From WikiMD's Food, Medicine & Wellness Encyclopedia
Afimoxifene
Afimoxifene, also known as 4-hydroxytamoxifen, is a selective estrogen receptor modulator (SERM) that is recognized as the active metabolite of the well-known drug, tamoxifen. Unlike tamoxifen, which is typically administered orally, afimoxifene is formulated as a transdermal gel.
Ascend Therapeutics, Inc. is the company behind the development of afimoxifene, marketing it under the trademark name TamoGel. This transdermal gel formulation provides a unique method of delivery, which may offer advantages over traditional oral administration.
Afimoxifene has undergone several clinical trials to evaluate its efficacy and safety:
Phase II Clinical Trial: A significant phase II clinical trial was conducted focusing on the potential use of afimoxifene for the treatment of cyclical mastalgia, a condition characterized by breast pain related to menstrual cycles.
Comparative Study with Tamoxifen: A noteworthy study carried out in France included 55 women and indicated that the topical application of afimoxifene directly to the skin was as effective as orally-administered tamoxifen tablets in decelerating the growth of breast cancer. The advantages of such topical application include a significant reduction in systemic levels (by a factor of nine), which can potentially minimize the undesired side effects commonly associated with tamoxifen. A subsequent trial in the US is set to compare the outcomes of 6 weeks of afimoxifene use prior to undergoing breast cancer surgery.
One of the primary anticipated benefits of afimoxifene's topical application is a marked decrease in the systemic exposure to the drug. This could lead to a significant reduction in the side effects generally seen with tamoxifen, making the treatment more tolerable for patients.
