Impact of P-glycoprotein on clopidogrel absorption

• Published in: Clinical pharmacology and therapeutics Vol. 80; no. 5; p. 486
• Main Authors: Taubert, Dirk, von Beckerath, Nicolas, Grimberg, Gundula, Lazar, Andreas, Jung, Norma, Goeser, Tobias, Kastrati, Adnan, Schömig, Albert, Schömig, Edgar
• Format: Journal Article
• Language: English
• Published: United States 01.11.2006
• Subjects: Administration, Oral; Area Under Curve; ATP-Binding Cassette, Sub-Family B, Member 1 - antagonists & inhibitors; ATP-Binding Cassette, Sub-Family B, Member 1 - genetics; ATP-Binding Cassette, Sub-Family B, Member 1 - metabolism; Biological Availability; Caco-2 Cells; Cell Membrane Permeability - drug effects; Coronary Artery Disease - genetics; Coronary Artery Disease - metabolism; Coronary Artery Disease - therapy; Dose-Response Relationship, Drug; Down-Regulation - drug effects; Down-Regulation - genetics; Gene Expression - drug effects; Genotype; Humans; Intestinal Absorption; Platelet Aggregation Inhibitors - administration & dosage; Platelet Aggregation Inhibitors - metabolism; Platelet Aggregation Inhibitors - pharmacokinetics; Polymorphism, Single Nucleotide - genetics; RNA, Messenger - genetics; RNA, Messenger - metabolism; Ticlopidine - administration & dosage; Ticlopidine - analogs & derivatives; Ticlopidine - metabolism; Ticlopidine - pharmacokinetics
• ISSN: 0009-9236
• DOI: 10.1016/j.clpt.2006.07.007

The antiplatelet activity of clopidogrel is characterized by considerable interindividual differences. Variable intestinal absorption is suggested to contribute to the inconsistencies in response. We tested the hypothesis that the intestinal efflux transporter P-glycoprotein (P-gp) limits the oral b...