Anticancer Drugs Flashcards
Anti cancer drugs are most toxic to _____________
Rapidly dividing cells: Bone marrow GI tract Hair follicles Renal Reproductive and teratogenesis
MOA for alkylating agents
Alkylate DNA —> cause miscoding, breakage, crosslinking
Not cell-cycle specific
Most effect on rapidly proliferating cells
Alkylating agent toxicity
POTENT VESICANTS —> cause major vesicle blisters, particularly at injection site (possible infection)
Cyclophosphamide
Alkylating agent - most widely used
Can be taken orally
Must be given together with MESNA to deal with acrolein (or you’ll get hemorrhagic cystitis)
Mechlorethamine
Alkylating agent for HL/NHL
Toxicity —> Renal Damage
COMBINE with allopurinol
Carmustine
Great for brain tumors because cross BBB
Alkylating agent
Cisplatin
Platinum analog
Cross-link DNA and “glunk” it up
Renal toxicity
ACOUSTIC NERVE DAMAGE - irreversable
Doxorubicin
Antibiotic widely used against lymphomas, leukemia’s, sarcomas
Intercalated into DNA —> DNA destruction
CARDITOXIC (further increased by iron so give with an iron chelator like dexrazoxane)
Methotrexate
Folate antimetabolite
Give Leucovorin AFTER methotrexate to rescue the folic acid
Major side fx: mucositis, thrombocytopenia
6-Mercaptopurine
Converted by HGPRT to a ribonucleotide —> inhibits DNA synthesis
Resistance develops b/c of decreased level of HGPRT
Leucovorin given after 6-MP treatment to rescue the folic acid
DO NOT give with allopurinol —> fatal blood dyscrasias
5-Fluorouracil
Inhibits thymidylate synthase (TS) —> blocks DNA synthesis
Response increased by leucovorin - given PRIOR to 5-FU administration
Biggest side fx = oral and GI ulcers
Bleomycin Sulfate
Antitumor antibiotic Specifically targets G2 and M of the cell cycle KEY Fx: • LITTLE MYELOSUPPRESSION • Pulmonary fibrosis • Hypersensitivity
Vincristine/Vinblastine
Bind to tubular —> cell cycle arrest in metaphase
Neurotoxic
Vincristine - more neurotoxic, less myelosuppression
Vinblastine - less neurotoxic, more myelosuppression
Paclitaxel
Binds beta-tubulin—> inhibits depolymerization
Adverse fx:
SEVERE MYELOSUPPRESSION
Anemia
Peripheral neuropathy
Imatinib (Gleevec)
Only useful against CML because inhibits BCR-ABL
Side fx: Fluid retention - ankle and periorbital edema
Cetuximab
Monoclonal antibody binds to EGF receptor to inhibit the tyrosine kinase activity —> growth inhibition and apoptosis
Erlotinib
Blocks ATP binding to EGF receptor to inhibit the tyrosine kinase activity —> growth inhibition and apoptosis
Epidermal growth factor inhibitors
Cetuximab
Erlotinib
Must test for EGFR expression and mutations
Angiogenesis Inhibitor
Bevacizumab
Binds to VEGF and prevents binding to VEGF receptor
Can cause bleeding and thromboembolism
