Selective estrogen receptor modulators: a controversial approach for managing postmenopausal health

Hormone replacement therapy (HRT) is considered the standard of care for managing the acute (e.g., hot flashes, vaginal dryness) and long-term (e.g., increased risk of cardiovascular disease, osteoporosis) sequelae of menopause. A group of synthetic nonsteroidal compounds, which act on the estrogen receptor, have been promoted for use as an alternative to hormonal therapy for postmenopausal women. Originally called antiestrogens because of their ability to antagonize the action of estrogen, these compounds possess both agonist and antagonist properties of estrogen action. They are now referred to as selective estrogen receptor modulators (SERMs). This article reviews the mechanism of action and the efficacy and safety data for SERMs currently used for clinical purposes. These data may indicate why the use of SERMs is a controversial alternative to HRT.