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<p>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 <sup>177</sup>Lu. The binding activity in vitro and biodistribution in vivo of [<sup>177</sup>Lu]Lu-DOTA-Fab-Cetuximab were investigated. The [<sup>177</sup>Lu]Lu-labeled Fab fragment showed improved tumor penetration and faster blood clearance compared to the full-length antibody.</p>

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

  • 期刊论文

  • 发表日期：

    2025年3月4日

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  • Yuan-Yuan Li,
  • Jia-Yan Yu,
  • Tao Wang,
  • Jing Wang,
  • Peng Zhao,
  • Xia Yang,
  • Hong-Yuan Wei,
  • Yue Chen

摘要

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.