Mack Fiona, Ritchie Michael, Sapra Puja
Oncology Research Unit, World Wide Research and Development, Pfizer Inc, Pearl River, NY.
Oncology Research Unit, World Wide Research and Development, Pfizer Inc, Pearl River, NY.
Semin Oncol. 2014 Oct;41(5):637-52. doi: 10.1053/j.seminoncol.2014.08.001. Epub 2014 Aug 12.
Antibody-drug conjugates (ADCs) represent a promising therapeutic modality for the clinical management of cancer. The recent approvals of brentuximab vedotin and ado-trastuzumab emtansine plus emerging data for many molecules in clinical trials highlight the potential for ADCs to offer new therapeutic options for patients. Currently, more than 30 ADCs are being evaluated in early- or late-stage clinical trials. Accordingly, much has been done to refine and transform the early-generation ADCs to the highly effective products that we now have in clinical development. These changes include a better understanding of optimal target selection, advances in antibody engineering, improvements in linker/payload conjugation strategies, and the generation of highly potent ADC payloads. In this review, we detail the current status of ADCs in both preclinical and clinical development, highlight technological advancements in ADC development, and speculate towards the future of this targeted therapeutic platform.
抗体药物偶联物（ADCs）是癌症临床治疗中一种很有前景的治疗方式。近期，brentuximab vedotin和ado曲妥珠单抗（ado-trastuzumab emtansine）获批上市，以及许多分子在临床试验中的新数据都凸显了ADCs为患者提供新治疗选择的潜力。目前，超过30种ADCs正在进行早期或晚期临床试验评估。因此，人们做了大量工作，将早期一代的ADCs优化并转化为我们目前正在临床开发的高效产品。这些变化包括对最佳靶点选择有了更好的理解、抗体工程取得进展、连接子/载荷偶联策略得到改进，以及产生了高效的ADCs载荷。在本综述中，我们详细介绍了ADCs在临床前和临床开发中的现状，强调了ADCs开发中的技术进步，并对这个靶向治疗平台的未来进行了展望。
