About Raloxifene

Mechanism of Action: Raloxifene is a selective estrogen receptor modulator (SERM) that acts as an estrogen agonist on bone and lipid metabolism while antagonizing estrogen in breast and uterine tissue.

Indications & Off-Label Uses: FDA-approved for prevention and treatment of osteoporosis in postmenopausal women and reduction of breast cancer risk. Off-label use in men in testosterone therapy to mitigate estrogen-related side effects.

FDA Status: Approved for osteoporosis and breast cancer risk reduction; other uses are off-label.

Clinical Evidence: Demonstrated efficacy in increasing bone mineral density and lowering vertebral fracture risk in postmenopausal women. Evidence for use in men for treatment of estrogen-related side effects while on testosterone therapy (such as gynecomastia) or for general “anti-aging” purposes is limited.

Safety & Monitoring: Common adverse effects include hot flashes, leg cramps, and increased risk of venous thromboembolism. Monitoring of bone density and thromboembolic risk is recommended.