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. 2021 Mar 13;11(3):201. doi: 10.3390/jpm11030201

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© 2021 by the authors.

Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/).

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Overview of tamoxifen metabolites formed during first phase hepatic metabolism. Only isomers of 4OHtam and endoxifen are shown, other metabolites may also be subject to isomerism. Blue, red, orange, and green lines represent hydroxylation, demethylation, N-oxidation and non-enzymatic isomerization, respectively. Numbered arrows represent the following CYP450 enzymes involved in generation of active metabolites and their less active isomers: (1) CYP3A4/5, CYP1A1/2, CYP2C9/19, CYP2D6 (2) Unknown (3) CYP2D6 (4) CYP3A4/5, CYP2C19, CYP2D6. (5) CYP2C9/19, CYP2D6, CYP3A4, CYP2B6 (6) CYP2B6, CYP2D6. Modified from [28].