potential antineoplastic activity. Upon administration and conversion from CEP-9722, CEP-8983 selectively binds to PARP 1 and 2, preventing repair\nof damaged DNA via base excision repair (BER). This agent enhances the accumulation of DNA strand breaks and promotes genomic instability and apoptosis. CEP-8983 may potentiate the cytotoxicity of DNA-damaging agents and reverse tumor cell chemo- and radioresistance.\n PARP catalyzes post-translational ADP-ribosylation of nuclear proteins that signal and recruit other\nproteins to repair damaged DNA and can be activated by single strand breaks in DNA. C84880 649523 PI3K/mTOR kinase inhibitor PF-04691502 An agent targeting the phosphatidylinositol 3 kinase (PI3K) and mammalian target of rapamycin (mTOR) in the PI3K/mTOR signaling pathway, with potential antineoplastic activity. PI3K/mTOR kinase inhibitor PF-04691502 inhibits both PI3K and mTOR kinases, which may result in apoptosis and growth inhibition of cancer cells overexpressing PI3K/mTOR. Activation of the PI3K/mTOR pathway promotes cell growth, survival, and resistance to chemotherapy and radiotherapy; mTOR, a serine/threonine kinase downstream of PI3K, may also be activated independent of PI3K. C84837 649764 anti-nerve growth factor monoclonal antibody JNJ-42160443 A monoclonal antibody directed against nerve growth factor (NGF) with potential analgesic activity. Upon administration, anti-nerve growth factor monoclonal antibody JNJ-42160443 binds to NGF, preventing its binding to and activation of the NGF receptors TrkA and p75NTR. Inhibition of the NGF pathway may prevent the perception of pain and may induce analgesia. NGF, a neurotrophic factor that plays a key role in neuropathic and inflammatory-induced pain, promotes hyperalgesia and allodynia. C84838 649799 triamcinolone acetonide The acetonide salt of triamcinolone, a synthetic glucocorticosteroid with immunosuppressive and anti-inflammatory activities. Triamcinolone binds to specific cytosolic glucocorticoid receptors, which subsequently interact with the glucocorticoid receptor response element on DNA, gene expression is altered so that the synthesis of certain anti-inflammatory proteins is induced while the synthesis of certain inflammatory mediators is inhibited. Consequently, chronic inflammatory and autoimmune reactions are reduced. 650024 ghrelin peptide analogue A ghrelin peptide analogue with potential anti-cachexia activity. Upon subcutaneous administration, ghrelin peptide analogue binds to and stimulates the G protein-coupled growth hormone secretagogue receptor (GHSR) in the central nervous system (CNS), thereby mimicking the appetite-stimulating and growth hormone-releasing effects of endogenous ghrelin. Stimulation of GHSR may also reduce the production of the pro-inflammatory cytokines TNF-alpha and interleukin-6, which may play direct roles in cancer-related loss of appetite. Ghrelin, naturally secreted by gastric endocrine cells, is a 28 amino acid peptide and an endogenous ligand for GHSR. C84868 650025 taxol analogue SID 530 An intravenous formulation containing docetaxel, a semi-synthetic, second-generation taxane derived from a compound found in the European yew tree, Taxus baccata, with potential antineoplastic activity. Taxol analogue SID 530 binds to and stabilizes tubulin, inhibiting microtubule disassembly, which results in cell-cycle arrest at the G2/M phase and cell death. C84839 650036 oncolytic HSV-1716 A neuroattenuated, replication-restricted, ICP34.5 deleted (RL1 gene)-mutant herpes simplex virus (HSV) type I, constructed from wild-type strain 17, with potential oncolytic activity. Upon intratumoral injection, oncolytic HSV1716 transfects, replicates in, and lyses rapidly dividing cells such as tumor cells. Because the RL1 gene is deleted , HSV1716 is unable to replicate in non-dividing cells. C84840 650124 PAK4 inhibitor PF-03758309 An orally bioavailable small-molecule inhibitor of p21-activated kinase 4 (PAK4) with potential antineoplastic activity. PAK4 inhibitor PF-03758309 binds to PAK4, inhibiting PAK4 activity and cancer cell growth. PAK4, a serine/threonine kinase belonging to the p21-activated kinase (PAK) family, is often upregulated in a variety of cancer cell types and plays an important role in cancer cell motility, proliferation, and survival. C84841 650159 human trefoil factor 1-secreting Lactococcus lactis AG013 An oral rinse solution containing a strain of the bacteria Lactococcus lactis (L. lactis) genetically modified to express human Trefoil Factor 1 (hTFF1) with potential cytoprotective activity. With oral rinsing, human trefoil factor 1-secreting Lactococcus lactis AG013 may secrete and deliver hTFF1 to oral mucosal tissue, protecting or promoting the healing of damaged oral mucosa. hTFF1, a peptide belonging to the Trefoil factors family (TFF), is normally secreted by mucous epithelia and is involved in protecting mucosal tissue and maintaining mucosal surface integrity. C84842 650426 Montanide ISA 51 VG An water-in-oil (w/o) emulsion with immunomoadjuvant activity. Montanide ISA 51 VG appears to act by enhancing the immune system’s cytotoxic T-lymphocyte (CTL) response against antigen(s) in vaccines. The surfactant mannide monooleate in Montanide ISA 51 VG contains vegetable-grade (VG) oleic acid derived from olive oil. C84843 650427 HLA-A*0201-restricted TRP2-gp100-EphA2-HER2 multipeptide vaccine A cancer vaccine containing four HLA-A*0201-restricted peptide epitopes with potential immunostimulatory and antitumor activities. Vaccine peptide epitopes are derived from the tumor associated antigens (TAAs) tyrosinase-related protein 2 (TRP2), glycoprotein 100 (gp100), Ephrin receptor A2 (EphA2) and human epidermal growth factor receptor 2 (HER2). Upon administration, HLA-A*0201-restricted TRp2-gp100-EphA2-HER2 multipeptide vaccine may stimulate a cytotoxic T lymphocyte (CTL) response against TRP2-gp100-EphA2-HER2-expressing tumor cells, resulting in tumor cell lysis and decreased tumor cell proliferation. HLA-A*0201 is an MHC class I molecule that presents antigenic peptides to CD8+ T cells; epitope design restricted to epitopes that bind most efficiently to HLA-A*0201 may improve antigenic peptide immunogenicity. C84844 650432 host dendritic cell vaccine-001 MSSM/BIIR A dendritic cell (DC) vaccine containing ex vivo expanded autologous DCs obtained from a patient with leukemia with potential immunostimulating activity. Upon reintroduction into the host, the host dendritic cell vaccine-001 MSSM/BIIR may stimulate the immune system to mount a leukemia-specific cytotoxic T lymphocyte (CTL) response. C84845 650689 Aurora kinase inhibitor TTP607 A small-molecule pan-Aurora kinase inhibitor with potential antineoplastic activity. Aurora kinase inhibitor TTP607 selectively binds to and inhibits Aurora kinases A, B and C, which may result in the disruption of the assembly of the mitotic spindle apparatus, disruption of chromosome segregation, and inhibition of cellular division and proliferation in Aurora kinase-overexpressing tumor cells.\nAurora kinases A, B and C, are serine/threonine kinases that play essential roles in mitotic checkpoint control and are overexpressed by a wide variety of tumor cell types. C84846 650831 anti-PKN3 siRNA Atu027 A lipoplexed formulation consisting of short-interfering RNAs (siRNAs) directed against protein kinase N3 (PKN3) encapsulated in catiogenic and fusiogenic lipids with potential antineoplastic activity. Upon administration, catiogenic and fusiogenic lipids promote anti-PKN3 siRNA Atu02 uptake by tumor cells; the siRNAs moieties are subsequently released once inside the cell. The siRNAs bind to PKN3 mRNAs, which may result in the inhibition of translation and expression of the PKN3 protein and, so, growth inhibition of tumor cells that overexpress PKN3. The protein kinase C-related molecule PKN3, downstream in the phosphoinositide-3-kinase (PI3K) signaling pathway, is upregulated in many tumor cells and plays an important role in invasive cell growth and metastasis. C84847 650842 nutritional supplement drink (pediatric) A liquid, milk protein-based, pediatric nutritional supplement containing a variety of vitamins and minerals. Nutritional supplement drink (pediatric) contains vitamins and minerals such as vitamin A, vitamin C, D, E and K, calcium, iron, thiamin, riboflavin, niacin, folate, vitamin B6, vitamin B12, pantothenic acid, biotin, phosphorus, iodine, magnesium, zinc, selenium, copper, manganese, chromium, molybdenum, chloride and choline. \nIn addition, this supplement contains soy protein isolate and medium-chain triglycerides (MCTs), sucrose and short-chain oligofructosaccharides. C84848 650941 glycerin enema An enema solution containing 5% glycerin, a trihydroxy alcohol with osmotic laxative activity. Upon rectal administration, glycerin enema creates an osmotic gradient thereby attracting water into the rectum. This increases volume, increases peristalsis, stimulates evacuation, and relieves constipation. C84849 651165 16, 16-dimethyl prostaglandin E2 A stable derivative of prostaglandin E2 (PGE2) with potential hematopoietic activity. Administration of 16,16 dimethyl-prostaglandin E2 (dmPGE2) appears to lead to increased formation of hematopoietic stem and progenitor cells. Even though the exact mechanism of action has yet to be fully elucidated, this agent may stimulate hematopoiesis by activating the Wnt signaling pathway, which increases cellular levels of beta-catenin, a subunit of the cadherin protein complex. C84850 651243 topoisomerase I inhibitor Genz-644282 A non-camptothecin inhibitor of topoisomerase I with potential antineoplastic activity. Topoisomerase I inhibitor Genz-644282 binds to and inhibits the enzyme topoisomerase I, which may result in the inhibition of repair of single-strand DNA breaks, DNA replication, and tumor cell growth in susceptible tumor cell populations. C84851 651245 sufentanil transdermal system A transdermal matrix patch formulation containing