用于癌症治疗的同型喜树碱抗体药物偶联物的合成与评价。
Synthesis and evaluation of homocamptothecin antibody-drug conjugates for cancer treatment.
机构信息
Shanghai Engineering Research Center of Molecular Therapeutics and New Drug Development, School of Chemistry and Molecular Engineering, East China Normal University, Shanghai, PR China.
Shanghai Engineering Research Center of Molecular Therapeutics and New Drug Development, School of Chemistry and Molecular Engineering, East China Normal University, Shanghai, PR China; Central Research Institute, Shanghai Pharmaceuticals Holding Company Limited, Shanghai, 201203, PR China.
出版信息
Eur J Med Chem. 2024 Dec 5;279:116899. doi: 10.1016/j.ejmech.2024.116899. Epub 2024 Sep 21.
As an emerging tumor therapeutic strategy, antibody-drug conjugates (ADCs) overcome the high toxicity of traditional small molecule chemotherapy and improve the targeting of treatment. In this study, we successfully constructed a novel ADC, Tras-16b, for the first time using homocamptothecin 16b as the payload. Tras-16b, at a dose of 3 mg/kg, exhibited comparable anti-tumor activity to Enhertu and demonstrated an enhanced safety profile in the NCI-N87 xenograft model. Notably, this is the first ADC developed based on homocamptothecin, marking a significant advancement with promising prospects for the structural modification of camptothecin ADCs.
作为一种新兴的肿瘤治疗策略，抗体药物偶联物（ADCs）克服了传统小分子化疗的高毒性，并提高了治疗的靶向性。在这项研究中，我们首次成功构建了一种新型 ADC，Tras-16b，使用同型喜树碱 16b 作为有效载荷。Tras-16b 在 3mg/kg 的剂量下，表现出与 Enhertu 相当的抗肿瘤活性，并在 NCI-N87 异种移植模型中显示出增强的安全性特征。值得注意的是，这是第一个基于同型喜树碱开发的 ADC，标志着喜树碱 ADCs 的结构修饰取得了重大进展，具有广阔的前景。
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