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Endogenous Probes for Drug Transporters: Balancing Vision With Reality

A D Rodrigues1, K S Taskar2, H Kusuhara3

  • 1Pharmacokinetics, Dynamics & Metabolism, Medicine Design, Pfizer Inc., Groton, Connecticut, USA.

Clinical Pharmacology and Therapeutics
|June 1, 2017
PubMed

Insights

Endogenous probes aid hepatic and renal drug transporter studies in early trials. Further characterization and validation are needed to expand their use in drug-drug interaction assessments.

Area of Science:

  • Pharmacology
  • Drug Metabolism
  • Clinical Pharmacology

Background:

  • Endogenous probes are identified for hepatic and renal drug transporters.
  • Clinical data suggest their utility in Phase I trials for phenotyping and drug-drug interaction (DDI) assessment.

Purpose of the Study:

  • To highlight the need for expanding the repertoire of endogenous probes.
  • To emphasize the necessity of further characterization and validation of existing probes.
  • To underscore the importance of building compound files for modeling.

Main Methods:

  • Literature review of endogenous probes for drug transporters.
  • Analysis of clinical data regarding probe application in Phase I trials.
  • Identification of gaps in current probe characterization and validation.

Main Results:

  • Existing endogenous probes show potential for subject phenotyping and DDI assessment.
  • There is a recognized need to expand the available menu of probes.
  • Further characterization and validation of current probes are required.

Conclusions:

  • Expanding and validating endogenous probes is crucial for advancing drug transporter research.
  • Enhanced probe utility will improve drug development through better phenotyping and DDI prediction.
  • Development of comprehensive compound files is essential for robust modeling exercises.

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