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Optimization of Radiochemical Reactions using Droplet Arrays
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Novel strategies for microdose studies using non-radiolabeled compounds.

Kazuya Maeda1, Yuichi Sugiyama

  • 1Department of Molecular Pharmacokinetics, Graduate School of Pharmaceutical Sciences, The University of Tokyo, Japan.

Advanced Drug Delivery Reviews
|February 25, 2011
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Summary

Microdosing with non-radiolabeled drugs and LC-MS/MS allows pharmacokinetic assessment in humans. This method enables efficient drug candidate selection and characterization of pharmacokinetic drivers.

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Area of Science:

  • Pharmacology
  • Analytical Chemistry

Background:

  • Traditional pharmacokinetic studies often require radiolabeled compounds, increasing complexity and cost.
  • Microdosing offers a way to assess drug behavior in humans early in development.
  • Liquid chromatography-tandem mass spectrometry (LC-MS/MS) provides high sensitivity for drug quantification.

Purpose of the Study:

  • To demonstrate the utility of non-radiolabeled microdosing coupled with LC-MS/MS for human pharmacokinetic assessment.
  • To highlight the advantages of microdosing for drug candidate selection and understanding pharmacokinetic determinants.

Main Methods:

  • Utilizing liquid chromatography-tandem mass spectrometry (LC-MS/MS) for sensitive quantification of non-radiolabeled drug candidates.
  • Administering microdoses of drug candidates to human subjects.
  • Conducting cassette and cocktail microdosing studies to assess multiple compounds or drug-drug/drug-transporter interactions simultaneously.

Main Results:

  • LC-MS/MS quantification limits are sufficient for pharmacokinetic parameter estimation from microdoses.
  • Demonstrated linear pharmacokinetics for fexofenadine from microdose to therapeutic dose.
  • Obtained plasma concentration-time profiles for nicardipine and its metabolites after microdosing.
  • Showcased the feasibility of cassette microdosing for simultaneous pharmacokinetic profiling of multiple drug candidates.
  • Illustrated the use of cocktail microdosing to identify factors influencing drug pharmacokinetics.

Conclusions:

  • Non-radiolabeled microdosing combined with LC-MS/MS is a viable strategy for early clinical pharmacokinetic assessment.
  • This approach facilitates efficient selection of drug candidates with favorable pharmacokinetic profiles.
  • Microdosing studies provide valuable insights into the factors governing drug pharmacokinetics, including enzyme and transporter roles.