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Reproductive Pharm > Breast Cancer: Anti-Estrogen treatment > Flashcards

Breast Cancer: Anti-Estrogen treatment Flashcards

1
Q

What is the typical responsiveness of anti-estrogen treatment in Estrogen sensitive tumors?

A

The tumors are typically responsive to treatment within 8-12 weeks. The average remission lasts 6-12 months

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2
Q

What drug is a Selective Estrogen Receptor Downregulator?

A

Fulvestrant

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3
Q

What is the MOA of Fulvestrant?

A

Fulvestrant is a pure antagonist of Estrogen. It binds to the ER and prevents dimerization which in turn prevent nuclear localization and increases degradation.

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4
Q

What is the ADME of Fulvestrant?

A

Monthly IM injections

Hepatic metabolism

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5
Q

What adverse effects are associated with fulvestrant?

A 
Essentially symptoms of menopause:
nausea
asthenia
vasodilation (hot flash)
Headache
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6
Q

What Drugs belong to the SERM group?

A

Tamoxifen
Raloxifen
Toremifene

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7
Q

What is the MOA of the SERMs?

A

Location dependent agonistic/antagonistic effects on estrogen receptors.

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8
Q

What is the effect of SERMs on bone?

A

SERMs have an agonistic effect on bone. Thus they increase bone density.

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9
Q

What effect do SERMs have on breast and other tissues?

A

They are antagonistic in breast tissue thus inhibiting tumor growth. In other tissues they increase apoA1 and decrease LDL, cholesterol, and lipoproteins.

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10
Q

What are some common and serious adverse effects of SERMs?

A

Teratogenic
Retinal degeneration
DVT/PE/stroke

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11
Q

What is the ADME of tamoxifen?

A

Daily PO,

metabolized by CYP2D6

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12
Q

What are some effects unique to tamoxifen?

A

Can cause endometrial hypertrophy
Vaginal bleeding
Endometrial cancer

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13
Q

What is the ATLAS study?

A

The ATLAS study showed that the benefit of 10yr adjuvant therapy with tamoxifen outweighed the potential risk of endometrial cancer.

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14
Q

What is the ADME of Raloxifene?

A

Monthly IM injections

No agonism in the Endometrium.

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15
Q

What is the ADME of Toremifene?

A

Derivative of tamoxifen
Daily PO
CYP3A4

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16
Q

What adverse effects are unique to Toremifene?

A

Prolongation of QT interval

Agonizes ER in endometrium

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17
Q

What drugs belong to aromatase inhibitor class?

A

Anastrozole
Letrozole
Exemestane

18
Q

When are the aromatase inhibitors used?

A

They are used for all ER+ post menopausal breast cancers.

19
Q

Which aromatase inhibitor is steroid derived?

A

Exemestane

20
Q

What is the MOA of aromatase inhibitors?

A

They prevent the conversion of testosterone to estrogen by aromatase (CYP19A1)

21
Q

What is the difference in MOA between steroidal and non-steroidal aromatase inhibitors?

A

The non-steroidal drugs are initiate reversible inhibition. The steroidal drug initiates irreversible inhibition.

22
Q

What is the ADME of the aromatase inhibitors?

A

daily PO

Hepatic metabolism

23
Q

What are the adverse effects of the aromatase inhibitors?

A

Hot flashes, Nausea
Hair thinning
Arthralgia
diarrhea

24
Q

How is HER2/neu testing done?

A

Immunohistochemistry

In situ hybridization

25
Q

Why is testing for HER2/neu important?

A

Because there are effective targeted therapies for HER2/neu tumors.

26
Q

What are the drugs used for HER2/neu therapy?

A

Trastuzumab
Pertuzumab
Lapatinib

27
Q

What is the MOA of trastuzumab?

A

Trastuzumab is a monclonal antibody against the HER2 extracellular domain

28
Q

What is the ADME of trastuzumab?

A

IV every 3 weeks

29
Q

What are some common adverse effects associated with trastuzumab?

A 
GI upset
Asthenia
Blood dyscrasias
Edema
Rash
Weight gain
URTIs
Dizziness
30
Q

What are the BBWs for trastuzumab?

A 
Cardiomyopathy
Infusion rxn
Pregnancy
ARDS/respiratory insufficiency
Hepatotoxicity
31
Q

What is Ado-trastuzumab emtansine?

A

A small cytotoxic drug that is linked to trastuzumab. Trastuzumab binds and through endocytosis delivers the cytotoxic drug.

32
Q

What are the unique BBWs for Ado-Trastuzumab?

A

HF
Liver disease
Pregnancy
Ventricular dysfunction

33
Q

What is the MOA of Pertuzumab?

A

mAb for HER2 dimerization domain.

34
Q

What is the ADME for Pertuzumab?

A

IV every 3 weeks

35
Q

What adverse effects are associated with Pertuzumab?

A

Hypersensitivity rxn

Common: GI upset/asthenia/blood dyscrasias/fatigue/alopecia/loss of appetite

Rare: Leukopenia, decreased LVEF

36
Q

What BBW is associated with Pertuzumab?

37
Q

What is the MOA for lapatinib?

A

Lapatinib is a tyrosine kinase inhibitor for HER1 and HER2. It competes for ATP binding site to prevent down stream signaling.

38
Q

What is the metabolism of Lapatinib?

A

CYP 3A4 and 3A5 metabolism

39
Q

What BBW is associated with Lapatinib?

A

Liver disease

40
Q

What adverse effects are associated with Lapatinib?

A

Common: GI, blood dyscrasias, rash, headache, Backache, Hand-Foot syndrome

Serious: Interstitial lung disease / pneumonitis, QT prolongation.

Reproductive Pharm (17 decks)

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