抗肿瘤抗体-药物偶联物的临床研究进展  

Antibody-drug Conjugates in Clinical Trials for Cancer Therapy

作　　者：丰雪[1] 龙亚一[1] 廖翰[1] 孙永[1] 韩文琦[1] 甄宇红[1] 

机构地区：[1]大连医科大学药学院,辽宁大连116044

出　　处：《现代生物医学进展》2013年第16期3164-3168,共5页Progress in Modern Biomedicine

基　　金：国家自然科学基金项目(21176046)

摘　　要：个体化靶向治疗已成为肿瘤临床治疗的新趋势。抗肿瘤靶向药物与传统的细胞毒性化疗药物相比具有特异性高、选择性强和非细胞毒性等优点,近年来发展迅速。抗体-药物偶联物(ADCs)属于抗肿瘤靶向药物,由抗体、"弹头"药物(细胞毒性药物)通过链分子连接而成。ADCs将抗体的靶向性与细胞毒性药物的抗肿瘤作用相结合,可以降低细胞毒性抗肿瘤药物的不良反应,提高肿瘤治疗的选择性,还能更好地应对靶向单抗的耐药性问题。目前,FDA已批准2种ADC药物上市,即Mylotarg和Adcetris,有多种ADCs处于I^III期临床试验阶段,取得了显著的临床效果。本文概述了以美登素,卡奇霉素、Auristantin等三种细胞毒性药物为"弹头"药物的ADCs药物的临床研究状况及临床试验结果,为ADCs的研究和应用提供参考。Individualized targeting therapy is a promising treatment for the cancer patients.Targeted antitumor drugs characterized with high specificity,selectivity and low cytotoxicity develop rapidly in recent years.Antibody-drug conjugates（ADCs） belong to the targeted antitumor drugs,the ADC molecule usually consists of antibody,linker and cytotoxic drugs.ADC can reduce the side effects and improves the efficacy of cytotoxic antitumor reagent by linking it to specific antibody and lower the resistance of monoclonal antibody by acting together with cytotoxic drugs.Up to now,two ADCs（Mylotarg and Adcetris）have been approved by FDA and more ADC candidates are in phase I-III clinical trials which show significantly clinical effects.This review summarized the clinical development state and results of clinical trials of the ADCs using Maytansinoid,Calicheamicin and Auristatin as cytotoxic drugs.It will provide reference for researching and applying ADCs.

关 键 词：抗体-药物偶联物 靶向抗肿瘤药物 美登素 卡奇霉素 Auristantin 

分 类 号：R730.5[医药卫生—肿瘤]