JOURNAL ARTICLE

(059) Estetrol(E4) is a Unique Estrogen With Selective Actions in Tissues Which Are Distinctly Different From the Actions of SERMs.

  • Published In: Journal of Sexual Medicine, 2023, v. 20. P. 1 1 of 3

  • Database: Academic Search Ultimate 2 of 3

  • Authored By: Foidart, J; Arnal, J; Lenfant, F; Taziaux, M; Houtman, R; Jost, M 3 of 3

Abstract

This article focuses on estetrol (E4), a unique estrogen with selective tissue actions that differ from those of selective estrogen receptor modulators (SERMs). E4 acts as a typical estrogen agonist on the endometrium and alleviates menopausal symptoms without stimulating breast proliferation or significantly affecting hepatic markers such as triglycerides and coagulation factors. Molecular studies show that E4 binds to the nuclear estrogen receptor alpha (ERα) similarly to estradiol (E2) and estriol (E3) but with much lower potency, and unlike SERMs, it does not alter ERα conformation or membrane receptor activity. These distinct properties suggest that E4 may offer a safer clinical profile, particularly regarding hepatic and coagulation effects.

Additional Information

  • Source:Journal of Sexual Medicine. 2023/06, Vol. 20, p1
  • Document Type:Article
  • Subject Area:Complementary and Alternative Medicine
  • Publication Date:2023
  • ISSN:1743-6095
  • DOI:10.1093/jsxmed/qdad068.054
  • Accession Number:171965923
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