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Volume 18, Issue 1
  • ISSN: 1874-4710
  • E-ISSN: 1874-4729

Abstract

Background

In this study, [64Cu]Cu-NODAGA-RGD-BBN was prepared and its preclinical assessments were evaluated for PET imaging of GRPR overexpressing tumors.

Methods

NODAGA-RGD-BBN heterodimer peptide was successfully labeled with cyclotron-produced copper-64 at optimized conditions. The radiochemical purity of the radiotracer was checked by HPLC and RTLC methods. The stability of the radiolabeled compound was assessed in PBS (4°C) and in human blood serum (37°C). Binding affinity and internalization of [64Cu]Cu-NODAGA-RGD-BBN were studied on PC3, LNCaP, and CHO cell lines. The biodistribution of the radiotracer was evaluated in normal and tumor-bearing mice.

Results

[64Cu]Cu-NODAGA-RGD-BBN was prepared with radiochemical purity >99 ± 0.7% (HPLC/ITLC) and specific activity of 18.5 ± 2.2 TBq/mmol. The radiotracer showed high stability in PBS (95 ± 1.05%) and in human blood serum (96 ± 1.24%) and, high affinity to the GRP expressing tumor cells. [64Cu]Cu-NODAGA-RGD-BBN showed hydrophilic (log = -1.14) and agonistic nature. The biodistribution and imaging studies demonstrated high uptake at the tumor site at all intervals post-injection and 3-4 h post-injection can be considered an appropriate time of imaging.

Conclusion

The results indicated that [64Cu]Cu-NODAGA-RGD-BBN radiolabeled heterodimer peptide can be considered as a high-potential agent for PET imaging of GRPR-overexpressing tumors.

© 2025 Bentham Science Publishers
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/content/journals/crp/10.2174/0118744710246897240209070005
2025-03-01
2025-06-01

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/content/journals/crp/10.2174/0118744710246897240209070005
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Development of [64Cu]Cu-NODAGA-RGD-BBN as a Novel Radiotracer for Dual Integrin and GRPR-targeted Tumor PET Imaging
Current Radiopharmaceuticals 18, 37 (2025); https://doi.org/10.2174/0118744710246897240209070005
/content/journals/crp/10.2174/0118744710246897240209070005
/content/journals/crp/10.2174/0118744710246897240209070005
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  • Article Type:     Research Article
Keyword(s): GRPR positive tumors; heterodimer peptide; human blood serum; imaging; PET; tumor cells

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