CDR clipping-induced heterodimerization: identification of a novel dimerization mechanism in a co-formulated antibody cocktail via a multifaceted mass spectrometry approach

Co-formulated antibody cocktails are becoming an increasingly popular therapeutic class; however, they present analytical challenges over traditional single monoclonal antibody (mAb) formulations. One paramount concern is the formation of heteromeric species that have unknown impacts on safety and e...

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Main Authors: Andrew J Heindel, Yang Shen, Timothy N Tiambeng, Yuetian Yan, Shunhai Wang, Ning Li
Format: Article
Language:English
Published: Taylor & Francis Group 2025-12-01
Series:mAbs
Subjects:
Online Access:https://www.tandfonline.com/doi/10.1080/19420862.2025.2546074
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author Andrew J Heindel
Yang Shen
Timothy N Tiambeng
Yuetian Yan
Shunhai Wang
Ning Li
author_facet Andrew J Heindel
Yang Shen
Timothy N Tiambeng
Yuetian Yan
Shunhai Wang
Ning Li
author_sort Andrew J Heindel
collection DOAJ
description Co-formulated antibody cocktails are becoming an increasingly popular therapeutic class; however, they present analytical challenges over traditional single monoclonal antibody (mAb) formulations. One paramount concern is the formation of heteromeric species that have unknown impacts on safety and efficacy. Consequently, effective approaches for identifying and characterizing high-molecular weight (HMW) impurities are critical to the successful development of this therapeutic class. In this study, we used a multifaceted mass spectrometry approach to characterize a unique dimer species formed between two co-formulated mAbs under thermal stress, revealing an intriguing dimerization mechanism that is driven by complementarity-determining region clipping-induced domain swap. Size exclusion chromatography-mass spectrometry, complemented by post-column denaturation, was utilized at both intact and subunit levels to pinpoint the dimerization interface. Additionally, by probing the disulfide bond susceptibility changes via limited reduction and middle-down analysis, the structural changes of the involved domains were studied. These results highlight the critical role of sophisticated analytical methods in comprehending and addressing the complexities linked to co-formulated mAb cocktails.
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institution Kabale University
issn 1942-0862
1942-0870
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publishDate 2025-12-01
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series mAbs
spelling doaj-art-d414abc220214dd5b3024ec51f83cd282025-08-20T03:36:58ZengTaylor & Francis GroupmAbs1942-08621942-08702025-12-0117110.1080/19420862.2025.2546074CDR clipping-induced heterodimerization: identification of a novel dimerization mechanism in a co-formulated antibody cocktail via a multifaceted mass spectrometry approachAndrew J Heindel0Yang Shen1Timothy N Tiambeng2Yuetian Yan3Shunhai Wang4Ning Li5Analytical Chemistry Group, Regeneron Pharmaceuticals, Inc., Tarrytown, NY, USAAntibody Engineering, Regeneron PharmaceuticalsInc, Inc., Tarrytown, NY, USAAnalytical Chemistry Group, Regeneron Pharmaceuticals, Inc., Tarrytown, NY, USAAnalytical Chemistry Group, Regeneron Pharmaceuticals, Inc., Tarrytown, NY, USAAnalytical Chemistry Group, Regeneron Pharmaceuticals, Inc., Tarrytown, NY, USAAnalytical Chemistry Group, Regeneron Pharmaceuticals, Inc., Tarrytown, NY, USACo-formulated antibody cocktails are becoming an increasingly popular therapeutic class; however, they present analytical challenges over traditional single monoclonal antibody (mAb) formulations. One paramount concern is the formation of heteromeric species that have unknown impacts on safety and efficacy. Consequently, effective approaches for identifying and characterizing high-molecular weight (HMW) impurities are critical to the successful development of this therapeutic class. In this study, we used a multifaceted mass spectrometry approach to characterize a unique dimer species formed between two co-formulated mAbs under thermal stress, revealing an intriguing dimerization mechanism that is driven by complementarity-determining region clipping-induced domain swap. Size exclusion chromatography-mass spectrometry, complemented by post-column denaturation, was utilized at both intact and subunit levels to pinpoint the dimerization interface. Additionally, by probing the disulfide bond susceptibility changes via limited reduction and middle-down analysis, the structural changes of the involved domains were studied. These results highlight the critical role of sophisticated analytical methods in comprehending and addressing the complexities linked to co-formulated mAb cocktails.https://www.tandfonline.com/doi/10.1080/19420862.2025.2546074Fixed dose combinationheterodimertherapeutic antibodymonoclonal antibodynative LC-MSpost-column denaturation
spellingShingle Andrew J Heindel
Yang Shen
Timothy N Tiambeng
Yuetian Yan
Shunhai Wang
Ning Li
CDR clipping-induced heterodimerization: identification of a novel dimerization mechanism in a co-formulated antibody cocktail via a multifaceted mass spectrometry approach
mAbs
Fixed dose combination
heterodimer
therapeutic antibody
monoclonal antibody
native LC-MS
post-column denaturation
title CDR clipping-induced heterodimerization: identification of a novel dimerization mechanism in a co-formulated antibody cocktail via a multifaceted mass spectrometry approach
title_full CDR clipping-induced heterodimerization: identification of a novel dimerization mechanism in a co-formulated antibody cocktail via a multifaceted mass spectrometry approach
title_fullStr CDR clipping-induced heterodimerization: identification of a novel dimerization mechanism in a co-formulated antibody cocktail via a multifaceted mass spectrometry approach
title_full_unstemmed CDR clipping-induced heterodimerization: identification of a novel dimerization mechanism in a co-formulated antibody cocktail via a multifaceted mass spectrometry approach
title_short CDR clipping-induced heterodimerization: identification of a novel dimerization mechanism in a co-formulated antibody cocktail via a multifaceted mass spectrometry approach
title_sort cdr clipping induced heterodimerization identification of a novel dimerization mechanism in a co formulated antibody cocktail via a multifaceted mass spectrometry approach
topic Fixed dose combination
heterodimer
therapeutic antibody
monoclonal antibody
native LC-MS
post-column denaturation
url https://www.tandfonline.com/doi/10.1080/19420862.2025.2546074
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