Ospemifene

Ospemifene (brand names Osphena and Senshio produced by Shionogi) is an oral medication indicated for the treatment of dyspareunia – pain during sexual intercourse – encountered by some women, more often in those who are post-menopausal. Ospemifene is a selective estrogen receptor modulator (SERM) acting similarly to an estrogen on the vaginal epithelium, building vaginal wall thickness which in turn reduces the pain associated with dyspareunia. Dyspareunia is most commonly caused by vulvovaginal atrophy.

The medication was approved by the US Food and Drug Administration in February 2013, and by the European Medicines Agency for marketing in the European Union in January 2015.

In the US, ospemifene is indicated for the treatment of moderate to severe dyspareunia, a symptom of vulvovaginal atrophy, due to menopause; or the treatment of moderate to severe vaginal dryness, a symptom of vulvar and vaginal atrophy, due to menopause.

In the EU, ospemifene is indicated for the treatment of moderate to severe symptomatic vulvar and vaginal atrophy in post-menopausal women.

Women with "undiagnosed abnormal genital bleeding; known or suspected estrogen-dependent neoplasia; active or history of deep vein thrombosis; pulmonary embolism; arterial thromboembolic disease; and are or may become pregnant" or "with known or suspected breast cancer or those with extreme hepatic impairment" should not take ospemifene.

Side effects associated with ospemifene include vaginal discharge, hot flashes, and diaphoresis. More serious adverse effects are similar to those of estrogens and estrogen receptor modulators. These include, but are not limited to, thromboembolism, allergic reactions, fatigue, and headache, and others could occur.

Ospemifene is a selective estrogen receptor modulator. As such, many of the effects produced by estrogens are produced by ospemifene. The boxed warning of the medication indicates ospemifene may thicken the endometrium, which could lead to unusual bleeding and endometrial cancer. For women taking estrogens, concurrently taking a type of drug called a progestin has been shown to decrease the occurrence of endometrial hyperplasia. In theory, progestins may be expected to attenuate ospemifene's effects on endometrial thickening. However clinical trials confirming this have not been conducted. Like estrogens, ospemifene also may increase the risk for cardiovascular events, including "stroke, coronary heart disease, venous thromboembolism," and others.

Ospemifene is "an estrogen agonist/antagonist that makes vaginal tissue thicker and less fragile resulting in a reduction in the amount of pain women experience with sexual intercourse." This medication should be used for the shortest amount of time possible due to associated adverse effects. Ospemifene might not have an adverse influence on coagulation, in contrast to estrogens and other SERMs like tamoxifen and raloxifene.