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Nuclear receptors, or NRs, are unique transcription factors that regulate gene transcription and affect the cellular pathways involved in reproduction, development, or metabolism. Their ability to be stimulated by small lipophilic ligands and control vital cellular processes makes them ideal drug targets. Nearly 10-15% of currently prescribed drugs target these receptors.
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Selective estrogen receptor modulators and bone health.

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  • 1New York University Grossman School of Medicine, New York, NY, USA.

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PubMed
Summary

Selective estrogen receptor modulators (SERMs) impact bone and breast tissues differently depending on the specific drug. While some SERMs show consistent effects, others vary by tissue, requiring careful patient consideration.

Keywords:
Selective estrogen receptor modulatorsbone densityeffects on bonefracture

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Area of Science:

  • Endocrinology
  • Pharmacology
  • Oncology

Background:

  • Selective estrogen receptor modulators (SERMs) are synthetic compounds targeting the estrogen receptor.
  • SERMs exhibit tissue-specific estrogen agonistic or antagonistic properties.

Purpose of the Study:

  • To review the preclinical and clinical effects of various SERMs on bone health.
  • To discuss the diverse actions of SERMs in different tissues.

Main Methods:

  • Literature review of preclinical and clinical studies on SERMs.
  • Analysis of data on tamoxifen, raloxifene, bazedoxifene, and ospemifene.
  • Comparison of SERM activity across bone, breast, uterus, and vagina.

Main Results:

  • SERMs demonstrate consistent effects on bone and breast tissues, acting as estrogen agonists/antagonists.
  • Clinical trial data supporting SERM efficacy varies significantly.
  • SERMs do not exhibit uniform activity in tissues such as the uterus and vagina.

Conclusions:

  • SERMs represent a diverse class of drugs with notable effects on bone and breast.
  • Healthcare providers must consider variable clinical data and tissue-specific actions for informed patient decision-making.
  • Shared decision-making is crucial for optimizing SERM therapy based on individual patient needs and potential outcomes.