抗体药物偶联物的研究进展

Progress in research on antibody-drug conjugates

传统的癌症化疗常伴随着系统毒性,靶向治疗已成为当今肿瘤研究领域的热点。抗体-药物偶联物(antibody drug conjugates,ADCs)利用单克隆抗体(m ABs)对肿瘤细胞表面过表达抗原的特异性,将"弹头"药物(细胞毒药物)选择性地输送到肿瘤细胞中以改善药物治疗窗。ADCs由"弹头"药物、抗体和药物的偶联链三个部分组成,其兼具了抗体的高特异性和细胞毒素的高活性。而随着抗体药物偶联物brentuximab vedotin(SGN-35,Adcetris)和trastuzumab emtansine(T-DM1,Kadcyla)的成功上市,ADCs引起了人们极大的关注。本文综述ADC的分子特征以及组分优化选择,并简单介绍ADC的发展历程。

Traditional cancer chemotherapy is often accompanied by systemic toxicity. Targeted therapy is a promising treatment for cancer patients. Antibody-drug conjugates （ADCs） use monoclonal antibodies （mAbs） to deliver a potent cytoxic compound selectively to tumor cells, thus improving the therapeutic index of chemotherapeutic agents. ADCs are composed of the monoclonal antibody, toxic payload and linker, which combine the targets-pecificity of monoclonal antibody and the highly active toxic payload. With the successful marketing approval of brentuximab vedotin （SGN-35, Adcetris ） and trastuzumab emtansine （T-DM1, Kadcyla）, ADCs have aroused wide public concern. This review aims to cover molecular characteristics of ADCs and optimal selection of components, and introduces the development of ADCs simply.