Afimoxifene
| Afimoxifene | |
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(Z)-4-(1-(4-(2-(dimethylamino)ethoxy)phenyl)-2-phenylbut-1-enyl)phenol |
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Other names
4-hydroxytamoxifen |
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| Identifiers | |
| CAS number | 68392-35-8  |
| PubChem | 449459 |
| ChemSpider | 395987 |
| KEGG | D06551 |
| ChEMBL | CHEMBL489 |
| Jmol-3D images | Image 1 Image 2 |
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| Properties | |
| Molecular formula | C26H29NO2 |
| Molar mass | 387.51396 |
 (verify) (what is:  / ?)Except where noted otherwise, data are given for materials in their standard state (at 25 °C, 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]
[edit] References
- ^ a b "Statement on a nonproprietary name adopted by the USAN council: Afimoxifene". American Medical Association. http://www.ama-assn.org/ama1/pub/upload/mm/365/afimoxifene.pdf. Retrieved 2008-03-26.
- ^ 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.
- ^ 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.
- ^ Hagan, Pat (6 Aug 2011). "Breast cancer gel shrinks tumours". Daily Mail (London). http://www.dailymail.co.uk/health/article-2023007/Breast-cancer-gel-shrinks-tumours--tablets-unpleasant-effects.html.
[edit] External links
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