The Cytochrome P450 2B6 (CYP2B6) Is the Main Catalyst of Efavirenz Primary and Secondary Metabolism: Implication for HIV/AIDS Therapy and Utility of Efavirenz as a Substrate Marker of CYP2B6…

By B. Ward, J. Gorski, David R. Jones, S. Hall, D. Flockhart, Z. Desta. Journal of Pharmacology and Experimental Therapeutics, 2003

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Polymorphism of human cytochrome P450 enzymes and its clinical impact (2009, background): “…et al., 2001), artemisinin (Svensson and Ashton, 1999), nevirapine (Erickson et al., 1999; Ward et al., 2003), efavirenz (Erickson et al., 1999; Ward et al., 2003), bupropion (Faucette et al., 2000; Hesse et al., 2000), sibutramine (Bae et al., 2008), propofol (Court et al., 2001; Oda et al.,…”
Comprehensive Evaluation of Tamoxifen Sequential Biotransformation by the Human Cytochrome P450 System in Vitro: Prominent Roles for CYP3A and CYP2D6 (2004, methodology): “Information on the activity of each P450 isoform, measured by specific reaction marker, and on P450 contents was provided by the supplier of the HLMs studied (see http://www. gentest.com) and has been detailed in our previous publication (Ward et al., 2003).”
Pharmacogenetics of efavirenz and central nervous system side effects: an Adult AIDS Clinical Trials Group study (2004, background): “Efavirenz is metabolized primarily by hepatic CYP2B6 with some involvement of CYP3A [15].”
Cytochrome P450 enzymes in drug metabolism: regulation of gene expression, enzyme activities, and impact of genetic variation. (2013, background): “A major clinical role of CYP2B6 polymorphism was established in HIV therapy, following the identification of CYP2B6 as the major enzyme responsible for 8-hydroxylation of efavirenz and its further hydroxylation to 8, 14-dihydroxyefavirenz (Ward et al., 2003).”