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Figure 1. Metabolic pathways of tamoxifen. The size of the arrow indicates the magnitude of the reaction. The most utilized pathway involves conversion of tamoxifen to N-desmethyltamoxifen by CYP3A. N-desmethylTAM is then converted to the most active antiestrogenic molecule, endoxifen, by CYP2D6. Adapted from Jin et al.3
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