Reaction: Tamoxifen to 1 product
- Reaction
- Reaction type
- N-dealkylation
- Direction
- Major circulating metabolite?
- Yes
- Spontaneous?
- No
- Activity
- unknown
- References
- Crewe HK, Notley LM, Wunsch RM, Lennard MS, Gillam EM: 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. [Article]
- Squirewell EJ, Qin X, Duffel MW: Endoxifen and other metabolites of tamoxifen inhibit human hydroxysteroid sulfotransferase 2A1 (hSULT2A1). Drug Metab Dispos. 2014 Nov;42(11):1843-50. doi: 10.1124/dmd.114.059709. Epub 2014 Aug 25. [Article]
- Cronin-Fenton DP, Damkier P, Lash TL: Metabolism and transport of tamoxifen in relation to its effectiveness: new perspectives on an ongoing controversy. Future Oncol. 2014 Jan;10(1):107-22. doi: 10.2217/fon.13.168. [Article]
- White IN: The tamoxifen dilemma. Carcinogenesis. 1999 Jul;20(7):1153-60. doi: 10.1093/carcin/20.7.1153. [Article]
- Klein DJ, Thorn CF, Desta Z, Flockhart DA, Altman RB, Klein TE: PharmGKB summary: tamoxifen pathway, pharmacokinetics. Pharmacogenet Genomics. 2013 Nov;23(11):643-7. doi: 10.1097/FPC.0b013e3283656bc1. [Article]
- Kemp JV, Adam HK, Wakeling AE, Slater R: 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. [Article]
- Comments
- Not Available
- Enzymes
Enzyme Km Vmax Role Cytochrome P450 2D6 Not Available Not Available implied Cytochrome P450 1A1 Not Available Not Available implied Cytochrome P450 1A2 Not Available Not Available implied Cytochrome P450 3A4 Not Available Not Available implied Cytochrome P450 1B1 Not Available Not Available implied Cytochrome P450 2C9 Not Available Not Available implied Cytochrome P450 2C19 Not Available Not Available implied Cytochrome P450 3A5 Not Available Not Available implied
