Mild Method for Succinimide Hydrolysis on ADCs: Impact on ADC Potency, Stability, Exposure, and Efficacy
Abstract
The stability of the connection between the antibody and the toxin can have a profound impact on ADC safety and efficacy. There has been increasing evidence in recent years that maleimide-based ADCs are prone to payload loss via a retro-Michael type reaction. Herein, we report a mild method for the hydrolysis of the succinimide-thioether ring which results in a “ring-opened” linker. ADCs containing this hydrolyzed succinimide linker show...
Paper Details
Title
Mild Method for Succinimide Hydrolysis on ADCs: Impact on ADC Potency, Stability, Exposure, and Efficacy
Published Date
Oct 6, 2014
Journal
Volume
25
Issue
10
Pages
1871 - 1880
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Notes
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