afimoxifene

Afimoxifene is a selective estrogen receptor modulator (SERM) of the triphenylethylene group and an active metabolite of tamoxifen. It exhibits both estrogenic and anti-estrogenic effects, with a higher affinity for the estrogen receptor than tamoxifen itself. Afimoxifene acts as an antagonist in breast cancer cells by binding to estrogen receptors (ERα and ERβ), inducing conformational changes that block or alter the expression of estrogen-dependent genes. It also functions as an agonist at the G protein-coupled estrogen receptor (GPER) with relatively low affinity, and as an antagonist at the estrogen-related receptors ERRβ and ERRγ. The drug is primarily under development as a topical gel formulation for conditions such as cyclical mastalgia, fibrocystic breast disease, gynecomastia, keloid scarring, hyperplasia of the breast, and for reducing mammographic breast density to lower breast cancer risk[1][2][3][5][6][7].

Brand names

TamoGel

Other names

4-hydroxytamoxifen4-OH tamoxifen4-OHT