CYP2A6 Substrates

    CYP2A6 substrates include, but are not limited to, efavirenz, letrozole, nicotine, pilocarpine, tegafur, and valproic acid. See glossary page for more information.


    CYP2A6 substrates are compounds that are metabolized by CYP2A6 (a cytochrome P450 enzyme), but do not necessarily affect its activity.

    In the presence of CYP2A6 inhibitors or inducers, the metabolism of CYP2A6 substrates can be affected. However, there are few clinically important drug interactions related to CYP2A6 activity.

    The table below outlines some of the most common or clinically relevant CYP2A6 substrates.[1][2][3] Importantly, this list is not exhaustive.

    CYP2A6 Substrates
    Valproic acid

    * Prodrugs are indicated with an asterisk


    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)