Current progress in identifying endogenous biomarker candidates for drug transporter phenotyping and their potential application to drug development

Drug transporters play important roles in the elimination of various compounds from the blood. Genetic variation and drug-drug interactions underlie the pharmacokinetic differences for the substrates of drug transporters. Some endogenous substrates of drug transporters have emerged as biomarkers to assess differences in drug transporter activity-not only in animals, but also in humans. Metabolomic analysis is a promising approach for identifying such endogenous substrates through their metabolites. The appropriateness of metabolites is supported by studies in vitro and in vivo, both in animals and through pharmacogenomic or drug-drug interaction studies in humans. This review summarizes current progress in identifying such endogenous biomarkers and applying them to drug transporter phenotyping. (C) 2020 The Japanese Society for the Study of Xenobiotics. Published by Elsevier Ltd. All rights reserved.

Automated summary

Drug transporters play crucial roles in eliminating compounds from the blood, with genetic variation and drug-drug interactions being underlying factors for pharmacokinetic differences of transporter substrates. Some endogenous substrates of drug transporters have been identified as biomarkers to assess transporter activity differences. Metabolomic analysis is a promising approach for identifying endogenous substrates through metabolites.