Endocrine Oncology

Question 1

Medications for postmenopausal women with ER+ breast cancer

Answer 1

SERM (tamoxifen), non-steroidal aromatase inhibitors (anastrozole, letrozole), steroidal aromatase inhibitor (exemestane), SERD (fulvestrant, elacetrant)

Question 2

Medications for premenopausal women with ER+ breast cancer

Answer 2

GnRH agonists (leuprolide, goserelin, tiptorelin), tamoxifen

Question 3

how does SERDs mechanism of action differ from SERMs?

Answer 3

is a down-modulator/ degrader of the estrogen receptor–causes rapid receptor degradation

Question 4

What is the mechanism of action for SERMs?

Answer 4

modulators of estrogen receptor; have agonist effects and antagonist effects
antagonist effect includes blocking estrogen receptor and hot flashes; agonist effect includes endometrial hyperplasia and bone resorption

Question 5

What medications are considered SERMs?

Answer 5

tamoxifen, raloxifene

Question 6

What medications are considered SERDs?

Answer 6

fulvestrant (IM), elacetrant (po)

Question 7

What is the mechanism of action of aromatase inhibitors?

Answer 7

prevents the conversion of testosterone to estradiol/androstenedione to estrone
-works in the adipose tissue

Question 8

What medications are considered aromatase inhibitors?

Answer 8

-anastrozole, letrozole (non-steroidal)
-competitive inhibitors
-exemestane (steroidal)
-irreversible inhibitor; looks similar to androstenedione

Question 9

What is the mechanism of action for GnRH analogs?

Answer 9

-downregulates pituitary GnRH receptors, increases pituitary desensitization

Question 10

What medications are considered GnRH analogs (breast cancer)?

Answer 10

Leuprolide, Goserelin

Question 11

What GnRH analogs are used in prostate cancer?

Answer 11

Leuprolide (lupron), goserelin (zoladex), triptorelin (Trelstar)

Question 12

What GnRH antagonists are used in prostate cancer and what is their difference in mechanism of action?

Answer 12

-does not result in flare of testosterone production
-degarelix (firmagon), relugolix (orgovyx)

Question 13

What medication inhibits 17a-hydrolase and CYP17,20 lyase?

Answer 13

abiraterone (Zytiga)
-AE’s include increased cholesterol

Question 14

What is the mechanism of action of Androgen receptor antagonists?

Answer 14

-prevents AR translocation to the nucleus (prevents DNA binding)

Question 15

What medications are AR antagonists?

Answer 15

Enzalutamide, apalutamide, Darolutimide

Question 16

What is unique about the action of the Tamoxifen as compared to Fulvestrant?

Answer 16

it activates ER in bone