CYP2B6 Substrates

    CYP2B6 substrates include, but are not limited to, bupropion, cyclophosphamide, efavirenz, ketamine, methadone, nicotine, selegiline, sertraline, temazepam, and tramadol. See glossary page for more information.

    Summary

    CYP2B6 substrates are compounds that are metabolized by CYP2B6 (a cytochrome P450 enzyme), but do not necessarily affect its activity.

    In the presence of CYP2B6 inhibitors or inducers, the metabolism of CYP2B6 substrates can be affected.

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

    CYP2B6 Substrates
    Bupropion
    Cyclophosphamide*
    Efavirenz
    Ketamine
    Methadone
    Nicotine
    Selegiline
    Sertraline
    Temazepam
    Tramadol

    * Prodrugs are indicated with an asterisk

    References

    1. ^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)
    2. ^Zanger UM, Schwab MCytochrome P450 enzymes in drug metabolism: regulation of gene expression, enzyme activities, and impact of genetic variation.Pharmacol Ther.(2013-Apr)
    3. ^Hakkola J, Hukkanen J, Turpeinen M, Pelkonen OInhibition and induction of CYP enzymes in humans: an update.Arch Toxicol.(2020-Nov)