Ospemifene is a
selective estrogen receptor modulator (
SERM), or
estrogen receptor agonist/antagonist, that was recently approved by the US Food and Drug Administration for the treatment of
dyspareunia associated with vulvar and vaginal
atrophy, a
chronic condition that affects up to 60% of postmenopausal women.
Ospemifene is the first and only nonestrogen compound approved for this indication. Compared with other approved
SERMs, such as
tamoxifen,
toremifene,
bazedoxifene, and
raloxifene, the
estrogen-like effects of
ospemifene in the vaginal epithelium are unique. This review first discusses the rationale for developing
ospemifene, including its mechanism of action, and then focuses on the clinical development of
ospemifene for the treatment of
dyspareunia associated with vulvar and vaginal
atrophy. Included are discussions of the effects of
ospemifene on the endometrium, serum
lipids, coagulation markers, bone, and
breast cancer. In conclusion,
ospemifene is a
SERM with a unique
estrogen agonist/antagonist tissue profile that was recently approved in the US for the treatment of
dyspareunia associated with vulvar and vaginal
atrophy in postmenopausal women.
Ospemifene warrants further clinical investigation for the treatment and prevention of
osteoporosis and
breast cancer.