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PHRM 864 > lecture 2 mabe > Flashcards

lecture 2 mabe Flashcards

1
Q

what is the function of 5a-reductase?

A

turns test into DHT

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2
Q

what is the function of aromatase?

A

turns androtenedione into estrone and testosterone into estradiol

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3
Q

what CYP is aromatase?

A

CYP19

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4
Q

what are the two stratgies in endocrine therapy?

A

stop steroid receptor function
decrease production of steroids

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5
Q

estrogen receptors primarily bind estrogen where in the cell?

A

cytoplasm

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6
Q

how will ER+ tumors be treated?

A

endocrine therapy

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7
Q

what are the 4 distinct diseases in breast cancer?

A

claudin low: treated with cytotoxic
BRCA1: tumor supressor
HER2-enriched: RTK
luminal A+B

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8
Q

what drug is a SERM?

A

tamoxifen

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9
Q

what is tamoxifen used for?

A

resected and metastatic ER+/PR+ breast cancer

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10
Q

what cyp coverts tamoxifen and to what?

A

CYP2D6 converts it to high affinity hydroxylated and demethylated metabolites
translocation and DNA binding in a tissue-specific manner

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11
Q

what are the antagonist and agonist effects of tamoxifen?

A

antagonist: blocks estrogen-dependent breast cancer cell proliferation. hot flashes
agonist: 3x endometrial cancer, preserve BMD

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12
Q

what was the first drug approved for breast cancer prevention in high-risk patients?

A

tamoxifen

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13
Q

what are SERDs?

A

fluvestrant and elacestrant

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14
Q

what is fluvestrant’s MOA? IM

A

pure ER antagonist (no agonist effects)

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15
Q

what is elacestrant MOA? PO

A

full SERD at high doses
partial agonist at low doses

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16
Q

what are SERDs (fluvestrant + elacestrant) approved for?

A

approved for ER+ metastatic breast cancer in postmenopausal women who progressed on other antiestrogen therapy

17
Q

what are the source of estrogen in postmenopausal women?

A

adipocytes
aromatase in adipocytes convert androtendione to estrone

18
Q

what is primary target for aromatase?

A

peripheral (adipose) tissue, not ovary

19
Q

what is primary application of aromatase?

A

estradiol suppression in postmenopausal women

20
Q

what are non-steroidal aromatase inhibitors?

A

letrozole and anastrozole

21
Q

letrozole and anastrozole uses?

A

potent + selective inhibitor or aromatase
primary indication: breast cancer in postmenopausal women
firstline or when started 3-5 years after tamoxifen

22
Q

what are steroidal aromatase inhibitors?

A

exemestane

23
Q

exemestane pharmacology?

A

suicide inhibitor
binds irreversibly @ active site and inactivates
indication: tx estrogen-responsive breast cancer postmenopausal women

24
Q

FSH + LH importance?

A

chronic admin of GnRH analogs –> downregulate GnRH receptor
decreased FSH –> decrease aromatase and estrogen

25
Q

what are GnRH analogs?

A

leuprolide, goserelin, triptorelin

26
Q

what are GnRH analogs indicated for in women?

A

premenopausal breast cancer

27
Q

what are GnRH analogs indicated for in men?

A

advanced prostate cancer
sides: gyno, sexual dysfunction
“flare” of test

28
Q

what are GnRH antagonist?

A

degarelix + relugolix

29
Q

what are GnRH antagonist indicated for?

A

advnaced prostate cancer
no flare
sides: gyno, sexual dysfunction

30
Q

what is the benefit of GnRH antagonist over analogs?

A

no flare up in men when used to treat prosate cancer

31
Q

what is abiraterone?

A

inhibits 17a-hydrolase and C17,20 lyase
CYP catalyzes conversion of pregnanolone and progesterone to DHEA and androtenedione

32
Q

what is a common side effect of abiraterone?

A

increase in cholesterol

33
Q

what are androgen receptor antagonist?

A

Enzalutamide, apalutamide, darolutimide

34
Q

what are androgen receptor antagonist used for?

A

metastatic + non metastatic prostate cancer

PHRM 864 (7 decks)

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