OATP1B1 Substrates

    OATP1B1 substrates include, but are not limited to, docetaxel, pitavastatin, rosuvastatin, and sorafenib. See glossary page for a more comprehensive list.

    Summary

    OATP1B1 substrates include drugs that use OATP1B1 — an organic anion-transporting polypeptide — for transport into cells in the body. OATP1B1 transporters are found primarily in the liver, where they can facilitate the entry of OATP1B1 substrates into the liver for metabolism and/or excretion.[1][2][3]

    Certain foods, medications, or supplements may alter OATP1B1 activity, potentially causing drug interactions by affecting the pharmacokinetics of drugs that are OATP1B1 substrates.[3]

    The table below outlines identified OATP1B1 substrates.[1][2][4]​​ Importantly, this list is not exhaustive.

    OATP1B1 Substrates
    Atorvastatin
    Bosentan
    Cefazolin
    Cerivastatin
    Darunavir
    Docetaxel
    Enalapril
    Ezetimibe
    Fluvastatin
    Hydroxyurea
    Lopinavir
    Mesalazine
    Methotrexate
    Nafcillin
    Olmesartan
    Penicillin G
    Pitavastatin
    Pravastatin
    Rifampicin
    Rosuvastatin
    Saquinavir
    Simvastatin
    Sorafenib
    Valsartan

    References

    1. ^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)
    2. ^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)
    3. ^Kalliokoski A, Niemi MImpact of OATP transporters on pharmacokinetics.Br J Pharmacol.(2009 Oct)
    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)