Drug intelligence / Profile preview

ospemifene

Development stage
Approved
Lead developer
Shionogi
Modality
Small Molecules
Administration
Oral
01

Overview

Ospemifene is a selective estrogen receptor modulator (SERM) that acts as an estrogen agonist/antagonist with tissue selective effects. It is primarily used to treat moderate to severe dyspareunia (painful sexual intercourse) and vaginal dryness caused by menopause. Ospemifene works by making vaginal tissue thicker and less fragile, which reduces pain during sexual intercourse. It has estrogen agonistic effects in the endometrium but shows anti-estrogenic activity in breast cancer cells. Unlike some other SERMs, ospemifene might not have an adverse influence on coagulation. The FDA approved ospemifene on February 26, 2013, and the European Commission approved it for marketing in the EU in January 2015.

Brand names
OsphenaSenshio
Other names
Ophenaospemifenodeaminohydroxytamoxifen
02

Targets

ESR1 (ERα)ESR2 (ERβ)

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