Evaluation of Proposed In Vivo Probe Substrates and Inhibitors for Phenotyping Transporter Activity in Humans

• Published in: Journal of clinical pharmacology Vol. 56 Suppl 7; p. S82
• Main Authors: Momper, Jeremiah D, Tsunoda, Shirley M, Ma, Joseph D
• Format: Journal Article
• Language: English
• Published: England 01.07.2016
• Subjects: Animals; ATP-Binding Cassette Transporters; Biological Transport - drug effects; Biological Transport - physiology; Decision Trees; Drug Evaluation, Preclinical - methods; Drug Interactions - physiology; Humans; Membrane Transport Modulators - metabolism; Membrane Transport Modulators - pharmacology; Membrane Transport Proteins - metabolism; Organic Anion Transporters - metabolism; Organic Cation Transport Proteins - metabolism; Pharmaceutical Preparations - administration & dosage; Pharmaceutical Preparations - metabolism; Phenotype; Substrate Specificity - physiology; drug development; biomarker; drug-drug interaction; phenotyping; transporter

Drug transporters are present in various tissues and have a significant role in drug absorption, distribution, and elimination. The International Transporter Consortium has identified 7 transporters of increasing importance from evidence of clinically significant transporter-mediated drug-drug inter...