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Afimoxifene - Wikipedia, the free encyclopedia

Afimoxifene

From Wikipedia, the free encyclopedia

Afimoxifene
IUPAC name (Z)-4-(1-(4-(2-(dimethylamino)ethoxy)phenyl)-2-phenylbut-1-enyl)phenol
Other names 4-hydroxytamoxifen
Identifiers
CAS number [68392-35-8]
PubChem 449459
SMILES CC\C(c1ccccc1)=C(c2ccc(OCCN(C)C)cc2)/c3ccc(O)cc3
Properties
Molecular formula C26H29NO2
Molar mass 387.51396
Except where noted otherwise, data are given for
materials in their standard state
(at 25 °C, 100 kPa)

Infobox disclaimer and references

Afimoxifene[1] is a selective estrogen receptor modulator whose active ingredient is 4-hydroxytamoxifen which is identical to 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]

[edit] References

  1. ^ a b Statement on a nonproprietary name adopted by the USAN council: Afimoxifene. American Medical Association. Retrieved on 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): 1062-75. 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): 389-97. doi:10.1007/s10549-007-9507-x. PMID 17351746. 

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