Rapid and specific immunoPET imaging of Nectin-4 in gastric cancer and non-small cell lung cancer using [64Cu]Cu-NOTA-EV-F(ab')2.

Purpose: This study aimed to develop and evaluate [64Cu]Cu-NOTA-EV-F(ab')2 as a rapid and specific immunoPET imaging probe targeting Nectin-4 in gastric cancer (GC) and non-small cell lung cancer (NSCLC). Materials and methods: F(ab')2 fragments were generated from enfortumab vedotin (EV) using IdeS...

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Publicado en:European Journal of Nuclear Medicine & Molecular Imaging Vol. 53; no. 1; pp. 619 - 633
Autores principales: Huang, Wenpeng, Sun, Xinyao, Li, Xiaoyan, Hsu, Jessica C., Qiu, Yongkang, DeLuca, Molly C., Engle, Jonathan W., Li, Liming, Lu, Jun, Wang, Tianyao, Kang, Lei, Cai, Weibo
Formato: Journal Article
Publicado: Springer Nature Dec2025
Acceso en línea:Ver este registro en EBSCOhost
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      dt: Dec2025
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      pub: Springer Nature
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        10.1007/s00259-025-07402-z
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        atl: Rapid and specific immunoPET imaging of Nectin-4 in gastric cancer and non-small cell lung cancer using [64Cu]Cu-NOTA-EV-F(ab')2.
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        au:
          Huang, Wenpeng
          Sun, Xinyao
          Li, Xiaoyan
          Hsu, Jessica C.
          Qiu, Yongkang
          DeLuca, Molly C.
          Engle, Jonathan W.
          Li, Liming
          Lu, Jun
          Wang, Tianyao
          Kang, Lei
          Cai, Weibo
        affil: https://ror.org/02z1vqm45 Department of Nuclear Medicine, Peking University First Hospital, 100034, Beijing, China
      sug:
      ab: Purpose: This study aimed to develop and evaluate [64Cu]Cu-NOTA-EV-F(ab')2 as a rapid and specific immunoPET imaging probe targeting Nectin-4 in gastric cancer (GC) and non-small cell lung cancer (NSCLC). Materials and methods: F(ab')2 fragments were generated from enfortumab vedotin (EV) using IdeS protease and conjugated with p-SCN-Bn-NOTA for radiolabeling with 64CuCl2. The radiochemical yield was 85.40 ± 2.43% (n = 5). In vitro binding affinity and specificity were assessed via flow cytometry and cell uptake assays using Nectin-4-positive (NCI-N87, H1975) and Nectin-4-low (HGC-27, H520) cell lines. In vivo PET imaging and biodistribution studies were conducted in murine models of GC and NSCLC to evaluate tumor targeting efficiency and tracer pharmacokinetics. Results: [64Cu]Cu-NOTA-EV-F(ab')2 demonstrated rapid tumor accumulation, with peak uptake observed at 4 h post-injection (10.23 ± 0.70%ID/g in NCI-N87 tumors, 3.03 ± 0.35%ID/g in HGC-27, 11.56 ± 1.12%ID/g in H1975, 2.77 ± 0.47%ID/g in H520). Compared to full-length EV, the tracer exhibited faster blood clearance and reduced off-target uptake. Blocking with excess EV-F(ab')2 significantly reduced subsequent tumor uptake (6.27 ± 0.49%ID/g in NCI-N87, P = 0.0029; 5.23 ± 0.31%ID/g in H1975, P = 0.00074), confirming Nectin-4 specificity. Ex vivo biodistribution analysis supported high tumor retention consistent with in vivo imaging findings. Conclusions: [64Cu]Cu-NOTA-EV-F(ab')2 offers rapid, specific, and high-contrast immunoPET imaging of Nectin-4-expressing tumors in GC and NSCLC models, highlighting its potential as a non-invasive diagnostic tool for Nectin-4-targeted cancer imaging.
      pubtype: Academic Journal
      doctype: Journal Article
      ougenre: Article
    language: English
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