the synthetic opioid sufentanil with analgesic activity. Sufentanil binds to and activates the mu-opioid receptors in the central nervous system (CNS), thereby mimicking the effects of the endogenous opioids. Binding of sufentanil to opioid receptors stimulates exchange of GTP for GDP, inhibits adenylate cyclase, and decreases intracellular cAMP. This inhibits the release of various nociceptive neurotransmitters, such as substance P, gamma-aminobutyric acid (GABA), dopamine, acetylcholine, noradrenaline, vasopressin, and somatostatin. In addition, sufentanil closes N-type voltage-gated calcium channels and opens calcium-dependent inwardly rectifying potassium channels, which results in hyperpolarization of neuronal membranes and a reduction in neuronal excitability, and, subsequently, analgesia and sedation. C84852 651246 morphine sulfate sustained-release tablet A sustained-release tablet formulation containing the sulfate salt of the opiate alkaloid morphine with analgesic activity. Morphine binds to and activates the mu-opioid receptors in the central nervous system (CNS), thereby mimicking the effects of the endogenous opioids. Binding of morphine to opioid receptors stimulates exchange of GTP for GDP, inhibits adenylate cyclase, and decreases intracellular cAMP. This inhibits the release of various nociceptive neurotransmitters, such as substance P, gamma-aminobutyric acid (GABA), dopamine, acetylcholine, noradrenaline, vasopressin, and somatostatin. In addition, morphine closes N-type voltage-gated calcium channels and opens calcium-dependent inwardly rectifying potassium channels, which results in hyperpolarization of neuronal membranes and a reduction in neuronal excitability, and subsequently, analgesia and sedation. C84853 651378 MAGE-A1, MAGE-A3, NY-ESO-1 peptides vaccine A cancer vaccine comprised of synthetic peptides derived from human melanoma antigen A1 (MAGE-A1), human melanoma antigen A3 (MAGE-A3) and cancer-testis antigen NY-ESO-1 with potential immunostimulating and antineoplastic activities. Upon administration, MAGE-A1/MAGE-A3/NY-ESO-1 peptides vaccine may stimulate the immune system to mount a cytotoxic T-cell (CTL) response against tumor cells expressing MAGE-A1, MAGE-A3 and NY-ESO-1, resulting in tumor cell lysis. The MAGE-A1, MAGE-A3, and NY-ESO-1 tumor-associated antigens (TAAS) are overexpressed by a variety of cancer cell types. C84854 651385 anti-CD70 antibody-drug conjugate MDX-1203 An antibody-drug conjugate (ADC) containing a fully human monoclonal antibody, directed against the extracellular domain of the human CD70 molecule, conjugated to a prodrug of a CC-1065 (rachelmycin) analogue via a stable peptide-based linker, with potential antineoplastic activity. The anti-CD70 antibody moiety of the anti-CD70 antibody-drug conjugate MDX-1203 selectively binds to the extracellular domain of CD70 on tumor cell surfaces. Upon internalization, the prodrug moiety is released and activated and binds to double-stranded B-DNA within the minor groove, thereby alkylating the –3 position of adenine, which may result in the inhibition of cellular proliferation of tumor cells that overexpress CD70. CD70, the ligand for the costimulatory receptor CD27 and a member of the tumor necrosis factor (TNF) family, is found on the surfaces of various types of cancer cells.\nThe antitumor antibiotic CC-1065, a DNA minor-groove-binding alkylating agent, was originally isolated from the bacterium Streptomyces zelensis. C84855 651465 resminostat An orally bioavailable inhibitor of histone deacetylases (HDACs) with potential antineoplastic activity. Resminostat binds to and inhibits HDACs leading to an accumulation of highly acetylated histones. This may result in an induction of chromatin remodeling, inhibition of the transcription of tumor suppressor genes, inhibition of tumor cell division and the induction of tumor cell apoptosis. HDACs, upregulated in many tumor types, are a class of enzymes that deacetylate chromatin histone proteins. C84856 651549 camptothecin-20(S)-O-propionate hydrate The hydrated, crystalline propionate ester (attached in position C-20) prodrug of camptothecin, an alkaloid isolated from the Chinese tree Camptotheca acuminata, with potential antineoplastic activity. Upon entry into cells, camptothecin-20(S)-O-propionate is hydrolyzed by esterases into the active form camptothecin. Camptothecin selectively stabilizes topoisomerase I-DNA covalent complexes, thereby inhibiting religation of topoisomerase I-mediated single-strand DNA breaks and producing potentially lethal double-strand DNA breaks when encountered by the DNA replication machinery, thus inhibiting DNA replication and triggering apoptotic cell death. Camptothecin readily undergoes hydrolysis at physiological pH, changing its conformation from the active, S-configured lactone structure to an inactive carboxylate form. The ester chain\nin the vicinity of the S-configured lactone moiety, a key determinant\nfor the chemotherapeutic efficacy of the camptothecins, inhibits protein binding, rendering this agent resistant to hydrolysis and prolonging its half-life. C84857 651550 MEK inhibitor TAK-733 An orally bioavailable small-molecule inhibitor of MEK1 and MEK2 (MEK1/2) with potential antineoplastic activity. MEK inhibitor TAK-733 selectively binds to and inhibits the activity of MEK1/2, preventing the activation of MEK1/2-dependent effector proteins and transcription factors, which may result in the inhibition of growth factor-mediated cell signaling and tumor cell proliferation.\nMEK1/2 (MAP2K1/K2) are dual-specificity threonine/tyrosine kinases that play key roles in the activation of the RAS/RAF/MEK/ERK pathway and are often upregulated in a variety of tumor cell types. C84858 651880 DEC-205/NY-ESO-1 fusion protein CDX-1401 A fusion protein consisting of a fully human monoclonal antibody directed against the endocytic dendritic cell (DC) receptor, DEC-205, linked to the tumor-associated antigen (TAA) NY-ESO-1 with potential immunostimulating and antineoplastic activities. The monoclonal antibody moiety of DEC-205/NY-ESO-1 fusion protein CDX-1401 binds to the endocytic DC receptor, which may result in DC endocytic internalization of this agent, specifically delivering the NY-ESO-1 moiety. DC processing of NY-ESO-1 may boost the immune system to mount a cytotoxic T-lymphocyte response (CTL) against cancer cells expressing NY-ESO-1. NY-ESO-1, a cell surface protein expressed in normal fetal and adult testes, is upregulated in a variety of tumor cell types. C84859 652136 ergocalciferol Vitamin D2, a fat-soluble vitamin important for many biochemical processes including the absorption and metabolism of calcium and phosphorus. In vivo, ergocalciferol is formed after sun (ultraviolet) irradiation of plant-derived ergosterol, another form of vitamin D. Ergocalciferol is the form of vitamin D usually found in vitamin supplements. 652185 clevidipine butyrate injectable emulsion An injectable phospholipid emulsion containing the butyrate salt of the synthetic, short-acting, dihydropyridine L-type calcium channel antagonist clevidipine with antihypertensive activity. Clevidipine specifically binds to calcium channels in vascular smooth muscle cells, inhibiting the influx of extracellular calcium ions into vascular smooth muscle cells. This results in dilatation of systemic arteries, a decrease in systemic vascular resistance and so a decrease in arterial blood pressure. This agent is metabolized by esterases in the blood and extravascular tissues to an inactive carboxylic acid metabolite. C72727 652192 membrane-disrupting peptide EP-100 A water-soluble, positively charged fusion protein consisting of a luteinizing hormone releasing hormone (LHRH) receptor-targeting ligand conjugated to the membrane-disrupting peptide CLIP 71 with membrane-disrupting and potential antineoplastic activities. The LHRH ligand moiety of membrane-disrupting peptide EP-100 specifically binds to LHRH receptors, which are upregulated on a variety of human cancer cell types. Subsequently, the positively charged CLIP 71 moiety of this agent interacts with the negatively charged membrane on the cancer cell surface, which may result in cell membrane disruption and cell lysis. C84860 652199 conjugated linoleic acid A slightly altered form of linoleic acid, an omega-6 fatty acid important to human health found in beef and dairy fats. 652615 menadione topical lotion A topical lotion containing the small organic molecule protein tyrosine phosphatase (PTP) inhibitor menadione (vitamin K3) with potential EGFR- and ErbB2/HER2-activating activities. Upon topical administration, menadione binds to and inhibits the activity of PTPs that dephosphorylate and inactivate EGFR and ErbB2 in human keratinocytes; local reversal of EGFR and ErbB2 inhibition associated with the systemic administration of EGFR inhibitors may help alleviate EGFR inhibitor-mediated skin toxicity. EGFR (epidermal growth factor receptor) and ErbB2/HER2 (erythroblastic leukemia viral oncogene homolog 2/ human epidermal growth factor receptor 2) are cell surface receptors that are upregulated in a number of cancer cells types and play important roles in the growth and maintenance of normal epithelial tissues. C84863 652798 telatinib mesylate The orally bioavailable mesylate salt of the 17-allylaminogeldanamycin (17-AAG) small-molecule inhibitor of several receptor protein tyrosine kinases with potential antiangiogenic and antineoplastic activities. Telatinib binds to and inhibits the vascular endothelial growth factor receptors (VEGFRs) type 2 and 3, platelet-derived growth factor receptor beta (PDGFRb) and c-Kit, which may result in the inhibition of angiogenesis and cellular proliferation in tumors in which these receptors are upregulated.\nThese telatinib-inhibited receptor protein tyrosine kinases are overexpressed or mutated in many tumor cell types and may play key roles in tumor angiogenesis and tumor cell proliferation. 