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Onc Med Chem FINAL

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Drug Class/Cell cycle specific
Drug
Mechanism of Action
Key Toxicity
Notes
DNA Crosslinking Agents (Inhibit DNA synthesis and function) (Cell cycle phase non-specific)   Chlorambucil   Reactive species - aziridinium ion; DNA alkylation   show PO  
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DNA Crosslinking Agents (Inhibit DNA synthesis and function) (Cell cycle phase non-specific)   Cyclophosphamide     Urotoxicity; Nephrotoxicity   show
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DNA Crosslinking Agents (Inhibit DNA synthesis and function) (Cell cycle phase non-specific)   Ifosfamide     Urotoxicity; Nephrotoxicity to a greater extent   show
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DNA Crosslinking Agents (Inhibit DNA synthesis and function) (Cell cycle phase non-specific)   Carmustine   DNA alkylation   Prolonged myelosuppression   show
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DNA Crosslinking Agents (Inhibit DNA synthesis and function) (Cell cycle phase non-specific)   Lomustine   show Prolonged myelosuppression   High lipid solubility  
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DNA Crosslinking Agents (Inhibit DNA synthesis and function) (Cell cycle phase non-specific)   Busulfan   show Skin hyper-pigmentation (Busulfan tan); Pulmonary fibrosis; adrenal insufficiency    
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show Procarbazine   DNA methylation   Myelosuppression    
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DNA Crosslinking Agents (Inhibit DNA synthesis and function) (Cell cycle phase non-specific)   Dacarbazine   DNA methylation   show  
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DNA Crosslinking Agents (Inhibit DNA synthesis and function) (Cell cycle phase non-specific)   Cisplatin   Intra-strand DNA cross-linking (active form generated by reaction with water)   Nephrotoxicity, Ototoxicity   show
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DNA Crosslinking Agents (Inhibit DNA synthesis and function) (Cell cycle phase non-specific)   Carboplatin   show Myelosuppression    
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DNA Crosslinking Agents (Inhibit DNA synthesis and function) (Cell cycle phase non-specific)   show Intra-strand DNA cross-linking (active form generated by reaction with water)   Peripheral neuropathy    
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Antitumor Antibiotics (Cell cycle phase non-specific)   Anthracyclines: Doxorubicin, Duanorubicin; Idarubicin; Epirubicin; Valrubicin   Inhibition of Topoisomerase IIα; Allow DNA nicking but prevent DNA religation   Cardiotoxicity (acute-ROS related; chronic-rubicinol related)   show
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Antitumor Antibiotics (Cell cycle phase non-specific)   Bleomycin   Free radical mediated DNA strand breaks   Pulmonary fibrosis, Skin toxicity   show
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Mitotic Inhibitors (Cell cycle M-phase specific)   show Inhibit microtubule polymerization   Neurotoxicity    
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Mitotic Inhibitors (Cell cycle M-phase specific)   Vinblastine   Inhibit microtubule polymerization   show  
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Mitotic Inhibitors (Cell cycle M-phase specific)   show Inhibit microtubule polymerization   Myelosuppression    
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Mitotic Inhibitors (Cell cycle M-phase specific)   show Inhibit microtubule depolymerization   Peripheral neuropathy   Hypersensitivity rxn (pre-treat patient w/ dexamethasone, H1 antagonists.  
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Mitotic Inhibitors (Cell cycle M-phase specific)   Docetaxel   Inhibit microtubule depolymerization   Fluid retention, Peripheral Neuropathy, Myelosuppression w/ neutropenia   show
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Topoisomerase Inhibitors (Interfere with nicked DNA resealing) (Cell cycle S-phase specific)   Topotecan   Inhibit topoisomerase I   show  
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Topoisomerase Inhibitors (Interfere with nicked DNA resealing) (Cell cycle S-phase specific)   show Inhibit topoisomerase I   Acute and delayed diarrhea   SN-38 is the active drug; UGT1A1*28/*6 homo-or heterozygotes will have reduced irinotecan metabolism, hence increased toxicity  
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show Etoposide   Inhibit topoisomerase II   Myelosuppression    
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show Teniposide   Inhibit topoisomerase II      
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Anitmetabolites (Mimic physiologic biomolecules) (Cell cycle S-phase specific)   show Direct Inhibition of thymidylate synthase   Myelosuppression, Hand and foot syndrome, mucositis, neurotoxicity   5-FdUMP is the active form; Metabolic inactivation by dihydropyrimidine dehydrogenase; Leucovorin enhances drug activity  
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Anitmetabolites (Mimic physiologic biomolecules) (Cell cycle S-phase specific)   Capecitabine   show Myelosuppression, Hand and foot syndrome, mucositis, neurotoxicity   5-FdUMP is the active form; Metabolic inactivation by dihydropyrimidine dehydrogenase; Leucovorin enhances drug activity  
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Anitmetabolites (Mimic physiologic biomolecules) (Cell cycle S-phase specific)   Methotrexate   Inhibits DHFR Inhibits purine biosynthesis   Myelosuppression, mucositis, diarrhea   show
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Anitmetabolites (Mimic physiologic biomolecules) (Cell cycle S-phase specific)   Pemetrexed   Inhibits DHFR Inhibits purine biosynthesis     show
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Anitmetabolites (Mimic physiologic biomolecules) (Cell cycle S-phase specific)   6-Mercaptopurine   show Myelosuppression   PO available; Bioactivated by HGPRT;  
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Anitmetabolites (Mimic physiologic biomolecules) (Cell cycle S-phase specific)   show Inhibits purine biosynthesis by inhibiting amidophosphoribosyltransferase   Myelosuppression   PO available; Bioactivated by HGPRT;  
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Anitmetabolites (Mimic physiologic biomolecules) (Cell cycle S-phase specific)   show Inhibits DNA synthesis and repair (inhibit DNA polymerase by competing with normal nucleotides); Inhibits DNA chain elongation (by inserting at 3’ end)   Myelosuppression    
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