Quantification of residual AEBSF-related impurities by reversed-phase liquid chromatography

J Chromatogr B Analyt Technol Biomed Life Sci. 2019 May 15:1116:19-23. doi: 10.1016/j.jchromb.2019.03.022. Epub 2019 Mar 20.

Abstract

During research of a broadly neutralizing antibody (bNAb) for HIV-1 infection, site-specific clipping was observed during cell culture incubation. Protease inhibitor, 4-(2-aminoethyl) benzenesulfonyl fluoride (AEBSF), was supplemented to the cell culture feeding to mitigate clipping as one of the control strategies. It led to the need and development of a new assay to monitor the free AEBSF-related impurities during the purification process. In this work, a reversed-phase liquid chromatography (RPLC-UV) method was developed to measure the total concentration of AEBSF and its major degradant product, 4-(aminoethyl) benzenesulfonic acid (AEBS-OH). This quantitative approach involved hydrolysis pre-treatment to drive all AEBSF to AEBS-OH, a filtration step to remove large molecules, followed by RPLC-UV analysis. The method was qualified and shown to be capable of measuring AEBS-OH down to 0.5 μM with good accuracy and precision, which was then applied for process clearance studies. The results demonstrated that a Protein A purification step in conjunction with a mock ultrafiltration/diafiltration (UF/DF) step could remove AEBSF-related impurities below the detection level. Overall, this study is the first to provide a unique approach for monitoring the clearance of free AEBSF and its related degradant, AEBS-OH, in support of the bNAb research.

Keywords: AEBS-OH; AEBSF; Antibody; Clipping; Impurity; Protease inhibitor; RPLC-UV; Residual.

MeSH terms

  • Anti-HIV Agents / chemistry
  • Anti-HIV Agents / standards
  • Antibodies, Neutralizing / chemistry
  • Chromatography, Reverse-Phase / methods*
  • Drug Contamination*
  • HIV Antibodies / chemistry
  • Humans
  • Limit of Detection
  • Linear Models
  • Reproducibility of Results
  • Sulfones / analysis*
  • Technology, Pharmaceutical

Substances

  • Anti-HIV Agents
  • Antibodies, Neutralizing
  • HIV Antibodies
  • Sulfones
  • 4-(2-aminoethyl)benzenesulfonylfluoride