title: Clinical relevance of drug efflux pumps in the gut.
abstract: Important export pumps expressed in the apical membrane of enterocytes are P-glycoprotein (P-gp), breast cancer resistance protein (BCRP) and multidrug resistance protein 2 (MRP2). They are believed to be a crucial part of the bodies' defense mechanisms against potentially toxic, orally administered xenobiotics. In particular P-gp and BCRP also limit the bioavailability of drugs. Inhibition of these intestinal export pumps by concomitantly administered drugs leads to increased plasma concentrations, whereas induction can reduce absorption of the substrate drugs and decrease plasma concentrations. The role of polymorphisms in genes encoding for these transporters will also be discussed. Taken together this review will focus on the role of intestinal export pumps using selected examples from clinical studies in humans.
authors.affiliation: Institute of Experimental & Clinical Pharmacology & Toxicology, Friedrich-Alexander-Universität Erlangen-Nürnberg, Erlangen, Germany.
authors.forename: Shingen
authors.initials: S
authors.lastname: Misaka
authors.forename: Fabian
authors.initials: F
authors.lastname: Müller
authors.forename: Martin F
authors.initials: MF
authors.lastname: Fromm
mesh_terms: D000818:Animals; D041981:Gastrointestinal Tract / Q000378:metabolism*; D006801:Humans; D007408:Intestinal Absorption / Q000502:physiology; D026901:Membrane Transport Proteins / Q000235:genetics / Q000378:metabolism*; D004364:Pharmaceutical Preparations / Q000378:metabolism*
chemical_list: D026901:Membrane Transport Proteins; D004364:Pharmaceutical Preparations