Cross-Species Differential Plasma Protein Binding of MBX-102/JNJ39659100: A Novel PPAR-γ Agonist
2008

Understanding MBX-102: A New Drug for Diabetes

publication Evidence: moderate

Author Information

Author(s): Holly J. Clarke, Francine Gregoire, Ma Fang, Robert Martin, Spring Zhao, Brian E. Lavan

Primary Institution: Metabolex, Inc.

Hypothesis

The study aims to evaluate the plasma protein binding of MBX-102 acid and the interspecies differences in free drug levels.

Conclusion

MBX-102 acid is highly protein-bound across species, with free drug levels being higher in rodents than in humans.

Supporting Evidence

  • MBX-102 acid is highly bound (>98%) to human, rat, and mouse albumin.
  • Free MBX-102 acid levels are higher in rodent plasma than in human plasma.
  • PPAR-γ transactivation by MBX-102 acid was higher in rat and mouse serum than in human serum.

Takeaway

This study looks at how a new diabetes drug, MBX-102, binds to proteins in the blood and how this varies between humans and animals.

Methodology

The study used equilibrium dialysis and PPAR-γ transactivation assays to evaluate plasma protein binding and species differences.

Limitations

The study could not analyze serum concentrations higher than 10% in the reporter assay, which may affect the results.

Statistical Information

P-Value

p<0.05

Statistical Significance

p<0.05

Digital Object Identifier (DOI)

10.1155/2008/465715

Want to read the original?

Access the complete publication on the publisher's website

View Original Publication