Research paperVariable contribution of cytochromes p450 2d6, 2c9 and 3a4 to the 4-hydroxylation of tamoxifen by human liver microsomes☆
References (36)
- et al.
Identification of the cytochrome P450 IIA family as the enzymes involved in the N-demethylation of tamoxifen in human liver microsomes
Biochem Pharmacol
(1991) - et al.
Determination of tamoxifen and biologically active metabolites in human breast tumour and plasma
Eur J Cancer Clin Oncol
(1981) - et al.
The metabolism of tamoxifen by human liver microsomes is not mediated by cytochrome P450IID6
Biochem Pharmacol
(1991) - et al.
Species differences in the covalent binding of [14C]tamoxifen to liver microsomes and the forms of cytochrome P450 involved
Biochem Pharmacol
(1995) - et al.
Irreversible binding and metabolism of propranolol by human liver microsomes—relationship to polymorphic oxidation
Biochem Pharmacol
(1987) - et al.
Protein measurement with the Polin phenol reagent
J Biol Chem
(1951) - et al.
The expression of human cytochrome P450IA1 in the yeast Saccharomyces cerevisiae
Biochem Pharmacol
(1991) - et al.
The carbon monoxide-binding pigment of liver microsomes. I. Evidence for its hemoprotein nature
J Biol Chem
(1964) - et al.
Tolbutamide hydroxylation by human liver microsomes
Biochem Pharmacol
(1988) - et al.
Human liver microsomal steroid metabolism: identification of the major microsomal steroid hormone 6β-hydroxylase cytochrome P450 enzyme
Arch Biochem Biophys
(1988)
Inhibition of rabbit liver microsomal oxidative metabolism and substrate binding by tamoxifen and the geometric isomers of clomiphene
Biochem Pharmacol
(1980)
A risk-benefit assessment of tamoxifen therapy
Drug Safety
(1993)
Tamoxifen: toxicities and drug resistance during the treatment and prevention of breast cancer
Annu Rev Pharmacol Toxicol
(1995)
Tamoxifen: a reappraisal of its pharmacodynamic and pharmacokinetic properties, and therapeutic use
Clin Pharmacokin
(1989)
A comparative study of tamoxifen metabolism in female rat, mouse and human liver microsomes
Carcinogenesis
(1994)
Metabolism of the antimammary cancer antiestrogenic agent tamoxifen. I. Cytochrome P450-catalysed N-demethylation and 4-hydroxylation
Drug Metab Dispos
(1993)
Involvement of cytochrome P4503A in catalysis of tamoxifen activation and covalent binding to rat and human liver microsomes
Carcinogenesis
(1994)
Both cytochromes P4501A1 and 3A4 are involved in the N-demethylation of tamoxifen
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2022, Pharmacological ResearchComparative metabolic study between two selective estrogen receptor modulators, toremifene and tamoxifen, in human liver microsomes
2015, Drug Metabolism and PharmacokineticsSulfation of afimoxifene, endoxifen, raloxifene, and fulvestrant by the human cytosolic sulfotransferases (SULTs): A systematic analysis
2015, Journal of Pharmacological SciencesCitation Excerpt :Both Phase I and Phase II enzymes have been reported to be involved in the metabolism of these drugs. Tamoxifen has been shown to be metabolized to N-desmethyltamoxifen by CYP3A enzymes (10) and to 4-hydroxytamoxifen and N-desmethyl-4-hydroxytamoxifen by CYP2D6 (11,12). These latter tamoxifen metabolites could be further subjected to sulfation and glucurnidation (13).
Genotypic variations of the CYP2D6 gene in patients with breast cancer treated with tamoxifen: Case series
2023, European Journal of Oncology Pharmacy
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This work was partly supported by the Commission of the European Communities (contract BMH1-CT 94-1622).
Copyright © 1996 Published by Elsevier Inc.