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Drug Class/Cell cycle specific

DNA Crosslinking Agents (Inhibit DNA synthesis and function) (Cell cycle phase non-specific)
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Drug Class/Cell cycle specific

DNA Crosslinking Agents (Inhibit DNA synthesis and function) (Cell cycle phase non-specific)
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Onc Med Chem FINAL

Drug Class/Cell cycle specificDrugMechanism of ActionKey Toxicity Notes
DNA Crosslinking Agents (Inhibit DNA synthesis and function) (Cell cycle phase non-specific) Chlorambucil Reactive species - aziridinium ion; DNA alkylation PO
DNA Crosslinking Agents (Inhibit DNA synthesis and function) (Cell cycle phase non-specific) Cyclophosphamide Urotoxicity; Nephrotoxicity Hemorrhagic cystitis managed by hydration, Mesna
DNA Crosslinking Agents (Inhibit DNA synthesis and function) (Cell cycle phase non-specific) Ifosfamide Urotoxicity; Nephrotoxicity to a greater extent Hemorrhagic cystitis managed by hydration, Mesna
DNA Crosslinking Agents (Inhibit DNA synthesis and function) (Cell cycle phase non-specific) Carmustine DNA alkylation Prolonged myelosuppression High lipid solubility
DNA Crosslinking Agents (Inhibit DNA synthesis and function) (Cell cycle phase non-specific) Lomustine DNA alkylation Prolonged myelosuppression High lipid solubility
DNA Crosslinking Agents (Inhibit DNA synthesis and function) (Cell cycle phase non-specific) Busulfan DNA alkylation Skin hyper-pigmentation (Busulfan tan); Pulmonary fibrosis; adrenal insufficiency
DNA Crosslinking Agents (Inhibit DNA synthesis and function) (Cell cycle phase non-specific) Procarbazine DNA methylation Myelosuppression
DNA Crosslinking Agents (Inhibit DNA synthesis and function) (Cell cycle phase non-specific) Dacarbazine DNA methylation Myelosuppression
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 Manage nephrotoxicity by pre-and post-hydration with normal saline
DNA Crosslinking Agents (Inhibit DNA synthesis and function) (Cell cycle phase non-specific) Carboplatin Intra-strand DNA cross-linking (active form generated by reaction with water) Myelosuppression
DNA Crosslinking Agents (Inhibit DNA synthesis and function) (Cell cycle phase non-specific) Oxaliplatin Intra-strand DNA cross-linking (active form generated by reaction with water) Peripheral neuropathy
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) Colors urine red
Antitumor Antibiotics (Cell cycle phase non-specific) Bleomycin Free radical mediated DNA strand breaks Pulmonary fibrosis, Skin toxicity No myelosuppression; Drug inactivation by bleomycin hydrase
Mitotic Inhibitors (Cell cycle M-phase specific) Vincristine Inhibit microtubule polymerization Neurotoxicity
Mitotic Inhibitors (Cell cycle M-phase specific) Vinblastine Inhibit microtubule polymerization Myelosuppression
Mitotic Inhibitors (Cell cycle M-phase specific) Vinorelbine Inhibit microtubule polymerization Myelosuppression
Mitotic Inhibitors (Cell cycle M-phase specific) Paclitaxel Inhibit microtubule depolymerization Peripheral neuropathy Hypersensitivity rxn (pre-treat patient w/ dexamethasone, H1 antagonists.
Mitotic Inhibitors (Cell cycle M-phase specific) Docetaxel Inhibit microtubule depolymerization Fluid retention, Peripheral Neuropathy, Myelosuppression w/ neutropenia Hypersensitivity rxn (pre-treat patient w/ dexamethasone, H1 antagonists.
Topoisomerase Inhibitors (Interfere with nicked DNA resealing) (Cell cycle S-phase specific) Topotecan Inhibit topoisomerase I Myelosuppression
Topoisomerase Inhibitors (Interfere with nicked DNA resealing) (Cell cycle S-phase specific) Irinotecan 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
Topoisomerase Inhibitors (Interfere with nicked DNA resealing) (Cell cycle S-phase specific) Etoposide Inhibit topoisomerase II Myelosuppression
Topoisomerase Inhibitors (Interfere with nicked DNA resealing) (Cell cycle S-phase specific) Teniposide Inhibit topoisomerase II
Anitmetabolites (Mimic physiologic biomolecules) (Cell cycle S-phase specific) 5-Fluorouracil (5-FU) 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
Anitmetabolites (Mimic physiologic biomolecules) (Cell cycle S-phase specific) Capecitabine 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
Anitmetabolites (Mimic physiologic biomolecules) (Cell cycle S-phase specific) Methotrexate Inhibits DHFR Inhibits purine biosynthesis Myelosuppression, mucositis, diarrhea Leucovorin rescue to mitigate drug toxicity
Anitmetabolites (Mimic physiologic biomolecules) (Cell cycle S-phase specific) Pemetrexed Inhibits DHFR Inhibits purine biosynthesis
Anitmetabolites (Mimic physiologic biomolecules) (Cell cycle S-phase specific) 6-Mercaptopurine Inhibits purine biosynthesis by inhibiting amidophosphoribosyltransferase Myelosuppression PO available; Bioactivated by HGPRT;
Anitmetabolites (Mimic physiologic biomolecules) (Cell cycle S-phase specific) 6-Thioguanine Inhibits purine biosynthesis by inhibiting amidophosphoribosyltransferase Myelosuppression PO available; Bioactivated by HGPRT;
Anitmetabolites (Mimic physiologic biomolecules) (Cell cycle S-phase specific) Cytarabine, Gemcitabine, Cladribine, Fludarabine Inhibits DNA synthesis and repair (inhibit DNA polymerase by competing with normal nucleotides); Inhibits DNA chain elongation (by inserting at 3’ end) Myelosuppression
Created by: KaylaHaase
 

 



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