Antiestrogens Flashcards
What are the treatments for breast cancer?
- Surgery of primary tumor and/or sentinel lymph node
- Radiation (depending on tumor)
- Adjuvant drug therapy, either chemo (only when it’s reach lymph node) or hormones
What are 2 common SERMs used to treat breast cancer?
Tamoxifen
Raloxifene
How does tamoxifen work?
Competitive estrogen antagonist in breast
Competitive estrogen agonist in bone and endometrium and increases thromboemoblic events in the liver
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
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
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.
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
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.
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
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.
What demographic of women does leuprolide work best in?
PREmenopausal women
How does Herceptin (Trastuzumab) work?
It inactivates HER2 receptor. HER2 receptor can become overexposed on 25% of breast cancer cells. Makes it more aggressive
What’s a super bad side effect of trastuzamab?
Cardiomyopathy
How does pertuzumab work?
It is a monoclonal antibody against HER2 that prevents the HER2 monomers from dimerizing.
How does laptinib work?
Newer HER2 and EGFR/HER1 inhibitor that specifically inhibits the receptors’ tyrosine kinase.
