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Reproductive > Breast and Endometrial Cancer Drugs > Flashcards

Breast and Endometrial Cancer Drugs Flashcards

1
Q

Aromatase inhibitors

A

anastrozole, exemestane, letrozole

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2
Q

SERMs

A

raloxifene, tamoxifen, toremifene

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3
Q

SERD

A

fulvestrant

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4
Q

GnRH agonist

A

goserelin

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5
Q

HER2 blockers

A

pertuzumab, trastuzumab, ado-trastuzumab emtasine

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6
Q

TKI

A

lapatinib

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7
Q

mTOR inhibitor

A

everolimus

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8
Q

What does BRCA enzyme do?

A

DNA damage repair during G2 and S phases

mutation causes division of cells w/ damaged DNA

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9
Q

What is the best tx for BRCA carriers?

A

prophylactic bilat mastectomy and salpingo-oophorectomy

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10
Q

how effective are SERMs in BRCA cases?

A

hardly at all for BRCA1

more effective for BRCA2

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11
Q

interventions for premenopausal women

A

surgical ablation of ovaries
GnRH agonists
SERMs

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12
Q

interventions for postmenopausal women

A

aromatase inhibitors

SERMS/SERDs

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13
Q

MOA of estrogen receptor

A

estrogen binds –> dimerization of receptor –> complex translocated to nucleus –> binds to DNA binding site –> associates w/ ERE and other cofactors

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14
Q

MOA of HER2/neu receptor

A

growth factor ligands bind –> dimerization of receptor –> activation of MAP kinase pathway

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15
Q

MOA of fulvestrant

A

estrogen antagonist –> downregulation of receptors

used in postmenopausal women

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16
Q

side effects of fulvestrant

A

menopause sx

17
Q

MOA SERMs

A

selective tissue estrogen agonist or antagonist (depends on what tissue)

18
Q

adverse effects of SERMs

A 
endometrial hyperplasia, VTE/stroke, vaginal bleeding, endometrial cancer, retinal degeneration, teratogen
prolonged QT (toremifene)
19
Q

significance of CYP metabolism w/ SERMs

A 
tamoxifen metabolized by CYP2D6 to more potent metabolites
poor metabolizers (w/ CYP2D6 variations) won't get full clinical effect of drug
20
Q

aromatase inhibitors MOA

A

block CYP19A1 activity –> blocking of aromatase activity

21
Q

adverse effects of aromatase inhibitors

A

arthralgia, diarrhea
teratogenic
menopause sx

22
Q

how is aromatase inhibitor best used?

A

after SERM therapy or swapping w/ SERM during treatment period

23
Q

pertuzumab MOA

A

blocks dimerization of HER2 receptor

24
Q

pertuzumab adverse effects

A

leukopenia

BBW for pregnancy

25
Q

trastuzumab MOA

A

binds to juxtaglomerular region of HER2 receptor

26
Q

trastuzumab adverse effects

A

cardiomyopathy, heart failure, renal failure, hepatotoxic, respiratory failure
BBW for cardiomyopathy, respiratory distress/insufficiency, pregnancy

27
Q

ado-trastuzumab emtasine (TDM1) MOA

A

trastuzumab linked to TDM1 –> taken into cell and broken apart in lysosome –> trastuzumab binds to receptor normally, TDM1 inhibits microtubule activity within cell

28
Q

ado-trastuzumab emtasine (TDM1) adverse effects

A

BBW for heart failure, hepatic dz, ventricular dysfunction, pregnancy

29
Q

lapitinib MOA

A

binds to intracellular ATP binding site on HER2 –> prevents activation

30
Q

metabolism of lapatinib

A

hepatic via CYP3A4

31
Q

lapatinib adverse effects

A

QT prolongation, interstitial lung dz

32
Q

goserelin MOA

A

GnRH agonist –> provides continuous supply of GnRH rather than pulsatile –> downregulation of receptors

33
Q

goserelin adverse effects

A

initial flare of dz –> bone pain from mets, hypercalcemia

eventually osteopenia, other menopause sx

34
Q

everolimus MOA

A

inhibits mTOR activity

35
Q

everolimus adverse effects

A

increased risk of infection, non-infectious pneumonitis

36
Q

conventional chemo adverse effects

A

doxorubicin – cardiotoxicity
cyclophosphamide – hemorrhagic cystitis
taxanes – peripheral neuropathy

37
Q

medroxyprogesterone MOA

A

progestin analog –> inhibits GnRH release

38
Q

megestrol MOA

A

progestin analog –> LH inhibition, differentiation/maintenance of endometrium

39
Q

endometrial cancer drugs

A

medroxyprogesterone, megestrol

Reproductive (8 decks)

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