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Objective <p>CXCR4 and integrin α<sub>v</sub>β<sub>3</sub> play important roles in tumor biology and are highly expressed in multiple types of tumors. This study aimed to synthesize, preclinically evaluate, and clinically validate a novel dual-targeted PET imaging probe <sup>68</sup>Ga-pentixafor-c(RGDfK) for its potential in imaging tumors.</p> Methods <p>The effects of <sup>68</sup>Ga-pentixafor-c(RGDfK) on cell viability, targeting specificity, and affinity were assessed in the U87MG cells. Micro-PET/CT imaging and biodistribution studies were conducted in U87MG tumor-bearing BALB/c nude mice to evaluate the probe’s in vivo pharmacokinetics. A prospective analysis was conducted on patients who underwent both <sup>68</sup>Ga-pentixafor-c(RGDfK) PET/CT and <sup>18</sup>F-FDG PET/CT. The results obtained from the two imaging modalities were compared.</p> Results <p>In vitro, <sup>68</sup>Ga-pentixafor-c(RGDfK) showed higher uptake activity, targeting specificity, and affinity in U87MG cells than <sup>68</sup>Ga-pentixafor. In vivo, tumor uptake was higher than in normal tissues (<i>P</i> &lt; 0.05), with renal excretion and low hepatobiliary excretion. Clinical results indicated that <sup>68</sup>Ga-pentixafor-c(RGDfK) PET/CT had higher sensitivity, specificity, and accuracy in diagnosing primary and metastatic lesions compared to <sup>18</sup>F-FDG PET/CT (93.1% vs. 74.7%, 79.2% vs. 62.5%, 90.1% vs. 72.1%, and 93.2% vs. 74.5%, 84.7% vs. 78%, 89.7% vs. 75.9%). The tumor-to-background ratio (TBR) at 120&#xa0;min delayed scanning was significantly higher than at 60&#xa0;min (<i>P</i> &lt; 0.05).</p> Conclusion <p><sup>68</sup>Ga-pentixafor-c(RGDfK) PET/CT demonstrated good safety and clinical feasibility in diagnosing tumors, particularly in differentiating benign and malignant lesions when <sup>18</sup>F-FDG PET/CT results are uncertain.</p>

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Synthesis, preclinical evaluation and clinical application of a novel heterodimeric tracer 68Ga-pentixafor-c(RGDfK) for PET-CT imaging

  • 期刊论文

  • 发表日期：

    2025年9月9日

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  • Fan Jia,
  • Dayong Hou,
  • Han Zhang,
  • Huihui You,
  • Liang Cheng,
  • Wei Liu,
  • Yue Zhao,
  • Xinyue Yang,
  • Xinglu Zhou,
  • Miao Yu,
  • Geng Hu,
  • Chenxu Guo,
  • Hongxue Meng,
  • Wanhai Xu,
  • Kezheng Wang

摘要

Objective

CXCR4 and integrin αvβ3 play important roles in tumor biology and are highly expressed in multiple types of tumors. This study aimed to synthesize, preclinically evaluate, and clinically validate a novel dual-targeted PET imaging probe 68Ga-pentixafor-c(RGDfK) for its potential in imaging tumors.

Methods

The effects of 68Ga-pentixafor-c(RGDfK) on cell viability, targeting specificity, and affinity were assessed in the U87MG cells. Micro-PET/CT imaging and biodistribution studies were conducted in U87MG tumor-bearing BALB/c nude mice to evaluate the probe’s in vivo pharmacokinetics. A prospective analysis was conducted on patients who underwent both 68Ga-pentixafor-c(RGDfK) PET/CT and 18F-FDG PET/CT. The results obtained from the two imaging modalities were compared.

Results

In vitro, 68Ga-pentixafor-c(RGDfK) showed higher uptake activity, targeting specificity, and affinity in U87MG cells than 68Ga-pentixafor. In vivo, tumor uptake was higher than in normal tissues (P < 0.05), with renal excretion and low hepatobiliary excretion. Clinical results indicated that 68Ga-pentixafor-c(RGDfK) PET/CT had higher sensitivity, specificity, and accuracy in diagnosing primary and metastatic lesions compared to 18F-FDG PET/CT (93.1% vs. 74.7%, 79.2% vs. 62.5%, 90.1% vs. 72.1%, and 93.2% vs. 74.5%, 84.7% vs. 78%, 89.7% vs. 75.9%). The tumor-to-background ratio (TBR) at 120 min delayed scanning was significantly higher than at 60 min (P < 0.05).

Conclusion

68Ga-pentixafor-c(RGDfK) PET/CT demonstrated good safety and clinical feasibility in diagnosing tumors, particularly in differentiating benign and malignant lesions when 18F-FDG PET/CT results are uncertain.