Selective estrogen receptor modulators

From bench to bedside and back

Michael D. Whitaker

Research output: Contribution to journalArticle

3 Citations (Scopus)

Abstract

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.

Original languageEnglish (US)
Pages (from-to)113-119
Number of pages7
JournalEndocrine Practice
Volume7
Issue number2
StatePublished - 2001

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Selective Estrogen Receptor Modulators
Estrogens
Breast
Menopause
Embolism
Venous Thrombosis
Estrogen Receptors
Bone Density
Central Nervous System
History

ASJC Scopus subject areas

  • Endocrinology

Cite this

Selective estrogen receptor modulators : From bench to bedside and back. / Whitaker, Michael D.

In: Endocrine Practice, Vol. 7, No. 2, 2001, p. 113-119.

Research output: Contribution to journalArticle

Whitaker, Michael D. / Selective estrogen receptor modulators : From bench to bedside and back. In: Endocrine Practice. 2001 ; Vol. 7, No. 2. pp. 113-119.
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