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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 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 | 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