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Licensed Unlicensed Requires Authentication Published by De Gruyter November 12, 2012

Cytochrome P450 2B6: function, genetics, and clinical relevance

Miia Turpeinen and Ulrich M. Zanger

Abstract

Cytochrome P450 (CYP) 2B6 belongs to the set of important hepatic drug-metabolizing CYPs. It makes up roughly 3%–6% of total hepatic CYP content and metabolizes several pharmaceuticals including bupropion, efavirenz, cyclophosphamide, pethidine, ketamine and propofol. The enzyme is susceptible to drug-drug interactions by enzyme induction and inhibition. In addition to drugs, CYP2B6 is able to both detoxify and bioactivate a number of procarcinogens and environmental agents including pesticides and herbicides. There is an extensive interindividual variability in the expression of CYP2B6, which is in part explained by extensive genetic polymorphism. CYP2B6 is one of the most polymorphic CYP genes in humans with over 100 described SNPs, numerous complex haplotypes and distinct ethnic and racial frequencies. This review summarizes the basic properties of CYP2B6 and the main characteristics of clinical relevance.


Corresponding author: Miia Turpeinen, Department of Pharmacology and Toxicology, University of Oulu, Aapistie 5B, 90230 Oulu, Finland

Conflict of interest statement

Authors’ conflict of interest disclosure: U. Zanger is named as coinventor of a patent on the detection of specific CYP2B6 polymorphisms for diagnostic purposes.

Research funding: MT was supported by the Emil Aaltonen Foundation. UMZ was supported by the German Federal Ministry of Education and Research (Virtual Liver Network grant 0315755), the 7FP EU Initial Training Network Program ‘Fighting Drug Failure’ (GA-2009-238132), and by the Robert-Bosch Foundation, Stuttgart, Germany.

Employment or leadership: None declared.

Honorarium: None declared.

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Received: 2012-7-19
Accepted: 2012-10-15
Published Online: 2012-11-12
Published in Print: 2012-12-01

©2012 by Walter de Gruyter Berlin Boston

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