CYP2B6 Inhibitors

    CYP2B6 inhibitors include, but are not limited to, canagliflozin, clopidogrel, clotrimazole, sertraline, oral contraceptives, and voriconazole. See glossary page for more information.

    Summary

    CYP2B6 inhibitors are compounds that reduce the activity of the CYP2B6 enzyme, which can reduce drug metabolism, potentially impacting the effects of drug therapy.

    CYP2B6 is a cytochrome P450 (CYP) enzyme that is thought to account for just 2 to 5% of total cytochrome P450 enzymes in the liver. CYP2B6 is involved in the metabolism of any medications that are CYP2B6 substrates, as well as various pesticides and other environmental chemicals.[1] CYP2B6 inhibitors can reduce the body’s metabolism of any of these substances.

    The table below outlines some of the most common or clinically relevant CYP2B6 inhibitors.[2][1][3] Importantly, this list is not exhaustive.

    CYP2B6 Inhibitors
    17-α-ethynylestradiol (oral contraceptives)
    Canagliflozin
    Clopidogrel
    Clotrimazole
    Sertraline
    Voriconazole

    References

    1. ^Zanger UM, Schwab MCytochrome P450 enzymes in drug metabolism: regulation of gene expression, enzyme activities, and impact of genetic variation.Pharmacol Ther.(2013-Apr)
    2. ^Song Y, Li C, Liu G, Liu R, Chen Y, Li W, Cao Z, Zhao B, Lu C, Liu YDrug-Metabolizing Cytochrome P450 Enzymes Have Multifarious Influences on Treatment Outcomes.Clin Pharmacokinet.(2021-May)
    3. ^Hakkola J, Hukkanen J, Turpeinen M, Pelkonen OInhibition and induction of CYP enzymes in humans: an update.Arch Toxicol.(2020-Nov)