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Flashcards in Breast & Endometrial Cancer Deck (38)
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1

MOA of Aromatase Inhibitors

Aromatase; Blocks production of estrone & estradiol

2

Aromatase Inhibitors (3)

Anastrozole, Exemestane, Letrozole

3

Aromatase Inhibitor Tox

Hot flashes; nausea; hair thinning; NO effect on adrenal steroids, thyroid, or other hormones; More arthralgia & diarrhea than tamoxifen but fewer gynecologic symptoms

4

Aromatase Inhibitors Metabolism

Hepatic

5

SERMs (3)

Raloxifene, Tamoxifen, Toremifene

6

Raloxifene MOA

SERM; ER agonist/antagonist-estrogen effect on bone & anti-estrogen effect on mammary tissue

7

Tamoxifen MOA

SERM; ER agonist/antagonist-estrogen effect on bone & anti-estrogen effect on mammary tissue

8

Toremifene MOA

SERM; Tamoxifen derivative w/ anti-estrogenic properties

9

Raloxifene Tox & BBW

Increased bone mineral density; Decreases serum cholesterol, LDL, & lipoproteins; Increases apolipoprotein-A1; Retinal degeneration at high doses

BBW= Thromboembolic Dz (DVT/PE) & Stroke

10

Raloxifene Admin

Monthly IM

11

SERMs & Pregnancy?

No, teratogens

12

Tamoxifen Tox & BBW

Increased bone mineral density; Decreases serum cholesterol, LDL, & lipoproteins; Increases apolipoprotein-A1; Retinal degeneration at high doses

BBW= Endometrial Hypertrophy, vaginal bleeding, endometrial cancer, thromboembolic dz (DVT/PE), stroke

13

Tamoxifen Admin

Daily PO

14

Toremifene Tox & BBW

Similar AE's to tamoxifen; Avoid w/ Hx of endometrial cancer/hyperplasia & thromboembolic dz

BBW= QT Prolongation (avoid in pre-existing conditions);

15

Toremifene Admin

Daily PO

16

Toremifene DDI

Avoid w/ CYP3A4 inhibitors

17

SERD (1)

Fulvestrant

18

Fulvestrant MOA

SERD; Pure antagonist, no estrogenic effects; Bulky substituent prevents dimerization of ER's in nucleus=sustained downregulation of ER expression

19

Fulvestrant Tox

Postmenopausal symptoms: nausea, asthenia, pain, vasodilation (hot flashes), and h/a

20

Fulvestrnat PK

Hepatic metabolism; monthly IM-sustained plasma levels

21

Fulvestrnat use

Tx for ER+ metastatic BC in PM women w/ dz progression following anti-estrogen therapy

22

Trastuzumab MOA

HER2/neu Antibody; Binds to the juxtaglomerular region of the extracellular domain of HER2

23

Trastuzumab Tox

Caution- HSR w/ initial dose; Common=GI upset, asthenia, blood dyscrasias, fatigue, peripheral edema, rash, wt gain, dizziness, URTIs, pharyngitis; Rare= cardiomyopathy & HF, renal failure, hepatotox, pneumonia, respiratory failure; BBWs

24

Trastuzumab BBW

BBWs=Cardiomyopathy, Infusion Rxns, Pregnancy, Respiratory Distress Syndrome, Respiratory Insufficiency

25

Lapatinib MOA

TKI

26

Lapatinib Tox

Common= GI tox, anemia, thrombocytopenia, hand-foot syndrome, rash pain, h/a, backache; Serious= interstitial lung dz/pneumonitis, QT prolongation

27

Lapatinib PK

Extensive hepatic metabolism- 3A4 + 3A5

28

Lapatinib DDI

CI'd w/ concurrent use of drugs that have AE's associated w/ pulmonary tox & QT prolongation

29

Lapatinib BBW

BBW=Liver Dz (b/c will lead to increased drug levels)- LFT monitoring required

30

Everolimus MOA

mTOR Inhibitor; Prevents cell proliferation & survival