A universal surrogate peptide to enable LC-MS/MS bioanalysis of a diversity of human monoclonal antibody and human Fc-fusion protein drug candidates in pre-clinical animal studies

Biomed Chromatogr. 2012 Aug;26(8):1024-32. doi: 10.1002/bmc.2759. Epub 2012 May 24.

Abstract

For the development of human antibody Fc (fraction crystallizable) region-containing therapeutic protein candidates, which can be either monoclonal antibodies (mAbs) or pharmacologically active proteins/peptides fused to the Fc region of human Immunoglobulin G (IgG), reliable quantification of these proteins in animal pharmacokinetic study plasma samples is critical. LC-MS/MS has emerged as a promising assay platform for this purpose. LC-MS/MS assays used for bioanalysis of human antibody Fc region-containing therapeutic protein candidates frequently rely upon quantification of a 'signature' surrogate peptide whose sequence is unique to the protein analyte of interest. One drawback of the signature peptide approach is that a new LC-MS/MS assay must be developed for each new human Fc region-containing therapeutic protein. To address this issue, we propose an alternative 'universal surrogate peptide' approach for the quantification of human antibody Fc region-containing therapeutic protein candidates in plasma samples from all nonclinical species. A single surrogate tryptic peptide was identified in the Fc region of most human antibody Fc-containing therapeutic protein candidates. An LC-MS-MS method based upon this peptide was shown to be capable of supporting bioanalysis of a diversity of human Fc region-containing therapeutic protein candidates in plasma samples of all commonly used animal species.

MeSH terms

  • Amino Acid Sequence
  • Animals
  • Antibodies, Monoclonal / blood
  • Antibodies, Monoclonal / chemistry*
  • Antibodies, Monoclonal / metabolism
  • Antibodies, Monoclonal / pharmacokinetics
  • Asparagine / chemistry
  • Asparagine / metabolism
  • Aspartic Acid / chemistry
  • Aspartic Acid / metabolism
  • Chromatography, Liquid / methods
  • Computer Simulation
  • Dogs
  • Drug Discovery / methods*
  • Drug Evaluation, Preclinical / methods*
  • Guinea Pigs
  • Humans
  • Hydrolysis
  • Immunoglobulin Fc Fragments / blood
  • Immunoglobulin Fc Fragments / chemistry*
  • Immunoglobulin Fc Fragments / metabolism
  • Macaca fascicularis
  • Macaca mulatta
  • Mice
  • Molecular Sequence Data
  • Peptide Fragments / blood
  • Peptide Fragments / chemistry*
  • Peptide Fragments / metabolism
  • Peptide Fragments / pharmacokinetics
  • Rabbits
  • Rats
  • Tandem Mass Spectrometry / methods
  • Trypsin / chemistry

Substances

  • Antibodies, Monoclonal
  • Immunoglobulin Fc Fragments
  • Peptide Fragments
  • Aspartic Acid
  • Asparagine
  • Trypsin