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The structure of antibody-drug conjugates (ADCs) consists of a cytotoxic drug conjugated to a monoclonal antibody. Due to its multiple components, complex bioanalytical strategies are needed to characterize an ADC’s pharmacokinetic properties. This chapter discusses bioanalytical assays and parameters required for the PK characterization, including: total antibody, total conjugated drug, unconjugated payload and its metabolites, drug-to-antibody ratio, and immunogenicity, using ligand binding and mass spectrometry-based approaches. Comprehensive ADC analysis entails an integrated understanding of antibody stability, linker chemistry, payload characteristics, and potential immunogenicity. Robust bioanalytical packages are imperative to elucidate exposure-response relationships and support further ADC optimization and development. Overall, analytical selectivity, sensitivity, and novelty are paramount to decipher the intricate disposition mechanisms of ADCs.

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Bioanalytical Methodologies for Pharmacokinetic Characterization of Antibody Drug Conjugates

  • 章节

  • 发表日期：

    2026年

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  • Y. -J. Xue,
  • Matthew V. Myers,
  • Jian Chen,
  • Mu Chen,
  • Brian Melo,
  • Martha Vallejo,
  • Stephen E. Maxwell,
  • Jim X. Shen,
  • Johanna R. Mora,
  • Sekhar Surapaneni

摘要

The structure of antibody-drug conjugates (ADCs) consists of a cytotoxic drug conjugated to a monoclonal antibody. Due to its multiple components, complex bioanalytical strategies are needed to characterize an ADC’s pharmacokinetic properties. This chapter discusses bioanalytical assays and parameters required for the PK characterization, including: total antibody, total conjugated drug, unconjugated payload and its metabolites, drug-to-antibody ratio, and immunogenicity, using ligand binding and mass spectrometry-based approaches. Comprehensive ADC analysis entails an integrated understanding of antibody stability, linker chemistry, payload characteristics, and potential immunogenicity. Robust bioanalytical packages are imperative to elucidate exposure-response relationships and support further ADC optimization and development. Overall, analytical selectivity, sensitivity, and novelty are paramount to decipher the intricate disposition mechanisms of ADCs.