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抗体化疗药物偶联物(Antibody-drug conjugate,ADC)是近年来发展起来的一种将抗体与高效细胞毒性小分子化合物偶联而成的免疫复合物。经过十几年的发展,ADC药物的研究已取得了突破性进展,目前已有两个ADC药物(Adcetris和Kadcyla)上市。文章从抗原,细胞毒性小分子化合物和Linker的选择及其偶联技术4方面对ADC药物设计的研究进展做了综述。
Antibody-drug conjugates (ADCs) are immune complexes that have been developed in recent years to conjugate antibodies to high-potency cytotoxic small-molecule compounds. After more than a decade of development, breakthroughs have been made in the study of ADC drugs. Two ADC drugs (Adcetris and Kadcyla) are currently on the market. This review summarizes the progress in the design of ADC drugs in terms of the selection of antigens, cytotoxic small molecule compounds and Linker and their coupling technologies.