Intestinal drug transporters: an overview

Adv Drug Deliv Rev. 2013 Oct;65(10):1340-56. doi: 10.1016/j.addr.2012.09.042. Epub 2012 Oct 4.


The importance of drug transporters as one of the determinants of pharmacokinetics has become increasingly evident. While much research has been conducted focusing the role of drug transporters in the liver and kidney less is known about the importance of uptake and efflux transporters identified in the intestine. Over the past years the effects of intestinal transporters have been studied using in vivo models, in situ organ perfusions, in vitro tissue preparations and cell lines. This review aims to describe up to date findings regarding the importance of intestinal transporters on drug absorption and bioavailability, highlighting areas in need of further research. Wu and Benet proposed a Biopharmaceutics Drug Disposition Classification System (BDDCS) that allows the prediction of transporter effects on the drug disposition of orally administered drugs. This review also discusses BDDCS predictions with respect to the role of intestinal transporters and intestinal transporter-metabolizing enzyme interplay on oral drug pharmacokinetics.

Keywords: BCRP; BDDCS; Intestinal drug transport; MCT; MRP; OATP; OCT; OCTN; P-gp; PEPT; Transporter–enzyme interplay.

Publication types

  • Review

MeSH terms

  • Animals
  • Biological Transport
  • Cytochrome P-450 CYP3A / metabolism
  • Humans
  • Intestinal Mucosa / metabolism*
  • Membrane Transport Proteins / metabolism*
  • Pharmaceutical Preparations / classification
  • Pharmaceutical Preparations / metabolism*


  • Membrane Transport Proteins
  • Pharmaceutical Preparations
  • Cytochrome P-450 CYP3A
  • CYP3A4 protein, human