摘要
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.
出处
《中国药物化学杂志》
CAS
CSCD
2017年第6期490-497,共8页
Chinese Journal of Medicinal Chemistry
基金
教育部创新团队发展计划
辽宁省高校创新团队支持计划资助
