Mechanism Folic acid analog that inhibits dihydrofolate reductase to decrease dTMP and decrease DNA and Protein synthesis
Toxicity
l. Myelosuppression, which is reversible with leucovorin (folinic acid) "rescue." 2. Macrovesicular fatty change in liver. 3. Mucositis. 4. Teratogenic. l. Myelosuppression, which is not reversible with leucovorin. Overdose: "rescue" with thymidine. 2. Photosensitivity Bone marrow, GI, liver. Metabolized by xanthine oxidase; thus I toxicity with allopurinol. Bone marrow depression, liver. Can be given with allopurinol. Leukopenia, thrombocytopenia, megaloblastic anemia.
5-fluorouracil (5-FU)
Colon cancer and other solid tumors, basal cell carcinoma, synery with MTX
6-mercaptopurine (6-MP)
6-thioguanine (6-TG)
Same as 6-MP
Cytarabine (ara-C)
ANTIBIOTICS Drug Dactinomycin (Actinomycin D) Doxorubicin (Adriamycin); daunorubicin Bleomycin Etoposide (VP-16); teniposide
Mechanism Intercalates in DNA Generate free radicals. Noncvalently intercalate in DNA to breaks in DNA to decrease replication Induces free radical formation, which causes breaks in DNA strands Inhibits topoisomerase II increase DNA degradation
Clinical Use Wilms tumor, Ewings sarcoma, rhabdomyosarcoma Hodgkins lymphomas; also for myelomas, sarcomas, and solid tumors Testicular cancer, Hodgins lymphoma Small cell carcinoma of the lung and prostate, testicular carcinoma
Toxicity
Myelosuppression. Cardiotoxicity, myelosuppression, and alopecia. Toxic to tissues with extravasation. Pulmonary fibrosis, skin changes. Minimal myelosuppression. Myelosuppression, Gl irritation, alopecia.
Clinical Use Non hodgkins lymphoma, breast and ovarian carcinomas. Also immunosuppressant
Toxicity
Myelosuppression; hemorrhagic cystitis, partially prevented with mesna (thiol group of mesna binds toxic metabolite). CNS toxicity (dizziness, ataxia). Pulmonary fibrosis, hyperpigmentation.
Brain tumors (including glioblastoma multiforme) CML. Also used to ablate patients bone marrow before bone marrow transplantation
Mechanism Alkaloids that bind to tubulin in Mphase and block polymerization of microtubules so that mitotic spindle cannot form. Microtubules are the vines of your cells. Hyperstabilize polymerized microtubules in M-phase so that mitotic spindle cannot break down. It is Taxing to stay polymerized.
Toxicity Vincristine- neurotoxicity (areflexia, peripheral block polymerization choriocarcinoma. neuritis), paralytic ileus. VinBLASTine BLASTs Bone marrow Myelosuppression and hypersensitivity.
Paclitaxel