Synthesis and evaluation of 177Lu-labeled anti-EGFR Fab antibody for lung cancer

IF 1.6 3区 化学 Q3 CHEMISTRY, ANALYTICAL Journal of Radioanalytical and Nuclear Chemistry Pub Date : 2025-03-04 DOI:10.1007/s10967-025-10030-4
Yuan-Yuan Li, Jia-Yan Yu, Tao Wang, Jing Wang, Peng Zhao, Xia Yang, Hong-Yuan Wei, Yue Chen
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Abstract

Fab fragments obtained via enzymatic digestion of full-length antibodies or by gene recombination technology have smaller molecular weight and greater penetration ability. Those advantages make it uniquely suited to deliver radionuclides. In this study, we prepared a Fab fragment from the anti-EGFR antibody Cetuximab and labeled it with 177Lu. The binding activity in vitro and biodistribution in vivo of [177Lu]Lu-DOTA-Fab-Cetuximab were investigated. The [177Lu]Lu-labeled Fab fragment showed improved tumor penetration and faster blood clearance compared to the full-length antibody.

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177lu标记肺癌抗egfr Fab抗体的合成及评价
通过酶切全长抗体或基因重组技术获得的Fab片段分子量更小,穿透能力更强。这些优点使它特别适合运送放射性核素。在本研究中,我们从抗egfr抗体西妥昔单抗中制备了Fab片段,并用177Lu标记。研究了[177Lu]Lu-DOTA-Fab-Cetuximab的体外结合活性和体内生物分布。与全长抗体相比,[177Lu] lu标记的Fab片段表现出更好的肿瘤穿透性和更快的血液清除。
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麦克林
Trypsin–EDTA solution
麦克林
phosphate buffered saline
麦克林
Trypsin–EDTA solution
麦克林
phosphate buffered saline (PBS)
阿拉丁
Citric Acid (CA)
阿拉丁
dimethyl sulfoxide (DMSO)
来源期刊
CiteScore
2.80
自引率
18.80%
发文量
504
审稿时长
2.2 months
期刊介绍: An international periodical publishing original papers, letters, review papers and short communications on nuclear chemistry. The subjects covered include: Nuclear chemistry, Radiochemistry, Radiation chemistry, Radiobiological chemistry, Environmental radiochemistry, Production and control of radioisotopes and labelled compounds, Nuclear power plant chemistry, Nuclear fuel chemistry, Radioanalytical chemistry, Radiation detection and measurement, Nuclear instrumentation and automation, etc.
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