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<p>This study reports the synthesis and in vitro as well as in vivo evaluation of [<sup>99m</sup>Tc]Tc–octapa–necitumumab for targeted imaging of squamous non-small cell lung cancer (NSCLC). Necitumumab was conjugated with p-SCN-Bn–H<sub>4</sub>Octapa and efficiently labeled with technetium-99m under mild conditions, yielding excellent radiochemical purity and favorable in vitro stability. The [<sup>99m</sup>Tc]Tc–octapa–necitumumab presented strong EGFR-specific in vitro binding and internalization in HCC827 cells. Biodistribution studies in tumor-bearing mice showed a tumor uptake of 5.85 ± 0.1% ID/g at 4&#xa0;h post-injection, with promising tumor-to-organ ratios, including 2.07 ± 0.18 for tumor-to-blood, 2.49 ± 0.20 for tumor-to-blocked tumor, 2.21 ± 0.18 for tumor-to-liver, 2.02 ± 0.15 for tumor-to-lung, 1.14 ± 0.06 for tumor-to-kidney, and 3.44 ± 0.57 for tumor-to-muscle. Rabbit SPECT studies validated selective tumor localization with insignificant off-target accumulation. These findings categorize [<sup>99m</sup>Tc]Tc–octapa–necitumumab as a novel radiotracer with potential for EGFR-targeted imaging in squamous NSCLC.</p>

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Synthesis and evaluation of [99mTc]Tc–octapa–necitumumab for targeted imaging of squamous non-small cell lung cancer

  • 期刊论文

  • 发表日期：

    2025年8月30日

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  • Saba Shirin,
  • Syed Qaiser Shah,
  • Ralph Santos-Oliveira,
  • Derya Ilem-Ozdemir,
  • Muhammad Imran,
  • Nadeem Ahmed Lodhi

摘要

This study reports the synthesis and in vitro as well as in vivo evaluation of [99mTc]Tc–octapa–necitumumab for targeted imaging of squamous non-small cell lung cancer (NSCLC). Necitumumab was conjugated with p-SCN-Bn–H4Octapa and efficiently labeled with technetium-99m under mild conditions, yielding excellent radiochemical purity and favorable in vitro stability. The [99mTc]Tc–octapa–necitumumab presented strong EGFR-specific in vitro binding and internalization in HCC827 cells. Biodistribution studies in tumor-bearing mice showed a tumor uptake of 5.85 ± 0.1% ID/g at 4 h post-injection, with promising tumor-to-organ ratios, including 2.07 ± 0.18 for tumor-to-blood, 2.49 ± 0.20 for tumor-to-blocked tumor, 2.21 ± 0.18 for tumor-to-liver, 2.02 ± 0.15 for tumor-to-lung, 1.14 ± 0.06 for tumor-to-kidney, and 3.44 ± 0.57 for tumor-to-muscle. Rabbit SPECT studies validated selective tumor localization with insignificant off-target accumulation. These findings categorize [99mTc]Tc–octapa–necitumumab as a novel radiotracer with potential for EGFR-targeted imaging in squamous NSCLC.