The evolving role of specific estrogen receptor modulators (SERMs)

Estrogens are the most effective therapy for women with postmenopausal problems. However, relatively few women use estrogen and then often for a limited time because of the fear of its carcinogenic effects on the uterus and breast; in addition, estrogen is not advised for women who have had breast cancer. Selective estrogen receptor modulators (SERMs) are agents with antagonist action on the uterus and breast and agonist action on the bones, cardiovascular system, and brain. Unlike estrogens, however, existing SERMs do not help alleviate the vasomotor and urogenital problems associated with menopause. A comprehensive review of the literature published from January 1995 to June 1999 was conducted. Reports were identified using Medline and Cancer Lit. The effect of menopausal problems on the health of women and the socioeconomic effects of menopause are discussed. All currently available and investigational SERMs are reviewed and discussed, including their mechanism of action, metabolism, dose scheduling, antitumor activity, and potential role in maintaining the health of menopausal women and in preventing breast cancer. (C) 2000 Elsevier Science Ltd. All rights reserved.