Details of the Metabolic Reaction (MR)

General Information of This Metabolic Reaction (MR) (ID: MR003530)
Formula
CYP3A5 ...
SVG example
Sulfation
Reactant 4-hydroxytamoxifen Product Endoxifen
Reactant Info Product Info
Metabolic Enzyme Cytochrome P450 3A5 (CYP3A5) DME Info
Cytochrome P450 3A43 (CYP3A43) DME Info
Metabolic Type Conjugation - Sulfation
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
MR003526 Tamoxifen citrate 4-hydroxytamoxifen Oxidation - 4-Hydroxylation Tamoxifen citrate [1], [2], [3], [4]
Other MR(s) That Metabolize The Reactant of This MR
MR ID Reactant Product MR Type Related Drug REF
MR003528 4-hydroxytamoxifen 4-hydroxytamoxifen sulfate Conjugation - Sulfation Tamoxifen citrate [5]
MR003527 4-hydroxytamoxifen Tamoxifen glucuronides Conjugation - Glucuronidation Tamoxifen citrate [5]
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 [6]
MR003516 N-Desmethyltamoxifen Endoxifen Oxidation - 4-Hydroxylation Tamoxifen citrate [5]
MR003529 4-hydroxytamoxifen sulfate Endoxifen Conjugation - Sulfation Tamoxifen citrate [5]
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 The tamoxifen dilemma. Carcinogenesis. 1999 Jul;20(7):1153-60.
5 PharmGKB:Tamoxifen citrate
6 Tamoxifen dose and serum concentrations of tamoxifen and six of its metabolites in routine clinical outpatient care

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