The effect of selective estrogen receptor modulators on type 2 diabetes onset in women: Basic and clinical insights

Beibei Xu1, Dragana Lovre1, Franck Mauvais-Jarvis1

  • 1Department of Medicine, Division of Endocrinology and Metabolism, Tulane University Health Sciences Center, School of Medicine, New Orleans, LA, USA.

Insights

Selective estrogen receptor modulators (SERMs) impact metabolic homeostasis, obesity, and diabetes. This review explores their effects in rodent models and postmenopausal women, highlighting therapeutic potential.

Area of Science:

  • Endocrinology
  • Pharmacology
  • Metabolic Research

Background:

  • Selective estrogen receptor modulators (SERMs) exhibit tissue-specific estrogen receptor (ER) agonist/antagonist activities.
  • First-generation SERMs (e.g., Tamoxifen) treat ER-positive breast cancer; second-generation (e.g., Raloxifene) prevent osteoporosis.
  • Third-generation SERMs, like bazedoxifene (BZA), prevent osteoporosis with reduced estrogenic effects on breast and uterus, and BZA with conjugated estrogens (CE) is a novel menopausal treatment.

Purpose of the Study:

  • To summarize current knowledge on the effects of SERMs on metabolic homeostasis, obesity, and diabetes.
  • To review findings from both rodent models and postmenopausal women.
  • To highlight the growing interest in SERMs for managing metabolic disturbances associated with menopause.

Main Methods:

  • Literature review and synthesis of existing research.
  • Analysis of studies involving rodent models investigating SERM effects on metabolism.
  • Examination of clinical data from postmenopausal women assessing SERM impacts on metabolic parameters.

Main Results:

  • SERMs demonstrate varied effects on metabolic homeostasis, influencing parameters like glucose metabolism, lipid profiles, and body weight.
  • Rodent models show potential for SERMs in mitigating metabolic syndrome and type 2 diabetes.
  • Clinical studies in postmenopausal women suggest SERMs may favorably impact metabolic health, though effects can be complex and context-dependent.

Conclusions:

  • SERMs, particularly newer generations, show promise in addressing metabolic dysregulation associated with menopause.
  • Further research is warranted to fully elucidate the mechanisms and clinical utility of SERMs in metabolic disease prevention and treatment.
  • The tissue-specific actions of SERMs offer a potential therapeutic avenue for managing menopausal symptoms and associated metabolic comorbidities.

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