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Transporter-Mediated Drug-Drug Interactions and Their Significance

  • Xiaodong LiuEmail author
Chapter
Part of the Advances in Experimental Medicine and Biology book series (AEMB, volume 1141)

Abstract

Drug transporters are considered to be determinants of drug disposition and effects/toxicities by affecting the absorption, distribution, and excretion of drugs. Drug transporters are generally divided into solute carrier (SLC) family and ATP binding cassette (ABC) family. Widely studied ABC family transporters include P-glycoprotein (P-GP), breast cancer resistance protein (BCRP), and multidrug resistance proteins (MRPs). SLC family transporters related to drug transport mainly include organic anion-transporting polypeptides (OATPs), organic anion transporters (OATs), organic cation transporters (OCTs), organic cation/carnitine transporters (OCTNs), peptide transporters (PEPTs), and multidrug/toxin extrusions (MATEs). These transporters are often expressed in tissues related to drug disposition, such as the small intestine, liver, and kidney, implicating intestinal absorption of drugs, uptake of drugs into hepatocytes, and renal/bile excretion of drugs. Most of therapeutic drugs are their substrates or inhibitors. When they are comedicated, serious drug-drug interactions (DDIs) may occur due to alterations in intestinal absorption, hepatic uptake, or renal/bile secretion of drugs, leading to enhancement of their activities or toxicities or therapeutic failure. This chapter will illustrate transporter-mediated DDIs (including food drug interaction) in human and their clinical significances.

Keywords

Transporter-mediated drug-drug interaction Intestinal absorption food-drug interaction Hepatic uptake Renal secretion Transporter 

Notes

Acknowledgment

The project was in part supported by the National Natural Science Foundation of China (No. 81872930; 81573490) and “Double First-Class” University project (No. CPU2018GY22).

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© Springer Nature Singapore Pte Ltd. 2019

Authors and Affiliations

  1. 1.China Pharmaceutical UniversityNanjingChina

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