Cancer Pharm drugs Flashcards
(17 cards)
Cyclophosphamide
- class: cytotoxics
- forms DNA adducts/ intercalating agent
- targets DNA replication, chemically modifies the DNA and blocks DNA replication
5-fluoro-uracil
- class: cytotoxics
- inhibits thymidylate synthetase
- stops the formation of deoxyribonucleotides and prevents formation of DNA
Methotrexate
- class: cytotoxics
- inhibits enzyme dihydrofolate reductase
- prevents purine synthesis
Vinca alkaloids (vincristine/ vinblastine)
- class: cytotoxics
- inhibit microtubule formation/ polymerization
side affects: peripheral neuropathy in addition to all cytotoxic side effects
Taxanes (paclitaxel)
- class: cytotoxics
- inhibit depolymerization / they stabilize the microtubules
side affects: peripheral neuropathy in addition to all cytotoxic side effects
cisplatin/ oxaliplatin
- class: cytotoxics
- form DNA adducts, usually @ N7 of guanine
- side effect: peripheral neuropathy
- nephrotoxicity for cisplatin more than oxaliplatin
- cytotoxic adverse events
Irinotecan
- class: cytotoxics
- Top1 inhibitor
-used in Folfirinox combo for colon cancer
Doxorubicin
- class: cytotoxics
targets: microtubules - lots of cardiotoxicity (bc oxidative stress, iron chelation?)
cytotoxics adverse effects
- leukopenia, lymphocytopenia, immunosuppression, thrombocytopenia, anemia, longterm: leukemia due to mutagenesis
- ulceration, mucositis, diarrhea, vomiting
- alopecia
- premature menopause, reduced spermatogenesis
- impaired wound healing
- teratogenic
- tissue damage at injection site
leucovorin
- used in combo with 5 FU
- can reduce methotrexate overdose toxicity
- enhances the binding of the 5-FU/ thymidylate synthase complex formation
Cetuximab
- Anti-EGFR
- targets HER1
- (panitumumab also targets HER1)
- resistance due to downstream activating KRAS mutation
- lots of skin reactions (GI and cutaneous)
Drugs targeting HER2
- pertuzumab & trastuzumab
- adverse effects of trastuzumab: cardiotoxicity. destroys the myocardium
- combining anti HER1 and anti HER2 has huge benefit
VEGF inhibitors
Bevacizumab
- inhibits the angiogenesis
- used in melanoma & colon/ pancreatic cancers
adverse events: hypertension, thromboembolisms, GI perforations
* alternate use- macular degeneration
EGFR kinase inhibitors & mutations
lung cancer - give gefitinib (theres also erlotinib)
- gefitinib resistance
- T790M mutation –> give osimertinib
- skin & GI toxocity
- can also acquire KRAS mutation
CML treatment
- Imatinib for bcr-abl fusion protein
- also treats GIST
- also respond to cit & PDGFR
Vemurafenib
- targets V 600 E BRAF mutation in melanoma
when resistance –> go to MEK inhibitors : trametinib & cobimetinib
Palbociclib
-inhibitor of cyclin-dependent kinases CDK4/6
for ER+ BC with letrazole
adverse effects: cytopenia, nausea, stomatitis, alopecia, upper respiratory infections, fatigue, peripheral neuropathy
