Analytical and bioanalytical technologies for characterizing antibody–drug conjugates

• ADCs are multi-component and require multiple assays for characterization.
• Analytical methods evaluate the physiochemical properties of the ADC.
• Bioanalytical assays evaluate exposure–response, stability, and distribution.
• Assays can be used in both evaluations if sample prep and sensitivity are optimized.

Antibody–drug conjugates (ADCs) require multiple assays for analytical and bioanalytical characterization due to their heterogeneous and dynamic nature. These assays can help address questions from the drug-loading distribution following conjugation to exposure–response relationships after dosing in vivo. This review describes new assay technologies that have been developed for physiochemical characterization and determination of pharmacokinetic parameters of ADCs.