Abstract
Selective estrogen receptor modulators (SERMs) are a class of compounds that bind to estrogen receptors, producing varying degrees of estrogen agonist effects in some domains (bone and lipids) and estrogen antagonist effects in others (breast and uterus).1 Tamoxifen was the first clinically used compound recognized to have a partial estrogen agonist/antagonist profile. Some2,3 but not all4 clinical trials of tamoxifen as adjuvant therapy for breast cancer have also found significant reductions in cardiovascular events among women assigned to tamoxifen treatment. This observation has led to speculation that tamoxifen or another SERM might be a reasonable alternative to conventional estrogen replacement for postmenopausal women. Raloxifene, a benzothiophene derivative of tamoxifen, was the first compound other than tamoxifen to be identified as a SERM because it prevented bone loss due to estrogen deprivation but did not cause endometrial hyperplasia in rats.5 It is currently approved only to treat osteoporosis, but there is great interest in determining whether it may benefit the cardiovascular system as well. Droloxifene, a compound structurally similar to tamoxifen, appears to share some of its beneficial effects6,7 but remains an investigational agent and has not been as thoroughly studied as the other two compounds. The cardiovascular effects of other SERMs, such as idoxifene and toremifene, have not been studied in detail. A discussion of other compounds that may have partial estrogen agonist/antagonist effects, such as soy phytoestrogens or tibolone, is beyond the scope of this brief review. We will focus on three areas known to be important indicators of cardiovascular health: lipids and lipoproteins, hemostatic factors, and markers of endothelial function. © 2001 by the Jacobs Institute of Women’s Health Published by Elsevier Science Inc. 1049-3867/01/$20.00 PII S1049-3867(01)00075-5
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