Glycan analysis of glycoprotein pharmaceuticals: Evaluation of analytical approaches to Z number determination in pharmaceutical erythropoietin products

Biologicals. 2011 Nov;39(6):396-403. doi: 10.1016/j.biologicals.2011.08.012. Epub 2011 Oct 10.

Abstract

N-Glycosylation of many glycoprotein drugs is important for biological activity and should therefore be the target of specific and quantitative analytical methods. In this study, we focus on the two N-glycan mapping approaches that are used in pharmacopoeial monograph to analyse N-glycans released from fifteen preparations of recombinant human erythropoietin supplied by ten Chinese manufacturers. Underivatised N-glycans were analysed by high performance anion-exchange chromatography with pulsed amperometric detection and fluorophore-labelled N-glycans were analysed by weak anion-exchange and normal-phase high performance liquid chromatography. N-glycans were also analysed by matrix assisted laser desorption ionisation mass spectrometry. The release of N-glycans by PNGase F was shown to be consistent. Z number, a mathematical expression of the total negatively charged N-glycans composition has provided a convenient way to summarise the complex dataset and it might be suitable for product consistency monitoring. However, this Z number reduces the information of individual acidic N-glycan structure and is also found to be method dependent. Therefore, its use requires clear specification and validation. In this study, we only found weak but positive correlation between the Z number and its bioactivity. Wide range of N-glycans yields were obtained from the fifteen preparations but the significance of their differences is unclear.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • 4-Aminobenzoic Acid / chemistry
  • Animals
  • Biological Assay
  • CHO Cells
  • Chromatography, High Pressure Liquid
  • Cricetinae
  • Cricetulus
  • Erythropoietin / analysis
  • Erythropoietin / genetics
  • Erythropoietin / pharmacology
  • Glycoproteins / chemistry*
  • Glycoproteins / metabolism
  • Glycoproteins / pharmacology
  • Humans
  • Mice
  • Peptide-N4-(N-acetyl-beta-glucosaminyl) Asparagine Amidase / metabolism
  • Pharmaceutical Preparations / chemistry*
  • Pharmaceutical Preparations / metabolism
  • Polysaccharides / analysis*
  • Polysaccharides / chemistry
  • Polysaccharides / metabolism
  • Recombinant Proteins / analysis
  • Recombinant Proteins / chemistry
  • Recombinant Proteins / pharmacology
  • Spectrometry, Mass, Matrix-Assisted Laser Desorption-Ionization

Substances

  • Glycoproteins
  • Pharmaceutical Preparations
  • Polysaccharides
  • Recombinant Proteins
  • Erythropoietin
  • Peptide-N4-(N-acetyl-beta-glucosaminyl) Asparagine Amidase
  • 4-Aminobenzoic Acid