Exam IV - Breast Cancer Flashcards
Tamoxifen
Indications
ER+, 1. Adjuvant for metstatic BC post mastectomy, axillary dissection, or radiation, or ↓ Cancer risk in other breast. 2. Adjuvant for DCIS 3. Prevention in high risk pts
Tamoxifen
Mechanism
SERM: selectibe estrogen receptor modulator 4-Hydroxy TAM and endoxifen (ERα antagonists in breast tissue, partial agonists in endomet & bone) prevent cell growth and mitosis →2° apoptosis from growth inhibition
Tamoxifen
ADME
A: 10 mg PO bid for 5-10 years. M: Liver. Pharmakogenetic Testing for CYP2D6 (enz is rate limiting step)
Tamoxifen
Advantages
- Pre & Post menopausal 2. More efficacious than raloxifene
Tamoxifen
Toxicities
- Menopausal sx: hot flashes 2. Vaginal discharge 3. Cataracts 4. Nausea Black Box: Can cause DVTs & PEs and endometrial cancer↑risk if extendedn beyond 5-10 yrs
Tamoxifen
Resistance
3-5 years
Raloxifene
Indications
Post menopausal, ER+ BC
Raloxifene
Mechanism
SERM: selectibe estrogen receptor modulator
Raloxifene
Advantages
- Doesn’t req CYP 2D6 activation 2. Less risk for endometrial cancer
Leuprolide
Indications
Premenopausal, ER+ BC, Prostate Cancer
Leuprolide
Mechanism
GnRH agonist in pituitary leads to ↓ LH and FSH which ↓ estrogen & progesterone reease from ovaries (or testosterone in testes to tx prostate cancer)
Leuprolide
Adverse
- Inidital admin will cause LH and FSH to ↑ 2. Hot flashes 3. Osteoporosis 4. Sexual dysfunction
Leuprolide
Contraindications
Pregnancy
Anastrazole
Indications
Postmenopausal ER+ BC
Anastrazole
Mechanism
Aromatase Inhibitor: prevents conversion of testosterone to estrogen