Intestinal and hepatic drug transporters: pharmacokinetic, pathophysiological, and pharmacogenetic roles

J Gastroenterol. 2015 May;50(5):508-19. doi: 10.1007/s00535-015-1061-4. Epub 2015 Mar 14.


The efficacy and safety of pharmacotherapies are determined by the complex processes involved in the interactions between drugs with the human body, including pharmacokinetic aspects. Among pharmacokinetic factors, it has been recognized that drug transporters play critical roles for absorption, distribution and excretion of drugs, regulating the membrane transport of drugs. The vast amounts of information on drug transporters collected in the past 20 years have been organized according to biochemical, molecular, genetic, and clinical analyses. Novel technologies, public databases, and regulatory guidelines have advanced the use of such information in drug development and clinical practice. In this review, we selected some clinically important drug transporters expressed in the intestine and liver, and introduced the research history and current knowledge of their pharmacokinetic, pathophysiological, and pharmacogenetic implications.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • ATP Binding Cassette Transporter, Subfamily B, Member 1 / metabolism
  • ATP-Binding Cassette Transporters / metabolism
  • Cytochrome P-450 Enzyme System / metabolism
  • Drug Carriers* / metabolism
  • Drug Carriers* / pharmacokinetics
  • Drug Carriers* / pharmacology
  • Drug Interactions
  • Evidence-Based Medicine
  • Humans
  • Intestinal Absorption* / genetics
  • Liver / metabolism*
  • Prescription Drugs / metabolism
  • Prescription Drugs / pharmacokinetics
  • Prescription Drugs / pharmacology


  • ATP Binding Cassette Transporter, Subfamily B, Member 1
  • ATP-Binding Cassette Transporters
  • Drug Carriers
  • Prescription Drugs
  • Cytochrome P-450 Enzyme System