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In February 2013, the FDA approved ospemifeme (Osphena 60 mg tablets, Shionogi Inc, Florham Park, NJ), an orally administered tissue-selective estrogen agonist/antagonist, for the treatment of dyspareunia caused by vulvar and vaginal atrophy (VVA) in menopausal women.1 As with its pharmacologic relatives tamoxifen and raloxifene, ospemifene acts as an estrogen agonist in some tissues and an estrogen antagonist in other tissues.
In clinical trials, ospemifene has been found to reduce pain with sexual intercourse and increase vaginal mucosal maturation and vaginal pH to a greater extent than placebo.2 Contraindications listed in package labeling for ospemifene include estrogen-dependent neoplasia and active or prior venous thromboembolism (VTE), stroke, or myocardial infarction.3 Although ospemifene has an estrogen-agonist impact on the endometrium, no cases of endometrial cancer were noted in clinical trials (the longest of which was 12 months).4 Adverse reactions most frequently reported in clinical trials were hot flushes (7.5% with ospemifene vs 2.6% with placebo), vaginal discharge (3.8% vs 0.3%, respectively), and muscle spasms (3.2% vs 0.9%, respectively).2
Women today have greater expectations regarding sexuality during their menopausal years. However, fewer menopausal women are using hormone therapy, leading to an epidemic of symptomatic VVA. Against this backdrop, new treatment options represent good news for women. Ospemifene may be of particular appeal for symptomatic women who prefer not to use estrogen vaginal cream, tablets, or the vaginal ring. However, in contrast to vaginal estrogen therapy, ospemifene increases hot flushes and may (like tamoxifen and raloxifene) increase the risk of VTE. As with vaginal estrogen, package labeling does not specifically recommend the use of progestin with ospemifene to prevent endometrial neoplasia in women with an intact uterus. However, and again, as with vaginal estrogen, endometrial monitoring should be considered in long-term users, and any vaginal bleeding occurring in users should be evaluated.
Use of vaginal or systemic estrogen is contraindicated in women with a history of breast cancer. As the package labeling indicates, “Osphena [ospemifene] 60 mg has not been adequately studied in women with breast cancer…”3 Accordingly, the FDA’s guidance is that, as with vaginal estrogen, ospemifene “…should not be used in women with known or suspected breast cancer or with a history of breast cancer.”1