IUPAC name
Other names
68392-35-8 N
3D model (Jmol) Interactive image
Interactive image
ChemSpider 395987 YesY
ECHA InfoCard 100.155.464
KEGG D06551 YesY
PubChem 449459
UNII 17197F0KYM YesY
Molar mass 387.51396
Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa).
N verify (what is YesYN ?)
Infobox references

Afimoxifene,[1] also known as 4-hydroxytamoxifen (4-OHT, 4-HT, OHTAM, others), is a selective estrogen receptor modulator and the active metabolite of tamoxifen.[2]

Afimoxifene is the active ingredient in a transdermal gel formulation developed by Ascend Therapeutics, Inc. under the trademark TamoGel.[1]

Afimoxifene has completed a phase II clinical trial for the treatment of cyclical mastalgia.[3]

A study in France on 55 women showed that rubbing afimoxifene on the skin was as good as tamoxifen tablets at slowing breast cancer growth. A US trial will compare 6 weeks use before breast cancer surgery. Skin application can reduce systemic levels by a factor of nine and this is expected to reduce the unpleasant side-effects of tamoxifen.[4]


  1. 1 2 "Statement on a nonproprietary name adopted by the USAN council: Afimoxifene" (PDF). American Medical Association. Retrieved 2008-03-26.
  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. 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.
  4. Hagan, Pat (6 Aug 2011). "Breast cancer gel shrinks tumours". Daily Mail. London.

External links

This article is issued from Wikipedia - version of the 10/19/2016. The text is available under the Creative Commons Attribution/Share Alike but additional terms may apply for the media files.