This book summarizes the related research achievements in Antibody-drug conjugates (ADCs) and their cell metabolism kinetics. The book has three main parts. The first part describes the basic theory of ADCs, including the basic concept and structure of ADCs, and the relationship between the targets of ADCs and their specific functions. The second part mainly introduces the endocytosis and intracellular metabolism of ADCs, including the relationship between endocytosis and ADC activity, the endocytosis and intracellular transport of ADCs, the distribution and metabolism of ADC in vivo. Then it discusses the new formats and research technology of ADCs, including the application of miniaturized antibodies in ADC synthesis, novel carriers for ADC design, the technology and application of site-specific conjugation, and approaches for analyzing the drug: antibody ratio (DAR), the study of pharmacokinetics of ADCs. This book combines the basic theory with the research technology. It can be used as a reference book for students, teachers and researchers of biomedical field.