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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。
Targeted personalized therapy has become a new trend of clinical treatment of tumors. Anti-tumor targeting drugs with traditional cytotoxic chemotherapy drugs compared with high specificity, selectivity and non-cytotoxicity and other advantages, the rapid development in recent years. Antibody-drug conjugates (ADCs) are antitumor drugs targeted by antibodies, “warheads” (cytotoxic drugs) linked by chain molecules. ADCs combine the targeting of antibodies with the antitumor effects of cytotoxic drugs to reduce the adverse effects of cytotoxic antitumor drugs, improve the selectivity of oncologic therapies, and better respond to the resistance of targeted mAbs problem. Currently, the FDA has approved the listing of two ADC drugs, Mylotarg and Adcetris, and many ADCs are in Phase I-III clinical trials with significant clinical results. This article summarizes the clinical research status and clinical trial results of ADCs drugs with three kinds of cytotoxic drugs, such as maytansine, calicheamicin, and Auristantin, as “warheads” drugs, providing reference for the research and application of ADCs.