Targeted Therapies Flashcards
SERMs
Tamoxifen
Competitive inhibitor of estradiol
Antagonist effects in breast cancer
Estrogenic effects on non breast tissues
Inc risk of thromboembolic events with age
Aromatase inhibitors
Anastrazole
Block the fxn of aromatase (converts androgens to estrogens)
Lower incidence of AE than Tamoxifen
Estrogen and feedback inhibition
Leoprolide acetate
Initially LH/FSH rise, until they turn off from constant GnRH stimulation
-mab
Monoclonal Ab
Infusion rxns, HTN, heart failure common with males
BCR-ABL
Imatinib
Inhibits BCR-ABL
Promotes fluid retention
EGFR
Erlotinib
Inhibits EGFR
Blocks enzymatic fxn of EGFR through competitive blockade
Pustular/popular rash
Cetuximab
Binds specifically to extracellular domain of EGFR
Trastusumab
HER2/neu inhibitor
Binds to external domain of HER2
SE: cardiac failure
VEGF
Class effects: potential for vessel injury in bleeding Bevacizumab Ab directed against VEGF-A Risk of bleeding and poor wound healing Thalidomide Withdrawn due to teratogenic effects
Bortezamib
Inhibitor of proteasome-mediated protein degradation, induce arrest at G2-M phase and apoptosis
NEUROPATHY
Rapamycins
mTOR inhibitors
Temsirolimus