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.

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