Anti-Cancer Agents Flashcards
S-phase specific agents
Methotrexate, 5-FU, cytarabine, azathioprine, and 6-MP
MOA of MTX
Inhibits dihydrofolate reductase which decreases dTMP synthesis
Non-neoplastic uses of MTX
Abortion, ectopic pregnancy, rheumatoid arthritis, and psorisasis
SE of MTX
Myelosuppression which is reversible with leucovorin, macrovesicular fatty change, teratogenic
MOA of 5-FU
Inhibits thymidylate synthase which decreases dTMP synthesis
SE of 5-FU
Myelosuppression which is not reversible with leucovorin, overdose rescue with thymidine
MOA of cytarabine
Pyrimidine analog
MOA of azathioprine and 6-MP
Purine analogs
Antitumor antibiotics
Dactinomycin, doxorubicin, and bleomycin
MOA of dactinomycin
Intercalates in DNA
Indications for dactinomycin
Wilm’s tumor, Ewing’s sarcoma, rhabdomyosarcoma (childhood tumors)
MOA fo doxorubicin
Generates free radicals that noncovalently intercalate in DNA which cause breaks in DNA
SE of doxorubicin
Cardiotoxicity (dilated cardiomyopathy), myelosuppresion, alopecia
Dexrazoxane to prevent cardiotoxicity
MOA of bleomycin
Induces free radical damage which causes breaks in DNA strands
Major side effect of bleomycin
Pulmonary fibrosis
MOA of cyclophosphamide and ifosfamide
Covalently X-link (interstrand) DNA at guanine N-7
Toxicity of cyclophoshamide
Myelosuppression, hemorrhagic cystitis (partially prevented with mesna)
MOA of nitrosoureas (carmustine, lomustine, semustine, streptozococin)
Requires bioactivation, crosses BBB
MOA of busulfan
Alkylates DNA
Indication of busulfan
CML
MOA of vincristine and vinblastine
Alkaloids that bind to tubulin in M phase and block polymerization of microtubules so that mitotic spindle cannot form
SE of vincristine
Neurotoxicity (areflexia, peripheral neuropathy, paralytic ileus)
SE of vinblastine
Bone marrow suppression
MOA of paclitaxel and other taxols
Hyperstabilize polymerized microtubules in M phase so that mitotic spindle cannot break down (anaphase cannot occur)
SE of paclitaxel and other taxols
Myelosuppresion and hypersensitivity
MOA of cisplatin and carboplatin
Cross-link DNA
SE of cisplatin
Nephrotoxicity and acoustic nerve damage (prevent nephrotoxicity with amifostine, which is a free radical scavenger)
MOA of etoposide and teniposide
Inhibits topoisomerase II which increases DNA degradation
Two specific tumors treated with etoposide
Testicular and small cell lung cancers
SE of etoposide
Myelosuppresion, GI irritation and alopecia
MOA of hydroxyurea
Inhibits ribonucleotide reducatase wich decreased DNA synthesis (S phase specific)
Indications of hydroxyurea
Melanoma, CML, sickle cell
MOA of prednisone, prednisolone
May trigger apoptosis
SE of prednisone
Cushing-like syndromes, immunosuppresion, cataracts, acne, osteoporosis, hypertension, peptic ulcers, hyperglycemia, psychosis
MOA of tamoxifen and raloxifene
SERMs- receptor antagonists in breast and agonists in bone; block the binding of estrogen in estrogen receptor-positive cells
Major side effect of tamoxifen
Increased risk of endometrial cancer
MOA of trastruzumab (Herceptin)
Monoclonal antibody against HER-2 (c-erbB2), a tyrosine kinase
MOA of imatinib (Gleevev)
Philadelphia chromosome bcr-able tyrosine kinase inhibitor
MOA of rituximab
Monoclonal antibody against CD20 which is found on most B-cell neoplasms
MOA of vemurafenib
Small molecular inhibitor of forms of the B-raf kinase with the 600E mutation (metastatic melanoma)
MOA of bevacizumab
Monoclonal antibody against VEFG which inhibits angiogenesis
Indication of bevacizumab
Solid tumors, first line Tx of metastatic colorectal cancer