Antibody-drug conjugates(ADCs)are novel targeted drugs that consist of covalently linked cytotoxic drugs and monoclonal antibodies.They selectively deliver cytotoxic drugs to tumor cells based on the targeting features of antibodies,leading to their anti-tumor effects while avoiding damage to healthy cells.The design principle of ADCs is complex,and the safety and effectiveness of ADCs depend on the selection of targets,antibodies,cytotoxic payloads and coupling modes.Despite the improvement of the stability,homogeneity and anti-tumor activity of ADCs upon three generations of technology,the great potential for the development of advanced ADCs remains in this field.This review briefly introduces the structure,function and development background of ADCs,systematically illustrates the design and optimization strategies of each components of ADC,and provides the analyses and prospects of the future development of ADCs.