17-AAG is a synthetic analogue of the benzoquinone ansamycin antibiotic geldanamycin and has also been found to inhibit the molecular chaperone Hsp90. C80869 652800 dHER2+AS15 vaccine A cancer vaccine consisting of a truncated recombinant HER2/neu peptide (dHER2) combined with the immunoadjuvant AS15 with potential immunostimulatory and antineoplastic activities. Upon administration, dHER2+AS15 vaccine may stimulate the host immune response to mount a cytotoxic T-lymphocyte (CTL) response against tumor cells that overexpress the HER2/neu protein, resulting in tumor cell lysis. The tumor-associated antigen (TAA) HER2/neu is often overexpressed by a variety of tumor cell types; dHER2 includes amino acids 1-645 or 1-653 of the extracellular domain (ECD) and an immunogenic carboxyl terminal autophosphorylation portion of the intracellular domain (ICD). AS15 is an adjuvant formulation that contains the adjuvant systems AS01B and AS07A; AS01 B is composed of liposomes containing 3D-MPL and QS21 and AS07A is composed of the synthetic oligodeoxynucleotide (ODN) Toll-like receptor-9 (TLR9) agonist CpG 7909. C84861 652940 Hedgehog inhibitor PF-04449913 An orally bioavailable small-molecule inhibitor of the Hedgehog (Hh) signaling pathway with potential antineoplastic activity. Hedgehog inhibitor PF-04449913 appears to inhibit Hh pathway signaling. The Hh signaling pathway plays an important role in cellular growth, differentiation and repair. Constitutive activation of Hh pathway signaling has been observed in various types of malignancies. C84862 653314 pomalidomide An orally bioavailable derivative of thalidomide with potential immunomodulating, antiangiogenic and antineoplastic activities. Although its exact mechanism of action has yet to be fully elucidated, pomalidomide appears to inhibit TNF-alpha production, enhance the activity of T cells and natural killer (NK) cells and enhance antibody-dependent cellular cytotoxicity (ADCC). In addition, pomalidomide may inhibit tumor angiogenesis, promote cell cycle arrest in susceptible tumor cell populations, and stimulate erythropoeisis. C72560 653634 MEK inhibitor AS703026 An orally bioavailable small-molecule inhibitor of MEK1 and MEK2 (MEK1/2) with potential antineoplastic activity. MEK inhibitor AS703026 selectively binds to and inhibits the activity of MEK1/2, preventing the activation of MEK1/2-dependent effector proteins and transcription factors, which may result in the inhibition of growth factor-mediated cell signaling and tumor cell proliferation. MEK1/2 (MAP2K1/K2) are dual-specificity threonine/tyrosine kinases that play key roles in the activation of the RAS/RAF/MEK/ERK pathway and are often upregulated in a variety of tumor cell types. C84864 653635 MEK inhibitor ARRY-438162 An orally active small-molecule inhibitor of MEK1 and MEK2 (MEK1/2) with potential antineoplastic activity. MEK inhibitor ARRY-438162, noncompetitive with ATP, binds to and inhibits the activity of MEK 1 and 2 (MEK1/2). Inhibition of MEK1/2 prevents the activation of MEK1/2 dependent effector proteins and transcription factors, which may result in the inhibition of growth factor-mediated cell signaling and tumor cell proliferation. MEK1/2 (MAP2K1/K2) are dual-specificity threonine/tyrosine kinases that play key roles in the activation of the RAS/RAF/MEK/ERK pathway and are often upregulated in a variety of tumor cell types. C84865 653977 specific androgen receptor modulator/lyase inhibitor TOK-001 An orally bioavailable small-molecule androgen receptor modulator and CYP17 lyase inhibitor with potential antiandrogen activity. TOK-001 exhibits three distinct mechanisms of action: 1) as an androgen receptor antagonist, 2) as a CYP17 lyase inhibitor and 3) by decreasing overall androgen receptor levels in prostate cancer tumors, all of which may result in a decrease in androgen-dependent growth signaling. Localized to the endoplasmic reticulum (ER), the cytochrome P450 enzyme CYP17 (P450C17 or CYP17A1) exhibits both \n17alpha-hydroxylase and 17,20-lyase activities, and plays a key role in the steroidogenic pathway that produces progestins, mineralocorticoids, glucocorticoids, androgens, and estrogens. C84866 653978 combretastatin A1 diphosphate The diphosphate prodrug of the stilbenoid combretastatin A1, originally isolated from the plant Combretum caffrum, with vascular-disrupting and antineoplastic activities. Upon administration, combretastatin A1 diphosphate (CA1P) is dephosphorylated to the active metabolite combretastatin A1 (CA1), which promotes rapid microtubule depolymerization; endothelial cell mitotic arrest and apoptosis, destruction of the tumor vasculature, disruption of tumor blood flow and tumor cell necrosis may ensue. In addition, orthoquinone intermediates, metabolized from combretastatin A1 by oxidative enzymes found to be elevated levels in some tumor types, may bind to tumor cell thiol-specific antioxidant proteins and DNA, and stimulate oxidative stress by enhancing superoxide/hydrogen peroxide production. CA1 binds to tubulin at the same site as colchicine but with higher affinity. C84867 653980 hTERT/survivin/melanoma tumor cell-derived mRNA-transfected dendritic cell vaccine A cancer vaccine containing dendritic cells (DCs) that are transfected with messenger RNA (mRNA) encoding human telomerase reverse transcriptase (hTERT) and survivin in addition to patient-specific melanoma-derived mRNA with potential immunostimulatory and antineoplastic activities. Upon administration, hTERT/survivin/melanoma tumor cell-derived mRNA-transfected dendritic cell vaccine may elicit a highly specific cytotoxic T-cell (CTL) response against melanoma cells expressing hTERT, survivin, and patient-specific melanoma-associated antigens. hTERT, the catalytic subunit of human telomerase, and survivin, a member of the inhibitor of apoptosis (IAP) family of proteins, may be upregulated in certain tumor cell types, playing key roles in tumor cell growth and survival. C84755 653982 clioquinol An orally bioavailable, lipophilic, copper-binding, halogenated 8-hydroxyquinoline with antifungal, antiparasitic and potential antitumor activities. Clioquinol forms a stable chelate with copper (copper (II) ions), which inhibits the chymotrypsin-like activity of the proteasome; consequently, ubiquitinated proteins may accumulate in tumor cells, followed by tumor cell apoptosis and the inhibition of tumor angiogenesis. In addition, the clioquinol-copper complex appears to decrease the expression of androgen receptors (AR) in human copper-enriched prostate cancer cells. Serum levels of copper are often elevated in patients with cancer; copper chelation may inhibit copper-dependent endothelial cell proliferation and tumor secretion of angiogenic factors. C65337 654328 resiquimod topical gel A topical gel containing the Toll-like receptor (TLR) agonist resiquimod, an imidazoquinolinamine and with potential immunomodulating activity. Resiquimod binds toTLR7 and 8, mainly on dendritic cells, macrophages, and B-lymphocytes, and activates the TLR signaling pathway, resulting in the induction of the nuclear translocation of transcription activator NF-kB and activation of other transcription factors; subsequently, gene expression increases and the production of cytokines increases, especially interferon-alpha (INF-a), resulting in the enhancement of T-helper 1 (Th1) immune responses. In addition, topical application of resiquimod appears to activate epidermal Langerhans cells, leading to an enhanced activation of T-lymphocytes. C88259 654329 WT1 mRNA-electroporated autologous dendritic cell vaccine A cancer vaccine containing autologous dendritic cells electroporated with full-length mRNA encoding Wilms' tumor 1 (WT1) antigen with potential immunostimulatory and antineoplastic activities. Upon administration, WT1 mRNA-electroporated autologous dendritic cell vaccine may elicit a cytotoxic T-cell (CTL) response against tumor cells expressing WT1. Wt1 is frequently overexpressed in a variety of tumor cell types and often correlates with disease progression and poor prognosis. 654580 Ad5.SSTR/TK.RGD An RGD-4C–modified, infectivity-enhanced, bicistronic type 5 adenovirus expressing herpes simplex virus thymidine kinase (HSV-tk) gene, a therapeutic suicide gene, and the somatostatin receptor type 2 (SSTR2) gene with potential antineoplastic activity. Modification with the double cyclic peptide RGD-4C allows the virus to bind to cellular integrins, frequently expressed on the surfaces of ovarian cancer cells, instead of the coxsackie and adenovirus (CAR) receptor, which is often nonfunctional in ovarian cancer cells. Upon intratumoral administration, Ad5.SSTR/TK.RGD transfects tumor cells and expresses the HSV-tk gene. After subsequent administration of a synthetic acyclic guanosine analogue prodrug like ganciclovir (GCV), expressed HSV-tk phosphorylates and activates the prodrug, which may result in inhibition of DNA synthesis and apoptosis in HSV-tk-expressing cancer cells. Additionally, as a bystander effect, adjacent non-transfected cells may be killed by the activated antiviral drug. SSTR2 expression allows imaging of gene transfer into tumor cells using a radiolabeled somatostatin analogue. C88261 654582 sodium bicarbonate solution An aqueous oral mouthwash solution containing the monosodium salt of carbonic acid with alkalinizing and antimucositis activities. Upon introduction into the mouth, the sodium bicarbonate dissociates, forming sodium and bicarbonate ions, which buffer excess hydrogen ion and elevates the oral pH. An alkaline oral environment is less prone to colonization with yeast and aciduric bacteria. In addition, this solution may help relieve mucositis and mucositis-induced pain by diluting human saliva, and cleansing and lubricating mucosal tissues of the mouth, tongue and oropharynx. C88262 654583 rosuvastatin A statin with antilipidemic and potential antineoplastic activities. Rosuvastatin selectively and competitively binds to and inhibits hepatic hydroxymethyl-glutaryl coenzyme A (HMG-CoA) reductase, the enzyme which catalyzes the conversion of HMG-CoA to mevalonate, a precursor of cholesterol. This leads to a decrease in hepatic cholesterol levels and increase in uptake of LDL cholesterol. In addition, rosuvastatin, like other statins, exhibits pro-apoptotic, growth inhibitory, and pro-differentiation activities in a variety of tumor cell types; these antineoplastic activities may be due, in part, to inhibition of the isoprenylation of Ras and Rho GTPases and related signaling cascades. 