Breast Cancer treatment (lecture) Flashcards
What is the MoA of tamoxifen?
SERM: Antagonist at breast, agonist at bone and endometrium
What are the two big side effects of tamoxifen in postmenopausal women?
Increase in endometrial carcinoma and thrombosis
How do SSRIs interfere with tamoxifen?
SSRIs are inhibitors of CYP2D6 (activator of tamoxifen)
What is the time limitation of SERM usage?
After 5 years may be harmful
What effect does tamoxifen have on LDL and bone density?
Lowers LDL and raises bone density
What is the advantage of raloxifene over tamoxifen?
Raloxifene is not a prodrug (fewer interactions with other drugs)
What is the MoA of fulvestrant?
estrogen receptor antagonist - prevents dimerization of estrogen receptor in all tissues
What is the indication of use for fulvestrant?
Metastatic breast cancer
What age group are aromatase inhibitors used in and why?
Postmenopausal - they inhibit aromatase in the adrenal glands effectively. Premenopausal women mainly get estrogen from the ovaries (not targeted effectively by aromatase inhibitors - too much aromatase)
What are the three aromatase inhibitors covered in lecture?
Anastrozole, Letrozole, and Exemastane
What are the three advantages of aromatase inhibitors?
No thrombotic events, no endometrial carcinoma, can use for more than 5 years
What is the GnRH agonist covered in lecture?
Leuprolide
How is leuprolide administered (2 things)?
Constant (as opposed to pulsatile) and with estrogen antagonist for first two weeks to counteract initial surge
What are the two anti-HER2 antibodies covered in lecture?
Trastuzumab and Pertuzumab
TraP HER2
What is the MoA of Lapatinib?
Inhibit tyrosine kinase associated with HER2
“tinib” are all tyrosine kinase inhibitors
