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