Flashcards in Other antineoplastic agents Deck (10):
Mechanism: Cross-link DNA.
Clinical use: Testicular, bladder, ovary, and lung carcinomas.
Toxicity: Nephrotoxicity and acoustic nerve damage. Prevent nephrotoxicity with amifostine (free radical scavenger) and chloride diuresis.
Mechanism: Inhibit topoisomerase II -> Increased DNA degradation.
Clinical use: Solid tumors, leukemias, lymphomas.
Toxicity: Myelosuppression, GI irritation, alopecia.
Mechanism: Inhibits ribonucleotide reductase
-> Decreased DNA Synthesis (S-phase specific).
Clinical use: Melanoma, CML, sickle cell disease (Increased HbF).
Toxicity: Bone marrow suppression, GI upset.
Mechanism: May trigger apoptosis. May even work on non dividing cells.
Clinical use: Most commonly used glucocorticoid in cancer chemotherapy. Used in CLL, non-Hodgkin's lymphomas (part of combination chemotherapy regimen). Also used as an immunosuppressant (e.g. autoimmune diseases).
Toxicity: Cushing-like symptoms; immunosuppression, cataracts, acne, osteoporosis, hypertension, peptic ulcers, hyperglycemia, psychosis.
Mechanism: SERMs-receptor antagonists in breast and agonists in bone. Block the binding of estrogen to estrogen receptor-positive cells.
Clinical use: Breast cancer treatment and prevention. Also useful to prevent osteoporosis.
Toxicity: Tamoxifen-partial agonist in endometrium, which increases the risk of endometrial cancer; "hot flashes".
Raloxifene-no increase in endometrial carcinoma because it is an endometrial antagonist.
Mechanism: Monoclonal antibody against HER-2 (c-erbB2), a tyrosine kinase. Helps kill breast cancer cells that over express HER-2, possibly through antibody-dependent cytotoxicity.
Clinical use: HER-2-positive breast cancer.
Mechanism: Philadelphia chromosome bcr-abl tyrosine kinase inhibitor.
Clinical use: GML, GI stromal tumors.
Toxicity: Fluid retention.
Mechanism: Monoclonal antibody against CD20, which is found on most B-cell neoplasms.
Clinical use: Non-Hodgkin's lymphoma, rheumatoid arthritis (with methotrexate).
Mechanism: Small molecule inhibitor of forms of the B-Raf kinase with the V600E mutation.
Clinical use: Metastatic melanoma.