Details of the Metabolic Reaction (MR)

General Information of This Metabolic Reaction (MR) (ID: MR003526)
Formula
CYP2D6 ...
SVG example
4-Hydroxylation
Reactant Tamoxifen citrate Product 4-hydroxytamoxifen
Reactant Info Product Info
Metabolic Enzyme Cytochrome P450 2D6 (CYP2D6) DME Info
Cytochrome P450 2B6 (CYP2B6) DME Info
Cytochrome P450 3A4 (CYP3A4) DME Info
Mephenytoin 4-hydroxylase (CYP2C19) DME Info
Metabolic Type Oxidation - 4-Hydroxylation
Other MR(s) Related to The Reactant of This MR
Other MR(s) That Metabolize The Reactant of This MR
MR ID Reactant Product MR Type Related Drug REF
MR003522 Tamoxifen citrate Alpha-hydroxytamoxifen Oxidation - Hydroxylation Tamoxifen citrate [1], [2]
MR003510 Tamoxifen citrate N-Desmethyltamoxifen Oxidation - N-Dealkylation Tamoxifen citrate [3], [4], [5], [6], [7]
MR003525 Tamoxifen citrate Tamoxifen N-oxide Oxidation - N-Oxidation Tamoxifen citrate [4], [2], [8]
Other MR(s) Related to The Product of This MR
Other MR(s) That Metabolize The Produtc of This MR
MR ID Reactant Product MR Type Related Drug REF
MR003528 4-hydroxytamoxifen 4-hydroxytamoxifen sulfate Conjugation - Sulfation Tamoxifen citrate [9]
MR003530 4-hydroxytamoxifen Endoxifen Conjugation - Sulfation Tamoxifen citrate [9]
MR003527 4-hydroxytamoxifen Tamoxifen glucuronides Conjugation - Glucuronidation Tamoxifen citrate [9]
References
1 [Effect of lithium on the hematopoietic stem cells] Acta Haematol Pol. 1989 Jan-Jun;20(1):99-106.
2 The tamoxifen dilemma. Carcinogenesis. 1999 Jul;20(7):1153-60.
3 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.
4 Endoxifen and other metabolites of tamoxifen inhibit human hydroxysteroid sulfotransferase 2A1 (hSULT2A1). Drug Metab Dispos. 2014 Nov;42(11):1843-50.
5 Metabolism and transport of tamoxifen in relation to its effectiveness: new perspectives on an ongoing controversy. Future Oncol. 2014 Jan;10(1):107-22.
6 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.
7 PharmGKB summary: tamoxifen pathway, pharmacokinetics Pharmacogenet Genomics. 2013 Nov;23(11):643-7. doi: 10.1097/FPC.0b013e3283656bc1.
8 Oxidation of tamoxifen by human flavin-containing monooxygenase (FMO) 1 and FMO3 to tamoxifen-N-oxide and its novel reduction back to tamoxifen by human cytochromes P450 and hemoglobin Drug Metab Dispos. 2005 Oct;33(10):1446-52. doi: 10.1124/dmd.104.000802.
9 PharmGKB:Tamoxifen citrate

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