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...

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Bibliographic Details
Published in:Drug metabolism and pharmacokinetics 2021-04, Vol.37, p.100358, Article 100358
Main Authors: Mochizuki, Tatsuki, Mizuno, Tadahaya, Maeda, Kazuya, Kusuhara, Hiroyuki
Format: Article
Language:English
Subjects:
Drug transporters
Drug–drug interactions
Endogenous biomarkers
Genetic variation
Metabolomics
Pharmacokinetics
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Summary: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. [Display omitted]
ISSN:1347-4367
1880-0920
DOI:10.1016/j.dmpk.2020.09.003