title: [Molecular mechanisms on drug transporters in the drug absorption and disposition].
abstract: The membrane transport processes of drugs are critical issues to determine their absorption, distribution and elimination. Recently, various drug transporters have been identified and characterized. The enterocyte peptide transporter PEPT1 mediates the absorption of peptide-like drugs including beta-lactam antibiotics as well as valacyclovir lacking peptide bond. In the kidney, the basolateral organic anion transporters (OAT1, OAT3) and cation transporters (OCT1, OCT2) mediate renal distribution of hydrophilic anionic and cationic drugs, respectively. The brush-border type OAT-K1/K2 were suggested to be a target transporter for methotrexate-leucovorine rescue therapy. The ATP-driven efflux pump P-glycoprotein appeared to be an interaction site between digoxin and clarithromycin or itraconazole in the kidney. In addition, the intestinal P-glycoprotein was suggested to act as an absorptive barrier for tacrolimus in recipients of liver and small bowel transplantation.
authors.affiliation: Department of Pharmacy, Kyoto University Hospital.
authors.forename: Satohiro
authors.initials: S
authors.lastname: Masuda
authors.forename: Ken
authors.initials: K
authors.lastname: Inui
mesh_terms: D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1 / Q000502:physiology; D000818:Animals; D002352:Carrier Proteins / Q000502:physiology; D004347:Drug Interactions; D006801:Humans; D026901:Membrane Transport Proteins / Q000502:physiology*; D027425:ATP-Binding Cassette, Sub-Family C Proteins / Q000502:physiology; D027361:Organic Anion Transporters / Q000502:physiology; D000074011:Peptide Transporter 1; D010599:Pharmacokinetics; D027981:Symporters
chemical_list: D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1; D002352:Carrier Proteins; D026901:Membrane Transport Proteins; D027425:ATP-Binding Cassette, Sub-Family C Proteins; D027361:Organic Anion Transporters; D000074011:Peptide Transporter 1; D027981:Symporters; C082186:SLC15A1 protein, human; C489940:Slc15a1 protein, rat; C101140:Slc21a4 protein, rat