Afimoxifene
 | |
| Names | |
|---|---|
| IUPAC name
(Z)-4-(1-(4-(2-(dimethylamino)ethoxy)phenyl)-2-phenylbut-1-enyl)phenol | |
| Other names
4-hydroxytamoxifen | |
| Identifiers | |
68392-35-8  | |
| ChEMBL | ChEMBL489  |
| ChemSpider | 395987 |
| Jmol interactive 3D | Image Image |
| KEGG | D06551 |
| PubChem | 449459 |
| UNII | 17197F0KYM |
| |
| |
| Properties | |
| C26H29NO2 | |
| Molar mass | 387.51396 |
| Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa). | |
| verify (what is ?) | |
| 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
- 1 2 "Statement on a nonproprietary name adopted by the USAN council: Afimoxifene" (PDF). American Medical Association. 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).
External links
- 4-hydroxytamoxifen at the US National Library of Medicine Medical Subject Headings (MeSH)
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