Clomiphene citrate

Clomiphene is a nonsteroidal triphenylethylene derivative. It acts as a selective estrogen receptor modulator (SERM), that impairs the activation of estrogen receptors (ERs) by 17beta-estradiol, similar to tamoxifen and raloxifene. It potently binds both ERalpha and ERbeta (Ki = 0.9 and 1.2nM, respectively). Clomiphene enhances the release of gonadotropin-releasing hormone, stimulating the release of follicle-stimulating hormone and luteinizing hormone, culminating in ovulation. Triphenylethylene antiestrogens may also be used as antileukemic drugs which kill cells by apoptosis mediated by oxidative stress and activation of PKC.