抗体偶联药物的研究进展  

Recent Advances of Antibody-Drug Conjugates

作　　者：吴雪瑶 刘阳[1,2] WU Xue-yao;LIU Yang(Institute of Polymer Chemistry,College of Chemistry,Key Laboratory of Functional Polymer Materials,Nankai University,Tianjin 300071,China;National Demonstration Center for Experimental Chemistry Education Nankai University,Tianjin 300071,China)

机构地区：[1]南开大学化学学院高分子化学研究所,功能高分子材料教育部重点实验室,天津300071 [2]南开大学化学国家级实验教学示范中心,天津300071

出　　处：《离子交换与吸附》2024年第2期127-137,I0002,共12页Ion Exchange and Adsorption

基　　金：科技部国家重点研发计划“纳米科技”项目(基金号2018YFA0209700);国家自然科学基金面上项目(基金号22077073)。

摘　　要：抗体偶联药物(Antibody-drug conjugates,ADC)是通过连接子将细胞毒药物与单克隆抗体进行连接的新型靶向药物。其利用抗体的靶向性将细胞毒药物选择性地输送至肿瘤细胞,在发挥抗肿瘤作用的同时,避免了对健康细胞的损伤。ADC的设计过程较为复杂,目标靶点、抗体、细胞毒性载荷以及偶联方式的选择均会影响ADC的安全性和有效性。经过三代技术的发展,ADC在稳定性、均质性以及抗肿瘤活性等方面均得到了较大提升,但仍存在较大的发展空间。本文简要介绍了ADC的结构、功能及发展历程,系统性阐述了ADC各组分的设计及优化策略,并对ADC的未来发展进行了分析和展望。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.

关 键 词：抗体偶联药物 单克隆抗体 细胞毒药物 连接子 偶联技术 

分 类 号：R979.1[医药卫生—药品]