654590 fluorine F 18 fluoro furanyl norprogesterone The progesterone derivative fluoro furanyl norprogesterone (FFNP), radiolabeled with fluorine F 18, with positron-emitting radioligand activity. Upon injection, fluorine F 18 fluoro furanyl norprogesterone (F18-FFNP) binds to progesterone receptors (PgR) in progesterone-responsive tissues. In PgR-positive breast cancer, positron emission tomography (PET) may then be used to quantitate hormone receptor status. C88263 654631 C-VISA BikDD: liposome A formulation composed of DOTAP:cholesterol liposome nanoparticles complexed with the plasmid C-VISA BiKDD, with potential antineoplastic activity. C-VISA BikDD: liposome consists of a pancreatic-cancer-specific expression vector “VISA” (VP16-GAL4-WPRE integrated systemic amplifier) and a pancreatic-cancer-specific promoter CCKAR (cholecystokinin type A receptor) (CCKAR-VISA or C-VISA) which drives expression of the gene BikDD, a mutant form of the potent proapoptotic gene Bik (Bcl-2 interacting killer). Upon administration and transduction into pancreatic tumor cells, expression of BikDD by C-VISA BikDD:liposome may induce pancreatic tumor cell apoptosis and suppress pancreatic tumor cell proliferation. BikDD binds with greater affinity to anti-apoptotic proteins bcl-2, bcl-xl, bcl-w and Mcl-1 and is more potent than wild-type Bik.\nDOTAP:cholesterol liposome is composed of cationic lipid dioleoyl-trimethylammonium propane (DOTAP) and cholesterol at molar ratio of 1:1. C88264 654636 Fluorine F 18 ISO-1 A radioconjugate consisting of the benzamide ligand ISO-1 labeled with the radioisotope fluorine F18 with positron-emitting radioisotope activity. Upon administration, fluorine [F18]ISO-1 binds to sigma-2 receptors, located on tumor cells, allowing visualization of sigma-2 receptor-expressing tumor cells with positron emission tomography (PET). Sigma-2 receptors, expressed in a variety of normal healthy tissues such as liver, kidneys, endocrine glands, and in the central nervous system, may be overexpressed in tumor cells. C88265 654729 chloroquine A 4-aminoquinoline with antimalarial, anti-inflammatory, and potential chemosensitization and radiosensitization activities. Although the mechanism is not well understood, chloroquine is shown to inhibit the parasitic enzyme heme polymerase that converts the toxic heme into non-toxic hemazoin, thereby resulting in the accumulation of toxic heme within the parasite. This agent may also interfere with the biosynthesis of nucleic acids. Chloroquine's potential chemosensitizing and radiosensitizing activities in cancer may be related to its inhibition of autophagy, a cellular mechanism involving lysosomal degradation that minimizes the production of reactive oxygen species (ROS) related to tumor reoxygenation and tumor exposure to chemotherapeutic agents and radiation. 654988 DHAP regimen A chemotherapy regimen consisting of dexamethasone, high-dose cytarabine (Ara-C) and cisplatin, used to treat relapsed and refractory non-Hodgkin's and Hodgkin's lymphoma. C63441 655018 VEGFR inhibitor KRN951 An orally bioavailable quinoline-urea derivative inhibitor of vascular endothelial growth factor receptors (VEGFRs) 1 and 2 with potential antiangiogenesis and antineoplastic activities. VEGFR inhibitor KRN951 inhibits VEGF-induced phosphorylation of VEGFRs 1 and 2, which may result in inhibition of migration, proliferation and survival of endothelial cells, microvessel formation, the inhibition of tumor cell proliferation, and tumor cell death. Expression of VEGFRs may be upregulated in a variety of tumor cell types. C88267 655023 Agaricus blazei Murill extract A dietary supplement containing an extract of the Basidiomycete fungus Agaricus blazei Murill with potential chemopreventive, antineoplastic and immunopotentiating activities. Agaricus blazei Murill extract contains high levels of phytochemicals, especially beta-D-glucans. Beta-D-glucans may promote dendritic cell (DC) maturation; increase interferon gamma (IFN-gamma), tumor necrosis factor alpha (TNF-alpha) and immunoglobulin levels; and may enhance natural killer (NK) cell activity, potentially boosting anti-tumor host immune responses. C88268 655231 high-selenium baker's yeast A baker’s yeast (Saccharomyces cerevisiae) containing high levels of the trace element selenium (Se) with potential chemopreventive, immunomodulating and antioxidant activities. Selenium is introduced into yeast during fermentation and incorporated into selenocompounds, such as selenomethionine and glutamyl SE methylselenocysteine. Selenium functions as a cofactor for antioxidant enzymes such as glutathione peroxidases and thioredoxin reductase. C88269 655232 glutathione A tripeptide comprised of three amino acids (cysteine, glutamic acid, and glycine) present in most mammalian tissue. Glutathione acts as an antioxidant, a free radical scavenger and a detoxifying agent. Glutathione is also important as a cofactor for the enzyme glutathione peroxidase, in the uptake of amino acids, and in the synthesis of leukotrienes. As a substrate for glutathione S-transferase, this agent reacts with a number of harmful chemical species, such as halides, epoxides and free radicals, to form harmless inactive products. In erythrocytes, these reactions prevent oxidative damage through the reduction of methemoglobin and peroxides. Glutathione is also involved in the formation and maintenance of disulfide bonds in proteins and in the transport of amino acids across cell membranes. 655580 PI3K inhibitor GSK2126458 A small-molecule pyridylsulfonamide inhibitor of phosphatidylinositol 3-kinase (PI3K) with potential antineoplastic activity. PI3K inhibitor GSK2126458 binds to and inhibits PI3K in the PI3K/mTOR signaling pathway, which may trigger the translocation of cytosolic Bax to the mitochondrial outer membrane, increasing mitochondrial membrane permeability and inducing apoptotic cell death. Bax is a member of the proapoptotic Bcl2 family of proteins. PI3K, often overexpressed in cancer cells, plays a crucial role in tumor cell regulation and survival. C88270 655950 PDK1 inhibitor AR-12 An orally bioavailable, small-molecule, celecoxib-derived inhibitor of phosphoinositide-dependent kinase-1 (PDK1) with potential antineoplastic activity. Devoid of any COX inhibiting activity, PDK1 inhibitor AR-12 binds to and inhibits the phosphorylation of 3-phosphoinositide-dependent kinase-1 (PDK-1).; subsequently, the phosphorylation and activation of the serine/threonine protein kinase Akt (protein kinase B or PKB) is inhibited, which may result in inhibition of the PI3K/Akt signaling pathway, inhibition of tumor cell proliferation, and the induction of tumor cell apoptosis. In addition, this agent appears to induce the activity of protein kinase R-like endoplasmic reticulum kinase (PERK), which plays a key role in the endoplasmic reticulum stress pathway.\nActivation and dysregulation of the PI3K/Akt signaling pathway is frequently associated with tumorigenesis and dysregulated PI3K/Akt signaling may contribute to tumor resistance to a variety of antineoplastic agents. C88271 655951 FGFR inhibitor AZD4547 An orally bioavailable inhibitor of the fibroblast growth factor receptor (FGFR) with potential antineoplastic activity. FGFR inhibitor AZD4547 binds to and inhibits FGFR, which may result in the inhibition of FGFR-related signal transduction pathways, and, so, the inhibition of tumor cell proliferation and tumor cell death. FGFR, up-regulated in many tumor cell types, is a receptor tyrosine kinase essential to tumor cellular proliferation, differentiation and survival. C88272 655952 pan-HER kinase inhibitor AC480 An orally bioavailable, small-molecule pan-HER tyrosine kinase inhibitor with potential antineoplastic and radiosensitizing activities. Pan-HER kinase inhibitor AC480 binds to and inhibits the human epidermal growth factor receptors (HER) HER1 (EGFR), HER2 (ErbB-2) and HER4, which may prevent downstream signaling and inhibit the proliferation of tumor cells that overexpress these receptors. In addition, this agent may enhance the radiosensitivity of certain tumor cell types that express HER1 and HER2 through cell cycle redistribution in G1 phase and inhibition of DNA repair. EGFRs, frequently overexpressed on tumor cells, play a key role in tumor cell proliferation and survival. C48380 655953 Smac mimetic GDC-0152 A second mitochondrial activator of caspases (Smac) mimetic inhibitor of IAPs (Inhibitor of Apoptosis Proteins) with potential antineoplastic activity. Smac mimetic GDC-0152 binds to the Smac binding groove on IAPs, including the direct caspase inhibitor X chromosome-linked IAP (XIAP) and the cellular IAPs 1 and 2, which may inhibit their activities and promote the induction of apoptosis through apoptotic signaling pathways. IAPs are overexpressed by many cancer cell types and suppress apoptosis by binding to and inhibiting active caspases-3, -7 and -9 via their baculoviral lAP repeat (BIR) domains. Smac, the endogenous IAP antagonist, relies on its N-terminal four amino-acid motif for binding to IAPs. C88274 655959 THL-P A proprietary, oral Chinese medicinal herb preparation with potential antioxidant, immunomodulating, and antineoplastic activities. THL-P (Tien-Hsien Liquid-P) contains fourteen Chinese medicinal herbs including: Cordyceps sinensis, Oldenlandia diffusa, Indigo pulverata levis, Polyporus umbellatus, Radix astragali, Panax ginseng, Solanum nigrum L., Pogostemon cablin, Atractylodis macrocephalae rhizoma, Trichosanthes radix, Clematis radix, Margarite, Ligustrum lucidum Ait and Glycyrrhiza radix. Administered as an oral liquid, THL-P may modulate the activity of natural killer (NK) cells, cytotoxic T-lymphocytes (CTLs), macrophages and polymorphonuclear leukocytes, and enhance the secretion of interleukins (ILs) and interferon-gamma (IFN-gamma). This agent may also induce G2/M cell cycle arrest and downregulate several important oncogenic signaling pathways. C88275 656155 technetium Tc 99m demobesin-4 A radioconjugate composed of the synthetic bombesin (BB) analog demobesin-4 bound to the radioisotope technetium Tc 99m with receptor ligand and gamma-emitting radioisotope activities. Upon intravenous administration, demobesin-4 selectively binds to the gastrin-releasing peptide receptor (GRPR) expressed on the surfaces of various tumor cell types; upon internalization, tumor cells expressing GRPRs bound to technetium Tc 99m can then be visualized using scintigraphy. GRPR, a bombesin receptor subtype, is frequently overexpressed on the surface of tumor cells such as prostate and breast cancer cells.