Use-Inspired Biomaterials & Integrated Nano Delivery (U-BiND) Systems Laboratory, Department of Pharmaceutical Sciences, Eugene Applebaum College of Pharmacy and Health Sciences, 259 Mack Ave, Wayne State University, Detroit, MI 48201, USA.
Use-Inspired Biomaterials & Integrated Nano Delivery (U-BiND) Systems Laboratory, Department of Pharmaceutical Sciences, Eugene Applebaum College of Pharmacy and Health Sciences, 259 Mack Ave, Wayne State University, Detroit, MI 48201, USA; Department of Pharmaceutics and Pharmaceutical Technology, College of Pharmacy, Taif University, Taif 26571, Saudi Arabia.
Drug Discov Today. 2017 Oct;22(10):1547-1556. doi: 10.1016/j.drudis.2017.05.011. Epub 2017 Jun 13.
Antibody-drug conjugates (ADCs), a potent class of anticancer therapeutics, comprise a high-affinity antibody (Ab) and cytotoxic payload coupled via a suitable linker for selective tumor cell killing. In the initial phase of their development, two ADCs, Mylotarg, and Adcetris were approved by the US Food and Drug Administration (FDA) for treating hematological cancer, but the real breakthrough came with the discovery of the breast cancer-targeting ADC, Kadcyla. With advances in bioengineering, linker chemistry, and potent cytotoxic payload, ADC technology has become a more powerful tool for targeted cancer therapy. In addition, ADCs with improved safety using humanized Abs with a unified 'drug:antibody ratio' (DAR) have been achieved. Concomitantly, there has been a significant increase in the number of clinical trials with anticancer ADCs with high translation potential.
抗体药物偶联物（ADCs）是一类强效的抗癌治疗药物，由高亲和力的抗体（Ab）和细胞毒性有效载荷通过合适的连接子偶联而成，用于选择性杀伤肿瘤细胞。在其开发的初始阶段，两种 ADC 药物 Mylotarg 和 Adcetris 已被美国食品和药物管理局（FDA）批准用于治疗血液系统癌症，但真正的突破来自于发现针对乳腺癌的 ADC 药物 Kadcyla。随着生物工程、连接子化学和有效细胞毒性载荷的进步，ADC 技术已成为靶向癌症治疗的更强大工具。此外，通过使用具有统一“药物：抗体比”（DAR）的人源化 Ab，实现了 ADC 安全性的提高。同时，具有高转化潜力的抗癌 ADC 的临床试验数量也显著增加。
