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<p>This study aimed to develop and evaluate [<sup>64</sup>Cu]Cu-PSMA-Q as a novel positron emission tomography (PET) imaging agent for prostate cancer detection, assessing its diagnostic accuracy and clinical applicability in comparison to [<sup>18</sup>F]FDG PET imaging. [<sup>64</sup>Cu]Cu-PSMA-Q was synthesized, purified, and subjected to comprehensive quality control. Its binding affinity, cellular uptake, and internalization were assessed in vitro using prostate-specific membrane antigen (PSMA)-positive LNCaP C4-2B cells. In vivo toxicity studies were conducted in 12 mouse models (6 per group). Small-animal PET/CT (positron emission tomography/computed tomography) imaging and biodistribution studies were performed on tumor-bearing mice. Clinical evaluation involved PET/CT imaging with [<sup>64</sup>Cu]Cu-PSMA-Q in 29 prostate cancer patients, with comparative analysis against [<sup>18</sup>F]FDG PET/CT imaging. Radiation dosimetry was calculated using OLINDA/EXM software, and diagnostic performance metrics, including maximum standardized uptake value (SUVmax), mean standardized uptake value (SUVmean), and tumor-to-background ratio, were analyzed using SPSS v24.0, with <i>P</i> &lt; 0.05 considered statistically significant. Comparative analyses utilized t-tests or Mann–Whitney <i>U</i> tests as appropriate. [<sup>64</sup>Cu]Cu-PSMA-Q achieved over 99% radiochemical purity and a specific activity of 20.5<b> ± </b>1&#xa0;GBq/μmol. In vitro studies demonstrated a dissociation constant (Kd) of 4.083&#xa0;nM, along with high cellular uptake and internalization in LNCaP C4-2B cells. No significant toxicity was observed in mouse models. Small -animal PET/CT imaging revealed peak tumor uptake at 4&#xa0;h post-injection in LNCaP C4-2B tumor xenografts. In clinical evaluations, [<sup>64</sup>Cu]Cu-PSMA-Q PET/CT detected more lesions than [<sup>18</sup>F]FDG, with significantly higher SUVmax, SUVmean, and tumor-to-background ratios. The mean effective radiation dose was calculated as 4.48 ± 0.99&#xa0;mSv. [<sup>64</sup>Cu]Cu-PSMA-Q PET/CT demonstrated superior lesion detection and higher tumor-to-background ratios compared to [<sup>18</sup>F]FDG PET/CT for prostate cancer visualization. Its advantageous properties, including a favorable half-life, excellent safety profile, and enhanced diagnostic accuracy, support its potential for broad clinical adoption. This study establishes a foundation for further validation of [<sup>64</sup>Cu]Cu-PSMA-Q in prostate cancer management.</p>

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Preclinical and clinical evaluation of [64Cu]Cu-PSMA-Q PET/CT for prostate cancer detection and its comparison with [18F]FDG imaging

  • 期刊论文

  • 出版模式：

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  • 发表日期：

    2025年4月25日

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  • Fei Chen,
  • Hao Zhang,
  • Yousheng Zhan,
  • Xiaohong Huang,
  • Zongxi He,
  • Daiyuan Ma,
  • Tielong Tang,
  • Suping Li

摘要

This study aimed to develop and evaluate [64Cu]Cu-PSMA-Q as a novel positron emission tomography (PET) imaging agent for prostate cancer detection, assessing its diagnostic accuracy and clinical applicability in comparison to [18F]FDG PET imaging. [64Cu]Cu-PSMA-Q was synthesized, purified, and subjected to comprehensive quality control. Its binding affinity, cellular uptake, and internalization were assessed in vitro using prostate-specific membrane antigen (PSMA)-positive LNCaP C4-2B cells. In vivo toxicity studies were conducted in 12 mouse models (6 per group). Small-animal PET/CT (positron emission tomography/computed tomography) imaging and biodistribution studies were performed on tumor-bearing mice. Clinical evaluation involved PET/CT imaging with [64Cu]Cu-PSMA-Q in 29 prostate cancer patients, with comparative analysis against [18F]FDG PET/CT imaging. Radiation dosimetry was calculated using OLINDA/EXM software, and diagnostic performance metrics, including maximum standardized uptake value (SUVmax), mean standardized uptake value (SUVmean), and tumor-to-background ratio, were analyzed using SPSS v24.0, with P < 0.05 considered statistically significant. Comparative analyses utilized t-tests or Mann–Whitney U tests as appropriate. [64Cu]Cu-PSMA-Q achieved over 99% radiochemical purity and a specific activity of 20.5 ± 1 GBq/μmol. In vitro studies demonstrated a dissociation constant (Kd) of 4.083 nM, along with high cellular uptake and internalization in LNCaP C4-2B cells. No significant toxicity was observed in mouse models. Small -animal PET/CT imaging revealed peak tumor uptake at 4 h post-injection in LNCaP C4-2B tumor xenografts. In clinical evaluations, [64Cu]Cu-PSMA-Q PET/CT detected more lesions than [18F]FDG, with significantly higher SUVmax, SUVmean, and tumor-to-background ratios. The mean effective radiation dose was calculated as 4.48 ± 0.99 mSv. [64Cu]Cu-PSMA-Q PET/CT demonstrated superior lesion detection and higher tumor-to-background ratios compared to [18F]FDG PET/CT for prostate cancer visualization. Its advantageous properties, including a favorable half-life, excellent safety profile, and enhanced diagnostic accuracy, support its potential for broad clinical adoption. This study establishes a foundation for further validation of [64Cu]Cu-PSMA-Q in prostate cancer management.