Ospemifene

Hormonal / PCT

Also known as: Osphena, FC-1271a, Deaminohydroxy Toremifene

Selective Estrogen Receptor ModulatorsResearch phase: FDA-approvedRegulatory: FDA-approved for moderate to severe dyspareunia due to vulvovaginal atrophy (2013). Available by prescription as Osphena.

Mechanism

Ospemifene is a SERM FDA-approved specifically for dyspareunia (painful intercourse) due to vulvovaginal atrophy in postmenopausal women. It acts as an estrogen agonist in vaginal tissue, restoring mucosal thickness and lubrication, while maintaining anti-estrogenic effects in breast and uterine tissue.

Technical detail

Ospemifene is a deaminated metabolite derivative of toremifene that acts as a tissue-selective ER agonist in vaginal epithelium, promoting mucosal maturation, increasing superficial cells, and reducing parabasal cells and vaginal pH. It demonstrates ER antagonism in breast tissue and minimal uterotrophic activity. Phase 3 trials demonstrated significant improvements in vaginal dryness, dyspareunia severity, and vaginal maturation index versus placebo. It is the first non-estrogen oral therapy approved for vulvovaginal atrophy.

Evidence

Efficacy and safety of ospemifene in postmenopausal women with moderate-to-severe vaginal dryness: a phase 3, randomized, double-blind, placebo-controlled, multicenter trial
Archer et al. (2019) — Menopause — PMID: 30694917
In 631 postmenopausal women with vulvovaginal atrophy and moderate-to-severe vaginal dryness, oral ospemifene 60 mg daily significantly improved vaginal cytology, pH, dryness severity, dyspareunia, and sexual-function measures versus placebo over 12 weeks, with no unexpected serious treatment-related adverse events or endometrial hyperplasia/carcinoma observed.
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