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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]


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