Details of the Metabolic Reaction (MR)

General Information of This Metabolic Reaction (MR) (ID: MR003516)
Formula
SVG example
4-Hydroxylation
Reactant N-Desmethyltamoxifen Product Endoxifen
Reactant Info Product Info
Metabolic Enzyme Cytochrome P450 2D6 (CYP2D6) DME Info
Metabolic Type Oxidation - 4-Hydroxylation
Other MR(s) Related to The Reactant of This MR
Other MR(s) That Produce The Reactant of This MR
MR ID Reactant Product MR Type Related Drug REF
MR003510 Tamoxifen citrate N-Desmethyltamoxifen Oxidation - N-Dealkylation Tamoxifen citrate [1], [2], [3], [4], [5]
Other MR(s) That Metabolize The Reactant of This MR
MR ID Reactant Product MR Type Related Drug REF
MR003511 N-Desmethyltamoxifen N,N-didesmethyltamoxifen Unclear Tamoxifen citrate [6]
MR003521 N-Desmethyltamoxifen N-desmethyltamoxifen sulfate Conjugation - Sulfation Tamoxifen citrate [6]
Other MR(s) Related to The Product of This MR
Other MR(s) That Produce The Product of This MR
MR ID Reactant Product MR Type Related Drug REF
MR005295 Cis-4-hydroxytamoxifen Endoxifen Oxidation - N-demethylation Cis-4-hydroxytamoxifen [7]
MR003530 4-hydroxytamoxifen Endoxifen Conjugation - Sulfation Tamoxifen citrate [6]
MR003529 4-hydroxytamoxifen sulfate Endoxifen Conjugation - Sulfation Tamoxifen citrate [6]
References
1 Metabolism of tamoxifen by recombinant human cytochrome P450 enzymes: formation of the 4-hydroxy, 4'-hydroxy and N-desmethyl metabolites and isomerization of trans-4-hydroxytamoxifen. Drug Metab Dispos. 2002 Aug;30(8):869-74.
2 Endoxifen and other metabolites of tamoxifen inhibit human hydroxysteroid sulfotransferase 2A1 (hSULT2A1). Drug Metab Dispos. 2014 Nov;42(11):1843-50.
3 Metabolism and transport of tamoxifen in relation to its effectiveness: new perspectives on an ongoing controversy. Future Oncol. 2014 Jan;10(1):107-22.
4 Identification and biological activity of tamoxifen metabolites in human serum Biochem Pharmacol. 1983 Jul 1;32(13):2045-52. doi: 10.1016/0006-2952(83)90425-2.
5 PharmGKB summary: tamoxifen pathway, pharmacokinetics Pharmacogenet Genomics. 2013 Nov;23(11):643-7. doi: 10.1097/FPC.0b013e3283656bc1.
6 PharmGKB:Tamoxifen citrate
7 Tamoxifen dose and serum concentrations of tamoxifen and six of its metabolites in routine clinical outpatient care

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