Afimoxifene Explained

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.^{[1] [2] [3]} The drug is under development under the tentative brand name TamoGel as a topical gel for the treatment of hyperplasia of the breast.^[4] It has completed a phase II clinical trial for cyclical mastalgia,^[5] 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).^[6] 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.^{[7] [8] [9]}

See also

• List of investigational sex-hormonal agents § Estrogenics
• List of selective estrogen receptor modulators

External links

• • Afimoxifene - AdisInsight

Notes and References

1. Web site: Afimoxifene - BHR Pharma . AdisInsight . Springer Nature Switzerland AG.
2. Desta Z, Ward BA, Soukhova NV, Flockhart DA . 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 . 310 . 3 . 1062–1075 . 10.1124/jpet.104.065607 . 15159443 . 21413981.
3. Web site: Statement on a nonproprietary name adopted by the USAN council: Afimoxifene . 2008-03-26 . American Medical Association.
4. Book: Management of Breast Diseases . Goyal A, Mansel RE . 16 November 2016 . Springer . 978-3-319-46356-8 . Jatoi I, Rody A . 77– . Mastalgia . https://books.google.com/books?id=f9iCDQAAQBAJ&pg=PA77.
5. Mansel R, Goyal A, Nestour EL, Masini-Etévé V, O'Connell K . December 2007 . A phase II trial of Afimoxifene (4-hydroxytamoxifen gel) for cyclical mastalgia in premenopausal women . Breast Cancer Research and Treatment . 106 . 3 . 389–397 . 10.1007/s10549-007-9507-x . 17351746 . 22382077.
6. Prossnitz ER, Arterburn JB . July 2015 . International Union of Basic and Clinical Pharmacology. XCVII. G Protein-Coupled Estrogen Receptor and Its Pharmacologic Modulators . Pharmacological Reviews . 67 . 3 . 505–540 . 10.1124/pr.114.009712 . 4485017 . 26023144.
7. Book: Hormones and Cancer: Breast and Prostate, An Issue of Endocrinology and Metabolism Clinics of North America . Levine AC . 3 October 2011 . Elsevier Health Sciences . 978-1-4557-1239-7 . 271–.
8. Book: Endocrine Disruptors in the Environment . Khetan SK . 23 May 2014 . Wiley . 978-1-118-89115-5 . 104– . Anti-Androgenic Chemicals . https://books.google.com/books?id=s2ajAwAAQBAJ&pg=PT104.
9. Ariazi EA, Jordan VC . 2006 . Estrogen-related receptors as emerging targets in cancer and metabolic disorders . Current Topics in Medicinal Chemistry . 6 . 3 . 203–215 . 10.2174/1568026610606030203 . 16515477.