Systematic Evaluation of Maleimide Spacer Impact on Drug-Linker Deconjugation in Antibody-Drug Conjugates <i>Ex Vivo</i> and <i>In Vivo</i>

) and ADC (conjugated antibody) ELISA pharmacokinetic (PK) profiles. While deconjugation profiles were generally consistent across methods, IP-MS provided more quantitative measurements and was more sensitive to subtle differences in deconjugation. Our findings shed light on the importance of the spacer structure on thiol-maleimide ADC stability.

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Publication Details

Journal
Bioconjugate Chemistry
Published
2026-03-31
DOI
https://doi.org/10.1021/acs.bioconjchem.5c00580
Primary Topic
HER2/EGFR in Cancer Research
Type
article
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Systematic Evaluation of Maleimide Spacer Impact on Drug-Linker Deconjugation in Antibody-Drug Conjugates Ex Vivo and In Vivo

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Systematic Evaluation of Maleimide Spacer Impact on Drug-Linker Deconjugation in Antibody-Drug Conjugates Ex Vivo and In Vivo

Raffaele Colombo, Jodi Wong, Kaylee J. Wu, D.A. Alonzo, Andrea Hernández Rojas, Graham A. E. Garnett, Vincent Fung, Stuart D. Barnscher, Luying Yang, Ambroise Wu, Tong Ding, Kevin Yin, Mark E. Petersen, Samir Das
article en

Abstract

) and ADC (conjugated antibody) ELISA pharmacokinetic (PK) profiles. While deconjugation profiles were generally consistent across methods, IP-MS provided more quantitative measurements and was more sensitive to subtle differences in deconjugation. Our findings shed light on the importance of the spacer structure on thiol-maleimide ADC stability.

Bioconjugate ChemistryVol. 37(4)
Zymeworks (Canada) (CA)
Zero hunger
Openalex Percentile: Top 32%
HER2/EGFR in Cancer Research
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