CYP2C8 Substrates

    CYP2C8 substrates include, but are not limited to, enzalutamide, imatinib, montelukast, paclitaxel, pioglitazone, repaglinide, and rosiglitazone. See glossary page for more information.

    Summary

    CYP2C8 substrates are compounds that are metabolized by CYP2C8 (a cytochrome P450 enzyme), but do not necessarily affect its activity.

    In the presence of CYP2C8 inhibitors or CYP2C8inducers|inducers, the metabolism of CYP2C8 substrates can be affected.

    The table below outlines some of the most common or clinically relevant CYP2C8 substrates.[1][2][3] Importantly, this list is not exhaustive.

    CYP2C8 Substrates
    Enzalutamide
    Imatinib
    Montelukast
    Paclitaxel
    Pioglitazone
    Repaglinide
    Rosiglitazone

    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)