Endocrine Cancer Mabe Flashcards
Which hormone is produced in the pituitary gland?
a. GnRH
b. LH
c. estrogen
d. progesterone
b. LH
Estrogen receptor primarily binds estrogen where in the cell?
a. On the plasma membrane
b. In the mitochondria
c. In the cytoplasm
d. In the nucleus
c. In the cytoplasm
(once bound moves into nucleus)
What enzyme converts androstenedione to estrone?
a. CYP19
b. 5alpha-reductase
c. 17, 20 lyase
d. P450scc
a. CYP19 (aromatase)
Which compound directly inhibits the activity of the estrogen receptor throughout the body?
a. Letrozole
b. Exemestane
c. Tamoxifen
d. Fulvestrant
d. Fulvestrant
(a and b are indirect; c can do some but not all tissues)
Which compound is referred to as a SERM?
a. Letrozole
b. Exemestane
c. Tamoxifen
d. Fulvestrant
c. Tamoxifen
What is unique about the action of the Tamoxifen as compared to Fulvestrant?
a. It leads to ER degradation
b. It holds ER out of the nucleus
c. It ejects ER from the cell
d. It activates ER in bone
d. It activates ER in bone marrow
(fulvestrant degreades)
Which of the following is not a hormone responsive cancer type?
a. Breast cancer
b. Ovarian cancer
c. Prostate Cancer
d. Endometrial cancer
b. Ovarian cancer
Which of the following is only used in the postmenopausal setting?
a. Letrozole
b. Tamoxifen
c. Leuprolide
d. Raloxifene
a. Letrozole
Which compound acts directly on AR?
a. Leuprolide
b. Abiraterone
c. Degarelix
d. Enzalutamide
d. Enzalutamide
glucocorticoids have anti-cancer effect in tx of blood cancers including which 3? (slide 4)
-pediatric acute lymphoblastic leukemia (ALL)
-multiple myeloma
-lymphomas
which is NOT one of the 3 most common glucocorticoids used for cancer?
a. dexamethasone
b. budesonide
c. prednisolone
d. methylprednisolone
b. budesonide
3 hormone-dependent cancers (slide 5)
breast, prostate, and endometrial cancer
hormonal therapies primarily target _______ (breast, endometrial) and __________ (prostate)
estradiol; dihydrotestosterone
two strategies to endocrine therapy (slide 8)
- stop steroid receptor function
- dec production of steroids
where is GnRH produced?
hypothalamus
Well differentiated tumors are more likely to be ____; poorly differentiated tumors are generally ____
a. ER- ; ER+
b. ER+ ; ER-
c. ER- ; ER-
d. ER+ ; ER+
b. ER+ ; ER-
T or F: hormone therapy in breast cancer is generally limited to ER+/PR+ tumors
T
4 molecular subtypes of breast cancer (slide 16)
Triple negative/Basal-like
HER2-enriched
Luminal B
Luminal A
T or F: tamoxifen is a prodrug
T
tamoxifen must be metabolized to _______ by 2D6, then to ________ by 3A4
4OH-TAM; endoxifen
2 estrogen antagonist effects of tamoxifen
-blocks estrogen-dependent breast cancer cell proliferation
-hot flashes due to anti-estrogen effects
2 estrogen agonist effects of tamoxifen
-incidence of endometrial cancer inc 3-fold
-preservation of bone density in postmenopausal women
T or F: tamoxifen is only effective in postmenopausal women
F (pre- and post-)
first drug approved for breast cancer prevention in high-risk pts
a. raloxifene
b. fulvestrant
c. letrozole
d. tamoxifen
d. tamoxifen
(reduces risk by 50%)
T or F: fulvestrant has only agonist effects
F (pure ER antagonist, NO agonist effects)
Fulvestrant and Elacestrant drug class
SERD
T or F: primary target of aromatase inhibitors are the ovaries
F (peripheral tissue/adipose tissue)
aromatase inhibitors primary application is estradiol suppression in ___________ women
a. premenopausal
b. postmenopausal
c. both
b. postmenopausal
2 non-steroidal aromatase inhibitors
anastrazole, letrozole
Letrozole and anastrozole are __________ inhibitors or aromatase activity
a. non-competitive
b. competitive
b. competitive
what drug is a steroidal aromatase inhibitor?
exemestane
exemestane is structurally related to what molecule?
androstenedione
T or F: adipocytes are a source of estrogen in postmenopausal women
T
does exemestane’s intermediate bind reversibly or irreversibly at the active site?
irreversibly
