The evolving role of specific estrogen receptor modulators (SERMs)

Estrogens are the most effective therapy for women with postmenopausal prob lems. However, relatively few women use estrogen and then often for a limit ed time because of the fear of its carcinogenic effects on the uterus and b reast; in addition, estrogen is not advised for women who have had breast c ancer. Selective estrogen receptor modulators (SERMs) are agents with antag onist action on the uterus and breast and agonist action on the bones, card iovascular system, and brain. Unlike estrogens, however, existing SERMs do not help alleviate the vasomotor and urogenital problems associated with me nopause. A comprehensive review of the literature published from January 19 95 to June 1999 was conducted. Reports were identified using Medline and Ca ncer Lit. The effect of menopausal problems on the health of women and the socioeconomic effects of menopause are discussed. All currently available a nd investigational SERMs are reviewed and discussed, including their mechan ism of action, metabolism, dose scheduling, antitumor activity, and potenti al role in maintaining the health of menopausal women and in preventing bre ast cancer. (C) 2000 Elsevier Science Ltd. All rights reserved.