The role of organic anion transporting polypeptides in drug absorption, distribution, excretion and drug-drug interactions

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The role of organic anion transporting polypeptides in drug absorption, distribution, excretion and drug-drug interactions.

INTRODUCTION The in vivo fate and effectiveness of a drug depends highly on its absorption, distribution, metabolism, excretion and toxicity (ADME-Tox). Organic anion transporting polypeptides (OATPs) are membrane proteins involved in the cellular uptake of various organic compounds, including clinically used drugs. Since OATPs are significant players in drug absorption and distribution, modula...

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Fruit juices as perpetrators of drug interactions: the role of organic anion-transporting polypeptides.

Grapefruit juice is widely recognized to cause important drug interactions via inhibition of CYP3A4, and a wider variety of fruit juices have been shown to inhibit influx transporters in enterocytes known as organic anion-transporting polypeptides (OATPs). Fruit juice coadministration significantly reduces the oral bioavailability of numerous important medicines relying on this anion transporte...

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Fruit juice, organic anion transporting polypeptides, and drug interactions in psychiatry.

Organic anion transporting polypeptides (OATPs) are a group of membrane transport proteins that facilitate the influx of endogenous and exogenous substances across biological membranes. OATPs are found in enterocytes and hepatocytes and in brain, kidney, and other tissues. In enterocytes, OATPs facilitate the gastrointestinal absorption of certain orally administered drugs. Fruit juices such as...

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Classification of Inhibitors of Hepatic Organic Anion Transporting Polypeptides (OATPs): Influence of Protein Expression on Drug–Drug Interactions

The hepatic organic anion transporting polypeptides (OATPs) influence the pharmacokinetics of several drug classes and are involved in many clinical drug-drug interactions. Predicting potential interactions with OATPs is, therefore, of value. Here, we developed in vitro and in silico models for identification and prediction of specific and general inhibitors of OATP1B1, OATP1B3, and OATP2B1. Th...

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P-glycoprotein- and organic anion-transporting polypeptide-mediated transport of periplocin may lead to drug–herb/drug–drug interactions

Periplocin, an active and toxic component of the traditional Chinese herbal medicine Periploca sepium Bge, is a cardiac glycoside compound that has been implicated in various clinical accidents. This study investigated the role of transporters in the intestinal absorption and biliary excretion of periplocin, as well as the possible metabolic mechanism of periplocin in liver S9. In a bidirection...

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ژورنال

عنوان ژورنال: Expert Opinion on Drug Metabolism & Toxicology

سال: 2016

ISSN: 1742-5255,1744-7607

DOI: 10.1080/17425255.2017.1253679