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Clinical data
Trade namesTamoGel
Other names4-Hydroxytamoxifen; 4-OHT; 4-HT; OHTAM
Routes of
Topical (gel)
CAS Number
PubChem CID
CompTox Dashboard (EPA)
ECHA InfoCard100.163.120 Edit this at Wikidata
Chemical and physical data
Molar mass387.523 g·mol−1
3D model (JSmol)

Afimoxifene is a selective estrogen receptor modulator (SERM) of the triphenylethylene group and the major 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.[1][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.[4]

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]

See also[edit]


  1. ^ a b
  2. ^ Desta Z, Ward BA, Soukhova NV, Flockhart DA (2004). "Comprehensive evaluation of tamoxifen sequential biotransformation by the human cytochrome P450 system in vitro: prominent roles for CYP3A and CYP2D6". J Pharmacol Exp Ther. 310 (3): 1062–1075. doi:10.1124/jpet.104.065607. PMID 15159443.
  3. ^ "Statement on a nonproprietary name adopted by the USAN council: Afimoxifene" (PDF). American Medical Association. Retrieved 2008-03-26.
  4. ^ a b Ismail Jatoi; Achim Rody (16 November 2016). Management of Breast Diseases. Springer. pp. 77–. ISBN 978-3-319-46356-8.
  5. ^ Mansel R, Goyal A, Nestour EL, Masini-Etévé V, O'Connell K (2007). "A phase II trial of Afimoxifene (4-hydroxytamoxifen gel) for cyclical mastalgia in premenopausal women". Breast Cancer Res. Treat. 106 (3): 389–397. doi:10.1007/s10549-007-9507-x. PMID 17351746.
  6. ^ Prossnitz ER, Arterburn JB (July 2015). "International Union of Basic and Clinical Pharmacology. XCVII. G Protein-Coupled Estrogen Receptor and Its Pharmacologic Modulators". Pharmacol. Rev. 67 (3): 505–40. doi:10.1124/pr.114.009712. PMC 4485017. PMID 26023144.
  7. ^ Alice C. Levine (3 October 2011). Hormones and Cancer: Breast and Prostate, An Issue of Endocrinology and Metabolism Clinics of North America. Elsevier Health Sciences. pp. 271–. ISBN 978-1-4557-1239-7.
  8. ^ Sushil K. Khetan (23 May 2014). Endocrine Disruptors in the Environment. Wiley. pp. 104–. ISBN 978-1-118-89115-5.

External links[edit]