\nDemobesin-4 was developed for technetium Tc 99m imaging of GRPR-expressing tumor cells. C88276 656307 lutetium Lu 177-DOTA-edotreotide A radioconjugate consisting of the octreotide derivative edotreotide (Tyr3-octreotide or TOC) labeled with lutetium Lu 177 with receptor ligand, beta-emitting radioisotope, and potential antineoplastic activities. Similar to the somatostatin analog octreotide, lutetium Lu 177-edotreotide binds to somatostatin receptors (SSTRs), especially type 2 receptors, present on the cell membranes of many types of neuroendocrine tumor cells. Upon binding and internalization, this radioconjugate specifically delivers a cytotoxic dose of beta radiation to SSTR-positive cells. Lutetium Lu 177-edotreotide is produced by substituting tyrosine for phenylalanine at the 3 position of the somatostatin analogue octreotide and chelating the substituted octreotide to Lu 177 via dodecanetetraacetic acid (DOTA). C88277 656309 multikinase inhibitor SAR103168 A multikinase inhibitor with potential antineoplastic activity. Upon intravenous infusion, multikinase inhibitor SAR103168 may, through the inhibition of multiple kinases, inhibit the phosphorylation and activation of signal transducer and activator of transcription 5 (STAT5). STAT5, a protein often upregulated in cancer cells, plays a key role in signal transduction pathways and the suppression of apoptosis. C88278 656523 MVA-FCU1 TG4023 A cancer vaccine comprised of a recombinant modified vaccinia Ankara (MVA) viral vector encoding the suicide gene FCU1with potential antineoplastic activity. FCU1 is a bifunctional yeast cytosine deaminase (CD) / uracil phosphoribosyltransferase (UPRT) fusion gene. Upon intratumoral administration, MVA-FCU1 TG4023 enters tumor cells where FCU1 is expressed. Subsequently, the noncytotoxic prodrug 5-fluorocytosine (5-FC) is administered systemically and is deaminated by CD in FCU1- transduced tumor cells into 5-fluorouracil (5-FU), which is then directly metabolized to 5-fluoro-uridine monophosphate (5-FUMP) by UPRT; 5-FUMP may then be further transformed to 5-fluoro-deoxyuridine\nmonophosphate (5-FdUMP), an irreversible inhibitor of thymidylate\nsynthase and, so, DNA synthesis through deprivation of deoxythymidine\ntriphosphate (dTTP). 5-FU and its active metabolites may then selectively kill tumor cells, avoiding toxicity in nonmalignant cells. The MVA viral vector, derived from the replication-competent strain Ankara, is a highly attenuated, replication-defective vaccinia strain incapable of virion assembly. C88279 656527 irinotecan/P-glycoprotein inhibitor HM30181AK combination tablet An orally bioavailable combination tablet containing the semisynthetic camptothecin derivative irinotecan and the multidrug resistance (MDR) efflux pump P-glycoprotein (P-gp) inhibitor HM30181AK, with potential antineoplastic activity. HM30181A binds to P-gp and prevents the P-gp-mediated efflux of irinotecan from tumor cells, which may result in greater intracellular concentrations of irinotecan and enhanced cytotoxicity. Retained intracellularly, the prodrug irinotecan is converted, by a carboxylesterase-converting enzyme, to the biologically active metabolite 7-ethyl-10-hydroxy-camptothecin (SN-38). SN-38 inhibits topoisomerase I activity by stabilizing the cleavable complex between topoisomerase I and DNA, resulting in DNA breaks that inhibit DNA replication and trigger apoptotic cell death. P-gp, encoded by the MDR-1 gene, is a member of the ATP-binding cassette (ABC) superfamily of transmembrane transporters and is overexpressed by some MDR tumors, preventing the intracellular accumulation of various cytotoxic agents. C88280 656651 necitumumab A fully human IgG1 monoclonal antibody directed against the epidermal growth factor receptor (EGFR) with potential antineoplastic activity. Necitumumab binds to and blocks the ligand binding site of EGFR, thereby preventing the activation and subsequent dimerization of the receptor. This may lead to an inhibition of EGFR-dependent downstream pathways and so inhibition of EGFR-dependent tumor cell proliferation and metastasis. EGFR, a member of the epidermal growth factor family of extracellular protein ligands, may be overexpressed on the cell surfaces of various tumor cell types. C88281 656695 antiperspirant cream F511 A cream formulation containing aluminum chlorohydrate with astringent and antiperspirant activities. Upon topical application of F511 cream, aluminium chlorohydrate forms a gel matrix in the sweat gland which subsequently reduces, then stops the flow of water. In addition, this agent exerts an astringent effect, thereby further preventing sweat formation. Hyperhidrosis appears to play a role in the development of certain mucocutaneous reactions, such as palmar-plantar erythrodysesthesia (PPE), upon administration of chemotherapeutic agents such as doxorubicin, 5-fluorouracil, and capecitabine. C88282 656851 anti-CD19 monoclonal antibody MEDI-551 A humanized immunoglobulin IgG1 kappa monoclonal antibody directed against the B-cell-specific membrane protein CD-19 with potential immunostimulating and antineoplastic activities. Anti-CD19 monoclonal antibody MEDI-551 binds to CD19, which may result in a cytotoxic T-lymphocyte (CTL) response and antibody-dependent cellular cytotoxicity (ADCC) to CD19-expressing B-cells. The Fc portion of MEDI-551 does not contain a fucose sugar moiety, which may contribute to its enhanced ADCC activity.\nCD19 is a membrane antigen that is widely expressed during B-cell development, from pro-B-cell to early plasma cell stages. C88283 656874 iodine I 124 FIAU A radioconjugate containing the nucleoside analog 2'-fluoro-2'-deoxy-1beta-D-arabinofuranosyl-5-iodouracil (FIAU) labeled with the radioisotope iodine I 124 with positron-emitting activity. Chemotherapeutic agents such as bortezomib may induce viral thymidine kinase expression in EBV- and Kaposi's sarcoma herpesvirus (KSHV)-associated tumors. Subsequent to chemotherapy induction of viral TK in these tumors, administered iodine I 124 FIAU is phosphorylated by expressed viral TK, becoming selectively trapped within TK-expressing tumor cells; these cells can then be visualized with positron emission tomography (PET). Viral TK is either not expressed or is expressed at very low levels in EBV- and Kaposi's sarcoma herpesvirus (KSHV)-associated tumors and may be activated by certain chemotherapeutic agents. C88284 656900 AC regimen A chemotherapy regimen consisting of doxorubicin hydrochloride (Adriamycin) and cyclophosphamide used in the adjuvant setting for the primary treatment of breast cancer. This regimen is also used for the treatment of recurrent and metastatic breast cancer. C63415 656988 ADE regimen An induction chemotherapy regimen consisting of cytarabine (Ara-C), daunorubicin and etoposide used for the treatment of childhood acute myeloid leukemia. C67207 656990 BEP regimen A chemotherapy regimen consisting of bleomycin, etoposide and cisplatin (Platinum) used for the treatment of adult and childhood ovarian and testicular germ cell tumors. C63488 656998 COPP regimen A chemotherapy regimen consisting of cyclophosphamide, vincristine (Oncovin), procarbazine and prednisone used for the treatment of Hodgkin and non-Hodgkin lymphomas. C63378 657030 CVP regimen A chemotherapy regimen consisting of cyclophosphamide, vincristine and prednisone used for the treatment of indolent non-Hodgkin lymphoma and chronic lymphocytic leukemia. C63449 657033 JEB regimen A chemotherapy regimen consisting of carboplatin (JM8), etoposide and bleomycin used for the treatment of childhood extracranial germ cell tumors. C67289 657046 TAC regimen An adjuvant chemotherapy regimen consisting of docetaxel (Taxotere), doxorubicin hydrochloride (Adriamycin) and cyclophosphamide used for the treatment of breast cancer. C63435 657053 VeIP regimen A chemotherapy regimen consisting of vinblastine (Velban), ifosfamide, mesna and cisplatin (Platinol-AQ) used for the treatment of advanced-stage extracranial germ cell tumors. C63489 657060 FOLFIRI-bevacizumab regimen A first-line chemotherapy regimen consisting of folinic acid (leucovorin), fluorouracil, irinotecan and bevacizumab used for the treatment of advanced-stage colorectal cancer. C63608 657148 ABVE regimen A chemotherapy regimen consisting of doxorubicin hydrochloride (Adriamycin), bleomycin, vincristine and etoposide used in combination with radiation therapy for the treatment of low-risk childhood Hodgkin lymphoma. C67162 657171 FEC Regimen A chemotherapy regimen consisting of fluorouracil, epirubicin and cyclophosphamide used in the adjuvant setting for the primary treatment of breast cancer. This regimen is also used for the treatment of recurrent and metastatic breast cancer. C63420 657226 pegylated recombinant