Selective estrogen receptor modulators (SERMs) in clinical practice

The objective of this literature review is to familiarize the reader with t he clinical data on selective estrogen receptor modulators (SERMs) and anti estrogens currently in use in the US, excluding data on breast effects. Fou r compounds in the SERM and antiestrogen families are presently in clinical use in the US: clomiphene (CC), tamoxifen (TAM), toremifene (TOR), and ral oxifene (RLX). The clinical database on these compounds is among the larges t available. Each compound demonstrates a specific profile for its target t issue effects, and this may differ between premenopausal and postmenopausal women. CC is the most widely used agent for ovulation induction. TAM is in dicated in the management of breast cancer and for prevention in women at h igh risk. TAM may have additional effects on the cardiovascular and skeleta l systems. TOR also is used for its effects on breast tissue and may have p ositive cardiovascular effects. RLX is approved in the management of osteop orosis with data supporting favorable effects on the cardiovascular system and breast tissue. TAM and TOR appear to have stimulatory effects on the ut erus and endometrium, whereas RLX is neutral. Few adverse events have been attributed to these agents, with hot flashes being the most common one. The re appears to be an increased risk of thromboembolic events with continuous use of TAM, TOR, and RLX. SERMs and antiestrogens continue to be studied e xtensively. Their evolving profiles support key roles for these agents in m odern day medicine, particularly in the management of postmenopausal women' s health. (J Soc Gynecol Investig 2000;7:S38-46) Copyright (C) 2000 by the Society for Gynecologic Investigation.