Principles of Chemotherapy - Experimental Oncology Graduate Study

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Antimetabolites, contd.Methotrexate• Competitively inhibits dihydrofolate reductase (DHFR), theenzyme that converts folic acid to reduced folate cofactors (i.e.,tetrahydrofolate).• Use includes osteosarcoma, non-Hodgkin's lymphoma,Hodgkin's disease, cutaneous T cell lymphoma, head and neckcancer, lung and breast cancers.• Given orally or intrathecally.• Toxicity: immunosuppressive.18
Antimetabolites, contd.Cytosine arabinoside (Ara-C)• Ara-C differs from deoxycytidine in having a β-OH group on the 2-position ofthe sugar, so its sugar moiety is arabinose rather than deoxyribose.• A competitive inhibitor of DNA polymerase; it also incorporates into DNA.• Used primarily to treat acute leukemia.• Bone marrow toxicity is major side effect.• Others: gemcitabine, fludarabine, cladribine.19
Page 1 and 2: ONCOLOGY 520CHEMOTHERAPYLecturer: D
Page 3 and 4: Combination CT• Improvements in C
Page 5 and 6: Therapeutic Index, contd.• Such d
Page 7 and 8: Relationship between remission and
Page 9 and 10: Classes of anticancer drugs• “C
Page 11 and 12: a. Nitrogen mustards• Bifunctiona
Page 13 and 14: Melphalan (LMelphalan(L-phenylalani
Page 15 and 16: . Chloroethyl nitrosoureas• The 2
Page 17: 2. AntimetabolitesDrugs that resemb
Page 21 and 22: Natural products, contd.Actinomycin
Page 23 and 24: Natural products, contd.VP-16 and V
Page 25 and 26: 4. “Platinating” agents: Cispla
Page 27 and 28: 1. Transport• Mutation/altered ex
Page 29 and 30: Nucleoside analog responsiveness an
Page 31 and 32: 2. Glutathione and associated enzym
Page 33 and 34: 4. Tolerance to DNA damage• In ma
Page 35 and 36: 5. Drug-specific mechanisms• Ctx:
Page 37 and 38: Cell-cycle phase specificity of CT
Page 39 and 40: [2] Use of high-dose CT through ove
Page 41 and 42: Bone marrow transplantation and gen
Page 43 and 44: Gleevec (imatinib mesylate), former
Page 45 and 46: Hypoxic-cell cell cytotoxins: Tirap

Principles of Chemotherapy - Experimental Oncology Graduate Study

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