Targeted Therapies

Question 1

SERMs

Answer 1

Tamoxifen
Competitive inhibitor of estradiol
Antagonist effects in breast cancer
Estrogenic effects on non breast tissues
Inc risk of thromboembolic events with age

Question 2

Aromatase inhibitors

Answer 2

Anastrazole
Block the fxn of aromatase (converts androgens to estrogens)
Lower incidence of AE than Tamoxifen

Question 3

Estrogen and feedback inhibition

Answer 3

Leoprolide acetate

Initially LH/FSH rise, until they turn off from constant GnRH stimulation

Question 4

-mab

Answer 4

Monoclonal Ab

Infusion rxns, HTN, heart failure common with males

Question 5

BCR-ABL

Answer 5

Imatinib
Inhibits BCR-ABL
Promotes fluid retention

Question 6

EGFR

Answer 6

Erlotinib
Inhibits EGFR
Blocks enzymatic fxn of EGFR through competitive blockade
Pustular/popular rash
Cetuximab
Binds specifically to extracellular domain of EGFR

Question 7

Trastusumab

Answer 7

HER2/neu inhibitor
Binds to external domain of HER2
SE: cardiac failure

Question 8

VEGF

Answer 8

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Withdrawn due to teratogenic effects

Question 9

Bortezamib

Answer 9

Inhibitor of proteasome-mediated protein degradation, induce arrest at G2-M phase and apoptosis
NEUROPATHY

Question 10

Rapamycins

Answer 10

mTOR inhibitors

Temsirolimus