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Flashcards in Antiestrogens Deck (15)
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1

What are the treatments for breast cancer?

1. Surgery of primary tumor and/or sentinel lymph node
2. Radiation (depending on tumor)
3. Adjuvant drug therapy, either chemo (only when it's reach lymph node) or hormones

2

What are 2 common SERMs used to treat breast cancer?

Tamoxifen
Raloxifene

3

How does tamoxifen work?

Competitive estrogen antagonist in breast

Competitive estrogen agonist in bone and endometrium and increases thromboemoblic events in the liver

4

How does raloxifine work?

It is another SERM that is also used for the tx and prevention of osteoporosis

Breast/uterine tissue: estrogen ANTAGONIST
Bones/lipid metabolism: estrogen AGONIST

*note this is an active drug, NOT a prodrug

5

How does Fulvestrant work and what does it treat?

Pure estrogen receptor ANTAGONIST (degrades the receptor)

Tx of E receptor positive metastatic breast cancer that was treated with tamoxifen

6

Aromatase inhibitors are effective in what demographic of women?

POST-menopausal women. This is because in the ovary, aromatase activity is very strong, so you can't possibly shut it down completely with this antagonist. But in post-menopausal women most of the estrogen is coming from the adrenal androgens, which you also completely shut down with this inhibitor.

7

What is aminoglutethimide?

It is a aromatase and desmolase inhibitor. Use as a 2nd line agent after tamoxifen for metastatic breast cancer. Need to supplement cortisol because you block all steroid synthesis.

NOT REALLY USED ANYMORE

8

What are 2 selective aromatase inhibitors that we actually still use?

Anastrozole
Letrozole

These are BETTER than tamoxifen for advanced breast cancer. Can be the initial therapy for breast cancer in postmenopausal women.

9

What are 2 progesterone analogs that we don't really use for breast cancer but might possibly be helpful in its treatment?

Megestrol
Medroxyprogesterone

stimulates appetite to help with anorexic/cachexic pts

10

What is Leuprolide and how does it work?

Remember, this was used with prostate cancer, but caused a flare of estrogens. When given persistently, this GnRH agonist will cause negative feedback that eventually shuts down estrogen production.

11

What demographic of women does leuprolide work best in?

PREmenopausal women

12

How does Herceptin (Trastuzumab) work?

It inactivates HER2 receptor. HER2 receptor can become overexposed on 25% of breast cancer cells. Makes it more aggressive

13

What's a super bad side effect of trastuzamab?

Cardiomyopathy

14

How does pertuzumab work?

It is a monoclonal antibody against HER2 that prevents the HER2 monomers from dimerizing.

15

How does laptinib work?

Newer HER2 and EGFR/HER1 inhibitor that specifically inhibits the receptors' tyrosine kinase.