Afimoxifene

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Afimoxifene
Afimoxifene2DACS.svg
Identifiers
CAS number 68392-35-8 YesY
PubChem 449459
ChemSpider 395987 YesY
KEGG D06551 YesY
ChEMBL CHEMBL489 YesY
Jmol-3D images Image 1
Image 2
Properties
Molecular formula C26H29NO2
Molar mass 387.51396
Except where noted otherwise, data are given for materials in their standard state (at 25 °C (77 °F), 100 kPa)
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Infobox references

Afimoxifene[1] (4-hydroxytamoxifen) is a selective estrogen receptor modulator which is the active metabolite of tamoxifen.[2] Afimoxifene is a transdermal gel formulation and is being 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]

References[edit]

  1. ^ a b "Statement on a nonproprietary name adopted by the USAN council: Afimoxifene". 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[edit]