Expression and function of efflux drug transporters in the intestine

Pharmacol Ther. 2006 Jan;109(1-2):137-61. doi: 10.1016/j.pharmthera.2005.06.005. Epub 2005 Oct 4.


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).

Publication types

  • Review

MeSH terms

  • ATP Binding Cassette Transporter, Subfamily B / metabolism
  • ATP Binding Cassette Transporter, Subfamily B, Member 1 / metabolism
  • ATP-Binding Cassette Transporters / chemistry
  • ATP-Binding Cassette Transporters / metabolism
  • Animals
  • Carrier Proteins / biosynthesis*
  • Carrier Proteins / metabolism*
  • Drug Resistance, Neoplasm
  • Humans
  • Intestinal Mucosa / metabolism*
  • Pharmaceutical Preparations / metabolism*


  • ATP Binding Cassette Transporter, Subfamily B
  • ATP Binding Cassette Transporter, Subfamily B, Member 1
  • ATP-Binding Cassette Transporters
  • Carrier Proteins
  • P-glycoprotein 2
  • Pharmaceutical Preparations