human arginase I BCT-100 A recombinant human arginase I (liver arginase) covalently attached, via a succinamide propionic acid (SPA) linker, to a polyethylene glycol (PEG) of molecular weight 5,000 [rhArg-peg(5,000mw)] with potential antineoplastic activity. Upon intravenous administration of pegylated recombinant human arginase I BCT-100, arginase metabolizes the amino acid arginine to ornithine and urea, depleting intracellular arginine, which may inhibit proliferation of cells that are auxotrophic for arginine such as hepatocellular carcinoma (HCC) cells. This agent may also work synergistically with various cytotoxic agents. C88286 657232 anti-CD45 monoclonal antibody BC8-streptavidin conjugate An immunoconjugate containing a monoclonal antibody directed against the CD45 antigen BC8, conjugated to streptavidin, a nonglycosylated homotetrameric protein that has four high affinity binding sites for biotin. Anti-CD45 BC8 antibody-streptavidin conjugate binds to CD45, a transmembrane protein tyrosine phosphatase that is expressed on the surface of normal and malignant hematopoietic cells. Upon administration of a biotin-based radioconjugate, the biotin moiety of the radioconjugate binds to the streptavidin moiety of anti-CD45 BC8 antibody-streptavidin conjugate and, upon cellular internalization, specifically delivers cytotoxic radiation to CD45-expressing tumor cells. C88287 657244 VAMP Regimen A chemotherapy regimen consisting of vincristine, doxorubicin hydrochloride (Adriamycin), methotrexate and prednisone used in combination with radiation therapy for the treatment of low-risk childhood Hodgkin lymphoma. C67161 657267 XELOX regimen A chemotherapy regimen consisting of capecitabine (Xeloda) and oxaliplatin used for the treatment of advanced-stage colorectal cancer. C63597 657271 FU-LV regimen An adjuvant chemotherapy regimen consisting of fluorouracil and leucovorin, administered in various doses and schedules, used for the treatment of colorectal cancer. C63595 657273 carboplatin-Taxol regimen A chemotherapy regimen consisting of carboplatin and paclitaxel (Taxol) used for the treatment of endometrial, epithelial ovarian, head and neck, and advanced-stage non-small cell lung cancers. C63402 657275 carboplatin-Taxol-bevacizumab regimen A chemoimmunotherapy regimen consisting of carboplatin, paclitaxel (Taxol) and bevacizumab used for the treatment of advanced-stage, nonsquamous non-small cell lung cancer. C63413 657337 gemcitabine-erlotinib regimen A first-line chemotherapy regimen consisting of gemcitabine and erlotinib used for the treatment of locally advanced and metastatic pancreatic cancer. C63503 657391 pNGVL4a-CRT/E7(detox) DNA vaccine A cancer vaccine consisting of the DNA plasmid pNGVL4a-A encoding calreticulin (CRT) linked to a detox form of human papillomavirus (HPV) type 16 E7 antigen, with potential immunomodulating and antineoplastic activities. Upon administration, this vaccine may generate a potent cytotoxic T-lymphocyte (CTL) response against E7-expressing tumor cells, resulting in tumor cell death. For E7(detox), the amino acids in E7 at positions 24 (cysteine to glycine) and 26 (glutamic acid to glycine) were substituted. CRT, a 46 kDa protein located in the lumen of the cell's endoplasmic reticulum (ER), may potentiate MHC class I presentation of HPV-16 E7 to E7-specific CD8-positive T cells.\nIn addition, pNGVL4a-A contains two short immunostimulatory DNA sequences (ISS) in the noncoding region, which may elicit the production of IFN- and IL-12 in transfected keratinocytes and dermal antigen presenting cells (APCs), resulting in a potent T helper cell type 1 response. C88289 657494 short chain fatty acid HQ-1004 A short chain fatty acid (SCFA) with potential herpes simplex virus thymidine kinase gene (HSV-TK)-inducing activity. Upon administration, short chain fatty acid HQ-1004 may induce the expression of thymidine kinase (TK) by a silenced HSV-TK, which may activate a co-administered antiviral prodrug such as ganciclovir, resulting in the destruction of virally-infected cancer cells. C88290 657496 EGFR inhibitor PF-00299804 A orally bioavailable, highly selective, second-generation small-molecule inhibitor of the pan-epidermal growth factor receptor (EGFR) family of tyrosine kinases (ErbB family) with potential antineoplastic activity. EGFR inhibitor PF-00299804 specifically and irreversibly binds to and inhibits human EGFR subtypes, resulting in inhibition of proliferation and induction of apoptosis in EGFR-expressing tumor cells. EGFRs play major roles in tumor cell proliferation and tumor vascularization, and are often overexpressed or mutated in various tumor cell types. C88291 657687 indium In 111 capromab pendetide A radioimmunoconjugate consisting of the murine IgG1 kappa monoclonal antibody capromab (7E11-C5.3), conjugated to the linker-chelator glycyl-tyrosyl-(N,-diethylenetriaminepentaacetic acid)-lysine hydrochloride (GYK-DTPA-HCl) and labeled with radioisotope indium In 111, with ligand-binding and gamma-emitting activities. Upon intravenous administration, indium In 111-capromab pendetide binds to a cytoplasmic epitope of human prostate specific membrane antigen (PSMA) expressed on prostate tumor cell surfaces via its capromab moiety and, upon internalization, allows radioimmunolocalization with gamma scintigraphy. PSMA is a cell surface glycoprotein abundantly expressed by prostate epithelium and is typically overexpressed by prostate cancer cells. C88292 657793 JAK2 inhibitor TG101348 An orally bioavailable, small-molecule, ATP-competitive inhibitor of Janus-associated kinase 2 (JAK2) with potential antineoplastic activity. JAK2 inhibitor TG101348 competes with JAK2 as well as the mutated form AK2V617F for ATP binding, which may result in inhibition of JAK2 activation, inhibition of the JAK-STAT signaling pathway, and the induction of tumor cell apoptosis. JAK2 is the most common mutated gene in bcr-abl-negative myeloproliferative disorders (MPDs); the mutated form JAK2V617F has a valine-to-phenylalanine modification at position 617 and plays a key role in tumor cell proliferation and survival. C88293 657800 bimatoprost ophthalmic solution A sterile ophthalmic solution containing 0.03% of a synthetic prostaglandin analog bimatoprost with hair-growing and anti-glaucoma activities. Applied once daily to the upper eyelid margin at the base of the eyelashes and, optionally, to the eyebrows, bimatoprost penetrates into the hair follicle and may, through a mechanism that has yet to be fully understood, stimulate the transition of hair follicles from the telogen phase into the anagen phase and may increase the duration of the time follicles spend in anagen. By increasing the numbers of hair follicles in and duration of anagen phase, bimatoprost may help increase eyebrow and eyelash growth and appearance, including their length, thickness and darkness. C88294 658036 tetraphenyl chlorin disulfonate A meso-tetraphenylchlorin substituted by two adjacent sulfonated groups with potential photosensitizing activity. Upon administration, tetraphenyl chlorin disulfonate incorporates into the cell’s endosome and lysosome membranes. Subsequently, cytotoxic agents are administered and accumulate in endosomal and lysosomal compartments; upon local activation by light, tetraphenyl chlorin disulfonate produces reactive oxygen species (ROS), such as singlet oxygen, damaging endo/lysosomal membranes and accumulated cytotoxic agents are released into the tumor cell cytosol. This photochemical internalization (PCI) method can enhance the efficacy and selectivity of cytotoxic agents. C88344 658276 ALK1 inhibitor ACE-041 A soluble fusion protein containing the extracellular domain of activin receptor-like kinase-1 (ALK1) fused to a human Fc domain (ALK1-Fc fusion protein), with potential antiangiogenic and antineoplastic activities. Upon administration, ALK1 inhibitor ACE-041 binds to various ALK1 ligands, preventing activation of tumor cell ALK1 receptors and so inhibiting the ALK1 signaling pathway; growth factor-induced angiogenesis is thus inhibited, which may result in the inhibition of tumor cell proliferation and tumor cell death. ALK1 is a type I cell surface\nreceptor with serine/threonine kinase activity that\nmediates signaling by members of the transforming\ngrowth factor-beta (TGFbeta) superfamily and plays a key role in angiogenesis; ligands for this receptor include TGFbeta1 and TGFbeta2. The Fc moiety of this fusion protein mediates clearance of ligand-fusion protein complexes by the reticuloendothelial system (RES). C88296 658411 FAK inhibitor GSK2256098 A focal adhesion kinase-1 (FAK) inhibitor with potential antiangiogenic and antineoplastic activities. FAK inhibitor GSK2256098 inhibits FAK, which may prevent the integrin-mediated activation of several downstream signal transduction pathways, including ERK, JNK/MAPK and PI3K/Akt, thereby inhibiting tumor cell migration, proliferation and survival, and tumor angiogenesis. The tyrosine kinase FAK is normally activated by binding to integrins in the extracellular matrix (ECM) but may be upregulated and constitutively activated in various tumor cell types. C88346 658431 calfactant A sterile suspension composed of an extract of bovine pulmonary surfactant with surfactant activity. Calfactant contains phospholipids, neutral lipids, and hydrophobic surfactant-associated proteins B (SP-B) and C (SP-C). Upon intratracheal administration, this agent, mimicking endogenous pulmonary surfactant, lines the alveoli and smallest bronchioles, keeping alveoli open during expiration by lowering surface tension. Resulting improvements in lung compliance and respiratory gas exchange may lead to improvements in ventilation and oxygenation. C80989 658594 magnesium oxide The oxide salt of magnesium with antacid, laxative and vascular smooth muscle relaxant activities. Magnesium combines with water to form magnesium hydroxide which reacts chemically to neutralize or buffer existing quantities of stomach acid; stomach-content and intra-esophageal pH rise, resulting in a decrease in pepsin activity. This agent's laxative effect is the result, in part, of osmotically mediated water retention, which subsequently stimulates peristalsis. In addition, magnesium ions may behave as calcium antagonists in vascular smooth muscle. 