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Ospemifene is a non-hormonal selective estrogen receptor modulator (SERM).1 It binds to estrogen receptor α (ERα) and ERβ (Kis = 380 and 410 nM, respectively). It increases vaginal weight and vaginal epithelial height (ED50s = 0.48 and 0.39 mg/kg per day, respectively) in an ovariectomized rat model of menopause. Ospemifene also increases progesterone receptor protein expression in vaginal epithelium and stroma and inhibits estrogen response element-mediated transactivation induced by 17β-estradiol (Item No. 10006315) in a reporter assay using MCF-7 cells. Formulations containing ospemifene have been used in the treatment of vulvar and vaginal atrophy-induced dyspareunia.
WARNING This product is not for human or veterinary use.
1. Vaginal effects of ospemifene in the ovariectomized rat preclinical model of menopause. J. Steroid Biochem. Mol. Biol. 138, 107-115 (2013).