抗体偶联药物（ADC）是由单克隆抗体和细胞毒性有效载荷通过连接子偶联而成，结合了单克隆抗体的高特异性靶向能力和细胞毒活性小分子高效杀伤作用的优点，实现了对癌细胞的精准高效清除，已成为抗癌药物研发的热点之一。自2000年美国食品药品监督管理局（FDA）批准第一个ADC药物吉妥珠单抗（Mylotarg）以来，迄今全球已有14个ADC药物获批上市。这类新型的抗癌药物正引领癌症靶向治疗的新时代。基于ADC药物的构建核心和抗肿瘤作用机制，对ADC药物的体内外代谢的研究进展进行综述，以期从代谢角度为ADC药物的设计、开发、临床前药理、毒理及后续研究提供参考。

Antibody-drug conjugates (ADC) are formed by coupling monoclonal antibodies and cytotoxic payloads through linkers. ADC drugs combine the advantages of high specific targeting ability of monoclonal antibodies and efficient killing effect of small cytotoxic molecules to achieve accurate and efficient removal of cancer cells, and have become one of the hot spots in the research and development of anticancer drugs. Since the food and Drug Administration (FDA) approved the first ADC drug Mylotarg (gemtuzumab ozogamicin) in 2000, so far, 14 ADC drugs have been approved for marketing in the world. This new anticancer drug is leading a new era of cancer targeted therapy. Based on the core construction and anti-tumor mechanism of ADC drugs, the research progress of in vitro and in vivo metabolism of ADC drugs is reviewed, in order to provide more references for the design, development, preclinical pharmacology / toxicology and follow-up research of ADC drugs from the perspective of metabolism.

R979.1;R965.3

江苏省创新能力建设计划科技公共服务平台项目(BM2021002)