School of Public Health, Health Science Center, Xi'an Jiaotong University, No.76 Yanta West Road, Xi'an, Shaanxi, 710061, China.
Department of Radiology, Memorial Sloan Kettering Cancer Center, New York, NY, 10065, USA.
ChemMedChem. 2024 Jun 3;19(11):e202300720. doi: 10.1002/cmdc.202300720. Epub 2024 Mar 11.
Conventional chemotherapy is insufficient for precise cancer treatment due to its lack of selectivity and inevitable side effects. Targeted drugs have emerged as a promising solution for precise cancer treatment. A common strategy is to conjugate therapeutic agents with ligands that can specifically bind to tumor cells, providing targeted therapy. Similar to the more successful antibody drug conjugates (ADCs), small molecule drug conjugates (SMDCs) are another promising class of targeted drugs, consisting of three parts: targeting ligand, cleavable linker and payload. Compared to ADCs, SMDCs have the advantages of smaller size, better permeability, simpler preparation process and non-immunogenicity, making them a promising alternative to ADCs. This review describes the characteristics of the targeting ligand, linker and payload of SMDCs and the criteria for selecting a suitable one. We also discuss recently reported SMDCs and list some successful SMDCs that have entered clinical trials.
由于缺乏选择性和不可避免的副作用，传统化疗在精确癌症治疗方面是不够的。靶向药物作为精确癌症治疗的一种有前途的解决方案已经出现。一种常见的策略是将治疗剂与可以特异性结合肿瘤细胞的配体缀合，提供靶向治疗。与更成功的抗体药物偶联物（ADC）类似，小分子药物偶联物（SMDC）是另一类有前途的靶向药物，由三部分组成：靶向配体、可切割接头和有效载荷。与 ADC 相比，SMDC 具有体积更小、渗透性更好、制备工艺更简单、非免疫原性等优点，是 ADC 的一种有前途的替代品。本文综述了 SMDC 的靶向配体、接头和有效载荷的特点以及选择合适的 SMDC 的标准。我们还讨论了最近报道的 SMDC，并列出了一些已进入临床试验的成功 SMDC。
