OBJECTIVE: To provide a brief review of the history of the development of 
selective estrogen receptor modulators (SERMs), the current data assessing the 
effect of SERMs at the organ level, and the mechanism of action of these agents.
METHODS: All the pertinent medical literature was reviewed, and the effects of 
SERMs on various end-organs were summarized.
RESULTS: SERMs have been available for clinical use since the late 1960s. By the 
late 1980s, several SERMs had become available that influenced clinical 
practice. Multiorgan effects of these compounds include variable clinical 
efficacy for treatment of menopausal symptoms involving the central nervous 
system, variable effects on the genitourinary tract, and, in general, positive 
effects on serum lipid levels. SERMs seem to affect bone density positively, 
albeit to variable degrees, depending on the agent being used. The greatest 
effect of SERMs has been on the breast, and current SERMs seem to have efficacy 
for prevention of breast cancer as opposed to the controversial effect of 
estrogen on the breast. Disadvantages of SERMs include exacerbation of 
menopausal symptoms and, as with estrogen, an increased incidence of venous 
thrombosis and pulmonary emboli. SERMs act by modifying the configuration of the 
estrogen receptor. Effects at the gene transcription level seem to be tissue 
specific, a factor that likely accounts for the variability of clinical action 
seen.
CONCLUSION: SERMs are a viable option for treatment of various problems 
associated with menopause.