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Clin Pharmacol Ther. 2018 Mar;103(3):434-448. doi: 10.1002/cpt.749. Epub 2017 Jul 14.

Endogenous Probes for Drug Transporters: Balancing Vision With Reality.

Author information

1
Pharmacokinetics, Dynamics & Metabolism, Medicine Design, Pfizer Inc., Groton, Connecticut, USA.
2
Mechanistic Safety and Disposition, IVIVT, GlaxoSmithKline, Ware, Hertfordshire, UK.
3
Laboratory of Molecular Pharmacokinetics, Graduate School of Pharmaceutical Sciences, University of Tokyo, Tokyo, Japan.
4
RIKEN Innovation Center, Research Cluster for Innovation, RIKEN, Kanagawa, Japan.

Abstract

Various endogenous probes have been identified for a number of hepatic and renal drug transporters and available clinical data indicate that they could be leveraged in phase I trials to facilitate subject phenotyping and drug-drug interaction (DDI) assessment. Despite the progress, however, it is recognized that the menu of probes needs expanding, that existing probes need further characterization and validation, and that compound files need to be built in support of probe absorption-metabolism-distribution-excretion-DDI modeling exercises.

PMID:
28560712
DOI:
10.1002/cpt.749

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