breast and endometrial cancer pharmacology

Question 1

fulvestrant use

Answer 1

effective in post-menopausal women only

Question 2

fulvestrant adverse effects

Answer 2

post-menopausal symptoms

Question 3

Tamoxifen and Raloxifene MOA

Answer 3

SERMs: tissue-specific estrogenic (bone and endometrium) and anti-estrogenic effects (breast)

Question 4

tamoxifen and raloxifene shared adverse effects

Answer 4

teratogenic, retinal degeneration at high dose, stroke

BBW: DVT/PE

Question 5

tamoxifen specific adverse effects

Answer 5

endometiral hypertrophy, endometrial cancer, and vaginal bleeding

Question 6

toremifene moa

Answer 6

SERM: derivative of tamoxifen with antiestrogenic effects

Question 7

toremifene adverse effects

Answer 7

teratogen; BBW - QT prolongation

Question 8

anastrozole and letrozole moa

Answer 8

non-steroidal reversible inhibition of aromatase (CYP19A1)

Question 9

exemestane moa

Answer 9

steroidal irreversible inhibition of aromatase (CYP19A1)

Question 10

aromatase inhibitors adverse effects

Answer 10

hair thinning, arthralgia, diarrhea, visual disturbances, teratogenic

Question 11

trastuzumab moa

Answer 11

binds to the juxtaglomerular region of the extracellular domain of HER2

Question 12

trastuzumab adverse effects

Answer 12

CHF, renal failure, hepatotoxicity, pneumonia, respiratory failure
BBW: cardiomyopathy, infusion reactions, pregnancy, respiratory distress syndrome and respiratory insufficiency

Question 13

trastuzumab emtansine (T-DM1) (Ado-Trastuzumab) moa

Answer 13

antibody-drug conjugation; trastuzumab binds HER-2 and emtansine breaks apart in the lysosome and DM-1 (cytotoxic) interferes with microtubules, preventing cell division

Question 14

pertuzumab moa

Answer 14

binds to the extracellular dimerization domain and blocks ligand dependent hetero-dimerization of HER2 with other epidermal growth factor receptors, including HER3&4

Question 15

pertuzumab adverse effects

Answer 15

decreased left ventricular ejection fraction, neutropenia, leukopenia
BBW: pregnancy

Question 16

lapatinib moa

Answer 16

receptor tyrosine kinase inhibitor that inhibits HER1&2 by binding to the intracellular domain of ErbB1 and ErbB2 receptors and competes with ATP

Question 17

lapatinib adverse effects

Answer 17

BBW: liver disease leads to high drug concentration and elevates liver enzymes
interstitial lung disease/pneumonitis, QT prolongation

Question 18

goserelin moa

Answer 18

GnRH agonist, 1st causes estrogen surge, then down regulation of the receptor

Question 19

goserelin adverse effects

Answer 19

amenorrhea, hot flashes, decreased libido, vaginal dryness, gynecomastia, decreased bone density, osteoporosis;
initially - increases pain from bone mets because of the initial estrogen surge

Question 20

everolimus moa

Answer 20

macrolide immunosuppressant; an along of sirolimus (mTOR inhibitor)

Question 21

everolimus adverse effects

Answer 21

non-infectious pneumonitis, blood dyscrasias, hyperglycemia, hyperlipidemia, hypertriglyceridemia, elevated creatinine, elevated liver enzymes
BBW: opportunistic infection, lymphoma, and squamous cell cancer

Question 22

medroxyprogesterone moa

Answer 22

progestin contraceptive that binds to the progestin receptors and blocks GnRH release

Question 23

medrozyprogesterone adverse effects

Answer 23

amenorrhea, edema, anorexia, weakness

Question 24

megestrol moa

Answer 24

synthetic oral progestin that suppresses pituitary LH release and enhances estrogen degradation

Question 25

megestrol adverse effects

Answer 25

weight gain due to increased appetite, hot flashes, malaise, asthenia, lethargy, tumor flare in birth control patients with bony metastases, thromboembolism or pulmonary embolism