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. 2017 Nov 1;8(59):100296–100311. doi: 10.18632/oncotarget.22220

Figure 1. The metabolic pathway of tamoxifen.

Figure 1

Tamoxifen is demethylated to N desmethyltamoxifen (NDM) mainly by CYP3A4/5. A relatively smaller proportion of tamoxifen is converted by CYP2D6 to 4-hydroxytamoxifen (4-OH tamoxifen). NDM is metabolized to endoxifen by CYP2D6, and 4-OH tamoxifen is metabolized to endoxifen by CYP3A4 [11]. In addition to these enzymes, various CYP enzymes (e.g., CYP1A2, CYP2C9, etc.) are involved in the metabolism of tamoxifen. Tamoxifen and its metabolites are further inactivated by UDP-glucuronosyltransferases (UGTs) and sulfotransferases (SULTs) [14, 15].