658708 chlorambucil-prednisone regimen A chemotherapy regimen consisting of chlorambucil and prednisone used for the treatment of chronic lymphocytic leukemia. C63752 658710 lisinopril An orally bioavailable, long-acting angiotensin-converting enzyme (ACE) inhibitor with antihypertensive activity. Lisinopril, a synthetic peptide derivative, specifically and competitively inhibits ACE, which results in a decrease in the production of the potent vasoconstrictor angiotensin II and, so, diminished vasopressor activity. In addition, angiotensin II-stimulated aldosterone secretion by the adrenal cortex is decreased which results in a decrease in sodium and water retention and an increase in serum potassium. 658712 carvedilol phosphate extended-release capsule An extended-release capsule formulation containing the phosphate salt of carvedilol, a nonselective beta-adrenergic blocking agent with alpha 1-adrenergic blocking activity. Carvedilol is a racemic mixture; the S(-) enantiomer non-selectively binds to and blocks beta-adrenergic receptors, exerting negative inotropic and chronotropic effects, leading to a reduction in cardiac output. Both R(+) and S(-) enantiomers bind to and block alpha 1-adrenergic receptors with equal potency, causing vasodilation and a reduction in peripheral vascular resistance. This agent has no intrinsic sympathomimetic activity. C88299 658906 ramosetron hydrochloride The hydrochloride salt of ramosetron, a selective serotonin (5-HT) receptor antagonist with potential antiemetic activity. Upon administration, ramosetron selectively binds to and blocks the activity of 5-HT subtype 3 (5-HT3) receptors located in the vagus nerve terminal and in the vomiting center in the central nervous system (CNS), suppressing chemotherapy-induced nausea and vomiting. C88299 659002 nadolol A non-selective beta-adrenergic antagonist with antihypertensive and antiarrhythmic activities. Nadolol competitively blocks beta-1 adrenergic receptors located in the heart and vascular smooth muscle, inhibiting the activities of the catecholamines epinephrine and norepinephrine and producing negative inotropic and chronotropic effects. This agent exhibits antiarrhythmic activity via the impairment of atrioventricular (AV) node conduction and a corresponding reduction in sinus rate. In the kidney, inhibition of the beta-2 receptor within the juxtaglomerular apparatus results in the inhibition of renin production and a subsequent reduction in angiotensin II and aldosterone levels, thus inhibiting angiotensin II-dependent vasoconstriction and aldosterone-dependent water retention. 659065 tomato-soy juice A juice containing tomato extract and soy protein with potential chemopreventive and antiproliferative activities. Tomato-soy juice contains phytochemicals, including flavonoids, such as the soy isoflavone genistein, and carotenoids, including lycopene. These phytochemicals may exhibit antioxidative activity, antitumor activity by modulating certain tumor-associated signal transduction pathways, and apoptosis-inducing activity. C88300 659158 Ang2/VEGF-binding peptides-antibody fusion protein CVX-241 A fusion protein containing angiopoietin-2 (Ang2) and vascular endothelial growth factor (VEGF) derived peptides covalently attached, via a proprietary diketone linker, to a proprietary humanized catalytic aldolase monoclonal antibody, with potential antiangiogenic and antineoplastic activities. The Ang2/VEGF peptide moieties of Ang2/VEGF-binding peptides-antibody fusion protein CVX-241 bind to Ang2 and VEGF receptors, which may inhibit tumor angiogenesis and tumor cell proliferation. The proprietary humanized catalytic IgG1 monoclonal aldolase antibody contains reactive lysine residues in its binding sites, which react covalently with compounds having a diketone function; the Ang2 and VEGFR peptide moieties are then covalently attached to the diketone linkers via a proprietary spacer. Both VEGF and Ang2 are upregulated in a variety of cancer cell types and play a crucial role in angiogenesis. This agent possesses an enhanced half-life compared to the naked peptides. C88301 659161 pan FGFR kinase inhibitor BGJ398 An orally bioavailable pan inhibitor of human fibroblast growth factor receptors (FGFRs) with potential antiangiogenic and antineoplastic activities. pan FGFR kinase inhibitor BGJ398 selectively binds to and inhibits the activities of FGFRs, which may result in the inhibition of tumor angiogenesis and tumor cell proliferation, and the induction of tumor cell death. FGFRs are a family of receptor tyrosine kinases which may be upregulated in various tumor cell types and may be involved in tumor cell differentiation and proliferation, tumor angiogenesis, and tumor cell survival. C88302 659167 multitargeted tyrosine kinase inhibitor PLX3397 A capsule formulation containing a small-molecule receptor tyrosine kinase (RTK) inhibitor of KIT, CSF1R and FLT3 with potential antineoplastic activity. Multitargeted tyrosine kinase inhibitor PLX3397 binds to and inhibits phosphorylation of stem cell factor receptor (KIT), colony-stimulating factor-1 receptor (CSF1R) and FMS-like tyrosine kinase 3 (FLT3), which may result in the inhibition of tumor cell proliferation and down-modulation of macrophages, osteoclasts and mast cells involved in the osteolytic metastatic disease. FLT3, CSF1R and FLT3 are overexpressed or mutated in many cancer cell types and play major roles in tumor cell proliferation and metastasis. C88303 659335 demeclocycline hydrochloride The hydrochloride salt of demeclocycline, a broad-spectrum, tetracycline derivative exhibiting antimicrobial, aquaretic and chelating activities. In bacteria, demeclocycline binds reversibly to the 30S ribosomal subunit and blocks the binding of aminoacyl-tRNA to the A-site of the mRNA-ribosome complex, resulting in the inhibition of protein synthesis and bacterial cell death. In mammals, this agent interferes with the action of antidiuretic hormone (ADH) at the level of the renal collecting tubule, resulting in aquaresis. In addition, demeclocycline, which like other tetracyclines chelates calcium in bone and exhibits a yellow fluorescence under ultraviolet (UV) light, may be used as a fluorescent bone-labeling agent in bone histomorphometry. 659491 quaternary ammonium polyethylenimine nanoparticles A crosslinked nanoparticle formulation containing quaternary ammonium polyethylenimine (QA-PEI) with potential antibacterial activity. The cationic polymer PEI kills bacteria by rupturing their cell membranes without the development of resistance. \nQuaternary ammonium polyethylenimine nanoparticles can be incorporated into dental composite resins or silicon obturator prostheses and may prevent or delay bacterial growth. C88305 659598 anti-EGFRvIII immunotoxin MR1-1 A recombinant immunotoxin consisting of single-chain variable domain fragment antibody directed against the tumor-specific antigen EGFRvIII (MR1scFv) fused to domains II and III of the Pseudomonas exotoxin (PE38KDEL), with potential antineoplastic activity. Upon administration, the antibody moiety of anti-EGFRvIII immunotoxin MR1-1 binds to EGFRvIII; upon internalization, the exotoxin portion inhibits protein synthesis, resulting in a reduction in tumor cell proliferation of EGFRvIII- expressing tumor cells. EGFRvIII, a type III in-frame deletion mutation of the epidermal growth factor receptor (EGFR) gene, is expressed by a variety of cancers, including glioblastoma multiforme, non-small lung carcinoma, and breast carcinoma. Compared to intact IgG antibodies, single-chain antibodies such as MR1scFv are smaller and may penetrate tumors better. Pseudomonas exotoxin PE38KDEL was modified to remove the natural cell binding domain. C88307 659685 anti-CCR2 monoclonal antibody MLN1202 A humanized monoclonal antibody directed against the human chemokine receptor 2 (CCR2), with potential antiangiogenic, immunomodulating, antimetastatic, and antineoplastic activities. Anti-CCR2 human monoclonal antibody MLN1202 binds to CCR2 and prevents binding of the endothelium-derived CLL2 (monocyte chemoattractant protein-1 or MCP1) to its receptor CCR2, which may result in inhibition of CCR2 activation and so inhibition of angiogenesis, tumor cell migration, and tumor cell proliferation. In addition, this agent may reduce levels of C-reactive protein (CRP). The G-protein coupled receptor CCR2 is expressed on the surface of monocytes and macrophages, stimulates the migration and infiltration of these cell types, and plays an important role in inflammation, angiogenesis, and tumor cell migration and proliferation. C88308 659935 CXCR4 antagonist BKT140 An orally bioavailable inhibitor of CXC Chemokine Receptor 4 (CXCR4) with potential antineoplastic activity. CXCR4 antagonist BKT140 selectively binds to the chemokine receptor CXCR4, preventing the binding of stromal derived factor-1 (SDF-1 or CXCL12) to the CXCR4 receptor and subsequent receptor activation, which may result in decreased tumor cell proliferation and migration. In addition, inhibition of CXCR4 may induce mobilization of hematopoietic cells from the bone marrow into blood. The G protein-coupled receptor CXCR4 plays an important role in chemotaxis and angiogenesis and is upregulated in several tumor cell types; SDF-1/CXCR4 interaction induces retention of hematopoietic cells in the bone marrow. C88309 660070 allogeneic CMV/AdV-specific cytotoxic T lymphocytes A population of allogeneic cytotoxic T lymphocytes (CTLs) specifically reactive to cytomegalovirus (CMV) and adenovirus (AdV) with potential antiviral activity. Allogeneic CMV/AdV-specific cytotoxic T lymphocytes are prepared by exposing donor-derived CTLs to a lethally irradiated Epstein-Barr virus-positive lymphoblastoid B cell line (EBV-LCL) that has been transduced with a clinical-grade adenoviral vector (Ad5f35CMVpp65) as a source of CMV and AdV antigens. Infusion of these CTLs into stem cell transplant recipients may prevent CMV and AdV viral disease. C88310 660119 abatacept A soluble fusion protein consisting of the extracellular\ndomain of human cytotoxic T lymphocyte-associated antigen 4 (CTLA-4) linked to\na modified Fc (hinge, CH2, and CH3 domains) portion of human immunoglobulin G1\n(IgG1) with immunosuppressive activity. Abatacept binds CD80 and CD86 on antigen presenting cells (APCs), blocking interaction with CD28 on T lymphocytes, which initiates a co-stimulatory signal required for full activation of T lymphocytes. 