Death receptor 5 (DR5) is overexpressed in many tumors. Combination of the anti-DR5 antibody with radionuclides such as lutetium-177 (¹⁷⁷Lu) could enhance apoptosis and decrease the possibility of drug-induced resistance. In this study, a humanized anti-DR5 monoclonal antibody CTB006 was labeled with zirconium-89 (⁸⁹Zr) and ¹⁷⁷Lu to improve its efficiency for diagnosis and radiotherapy, respectively. The radiolabeled antibodies showed high tumor uptake in colon205 xenografts according to the results of micro-PET imaging and biodistribution. The ¹⁷⁷Lu-DOTA-CTB006 could inhibit tumor growth significantly.

死亡受体 5 (DR5) 在许多肿瘤中过度表达。抗 DR5 抗体与放射性核素如 lutetium-177 ( ¹⁷⁷ Lu ) 的组合可以增强细胞凋亡并降低药物诱导抗性的可能性。在本研究中，人源化抗 DR5 单克隆抗体 CTB006 分别用 zirconium-89 ( ⁸⁹ Zr) 和¹⁷⁷ Lu标记，以提高其诊断和放疗效率。根据显微PET成像和生物分布的结果，放射性标记的抗体在colon205异种移植物中显示出高肿瘤吸收。在¹⁷⁷路-DOTA-CTB006能显著抑制肿瘤的生长。