抗体–药物偶联（ADC）是现代“精准医疗”需求下药学发展的必然趋势。从2000年第一款ADC药物的上市成功到2020年ADC药物的研发层出不穷。肿瘤靶向治疗的发展带动了ADC药物研发领域的快速兴起。ADC药物是使用具有特异性的单克隆抗体与具有生物活性的细胞毒素结合，将药物特异性递送至肿瘤表面位点，避免对正常细胞的杀伤，减少毒副作用。ADC为细胞毒性有效载荷提供了一种较为理想的递送方法。但是也必须清楚的认识到，由于肿瘤异质性、肿瘤代谢、肿瘤血供等多种因素导致的肿瘤耐药是ADC药物发展中所面临的一大挑战。从ADC药物的发展进程、临床应用及其所面临的耐药问题进行综述，探讨抗体偶联药物的临床应用及其所面临的挑战和策略。

Antibody-drug conjugates (ADC) is one of the inevitable pharmaceutical developments meets the demand of modern "precision medicine". Since the success of the first ADC drug had been listed in 2000, there has been an endless stream of ADC research and development during two decades. The development of tumor targeted therapy has led to the rapid rise in the field of ADC. ADC uses specific monoclonal antibodies to combine with bioactive cytotoxins to deliver specific drugs to tumor surface sites, in order to avoid killing normal cells and decreasing side effects. ADC provides an ideal delivery method for cytotoxic payloads. However, we must also clearly recognize that tumor drug resistance caused by tumor heterogeneity, tumor metabolism, tumor blood supply, and other elements is a major challenge in the development of ADC drugs. We review the development, clinical application, and drug resistance problems of ADC, and discuss the clinical application, challenges, and strategies of ADC.

R979.1

国家自然科学基金面上项目（81972252）；国家自然科学基金青年项目（81703401）；上海市卫健委2021年面上项目（202040382）