近年来，抗体药物偶联物（ADC）技术利用单克隆抗体（mAb）特异性地将有效的细胞毒性有效负载递送至肿瘤细胞，已成为一种有前途的肿瘤靶向治疗方法。 ADC 是一类功能强大的生物制药，它通过连接体将针对特定抗原的抗体和具有有效细胞毒性的小分子药物连接起来，从而能够选择性破坏癌细胞，同时最大限度地降低全身毒性。 DXd 是一种拓扑异构酶 I 抑制剂，可诱导 DNA 损伤，导致细胞周期停滞，使其成为 ADC 有效负载的选择。第一三共开发的 DXd-ADC 技术是一个尖端平台，可生产具有改进治疗指标的新一代 ADC，并在各种类型的癌症中显示出显着的治疗潜力。本综述对采用 DXd-ADC 技术开发的药物进行了全面评估，重点关注 DS-8201a、U3-1402、DS-1062a、DS-7300a、DS 的作用机制、药代动力学研究、临床前数据和临床结果-6157a 和 DS-6000a。通过整合现有数据，我们旨在为这些新型药物的当前治疗状况和未来前景提供有价值的见解。版权所有 © 2024 Elsevier Inc. 保留所有权利。

In recent years, antibody-drug conjugate (ADC) technology, which uses monoclonal antibodies (mAbs) to specifically deliver effective cytotoxic payloads to tumor cells, has become a promising method of tumor targeted therapy. ADCs are a powerful class of biopharmaceuticals that link antibodies targeting specific antigens and small molecule drugs with potent cytotoxicity via a linker, thus enabling selective destruction of cancer cells while minimizing systemic toxicity. DXd is a topoisomerase I inhibitor that induces DNA damage leading to cell cycle arrest, making it an option for ADC payloads. The DXd-ADC technology, developed by Daiichi Sankyo, is a cutting-edge platform that produces a new generation of ADCs with improved therapeutic metrics and has shown significant therapeutic potential in various types of cancer. This review provides a comprehensive assessment of drugs developed with DXd-ADC technology, with a focus on mechanisms of action, pharmacokinetics studies, preclinical data, and clinical outcomes for DS-8201a, U3-1402, DS-1062a, DS-7300a, DS-6157a, and DS-6000a. By integrating existing data, we aim to provide valuable insights into the current therapeutic status and future prospects of these novel agents.Copyright © 2024 Elsevier Inc. All rights reserved.