Effect of selective estrogen receptor modulators on metabolic homeostasis

Beibei Xu, Dragana Lovre, Franck Mauvais-Jarvis

Research output: Contribution to journalReview articlepeer-review

22 Scopus citations

Abstract

Selective estrogen receptor modulators (SERMs) are estrogen receptor (ER) ligands that exhibit either estrogen agonistic or antagonistic activity in a tissue-specific manner. The first and second generation SERMs, tamoxifen and raloxifene, are used for treatment of ER positive breast cancer and postmenopausal osteoporosis respectively. The third-generation SERM, bazedoxifene (BZA), effectively prevents osteoporosis while blocking the estrogenic stimulation in breast and uterus. Notably, BZA combined with conjugated estrogens (CE) in a tissue-selective estrogen complex (TSEC) is a new menopausal treatment. Postmenopausal estrogen deficiency predisposes to metabolic syndrome and type 2 diabetes, and therefore the effects of SERMs and TSECs on metabolic homeostasis are gaining attention. In this article, we summarize current knowledge about the impact of SERMs on metabolic homeostasis and metabolic disorders in animal models and postmenopausal women.

Original languageEnglish (US)
Pages (from-to)92-97
Number of pages6
JournalBiochimie
Volume124
DOIs
StatePublished - May 1 2016

Keywords

  • Bazedoxifene
  • Diabetes
  • Energy metabolism
  • Metabolic syndrome
  • Selective estrogen receptor modulators
  • Tissue-selective estrogen complex

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