Raloxifene
/ Selective estrogen receptor modulator (SERM); benzothiophene classALIAS · Evista (trade) · Raloxifene hydrochloride
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Tier 1. FDA-approved for postmenopausal osteoporosis prevention/treatment (1997) and reduction of invasive breast cancer risk in postmenopausal women (2007). Pivotal trials include MORE (osteoporosis), RUTH (cardiovascular outcomes in women at risk), and STAR (breast cancer chemoprevention versus tamoxifen).
Raloxifene binds the estrogen receptor and exerts tissue-selective agonist or antagonist activity depending on the cellular context — agonist in bone (preserves BMD) and lipids (modest LDL reduction), antagonist in breast and endometrium (reduces invasive ER-positive breast cancer incidence; does not stimulate endometrial proliferation, in contrast to tamoxifen).
Tier 1. MORE trial (Cummings 1999, JAMA) established BMD and vertebral-fracture-prevention efficacy. STAR trial (Vogel 2006, JAMA) directly compared raloxifene to tamoxifen for breast cancer chemoprevention, finding equivalent reduction in invasive breast cancer with a different adverse-event profile (less endometrial cancer, less thromboembolic risk than tamoxifen).
Increased venous thromboembolism risk (similar magnitude to oral estrogens), hot flashes, leg cramps. The RUTH trial established no overall cardiovascular benefit but a stroke-mortality signal in women at high baseline risk — the labelling reflects this.
Regulatory status
- FDA status:
- FDA-approved
- Compounding:
- Not eligible for compounding (approved, not in shortage)
Raloxifene is sometimes sold by research-chemical vendors with claims targeting male PCT (post-cycle therapy after anabolic-androgenic steroid use). The female-osteoporosis and breast-cancer-prevention literature does not extrapolate to that use case; published male-PCT data are essentially absent.