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Organic Anion Transporting Polypeptide (OATP) transporter expression, localization and function in the human
1Center of Drug Absorption and Transport, Department of Clinical Pharmacology, Felix-Hausdorff-Str. 3, University Medicine Greifswald, D-17487 Greifswald, Germany.
Pharmacology & Therapeutics
|October 23, 2018
Summary
Intestinal uptake transporters like organic anion transporting polypeptides (OATPs) are crucial for drug absorption. Recent findings challenge the traditional view of OATPs solely as uptake carriers in the human intestine.
Area of Science:
- Pharmacology
- Gastroenterology
- Drug Metabolism
Background:
- Intestinal transporters and drug metabolizing enzymes significantly influence the fate of oral medications, nutrients, and xenobiotics.
- Efflux transporters (e.g., ABCB1, ABCG2) can restrict oral drug bioavailability, while uptake carriers (e.g., PEPT1) may enhance intestinal absorption.
- Knowledge regarding intestinal uptake carriers, particularly organic anion transporting polypeptides (OATPs), lags behind that of efflux pumps.
Purpose of the Study:
- To provide a comprehensive and current review of organic anion transporting polypeptide (OATP) transporters in the human intestine.
- To critically evaluate the established role of intestinal OATPs as uptake carriers in light of recent research.
- To consolidate information on the expression, localization, and function of OATP transporters within the intestinal context.
Main Methods:
- Literature review of recent research on intestinal OATP transporters.
- Analysis of studies investigating OATP expression and localization in the human intestine.
- Synthesis of functional data regarding OATP-mediated transport in the intestinal environment.
Main Results:
- Organic anion transporting polypeptides (OATPs) are frequently implicated in drug-drug and food-drug interactions, often attributed to intestinal OATP inhibition.
- The concept of utilizing OATPs for targeted oral drug delivery to enhance absorption is based on their presumed uptake function.
- Emerging data from multiple research groups raise questions about the definitive role of intestinal OATPs as primary uptake transporters, challenging the existing paradigm.
Conclusions:
- The precise role of intestinal OATPs in drug absorption requires further clarification.
- Established roles of OATPs in drug interactions and delivery may need re-evaluation based on new evidence.
- A comprehensive understanding of OATP expression, localization, and function is essential for accurate drug disposition prediction and development.
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