TY - JOUR
T1 - Selective estrogen receptor modulators
T2 - From bench to bedside and back
AU - Whitaker, Michael D.
PY - 2001
Y1 - 2001
N2 - 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.
AB - 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.
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U2 - 10.4158/ep.7.2.113
DO - 10.4158/ep.7.2.113
M3 - Review article
C2 - 11421557
AN - SCOPUS:0035712265
SN - 1530-891X
VL - 7
SP - 113
EP - 119
JO - Endocrine Practice
JF - Endocrine Practice
IS - 2
ER -