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Afimoxifene

Chemical compound

Summary

Chemical compound

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Afimoxifene, also known as 4-hydroxytamoxifen (4-OHT) and by its tentative brand name TamoGel, is a selective estrogen receptor modulator (SERM) of the triphenylethylene group and an active metabolite of tamoxifen. The drug is under development under the tentative brand name TamoGel as a topical gel for the treatment of hyperplasia of the breast. It has completed a phase II clinical trial for cyclical mastalgia, but further studies are required before afimoxifene can be approved for this indication and marketed.

Afimoxifene is a SERM and hence acts as a tissue-selective agonist–antagonist of the estrogen receptors ERα and ERβ with mixed estrogenic and antiestrogenic activity depending on the tissue. It is also an agonist of the G protein-coupled estrogen receptor (GPER) with relatively low affinity (100–1,000 nM, relative to 3–6 nM for estradiol). In addition to its estrogenic and antiestrogenic activity, afimoxifene has been found to act as an antagonist of the estrogen-related receptors (ERRs) ERRβ and ERRγ.

References

References

  1. "Afimoxifene - BHR Pharma". Springer Nature Switzerland AG.
  2. (September 2004). "Comprehensive evaluation of tamoxifen sequential biotransformation by the human cytochrome P450 system in vitro: prominent roles for CYP3A and CYP2D6". The Journal of Pharmacology and Experimental Therapeutics.
  3. "Statement on a nonproprietary name adopted by the USAN council: Afimoxifene". American Medical Association.
  4. (16 November 2016). "Management of Breast Diseases". Springer.
  5. (December 2007). "A phase II trial of Afimoxifene (4-hydroxytamoxifen gel) for cyclical mastalgia in premenopausal women". Breast Cancer Research and Treatment.
  6. (July 2015). "International Union of Basic and Clinical Pharmacology. XCVII. G Protein-Coupled Estrogen Receptor and Its Pharmacologic Modulators". Pharmacological Reviews.
  7. (3 October 2011). "Hormones and Cancer: Breast and Prostate, An Issue of Endocrinology and Metabolism Clinics of North America". Elsevier Health Sciences.
  8. (23 May 2014). "Endocrine Disruptors in the Environment". Wiley.
  9. (2006). "Estrogen-related receptors as emerging targets in cancer and metabolic disorders". Current Topics in Medicinal Chemistry.
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This article was imported from Wikipedia and is available under the Creative Commons Attribution-ShareAlike 4.0 License. Content has been adapted to SurfDoc format. Original contributors can be found on the article history page.

dimethylamino-compounds experimental-cancer-drugs experimental-sex-hormone-agents gper-agonists human-drug-metabolites 2-phenoxyethanamines 4-hydroxyphenyl-compounds selective-estrogen-receptor-modulators triphenylethylenes ethanolamines
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