Expression and function of efflux drug transporters in the intestine.

Abstract:

:A variety of drug transporters expressed in the body control the fate of drugs by affecting absorption, distribution, and elimination processes. In the small intestine, transporters mediate the influx and efflux of endogenous or exogenous substances. In clinical pharmacotherapy, ATP-dependent efflux transporters (ATP-binding cassette [ABC] transporters) expressed on the apical membrane of the intestinal epithelial cells determine oral bioavailability, intestinal efflux clearance, and the site of drug-drug interaction of certain drugs. The expression and functional activity of efflux transporters exhibit marked interindividual variation and are relatively easily modulated by factors such as therapeutic drugs and daily foods and beverages. In this article, we will summarize the recent findings regarding the intestinal efflux transporters, especially P-glycoprotein (P-gp or human multidrug resistance gene [MDR] 1), multidrug resistance-associated protein 2 (MRP2), and breast cancer resistance protein (BCRP).

journal_name

Pharmacol Ther

authors

Takano M,Yumoto R,Murakami T

doi

10.1016/j.pharmthera.2005.06.005

subject

Has Abstract

pub_date

2006-01-01 00:00:00

pages

137-61

issue

1-2

eissn

0163-7258

issn

1879-016X

pii

S0163-7258(05)00137-3

journal_volume

109

pub_type

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