auristatin类抗体药物偶联物研究进展  

Auristatin class antibody drug conjugates:research advances

作　　者：王彦明[1,2] 郝伯钧[1,2] 钟武[2] 周辛波[2] 李松[1,2] 

机构地区：[1]沈阳药科大学制药工程学院,沈阳110016 [2]军事医学科学院毒物药物研究所,北京100850

出　　处：《国际药学研究杂志》2015年第4期427-438,共12页Journal of International Pharmaceutical Research

摘　　要：抗体药物偶联物(antibody drug conjugates,ADC)作为一种新型的生物靶向抗癌药物,结合了单克隆抗体的高靶向选择性和小分子毒素的高效性,在提高抗体药物疗效的同时也扩大了小分子毒素的临床应用范围。auristatin因其较高的生物活性已被广泛用于ADC并取得了巨大成功,在临床在研的ADC中占有主导地位。auristatin类化合物的结构特征不同于其他类毒素,这决定该类ADC对连接子的不同设计要求。本文对auristatin类ADC的各个组成构件及其临床试验进展进行综述,希望对相关药物的研发提供一定的参考。Antibody drug conjugates（ADC） are a novel biological targeted anti-cancer agents that have the specificity target of monoclonal antibody and the significant cytotoxicity of the drug. It can not only improve the curative effect of the antibody but also expand the scope of clinical application of the small molecule toxins. Auristatins have been widely used in ADC and has achieved great success because of their powerful biological activity. The structure feature of auristatins is different from that of other cytotoxins , which determine the design of this kind of ADC′ linker is different from others′. We review the progress in each component and the latest clinical research of the auristatin class ADC, which may benefit to the further development of ADC.

关 键 词：抗体药物偶联物 auristatin 抗体 连接子 抗肿瘤药 

分 类 号：R96[医药卫生—药理学]