May 01

Metabolism of therapeutic peptides

Glucagon peptide2Peptide and protein based drugs are significantly more complicated to work with than small molecules, and as yet do not have specific guidelines for their development with regards to in-vivo metabolites.

The analysis of metabolites from small molecule drugs is defined by the FDA in the metabolites in safety testing guidelines (MIST, 2008). Currently, analytical chemistry laboratories apply the same validation guidelines for regulated bioanalysis of peptides as they do for small molecules, therefore it is prudent to apply similar rules to the metabolite conundrum.

One particular challenge with peptide bioanalysis and metabolite identification is that they are significantly more complicated molecules to analyse than small molecules. However, with the vast improvement in liquid chromatography and mass spectrometric instrumentation over the past 10 years, their analysis has now become easier and even commonplace in standard bioanalytical laboratories.

The combination of two types of mass spectrometer – high resolution systems such as Time of Flight detectors, and quantitative systems such as triple quadrupoles, has enabled the rapid identification of unknown metabolites and their subsequent quantitation relative to the parent molecule.

At the Annual Peptides Congress, Richard Kay, Principal Scientist at LGC presented a poster on Metabolism of therapeutic peptides: from identification to quantitation”. Download the poster to find out more about:

  • Examples of in-vivo and in-vitro derived peptide metabolite ID
  • Quantitation of metabolites
  • Metabolite profiles


If you have any questions or would like further information on peptides, please don’t hesitate to contact us.

1 comment

  1. amino acid analysis services

    This is really great resource for researching on bioanalysis of peptides, which is much more difficult than small molecular to be analyzed. I believe with the help of liquid chromatography and mass spectrometric instrumentation, this technology will become more and more easier.

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