Drug intelligence / Profile preview

ospemifene + prasterone

Development stage
Preclinical
Lead developer
Shionogi
Modality
Small Molecules
Administration
Oral, Intravaginal
01

Overview

**Ospemifene + prasterone** is a hypothetical or investigational combination therapy for menopausal genitourinary syndrome, particularly moderate to severe dyspareunia and vaginal atrophy.\n- **Ospemifene** is a selective estrogen receptor modulator (SERM) with estrogen agonist/antagonist activity, acting primarily through estrogen receptors. It is orally administered and indicated for moderate to severe dyspareunia associated with vulvar and vaginal atrophy in postmenopausal women[3].\n- **Prasterone** (dehydroepiandrosterone, DHEA) is an intravaginal steroid hormone precursor that exerts its therapeutic effect locally by acting as an endogenous source of estrogens and androgens in vaginal tissue, thus improving the symptoms of genitourinary syndrome of menopause[5][6].\nBoth are independently approved agents for treating vulvovaginal atrophy and dyspareunia but are not currently marketed together as a fixed-dose combination product. There is no evidence of a combination product with both active substances approved or marketed as of the current date.

02

Targets

AR (Adrenergic receptors)ESR1 (ERα)ESR2 (ERβ)

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