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<p>Pancreatic cancer exhibits a high mortality rate globally, making precise diagnosis particularly critical. Integrin αvβ6 is a promising target for pancreatic cancer imaging, however, high gastrointestinal uptake has been a significant challenge in the clinical translation of previously developed αvβ6-targeted PET probes. In this study, we produced and purified high-quality <sup>64</sup>Cu using a medical cyclotron, and developed a <sup>64</sup>Cu-labeled αvβ6-targeted molecular imaging probe. Target specificity and binding affinity were evaluated through cell uptake, blocking, and competitive binding assays. Leveraging the relatively long half-life of <sup>64</sup>Cu, multi-time-point Micro-PET/CT imaging was performed to explore the feasibility of obtaining high tumor-to-background ratios with low gastrointestinal uptake at extended time points. <sup>64</sup>Cu-αvβ6 exhibits high affinity for integrin αvβ6 both in vitro and in vivo. Micro-PET/CT imaging in BxPC-3 (αvβ6 +) tumor-bearing nude mice showed good tumor visualization at all time points, with radioactivity uptake still observed at 24 h. Gastrointestinal uptake was significantly reduced after 8 h, yielding high-quality images with favorable tumor-to-background ratios.</p>

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Preclinical evaluation of a 64Cu-labeled αvβ6-targeting peptide PET probe for pancreatic cancer: from radiometal production to molecular probe validation

  • 期刊论文

  • 发表日期：

    2026年2月5日

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  • Xiao Pang,
  • Liujing Zhao,
  • Yanqin Yu,
  • Yousheng Zhan,
  • Yuchuan Zhou,
  • Daiyuan Ma,
  • Suping Li

摘要

Pancreatic cancer exhibits a high mortality rate globally, making precise diagnosis particularly critical. Integrin αvβ6 is a promising target for pancreatic cancer imaging, however, high gastrointestinal uptake has been a significant challenge in the clinical translation of previously developed αvβ6-targeted PET probes. In this study, we produced and purified high-quality 64Cu using a medical cyclotron, and developed a 64Cu-labeled αvβ6-targeted molecular imaging probe. Target specificity and binding affinity were evaluated through cell uptake, blocking, and competitive binding assays. Leveraging the relatively long half-life of 64Cu, multi-time-point Micro-PET/CT imaging was performed to explore the feasibility of obtaining high tumor-to-background ratios with low gastrointestinal uptake at extended time points. 64Cu-αvβ6 exhibits high affinity for integrin αvβ6 both in vitro and in vivo. Micro-PET/CT imaging in BxPC-3 (αvβ6 +) tumor-bearing nude mice showed good tumor visualization at all time points, with radioactivity uptake still observed at 24 h. Gastrointestinal uptake was significantly reduced after 8 h, yielding high-quality images with favorable tumor-to-background ratios.