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Cancer Drugs

- I -

  • ibandronate

  • A synthetic nitrogen-containing bisphosphonate. Ibandronate 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.

  • idarubicin

  • A semisynthetic anthracycline antineoplastic antibiotic derived from daunorubicin. Idarubicin intercalates into DNA and interacts with topoisomerase II, thereby inhibiting DNA replication and repair and RNA and protein synthesis. Due to its high lipophilicity, idarubicin penetrates cell membranes better than other anthracycline antibiotics. Idarubicin hydrochloride is the therapeutic form of this drug.

  • Ifosfamidum

  • (Other name for: ifosfamide)

  • 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.

  • 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.

  • imatinib mesylate

  • The mesylate salt of an antineoplastic agent that inhibits the Bcr-Abl fusion protein tyrosine kinase, an abnormal enzyme produced by chronic myeloid leukemia cells that harbor the Philadelphia chromosome. Imatinib also inhibits the receptor tyrosine kinases for platelet-derived growth factor (PDGF) and stem cell factor (SCF)/c-kit; the SCF/c-kit receptor tyrosine kinase is activated in gastrointestinal stromal tumor (GIST). This agent inhibits proliferation and induces apoptosis in cells that overexpress these oncoproteins.

  • 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.

  • 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.

  • Immucell WGP

  • (Other name for: beta-glucan)

  • 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.

  • 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.

  • inalimarev

  • A cancer vaccine comprised of a recombinant vaccinia viral vector encoding the carcinoembryonic antigen (CEA), MUC-1, a transmembrane glycoprotein secreted by glandular 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 activate a cytotoxic T-cells response against CEA- and MUC-1-expressing tumor cells.

  • 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.

  • 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.

  • 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.

  • Indocin

  • (Other name for: indomethacin)

  • 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.

  • 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.

  • 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.

  • 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.

  • Innohep

  • (Other name for: tinzaparin sodium)

  • 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).

  • 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.

  • 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).

  • 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.

  • 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.

  • 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.

  • 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).

  • 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.

  • 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.

  • 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.

  • 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).

  • Intron A

  • (Other name for: interferon alfa)

  • Intron A

  • (Other name for: recombinant interferon alfa-2b)

  • iodine I 124 chimeric monoclonal antibody cG250

  • A radioimmunoconjugate comprised of the chimeric monoclonal antibody G-250 conjugated with iodine I 124 with potential imaging properties. The antibody moiety of iodine I 124 chimeric monoclonal antibody G-250 may bind to renal cell carcinoma cells that express the renal cell carcinoma-associated antigen G-250, allowing detection of tumor-localized iodine I 124 with diagnostic imaging.

  • 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.

  • 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.

  • 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.

  • 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.

  • iodine I 131 lipiodol

  • A cytotoxic radioconjugate consisting of lipiodol, an iodinated ethyl ester derived from poppy seed oil, labeled with iodine 131 (I-131). I-131 Lipiodol accumulates in hepatocellular carcinoma and hepatoblastoma tumor cells, resulting in targeted cytotoxicity to tumor cells while sparing surrounding normal cells and tissues.

  • iodine I 131 metaiodobenzylguanidine

  • An I 131 radioiodinated synthetic analogue of the neurotransmitter norepinephrine. Meta-iodobenzylguanidine localizes to adrenergic tissue and, in radioiodinated forms, may be used to image or eradicate tumor cells that take up and metabolize norepinephrine.

  • 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.

  • 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 properties. 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.

  • iodine I 131 monoclonal antibody 8H9

  • A radioimmunoconjugate consisting of 8H9, a murine IgG1 anti-tenascin monoclonal antibody, radiolabeled with iodine 131 (I 131) with radioimaging and radioimmunotherapeutic properties. Monoclonal antibody 8H9 radiolabeled with I 131 may be used to radioimage and/or destroy tumor cells expressing tenascin. Tenascin is an extracellular matrix protein which is overexpressed in gliomas and other cancers.

  • 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.

  • 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.

  • iodine I 131 tositumomab

  • A monoclonal antibody directed against a protein (CD20) expressed on the surface of B-lymphocytes and radiolabeled with the radioisotope I 131 with potential antineoplastic activity. Iodine I 131 tositumomab delivers radiation selectively to neoplastic CD20-expressing B-lymphocytes cells, thereby decreasing the risk of systemic radiotoxicity.

  • Iodotope

  • (Other name for: iodine I 131)

  • IPI-504

  • A small-molecule inhibitor of heat shock protein 90 (HSP90) with antiproliferative and antineoplastic activity. IPI-504 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. IPI-504-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.

  • 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.

  • Iressa

  • (Other name for: gefitinib)

  • 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.

  • 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.

  • 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.

  • 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.

  • Iscar

  • (Other name for: mistletoe extract)

  • Iscomatrix

  • (Other name for: saponin-cholesterol-phospholipid adjuvant)

  • 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.

  • isotretinoin

  • A naturally-occurring retinoic acid with potential antineoplastic activity and teratogenic properties. 13-cis retinoic acid binds to and activates nuclear retinoic acid receptors (RAR), thereby regulating cell proliferation and differentiation. This agent also exhibits immunomodulatory and anti-inflammatory responses and inhibits ornithine decarboxylase, thereby decreasing polyamine synthesis and keratinization.

  • Isovorin

  • (Other name for: L-leucovorin)

  • 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.

  • 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). pDC, through cell-cell contact, and IFN-alpha and -beta, in turn, 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.

  • 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.

  • Iveegam EN

  • (Other name for: immune globulin)

  • ixabepilone

  • A semisynthetic analogue of epothilone B with antineoplastic activity. Ixabepilone (BMS-247550) 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.

  • Ixoten

  • (Other name for: trofosfamide)


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Cancer Drugs


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