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89Zr and 177Lu labeling of anti-DR5 monoclonal antibody for colorectal cancer targeting PET-imaging and radiotherapy

Journal 2021 · IF 1.371 · 330(3): 997-1005 · 发表于 2021 年 9 月 18 日
作者: Yang Yuchuan,Wang Jing,Liu Wei,Deng Hao,Zhao Peng,Liao Wei,Wang Guanquan,Wei Hongyuan,Zhuo Liangang,Yang Xia
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摘要

Death receptor 5 (DR5) is overexpressed in many tumors. Combination of the anti-DR5 antibody with radionuclides such as lutetium-177 ( 177 Lu) 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 ( 89 Zr) and 177 Lu 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 177 Lu-DOTA-CTB006 could inhibit tumor growth significantly.