Breast Cancer Pharm

Question 1

What are the aromatase inhibitors?

Answer 1

Anastrozole, Exemestane, Letrozole

Question 2

MOA of aromatase inhibitors?

Answer 2

Blocks CYP19A1 mediated production of estrone & estradiol; actions are highly specific & no effects are observed on other organs or hormones

Question 3

Adverse effects of aromatase inhibitors?

Answer 3

hot flashes, nausea, hair thinning, arthralgia, diarrhea

Question 4

Route of administration of aromatase inhibitors?

Answer 4

oral

Question 5

Which aromatase inhibitors are reversible?

Answer 5

Anastrozole & Letrozole

Question 6

Which aromatase inhibitors are irreversible?

Answer 6

Exemestane

Question 7

What are the SERMs?

Answer 7

Raloxifene, Tamoxifen, Toremifene

Question 8

MOA of Raloxifene?

Answer 8

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

Question 9

MOA of tamoxifen?

Answer 9

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

Question 10

MOA of toremifene?

Answer 10

Derivative of tamoxifen with antiestrogenic properties

Question 11

Route of administration of the SERMs?

Answer 11

Raloxifene is give IM monthly; Tamoxifen & Toremifene are given orally daily

Question 12

Adverse effects of Raloxifene?

Answer 12

teratogen; decreases bone metabolism, serum cholesterol, & LDL; retinal degeneration (high doses); increases apolipoprotein A1

Question 13

Adverse effects of Tamoxifen?

Answer 13

teratogen; decreases bone metabolism, serum cholesterol, & LDL; retinal degeneration (high doses); increases apolipoprotein A1

Question 14

Adverse effects of Toremifene?

Answer 14

QT prolongation; teratogen

Question 15

Which SERMs have a BBW for DVT, PE, & stroke?

Answer 15

Raloxifene & Tamoxifen

Question 16

Which SERM has a BBW for endometrial hypertrophy, endometrial cancer, & vaginal bleeding?

Answer 16

Tamoxifen

Question 17

Which SERM undergoes CYP3A4 metabolism?

Answer 17

Toremifene

Question 18

What drug is a SERD?

Answer 18

Fulvestrant

Question 19

MOA of Fulvestrant?

Answer 19

Binds ER but carries a bulky substituent that prevents crucial dimerization of ER in the nucleus thus down-regulating ER expression

Question 20

Adverse effects of Fulvestrant?

Answer 20

nausea, asthenia, pain, vasodilation (hot flashes), HA

Question 21

What breast cancer drug is a GnRH agonist?

Answer 21

Goserelin

Question 22

What is the route of administration of fulvestrant?

Answer 22

IM (monthly)

Question 23

What is the route of administration of Goserelin?

Answer 23

SC every 28 days in the upper abdominal wall

Question 24

What is the MOA of Goserelin?

Answer 24

down-regulation of GnRH receptor on the pituitary gland ultimately decreasing the production of FSH & LH

Question 25

What are the adverse effects of Goserelin?

Answer 25

amenorrhea, hot flashes, decreased libido, vaginal dryness, emotional lability, depression, sweating, gynecomastia, HA, N/V, peripheral edema, lethargy, anorexia, decreased bone density, osteopenia/osteoporosis

Question 26

What drug causes an initial transient disease flare involving bone pain, hypercalcemia, & breast pain/tenderness?

Answer 26

Goserelin

Question 27

What are the Her2/neu antibodies?

Answer 27

Pertuzumab, Trastuzumab, & Ado-Trastuzumab Emtasine

Question 28

What is the route of administration of the Her2/neu antibodies?

Answer 28

IV every 21 days

Question 29

What is the MOA of pertuzumab?

Answer 29

binds extracellular dimerization domain blocking ligand-dependent heterodimerization of HER2 w/ other epidermal growth factor receptors

Question 30

What is the MOA of Trastuzumab?

Answer 30

Binds the juxtaglomerular region of the extracellular domain of HER2

Question 31

What is the MOA of Ado-Trastuzumab Emtasine?

Answer 31

Binds to the HER2 receptor & allows the thioester-linked chemotherapeutic to act on microtubules upon internalization preventing cell division

Question 32

What are the adverse effects of Pertuzumab?

Answer 32

Gi upset, asthenia, blood dyscrasias, fatigue, alopecia, loss of appetite, decreased LVEF, neutropenia, leukopenia

Question 33

What drugs are often used in combination with a taxane to treat breast cancer?

Answer 33

Pertuzumab & Trastuzumab

Question 34

What are the adverse effects of Traztuzumab?

Answer 34

Gi upset, asthenia, blood dyscrasias, fatigue, peripheral edema, rash, weight gain, dizziness, URTIs, pharyngitis, fatigue, cardiomyopathy, heart failure, renal failure, hepatotoxicity, pneumonia, respiratory failure

Question 35

What are the BBWs for Pertuzumab?

Answer 35

pregnancy

Question 36

What are the BBWs for Trastuzumab?

Answer 36

cardiomyopathy, infusion reactions, pregnancy, respiratory distress syndrome, & respiratory insufficiency

Question 37

What are the BBWs for Ado-Trastuzumab Emtasine?

Answer 37

heart failure, hepatic disease, pregnancy, & ventricular dysfunction

Question 38

What oral TKI treats breast cancer?

Answer 38

Lapatinib

Question 39

MOA of Lapatinib?

Answer 39

inhibits HER1 & HER2 by binding the intracellular domain of ErbB1 & ErbB2 receptors & competes with ATP ultimately preventing receptor activation

Question 40

What are the adverse effects of Lapatinib?

Answer 40

Gi issues, anemia, thrombocytopenia, hand-foot syndrome, rash, HA, backache, interstitial lung disease, pneumonitis, QT prolongation

Question 41

What breast cancer drug has extensive hepatic metabolism and requires monitoring of LFTs?

Answer 41

Lapatinib

Question 42

What TKI has a BBW for liver disease?

Answer 42

Lapatinib

Question 43

What mTOR inhibitor is given orally to treat breast cancer?

Answer 43

Everolimus

Question 44

What is the MOA of Everolimus?

Answer 44

Binds FKBP12 to block mTOR action thus preventing cell proliferation & survival

Question 45

What breast cancer drug has the serious adverse effects of increased opportunistic infections, neoplasia, lymphoma, & SCC?

Answer 45

Everolimus

Question 46

What breast cancer drug can inhibit CYP3A4, CYP2D6, & P-gp?

Answer 46

Everolimus

Question 47

What 2 drugs are used to treat endometrial cancer?

Answer 47

Medroxyprogesterone & Megestrol

Question 48

What is the MOA of Medroxyprogesterone?

Answer 48

Binds progestin receptors & blocks GnRH release

Question 49

What ist he MOA of Megestrol?

Answer 49

Suppresses pituitary LH release, enhances estrogen degradation, & promotes differentiation/maintenance of endometrial tissue

Question 50

What are the adverse effects of medroxyprogesterone?

Answer 50

amenorrhea, anorexia, edema, weakness

Question 51

What are the adverse effects of megestrol?

Answer 51

weight gain, hot flashes, malaise, asthenia, leathery, diaphoresis, rash, thrombophlebitis, thrombo- or pulmonary embolism; tumor flare, & hypercalcemia in pts w/ bone metastases

Question 52

What endometrial cancer drug can also be used to treat breast cancer or anorexia/cachexia?

Answer 52

Megestrol

Question 53

What breast cancer drug has the adverse effects of hyperglycemia, hyperlipidemia, & Hypertriglyceridemia?

Answer 53

Everolimus