Vulvovaginal atrophy (VVA) and dyspareunia are common problems experienced by postmenopausal women, although few seek treatment. Symptom‐based therapies include nonhormonal vaginal lubricants, vaginal moisturizers, low‐dose vaginal estrogen, and systemic estrogen. The 2013 United States Food and Drug Administration approval of ospemifene, an estrogen agonist/antagonist for the treatment of moderate‐to‐severe dyspareunia associated with VVA, increased options available to women. Several studies have evaluated the effects of ospemifene on VVA and dyspareunia and indicate an improvement in subjective findings. Objective findings such as a decrease in pH and recovery of a premenopausal vaginal maturation index have been reported. Beneficial effects have also been demonstrated in bone. Evaluations of breast health support the safety of ospemifene, although data are limited to 1 year. Short‐term risks appear to be limited and include the development of hot flushes. Until additional comparative studies of ospemifene and estrogens have been performed, ospemifene should be recommended for women with symptoms of VVA and dyspareunia who are unable to tolerate or unwilling to take local or systemic estrogens. In this review, current evidence for the safety and efficacy of ospemifene in the treatment of moderate‐to‐severe VVA and dyspareunia are evaluated.