Current Chromatography Developments in Intact Protein (Top-Down) Therapeutics Bioanalysis by LC-HRMS
Lijuan Kang, Senior Scientist, Janssen Pharmaceutical Company

Intact (top-down) protein bioanalysis is being developed as a complementary approach to bottom-up analysis for protein therapeutics. It has unique advantages in providing simultaneous catabolite identification and quantitative bioanalysis. However, this approach also faces challenges such as poor chromatographic peaks and inadequate assay sensitivity. In current work, different conditions such as HPLC columns were screened to optimize chromatography for the intact protein analysis. To improve the assay sensitivity, micro-flow LC-MS has been explored. Micro-flow LC-MS is known to enhance sampling and ionization efficiency and has been demonstrated to improve sensitivity for small molecules and peptides, but so far has not been reported for the intact protein bioanalysis. This talk will discuss important considerations when applying micro-flow LC for intact protein bioanalysis and compare preliminary results obtained under different configurations. The data showed that application of micro-flow LC-MS, while being successfully used for the bottom-up protein bioanalysis, warranted further exploration since many parameters such as column chemistry and system configuration affect the performance of micro-flow LC-MS.

A Useful Reversed-Phase LC Method Development Strategy for Large Protein Variants
Barry Boyes, Vice President of R&D, Advanced Materials Technology

The number of biotherapeutic drugs including monoclonal antibodies (mAbs) and their related products, such as antibody-drug conjugates (ADCs), have been growing rapidly, particularly in the last decade. The development and commercialization of these complex entities is a complicated process and requires a significant amount of effort and capability — especially in chromatographic separations. This has created a need for chromatographers to have effective strategies for LC separations of large (>50,000 MW) and complex proteins, such as mAbs and their variants. In this webinar, we will discuss how to approach your method development strategy by adjusting various parameters of your separation to ensure that you are seeing more of the variants of your complex proteins. These parameters include pore size, bonded phase chemistry, mobile phase modifiers, mobile phase additives, and column temperature. Systematic selection and adjustment of these variables leads to improved resolution of highly similar protein variants. An example of this approach is high-resolution intact protein LC–MS analysis of difficult IgG mixtures, such as the complex mixtures of lower abundance free sulfhydryl variants present in therapeutic mAbs.

Panel:
Naidong Weng, Head of East Coast Bioanalytical Chemistry and Pharmacokinetics, Jansen Research and Development
Thomas Waeghe, Senior Scientist, MAC-MOD Analytical
Lijuan Kang, Senior Scientist, Janssen Pharmaceutical Company
Barry Boyes, Vice President of R&D, Advanced Materials Technology
Michael Dong, Principal, MWD Consulting

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