CYP2B6

This gene, CYP2B6, encodes a member of the cytochrome P450 superfamily of enzymes. The cytochrome P450 proteins are monooxygenases which catalyze many reactions involved in drug metabolism and synthesis of cholesterol, steroids and other lipids. This protein localizes to the endoplasmic reticulum and its expression is induced by phenobarbital. The enzyme is known to metabolize some xenobiotics, such as the anti-cancer drugs cyclophosphamide and ifosphamide.

Transcript variants for this gene have been described; however, it has not been resolved whether these transcripts are in fact produced by this gene or by a closely related pseudogene, CYP2B7. Both the gene and the pseudogene are located in the middle of a CYP2A pseudogene found in a large cluster of cytochrome P450 genes from the CYP2A, CYP2B and CYP2F subfamilies on chromosome 19q.

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Following is a table of selected substrates, inducers and inhibitors of CYP2B6.

Inhibitors of CYP2B6 can be classified by their potency, such as:

• Strong inhibitor being one that causes at least a 5-fold increase in the plasma AUC values, or more than 80% decrease in clearance.{{cite web|url=https://www.fda.gov/Drugs/DevelopmentApprovalProcess/DevelopmentResources/DrugInteractionsLabeling/ucm093664.htm#classInhibit|title=Drug Interactions & Labeling - Drug Development and Drug Interactions: Table of Substrates, Inhibitors and Inducers|last=Center for Drug Evaluation and Research|website=www.fda.gov|language=en|access-date=2016-06-01}}
• Moderate inhibitor being one that causes at least a 2-fold increase in the plasma AUC values, or 50-80% decrease in clearance.
• Weak inhibitor being one that causes at least a 1.25-fold but less than 2-fold increase in the plasma AUC values, or 20-50% decrease in clearance.

