OATP2B1 Substrates

    OATP2B1 substrates include, but are not limited to, aliskiren, atenolol, celiprolol, fexofenadine, and rosuvastatin. See glossary page for a more comprehensive list.

    Summary

    OATP2B1 substrates include drugs that use OATP2B1 — an organic anion-transporting polypeptide — for transport into cells in the body. OATP2B1 transporters are found in the intestine, where they can facilitate the absorption of OATP2B1 substrates into the blood, as well as the liver, where substrates can undergo metabolism and/or excretion.[1][2][3]

    Certain foods, medications, or supplements may alter OATP2B1 activity, potentially causing drug interactions by affecting the pharmacokinetics of drugs that are OATP2B1 substrates.[1]

    The table below outlines identified OATP2B1 substrates.[2][3][4]​​ Importantly, this list is not exhaustive.

    OATP2B1 Substrates
    Aliskiren
    Atenolol
    Atorvastatin
    Bosentan
    Celiprolol
    Ezetimibe
    Fexofenadine
    Flavopiridol
    Fluvastatin
    Glibenclamide
    Latanoprost
    Mesalazine
    Montelukast
    Penicillin G
    Pitavastatin
    Pravastatin
    Rosuvastatin
    Talinolol
    Tebipenem pivoxil

    References

    1. ^Kalliokoski A, Niemi MImpact of OATP transporters on pharmacokinetics.Br J Pharmacol.(2009 Oct)
    2. ^Roth M, Obaidat A, Hagenbuch BOATPs, OATs and OCTs: the organic anion and cation transporters of the SLCO and SLC22A gene superfamilies.Br J Pharmacol.(2012 Mar)
    3. ^Kovacsics D, Patik I, Özvegy-Laczka CThe role of organic anion transporting polypeptides in drug absorption, distribution, excretion and drug-drug interactions.Expert Opin Drug Metab Toxicol.(2017 Apr)
    4. ^Yu J, Zhou Z, Tay-Sontheimer J, Levy RH, Ragueneau-Majlessi IIntestinal Drug Interactions Mediated by OATPs: A Systematic Review of Preclinical and Clinical Findings.J Pharm Sci.(2017 Sep)