抗体偶联药物研究进展

Progress in Research on Antibody-Drug Conjugates

抗体偶联药物(antibody drug conjugates,ADCs)是通过化学键将毒性小分子与单克隆抗体偶联的靶向抗肿瘤药物,其充分利用了抗体的特异性和毒性小分子的高抗肿瘤活性,达到了高效低毒的目的。抗体、连接物以及毒性小分子是ADCs的3个重要组成部分,文章介绍了ADCs制备中靶点选择,抗体小型化和人源化改造,高活性毒性小分子使用,可断开和不可断开连接物的特点以及越来越受关注的定点偶联策略,为ADCs临床前研发提供依据。

Antibody drug conjugates（ADCs）, which couple monoclonal antibodies（rnAb） and cytotoxic drug together by chemical bond, are targeted anticancer drugs. ADCs fully take advantage of the specificity of mAb and the high anticancer activity of cytotoxic drug to achieve the efficiency and low-toxic anticancer effects. Cytotoxic drug, mAb and linker are three significant parts of ADC. In this review, target selection, mAb miniaturization and humanization, potent cytotoxic drug application, characteristics of cleavable and non-cleavable linkers and popular site-specific conjugation were described, which were aim to provide evidence for preclinical studies of ADCs.