Application of Tracer Kinetics in Drug Development: A Valuable but Underused Tool in Clinical Pharmacology

Clinical pharmacology has generally involved the study of pharmacokinetics/pharmacodynamics (PK/PD) under reasonably controlled experimental conditions including:

  • Known dose/concentration/volume of study drug (extent of input)
  • Known infusion duration into a given bodily compartment (rate of input)
  • Accessible compartments for sampling: Blood, Urine, CSF, etc.
  • The drug and its metabolites are distinguishable from endogenous compounds
  • Rapidly changing biomarkers following drug administration
  • Ability to determine routes of elimination using “hot” drug (ADME study)
  • Use of healthy volunteers to ease the feasibility of PK/PD assessments

Quantitative PK/PD analyses tools using drug/metabolite/biomarker static concentration data have become a cornerstone in drug R&D.

But what other quantitative tools are available when we face less controlled conditions?

Tracers can be substances such as dyes or drugs labelled with radioactive or stable isotopes. Tracer kinetics analysis allows the study of more than one form of a compound simultaneously thereby opening new opportunities such as tracing two isoforms of the same drug given by two routes or obtaining rates of production, pool size, and half-life of endogenous substances.

Tracers have been mostly relegated to nutrition and sport sciences, but there are instances where this technique could prove powerful in drug development. In this webinar, Pau Aceves, Associate Director of Consulting Services at Certara, presented case studies on how tracer kinetics were used to inform development of new drugs for lung, CNS, and liver diseases. By watching this webinar, you will learn how tracer kinetics can be leveraged for PK, PD, and in silico modeling applications.