Deruxtecan is a potent topoisomerase I inhibitor that serves as the cytotoxic payload in antibody–drug conjugates like Trastuzumab deruxtecan and Patritumab deruxtecan, enabling targeted anti-tumor activity. Deruxtecan exhibited superior membrane permeability with a log D value of 2.3[1][2].
References:
[1] Ogitani Y, Hagihara K, Oitate M, Naito H, Toshinori, Agatsuma T. Bystander killing effect of DS-8201a, a novel anti-human epidermal growth factor receptor 2 antibody-drug conjugate, in tumors with human epidermal growth factor receptor 2 heterogeneity. Cancer Sci. 2016 Jul;107(7):1039-46.
[2] Jänne P A, Baik C, Su W C, et al. Efficacy and Safety of Patritumab Deruxtecan (HER3-DXd) in EGFR Inhibitor-Resistant, EGFR-Mutated Non-Small Cell Lung Cancer.Cancer Discov. 2022 Jan;12(1):74-89.
Deruxtecan 是一种强效拓扑异构酶 I 抑制剂，可作为抗体-药物偶联物（如 Trastuzumab deruxtecan 和 Patritumab deruxtecan）的细胞毒载荷，实现靶向抗肿瘤活性。Deruxtecan 表现出优异的膜渗透性，其 log D 值为 2.3[1][2]。