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J. Pers. Med. 2017, 7(4), 18;

Variation in CYP2A6 Activity and Personalized Medicine

Campbell Family Mental Health Research Institute, Centre for Addiction and Mental Health (CAMH), Toronto, ON M5T 1R8, Canada
Department of Pharmacology and Toxicology, University of Toronto, Toronto, ON M5S 1A8, Canada
Department of Psychiatry, University of Toronto, Toronto, ON M5T 1R8, Canada
Author to whom correspondence should be addressed.
Academic Editor: Stephen B. Liggett
Received: 7 October 2017 / Revised: 17 November 2017 / Accepted: 27 November 2017 / Published: 1 December 2017
(This article belongs to the Special Issue Cytochrome P450 Variation in Pharmacogenomics)
Full-Text   |   PDF [762 KB, uploaded 1 December 2017]   |  


The cytochrome P450 2A6 (CYP2A6) enzyme metabolizes several clinically relevant substrates, including nicotine—the primary psychoactive component in cigarette smoke. The gene that encodes the CYP2A6 enzyme is highly polymorphic, resulting in extensive interindividual variation in CYP2A6 enzyme activity and the rate of metabolism of nicotine and other CYP2A6 substrates including cotinine, tegafur, letrozole, efavirenz, valproic acid, pilocarpine, artemisinin, artesunate, SM-12502, caffeine, and tyrosol. CYP2A6 expression and activity are also impacted by non-genetic factors, including induction or inhibition by pharmacological, endogenous, and dietary substances, as well as age-related changes, or interactions with other hepatic enzymes, co-enzymes, and co-factors. As variation in CYP2A6 activity is associated with smoking behavior, smoking cessation, tobacco-related lung cancer risk, and with altered metabolism and resulting clinical responses for several therapeutics, CYP2A6 expression and enzyme activity is an important clinical consideration. This review will discuss sources of variation in CYP2A6 enzyme activity, with a focus on the impact of CYP2A6 genetic variation on metabolism of the CYP2A6 substrates. View Full-Text
Keywords: pharmacogenetics; pharmacogenomics; drug metabolism; CYP2A6; smoking; nicotine; genetic variation; SNP; inhibitor; inducer pharmacogenetics; pharmacogenomics; drug metabolism; CYP2A6; smoking; nicotine; genetic variation; SNP; inhibitor; inducer

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Tanner, J.-A.; Tyndale, R.F. Variation in CYP2A6 Activity and Personalized Medicine. J. Pers. Med. 2017, 7, 18.

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