Raloxifene (Evista) is a second-generation SERM approved in 1997 for postmenopausal osteoporosis, with a secondary indication for breast cancer prevention in high-risk women. Where tamoxifen is a partial activator in the uterus (creating an endometrial cancer risk), raloxifene is a blocker there as well as in the breast, eliminating that risk. It still acts as a partial activator in bone and liver, supporting the bone density and lipid-profile improvements. Trade-offs: more hot flashes than tamoxifen and increased risk of blood clots. The MORE and STAR trials established its osteoporosis and breast-cancer-prevention efficacy, respectively. Not stocked by Kodiac. This monograph is provided for research and educational reference.
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Second-generation SERM (benzothiophene)
A benzothiophene SERM; an osteoporosis drug with breast cancer prevention activity but no uterine partial agonism, distinguishing it from tamoxifen.
Abstract
Raloxifene ([6-hydroxy-2-(4-hydroxyphenyl)benzothiophen-3-yl]-[4-(2-piperidin-1-ylethoxy)phenyl]methanone; CAS 84449-90-1; molecular formula C28H27NO4S; molecular weight 473.58) is a benzothiophene second-generation SERM developed at Eli Lilly and approved by the FDA in 1997 under the trade name Evista. Distinct from tamoxifen by tissue selectivity profile: ER antagonism in breast and uterus, partial agonism in bone and liver. The absence of uterine partial agonism eliminates the endometrial cancer risk seen with tamoxifen and is the principal distinguishing clinical feature. Plasma half-life is approximately 27 hours; metabolism is via glucuronidation. Approved for postmenopausal osteoporosis treatment and prevention, and for breast cancer risk reduction in postmenopausal women at high risk. The MORE and STAR trials established the breast cancer prevention activity. Adverse events include thromboembolism (similar to tamoxifen), hot flashes, and leg cramps. Used as the canonical second-generation SERM with bone-selective profile.
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