Endogenous Probes for Drug Transporters: Balancing Vision With Reality

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


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.

Publication types

  • Review

MeSH terms

  • Animals
  • Biological Transport
  • Carrier Proteins / genetics*
  • Drug Interactions
  • Humans
  • Molecular Probes*
  • Pharmaceutical Preparations / metabolism*
  • Pharmacokinetics


  • Carrier Proteins
  • Molecular Probes
  • Pharmaceutical Preparations