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Complex biotherapeutic modalities such as antibody-drug conjugates (ADC), present significant challenges for the comprehensive bioanalytical characterization of their pharmacokinetics (PK) and catabolism in both pre-clinical and clinical settings. Thus, the bioanalytical strategy for ADCs must be designed to address the specific structural elements of the protein scaffold, linker and warhead. A typical bioanalytical strategy for ADCs involves quantification of the Total ADC, Total IgG and Free Warhead concentrations. Herein, we present bioanalytical charact