n-desmethyltamoxifen

N-desmethyltamoxifen is a major metabolite of the selective estrogen receptor modulator (SERM) tamoxifen. It is formed in the liver primarily by cytochrome P450 enzymes CYP3A4 and CYP3A5. While it has anti-estrogenic activity by blocking estrogen binding to estrogen receptors, it is further metabolized to endoxifen, which is considered the major active form of tamoxifen. Beyond its anti-estrogenic properties, n-desmethyltamoxifen also acts as a potent inhibitor of protein kinase C (PKC) and plays a role in regulating ceramide metabolism, limiting ceramide glycosylation, hydrolysis, and sphingosine phosphorylation. It has demonstrated inhibitory effects on the growth of various cancer cell lines, including glioma and mammary carcinoma cells, in in vitro studies.

Other names

NortamoxifenNDMTAMdemethyltamoxifenDesmethyltamoxifen, n-ICI-55548ICI55548ICI 55548ICI 55,5482-[4-[(Z)-1,2-diphenylbut-1-enyl]phenoxy]-N-methylethanamine