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  • 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.
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