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• {{cite journal | vauthors = Gounden V, van Niekerk C, Snyman T, George JA | title = Presence of the CYP2B6 516G> T polymorphism, increased plasma Efavirenz concentrations and early neuropsychiatric side effects in South African HIV-infected patients | journal = AIDS Research and Therapy | volume = 7 | pages = 32 | date = August 2010 | pmid = 20723261 | pmc = 2933581 | doi = 10.1186/1742-6405-7-32 | doi-access = free }}
• {{cite journal | vauthors = Yang K, Koh KH, Jeong H | title = Induction of CYP2B6 and CYP3A4 expression by 1-aminobenzotriazole (ABT) in human hepatocytes | journal = Drug Metabolism Letters | volume = 4 | issue = 3 | pages = 129–33 | date = August 2010 | pmid = 20642445 | doi = 10.2174/187231210791698410 | pmc = 3697095 }}
• {{cite journal | vauthors = Ngaimisi E, Mugusi S, Minzi OM, Sasi P, Riedel KD, Suda A, Ueda N, Janabi M, Mugusi F, Haefeli WE, Burhenne J, Aklillu E | title = Long-term efavirenz autoinduction and its effect on plasma exposure in HIV patients | journal = Clinical Pharmacology and Therapeutics | volume = 88 | issue = 5 | pages = 676–84 | date = November 2010 | pmid = 20881953 | doi = 10.1038/clpt.2010.172 | s2cid = 24749169 }}
• {{cite journal | vauthors = Smith G, Stubbins MJ, Harries LW, Wolf CR | title = Molecular genetics of the human cytochrome P450 monooxygenase superfamily | journal = Xenobiotica; the Fate of Foreign Compounds in Biological Systems | volume = 28 | issue = 12 | pages = 1129–65 | date = December 1998 | pmid = 9890157 | doi = 10.1080/004982598238868 }}
• {{cite journal | vauthors = Svärd J, Spiers JP, Mulcahy F, Hennessy M | s2cid = 205996665 | title = Nuclear receptor-mediated induction of CYP450 by antiretrovirals: functional consequences of NR1I2 (PXR) polymorphisms and differential prevalence in whites and sub-Saharan Africans | journal = Journal of Acquired Immune Deficiency Syndromes | volume = 55 | issue = 5 | pages = 536–49 | date = December 2010 | pmid = 20861742 | doi = 10.1097/QAI.0b013e3181f52f0c | doi-access = free }}
• {{cite journal | vauthors = Melanson SE, Stevenson K, Kim H, Antin JH, Court MH, Ho VT, Ritz J, Soiffer RJ, Kuo FC, Longtine JA, Jarolim P | title = Allelic variations in CYP2B6 and CYP2C19 and survival of patients receiving cyclophosphamide prior to myeloablative hematopoietic stem cell transplantation | journal = American Journal of Hematology | volume = 85 | issue = 12 | pages = 967–71 | date = December 2010 | pmid = 21108329 | doi = 10.1002/ajh.21889 | s2cid = 25737167 | doi-access = free }}
• {{cite journal | vauthors = Yuan ZH, Liu Q, Zhang Y, Liu HX, Zhao J, Zhu P | s2cid = 19318796 | title = CYP2B6 gene single nucleotide polymorphisms and leukemia susceptibility | journal = Annals of Hematology | volume = 90 | issue = 3 | pages = 293–9 | date = March 2011 | pmid = 20878158 | doi = 10.1007/s00277-010-1085-z }}
• {{cite journal | vauthors = Nelson DR, Zeldin DC, Hoffman SM, Maltais LJ, Wain HM, Nebert DW | title = Comparison of cytochrome P450 (CYP) genes from the mouse and human genomes, including nomenclature recommendations for genes, pseudogenes and alternative-splice variants | journal = Pharmacogenetics | volume = 14 | issue = 1 | pages = 1–18 | date = January 2004 | pmid = 15128046 | doi = 10.1097/00008571-200401000-00001 }}
• {{cite journal | vauthors = Mo SL, Liu YH, Duan W, Wei MQ, Kanwar JR, Zhou SF | title = Substrate specificity, regulation, and polymorphism of human cytochrome P450 2B6 | journal = Current Drug Metabolism | volume = 10 | issue = 7 | pages = 730–53 | date = September 2009 | pmid = 19702527 | doi = 10.2174/138920009789895534 }}
• {{cite journal | vauthors = Cabrera Figueroa S, Fernández de Gatta M, Hernández García L, Domínguez-Gil Hurlé A, Bustos Bernal C, Sepúlveda Correa R, García Sánchez MJ | s2cid = 24793535 | title = The convergence of therapeutic drug monitoring and pharmacogenetic testing to optimize efavirenz therapy | journal = Therapeutic Drug Monitoring | volume = 32 | issue = 5 | pages = 579–85 | date = October 2010 | pmid = 20720517 | doi = 10.1097/FTD.0b013e3181f0634c }}
