CYP2A6 Inhibitors

    CYP2A6 inhibitors include, but are not limited to, letrozole, pilocarpine, and selegiline. See glossary page for more information.


    CYP2A6 inhibitors are compounds that reduce the activity of the CYP2A6 enzyme, which can reduce drug metabolism, potentially impacting the effects of drug therapy.

    CYP2A6 is a cytochrome P450 (CYP) enzyme found primarily in the liver that is involved in the metabolism of any medications that are CYP2A6 substrates. However, there are few clinically important drug interactions related to CYP2A6 activity.[1]

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

    CYP2A6 Inhibitors


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