An ex vivo potency assay to assess active drug levels of a GLP-1 agonistic peptide during preclinical safety studies

Bioanalysis. 2015 Dec;7(24):3063-72. doi: 10.4155/bio.15.189. Epub 2015 Oct 6.

Abstract

Background: During development of biologics, safety and efficacy assessments are often hampered by immune responses to the treatment. To assess active exposure of a drug peptide in a toxicology study, we developed an ex vivo potency assay which complemented the total drug quantification assay.

Methodology: Compound activity was assessed in samples of treated monkeys by cell-based cAMP measurements. For each animal, activity was compared with its predose sample to which the compound has been added at the postdose concentration as determined by a total LC-MS/MS assay.

Conclusion: We were able to show that despite a high total test compound level, activity was reduced tremendously in antidrug-antibody-positive monkeys. Therefore, the applied ex vivo potency assay supplements drug quantification methods to determine active exposures.

MeSH terms

  • Animals
  • Biological Assay / methods*
  • Chromatography, Liquid / methods*
  • Cyclic AMP / metabolism*
  • Drug Evaluation, Preclinical
  • Female
  • Glucagon-Like Peptide 1 / agonists*
  • Macaca fascicularis
  • Male
  • Peptide Fragments / blood*
  • Peptide Fragments / pharmacology
  • Tandem Mass Spectrometry / methods*

Substances

  • Peptide Fragments
  • Glucagon-Like Peptide 1
  • Cyclic AMP