660135 JAK1/2 inhibitor CYT387 An orally bioavailable small-molecule inhibitor of Janus kinases 1 and 2 (JAK1/2) with potential antineoplastic activity. JAK1/2 inhibitor CYT387 competes with JAK1/2 for ATP binding, which may result in inhibition of JAK1/2 activation, inhibition of the JAK-STAT signaling pathway, and so the induction of apoptosis and a reduction of tumor cell proliferation in JAK1/2-expressing tumor cells. JAK2 is the most common mutated gene in bcr-abl-negative myeloproliferative disorders; the JAK2V617F gain-of-function mutation involves a valine-to-phenylalanine modification at position 617. The JAK-STAT signaling pathway is a major mediator of cytokine activity and is often dysregulated in a variety of tumor cell types. C88311 660138 CDK2/TRKA inhibitor PHA-848125 AC An orally bioavailable inhibitor of cyclin-dependent kinases (CDKs) and thropomyosin receptor kinase A (TRKA), with potential antineoplastic activity. CDK2/TRKA inhibitor PHA-848125 AC potently inhibits cyclin-dependent kinase 2 (CDK2) and exhibits activity against other CDKs including CDK1 and CDK4, in addition to TRKA. Inhibition of these kinases may result in cell cycle arrest and apoptosis of tumor cells that express these kinases. CDKs are serine/threonine kinases involved in regulation of the cell cycle and may be overexpressed in some cancer cell types. The neurotrophin receptor TRKA is mutated in a variety of cancer cell types. C88312 660210 Polo-like kinase 1 inhibitor NMS-1286937 An orally bioavailable, small-molecule Polo-like kinase 1 (PLK1) inhibitor with potential antineoplastic activity. Polo-like kinase 1 inhibitor NMS-1286937 selectively inhibits PLK1, inducing selective G2/M cell-cycle arrest followed by apoptosis in a variety of tumor cells while causing reversible cell-cycle arrest at the G1 and G2 stages without apoptosis in normal cells. PLK1 inhibition may result in the inhibition of proliferation in PLK1-overexpressing tumor cells. PLK1 is a serine/threonine protein kinase crucial in the regulation of mitosis. C88313 660212 MET tyrosine kinase inhibitor EMD 1214063 An inhibitor of MET tyrosine kinase with potential antineoplastic activity. MET tyrosine kinase inhibitor EMD 1214063 selectively binds to MET tyrosine kinase and disrupts MET signal transduction pathways, which may induce apoptosis in tumor cells overexpressing this kinase. The receptor tyrosine kinase MET (also known as hepatocyte growth factor receptor or HGFR), is the product of the proto-oncogene c-Met and is overexpressed or mutated in many tumor cell types; this protein plays key roles in tumor cell proliferation, survival, invasion, and metastasis, and tumor angiogenesis. C88314 660730 anti-CD70 monoclonal antibody SGN-75 An antibody-drug conjugate (ADC) consisting of a humanized monoclonal antibody, directed against the extracellular domain of the human CD70 molecule, conjugated to the auristatin analogue monomethyl auristatin phenylalanine (MMAF), with potential antineoplastic activity. The anti-CD70 antibody moiety of anti-CD70 antibody-drug conjugate SGN-75 selectively binds to the extracellular domain of CD70 on tumor cell surfaces. Upon internalization, the MMAF moiety is released, binds to tubulin and inhibits its polymerization, which may result in G2/M phase arrest, tumor cell apoptosis and inhibition of cellular proliferation in tumor cells that overexpress CD70. CD70, the ligand for the costimulatory receptor CD27 and a member of the tumor necrosis factor (TNF) family, is found on the surfaces of various types of cancer cells. C88315 660731 CDC7 kinase inhibitor NMS-1116354 An orally bioavailable cell division cycle 7 homolog (CDC7) kinase inhibitor with potential antineoplastic activity. CDC7 kinase inhibitor NMS-1116354 binds to and inhibits the activity of CDC7, which may result in the inhibition of DNA replication and mitosis, the induction of tumor cell apoptosis, and the inhibition of tumor cell proliferation in CDC7-overexpressing tumor cells. The serine-threonine kinase CDC7 initiates DNA replication by phosphorylating MCM2 (minichromosome maintenance complex component 2) at Ser40 and Ser53. C88316 660810 HER2Bi-armed activated T cells Activated T cells (ATC) that have been coated with bispecific antibodies (BiAb), with potential antineoplastic and immunomodulating activities. In vitro, T cells are activated through exposure to the anti-CD3 murine monoclonal antibody OKT3 and interleukin 2 for 14 days and then armed with anti-CD3 × anti-Her2 bispecific antibody (Her2Bi). Upon administration, HER2Bi-armed activated T cells attach to CD3-expressing T cells and HER2/neu-expressing tumor cells, selectively cross-linking T cells and tumor cells; this may result in the recruitment and activation of cytotoxic T lymphocytes (CTLs), CTL perforin-mediated tumor cell cytolysis, and the secretion of antitumor cytokines and chemokines. C88317 660818 perindopril erbumine The tert-butylamine salt of perindopril, the ethyl ester of a non-sulfhydryl angiotensin converting enzyme (ACE) inhibitor with antihypertensive activity. Upon hydrolysis, perindopril erbumine is converted to its active form perindoprilat, inhibiting ACE and the conversion of angiotensin I to angiotensin II; consequently, angiotensin II-mediated vasoconstriction and angiotensin II-stimulated aldosterone secretion from the adrenal cortex are inhibited and diuresis and natriuresis ensue. 660819 bisoprolol fumarate The fumarate salt of a synthetic phenoxy-2-propanol-derived cardioselective beta-1 adrenergic receptor antagonist with antihypertensive and potential cardioprotective activities. Devoid of intrinsic sympathomimetic activity, bisoprolol selectively and competitively binds to and blocks beta-1 adrenergic receptors in the heart, decreasing cardiac contractility and rate, reducing cardiac output, and lowering blood pressure. In addition, this agent may exhibit antihypertensive activity through the inhibition of renin secretion by juxtaglomerular epithelioid (JGE) cells in the kidney, thus inhibiting activation of the renin-angiotensin system (RAS). Bisoprolol has been shown to be cardioprotective in animal models. 660850 HSV-1 HF10 A non-engineered, naturally oncolytic, replication-competent spontaneous herpes simplex virus (HSV) type I mutant variant. Upon intratumoral injection, HSV1 HF10 transfects, replicates in, and lyses rapidly dividing cells such as tumor cells. In addition, this agent may increase host immune responses that may kill non-infected tumor cells. C88318 661035 recombinant interleukin-15 A recombinant agent that is chemically identical or similar to the endogenous cytokine interleukin-15 (IL-15) with immunomodulating activity. IL-15, secreted by mononuclear phagocytes (and some other cell types) following viral infection, regulates T and natural killer cell activation and proliferation. This cytokine induces activation of transcription activators STAT3, STAT5, and STAT6 via JAK kinase signal transduction pathways in mast cells, T cells, and dendritic epidermal T cells. IL-15 and interleukin-2 (IL-2) are structurally similar and share many biological activities; both may bind to common hematopoietin receptor subunits, negatively regulating each other's activity. CD8+ memory T cell number has been shown to be regulated by a balance between IL-15 and IL-2. C1545 663166 glucuronic acid A carboxylic acid with structural similarity to glucose with detoxifying activity. The xenobiotic metabolism of various substances such as drugs, pollutants, bilirubin, androgens, estrogens, mineralocorticoids, glucocorticoids, fatty acid derivatives, retinoids, and bile acids involves glucuronidation, a process in which water-soluble, excretable glucuronides of these substances are formed via glycosidic linkages to glucuronic acid. UDP-glucuronic acid, formed in the liver through the linkage of glucuronic acid to uridine diphosphate (UDP) via a glycosidic bond, is an intermediate in the process of glucuronidation. C63810 669084 doxycycline hyclate The hyclate salt of the synthetic, broad-spectrum tetracycline doxycycline with antimicrobial activity. Doxycycline binds reversibly to the 30S ribosomal subunit and possibly to the 50S ribosomal subunit, blocking the binding of aminoacyl-tRNA to the mRNA-ribosome complex, which results in an inhibition of bacterial protein synthesis. In addition, this agent may inhibit collagenase activity. C29007 670427 topical phenylephrine solution 670650 topiramate A sulfamate-substituted monosaccharide with anticonvulsant activity. Although the mechanism of action has not been fully elucidated, topiramate appears to antagonize kainate/AMPA subtype glutamate receptors, which results in stabilization of hyper-excited neural membranes, inhibition of repetitive neuronal firing, and a decrease in propagation of synaptic impulses, thus impeding seizure activity. In addition, this agent enhances chloride channels activated by the inhibitory neurotransmitter GABA. Kainate/AMPA subtype glutamate receptors are ligand-activated cation channels that mediate the fast component of excitatory postsynaptic currents in neurons of the central nervous system.