pipendoxifene

Pipendoxifene is a nonsteroidal selective estrogen receptor modulator (SERM) of the 2-phenylindole class with potential antineoplastic activity. It was developed as an investigational treatment for breast cancer, particularly metastatic and tamoxifen-resistant forms. Pipendoxifene antagonizes the binding of estradiol to estrogen receptor alpha (ERα), thereby inhibiting ERα-mediated gene expression and blocking estrogen-stimulated growth in estrogen-dependent breast cancer cells. Unlike some other SERMs such as tamoxifen, pipendoxifene does not stimulate endometrial tissue in preclinical models, suggesting a potentially improved safety profile regarding endometrial hyperplasia or cancer risk. The drug reached phase II clinical trials but its development was discontinued and it was never marketed.

Other names

198480-55-6pipendoxifene [INN]