国际药学研究杂志
國際藥學研究雜誌
국제약학연구잡지
INTERNATIONAL JOURNAL OF PHARMACEUTICAL RESEARCH
2015年
4期
427-438
,共12页
王彦明%郝伯钧%钟武%周辛波%李松
王彥明%郝伯鈞%鐘武%週辛波%李鬆
왕언명%학백균%종무%주신파%리송
抗体药物偶联物%auristatin%抗体%连接子%抗肿瘤药
抗體藥物偶聯物%auristatin%抗體%連接子%抗腫瘤藥
항체약물우련물%auristatin%항체%련접자%항종류약
antibody-drug conjugates%auristatin%antibody%linker%antineoplastic agents
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。
抗體藥物偶聯物(antibody drug conjugates,ADC)作為一種新型的生物靶嚮抗癌藥物,結閤瞭單剋隆抗體的高靶嚮選擇性和小分子毒素的高效性,在提高抗體藥物療效的同時也擴大瞭小分子毒素的臨床應用範圍。auristatin因其較高的生物活性已被廣汎用于ADC併取得瞭巨大成功,在臨床在研的ADC中佔有主導地位。auristatin類化閤物的結構特徵不同于其他類毒素,這決定該類ADC對連接子的不同設計要求。本文對auristatin類ADC的各箇組成構件及其臨床試驗進展進行綜述,希望對相關藥物的研髮提供一定的參攷。
항체약물우련물(antibody drug conjugates,ADC)작위일충신형적생물파향항암약물,결합료단극륭항체적고파향선택성화소분자독소적고효성,재제고항체약물료효적동시야확대료소분자독소적림상응용범위。auristatin인기교고적생물활성이피엄범용우ADC병취득료거대성공,재림상재연적ADC중점유주도지위。auristatin류화합물적결구특정불동우기타류독소,저결정해류ADC대련접자적불동설계요구。본문대auristatin류ADC적각개조성구건급기림상시험진전진행종술,희망대상관약물적연발제공일정적삼고。
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.