Insights into CYP2B6-mediated drug-drug interactions.
Article Details
- CitationCopy to clipboard
Hedrich WD, Hassan HE, Wang H
Insights into CYP2B6-mediated drug-drug interactions.
Acta Pharm Sin B. 2016 Sep;6(5):413-425. doi: 10.1016/j.apsb.2016.07.016. Epub 2016 Aug 9.
- PubMed ID
- 27709010 [ View in PubMed]
- Abstract
Mounting evidence demonstrates that CYP2B6 plays a much larger role in human drug metabolism than was previously believed. The discovery of multiple important substrates of CYP2B6 as well as polymorphic differences has sparked increasing interest in the genetic and xenobiotic factors contributing to the expression and function of the enzyme. The expression of CYP2B6 is regulated primarily by the xenobiotic receptors constitutive androstane receptor (CAR) and pregnane X receptor (PXR) in the liver. In addition to CYP2B6, these receptors also mediate the inductive expression of CYP3A4, and a number of important phase II enzymes and drug transporters. CYP2B6 has been demonstrated to play a role in the metabolism of 2%-10% of clinically used drugs including widely used antineoplastic agents cyclophosphamide and ifosfamide, anesthetics propofol and ketamine, synthetic opioids pethidine and methadone, and the antiretrovirals nevirapine and efavirenz, among others. Significant inter-individual variability in the expression and function of the human CYP2B6 gene exists and can result in altered clinical outcomes in patients receiving treatment with CYP2B6-substrate drugs. These variances arise from a number of sources including genetic polymorphism, and xenobiotic intervention. In this review, we will provide an overview of the key players in CYP2B6 expression and function and highlight recent advances made in assessing clinical ramifications of important CYP2B6-mediated drug-drug interactions.
DrugBank Data that Cites this Article
- Drug Enzymes
Drug Enzyme Kind Organism Pharmacological Action Actions Artemether Cytochrome P450 2B6 Protein Humans UnknownSubstrateInducerDetails Artemisinin Cytochrome P450 2B6 Protein Humans NoSubstrateInducerDetails Clotiazepam Cytochrome P450 2B6 Protein Humans UnknownSubstrateDetails Diazepam Cytochrome P450 2B6 Protein Humans UnknownSubstrateDetails Lidocaine Cytochrome P450 2B6 Protein Humans UnknownSubstrateDetails Meperidine Cytochrome P450 2B6 Protein Humans NoSubstrateDetails Methylphenobarbital Cytochrome P450 2B6 Protein Humans UnknownSubstrateDetails Nevirapine Cytochrome P450 2B6 Protein Humans UnknownSubstrateInducerDetails Tamoxifen Cytochrome P450 2B6 Protein Humans UnknownSubstrateInhibitorDetails Testosterone cypionate Cytochrome P450 2B6 Protein Humans UnknownSubstrateDetails Testosterone enanthate Cytochrome P450 2B6 Protein Humans UnknownSubstrateDetails Testosterone undecanoate Cytochrome P450 2B6 Protein Humans UnknownSubstrateDetails Valproic acid Cytochrome P450 2B6 Protein Humans UnknownSubstrateDetails - Drug Interactions
Drugs Interaction Integrate drug-drug
interactions in your softwareAmitriptylineRaloxifene The metabolism of Amitriptyline can be decreased when combined with Raloxifene. AmitriptylineMemantine The metabolism of Amitriptyline can be decreased when combined with Memantine. AmitriptylineThiotepa The metabolism of Amitriptyline can be decreased when combined with Thiotepa. AmitriptylinePiperaquine The metabolism of Amitriptyline can be decreased when combined with Piperaquine. AmitriptylineNicotine The metabolism of Amitriptyline can be decreased when combined with Nicotine. AmitriptylineThiosulfuric acid The metabolism of Amitriptyline can be increased when combined with Thiosulfuric acid. AmitriptylinePalovarotene The metabolism of Amitriptyline can be increased when combined with Palovarotene. AntipyrineRaloxifene The metabolism of Antipyrine can be decreased when combined with Raloxifene. AntipyrineMemantine The metabolism of Antipyrine can be decreased when combined with Memantine. AntipyrineRilpivirine The metabolism of Antipyrine can be decreased when combined with Rilpivirine. 
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