• {{cite journal | vauthors = Ribaudo HJ, Liu H, Schwab M, Schaeffeler E, Eichelbaum M, Motsinger-Reif AA, Ritchie MD, Zanger UM, Acosta EP, Morse GD, Gulick RM, Robbins GK, Clifford D, Haas DW | title = Effect of CYP2B6, ABCB1, and CYP3A5 polymorphisms on efavirenz pharmacokinetics and treatment response: an AIDS Clinical Trials Group study | journal = The Journal of Infectious Diseases | volume = 202 | issue = 5 | pages = 717–22 | date = September 2010 | pmid = 20662624 | pmc = 2919241 | doi = 10.1086/655470 }}
• {{cite journal | vauthors = Shimada M, Miyagawa T, Kawashima M, Tanaka S, Honda Y, Honda M, Tokunaga K | s2cid = 24207887 | title = An approach based on a genome-wide association study reveals candidate loci for narcolepsy | journal = Human Genetics | volume = 128 | issue = 4 | pages = 433–41 | date = October 2010 | pmid = 20677014 | doi = 10.1007/s00439-010-0862-z }}
• {{cite journal | vauthors = Jamshidi Y, Moreton M, McKeown DA, Andrews S, Nithiyananthan T, Tinworth L, Holt DW, Sadiq ST | title = Tribal ethnicity and CYP2B6 genetics in Ugandan and Zimbabwean populations in the UK: implications for efavirenz dosing in HIV infection | journal = The Journal of Antimicrobial Chemotherapy | volume = 65 | issue = 12 | pages = 2614–9 | date = December 2010 | pmid = 20952418 | doi = 10.1093/jac/dkq369 | doi-access = free }}
• {{cite journal | vauthors = Lindfelt T, O'Brien J, Song JC, Patel R, Winslow DL | s2cid = 24188775 | title = Efavirenz plasma concentrations and cytochrome 2B6 polymorphisms | journal = The Annals of Pharmacotherapy | volume = 44 | issue = 10 | pages = 1572–8 | date = October 2010 | pmid = 20841522 | doi = 10.1345/aph.1P141 }}
• {{cite journal | vauthors = Chung JY, Cho JY, Lim HS, Kim JR, Yu KS, Lim KS, Shin SG, Jang IJ | s2cid = 15380723 | title = Effects of pregnane X receptor (NR1I2) and CYP2B6 genetic polymorphisms on the induction of bupropion hydroxylation by rifampin | journal = Drug Metabolism and Disposition | volume = 39 | issue = 1 | pages = 92–7 | date = January 2011 | pmid = 20876786 | doi = 10.1124/dmd.110.035246 }}
• {{cite journal | vauthors = He C, Kraft P, Chasman DI, Buring JE, Chen C, Hankinson SE, Paré G, Chanock S, Ridker PM, Hunter DJ | title = A large-scale candidate gene association study of age at menarche and age at natural menopause | journal = Human Genetics | volume = 128 | issue = 5 | pages = 515–27 | date = November 2010 | pmid = 20734064 | pmc = 2967297 | doi = 10.1007/s00439-010-0878-4 }}
• {{cite journal | vauthors = Lampreabe I, Gainza de los Rios FJ, Arrieta Gutiérrez A, Jofre-Monseny L, Rodriguez M, Amenabar Iribar JJ, Zárraga Larrondo S, Tejedor D, Martinez A, Olano-Martin E | title = Toward personalized medicine in renal transplantation | journal = Transplantation Proceedings | volume = 42 | issue = 8 | pages = 2864–7 | date = October 2010 | pmid = 20970553 | doi = 10.1016/j.transproceed.2010.08.009 }}
• {{cite journal | vauthors = Elens L, Vandercam B, Yombi JC, Lison D, Wallemacq P, Haufroid V | title = Influence of host genetic factors on efavirenz plasma and intracellular pharmacokinetics in HIV-1-infected patients | journal = Pharmacogenomics | volume = 11 | issue = 9 | pages = 1223–34 | date = September 2010 | pmid = 20860463 | doi = 10.2217/pgs.10.94 }}
• {{cite journal | vauthors = Chou M, Bertrand J, Segeral O, Verstuyft C, Borand L, Comets E, Le Tiec C, Becquemont L, Ouk V, Mentre F, Taburet AM | title = Population pharmacokinetic-pharmacogenetic study of nevirapine in HIV-infected Cambodian patients | journal = Antimicrobial Agents and Chemotherapy | volume = 54 | issue = 10 | pages = 4432–9 | date = October 2010 | pmid = 20696882 | pmc = 2944557 | doi = 10.1128/AAC.00512-10 | url = http://www.hal.inserm.fr/inserm-00517725/document }}
• {{cite journal | vauthors = Bunten H, Liang WJ, Pounder DJ, Seneviratne C, Osselton D | title = OPRM1 and CYP2B6 gene variants as risk factors in methadone-related deaths | journal = Clinical Pharmacology and Therapeutics | volume = 88 | issue = 3 | pages = 383–9 | date = September 2010 | pmid = 20668445 | doi = 10.1038/clpt.2010.127 | s2cid = 28983025 }}

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• {{MeshName|CYP2B6}}
• {{UCSC gene info|CYP2B6}}
• {{PDBe-KB2|P20813|Cytochrome P450 2B6}}

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{{Cytochrome P450}}

{{Enzymes}}

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Category:EC 1.14.14