Linker substitution influences succinimide ring hydrolysis equilibrium impacting the stability of attachment to antibody–drug conjugates

Maleimide is used in antibody–drug conjugate (ADC) generation to attach the drug-linker to the antibody. Maleimide linkers with hydrolysis-enabled maleimides were designed. Corresponding ADCs were made and subjected to thermal stress, and succinimide ring hydrolysis and drug release were measured.