Pharmacologic evaluation of ospemifene.

IMPORTANCE OF THE FIELD: Millions of women worldwide suffer from vulvovaginal atrophy (VVA) associated with menopause, and many women report that this adversely affects their quality of life. Ospemifene is a non-hormonal estrogen receptor agonist/antagonist effective in the treatment of VVA. Although similar in structure to other estrogen receptor agonists/antagonists that have antagonistic effects on the vagina, ospemifene has an estrogen-like effect on vaginal epithelium. This review focuses on ospemifene including its pharmacologic properties, clinical efficacy and safety. AREAS COVERED IN THIS REVIEW: The paper provides information on the phamacodynamic and pharmacokinetic properties of ospemifene. It also contains an overview of its preclinical and clinical efficacy as well as its clinical safety. WHAT THE READER WILL GAIN: From this paper, the reader will gain an appreciation for a new non-hormonal estrogen receptor agonist/antagonist, ospemifene. TAKE HOME MESSAGE: The pharmacologic properties of ospemifene make it a logical candidate for the treatment of women with moderate to severe symptoms of VVA associated with menopause. Clinical trials have confirmed that daily doses are well-tolerated and that it is effective in normalizing vaginal maturation index and pH as well as improving the symptoms associated with VVA including dyspareunia.