title: Intestinal efflux transporters and drug absorption.
abstract: BACKGROUND
  The intestinal epithelial membrane expresses ATP-binding cassette (ABC) transporters such as P-glycoprotein (P-gp), multi-drug resistance-associated proteins (MRPs) and breast cancer resistance protein (BCRP), in addition to various solute carrier (SLC) transporters. These ABC transporters affect the oral bioavailability of their substrate drugs.
  
  
  OBJECTIVE
  To review the contribution of ABC efflux transporters such as P-gp, MRP2, MRP3, and BCRP in the intestinal absorption of substrate drugs.
  
  
  METHODS
  Discussion was made by focusing on the site-specific expression and function of these ABC transporters, and the solubility and permeability of their substrate compounds.
  
  
  CONCLUSIONS
  The increase in the solubility and permeability of orally administered drugs could be the key to escape barrier function of ABC transporters, especially P-gp.
authors.affiliation: Hiroshima International University, Faculty of Pharmaceutical Sciences, Laboratory of Biopharmaceutics and Pharmacokinetics, 5-1-1 Hiro-koshingai, Kure, Hiroshima 737-0112, Japan. t-muraka@ps.hirokoku-u.ac.jp
authors.forename: Teruo
authors.initials: T
authors.lastname: Murakami
authors.forename: Mikihisa
authors.initials: M
authors.lastname: Takano
mesh_terms: D018528:ATP-Binding Cassette Transporters / Q000096:biosynthesis / Q000235:genetics / Q000378:metabolism; D000818:Animals; D002352:Carrier Proteins / Q000235:genetics / Q000378:metabolism*; D020895:Enterocytes / Q000378:metabolism; D006801:Humans; D007408:Intestinal Absorption / Q000235:genetics / Q000502:physiology*; D007413:Intestinal Mucosa / Q000378:metabolism*; D004364:Pharmaceutical Preparations / Q000737:chemistry / Q000378:metabolism*; D012995:Solubility
chemical_list: D018528:ATP-Binding Cassette Transporters; D002352:Carrier Proteins; D004364:Pharmaceutical Preparations