NCIt definition : A main metabolite of the selective estrogen receptor modulator tamoxifen with anti-estrogen
activity. N-desmethyltamoxifen blocks estrogen from binding to the estrogen receptor.
This may inhibit estrogen-associated signaling and tumor growth in estrogen-positive
tumor cells. Conversion of N-desmethyltamoxifen from tamoxifen is catalyzed by cytochrome
P-450 enzymes 3A4 and 3A5. N-desmethyltamoxifen is further hydroxylated, mainly by
CYP2D6, to endoxifen, the major clinically active metabolite of tamoxifen.;