Summary
OATP1A2 substrates include drugs that use OATP1A2 — an organic anion-transporting polypeptide — for transport into the cells of various organs and tissues in the body. OATP1A2 transporters are found in the intestine, liver, kidney, and blood-brain barrier, where they can facilitate the absorption of OATP1A2 substrates into the blood and brain as well as their metabolism and excretion via the liver and kidney.[1][2][3]
Certain foods, medications, or supplements may alter OATP1A2 activity, potentially causing drug interactions by affecting the pharmacokinetics of drugs that are OATP1A2 substrates.[1]
The table below outlines identified OATP1A2 substrates.[2][3][4][5] Importantly, this list is not exhaustive.
| OATP1A2 Substrates |
|---|
| Acebutolol |
| Aliskiren |
| Atenolol |
| Celiprolol |
| Ciprofloxacin |
| Darunavir |
| Docetaxel |
| Enoxacin |
| Erythromycin |
| Fexofenadine |
| Gatifloxacin |
| Hydroxyurea |
| Imatinib |
| Labetolol |
| Levofloxacin |
| Lopinavir |
| Methotrexate |
| Nadolol |
| Norfloxacin |
| Pitavastatin |
| Pravastatin |
| Rocuronium |
| Rosuvastatin |
| Saquinavir |
| Sildenafil |
| Sotalol |
| Talinolol |
| Tebipenem pivoxil |
| Triptans |
References
- ^Kalliokoski A, Niemi MImpact of OATP transporters on pharmacokinetics.Br J Pharmacol.(2009 Oct)
- ^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)
- ^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)
- ^Bailey DGFruit juice inhibition of uptake transport: a new type of food-drug interaction.Br J Clin Pharmacol.(2010 Nov)