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Background <p>The aim of this work was to demonstrate the suitability of AAZTA chelator conjugated to a FAPI-46-derived FAP inhibitor and labelled with gallium-68 as a potential PET tracer.</p> Results <p>Gallium-68 radiolabelling was achieved with high radiochemical yield at room temperature. The new tracer was stable in different media, showing specific binding to FAP-protein both in vitro and in vivo, and a suitable biodistribution and clearance. High tumor uptake of the tracer (1.01 ± 0.12 SUV 35&#xa0;min p.i.) was found in 4T1-tumor bearing mice, and blocking experiments demonstrated the high target specificity.</p> Conclusion <p>The substitution of the DOTA chelator with the AAZTA ligand on FAPI-46 moiety allowed a fast radiolabelling at room temperature of the PET tracer without influencing the biodistribution properties, such as clearance and FAP-mediated tumor uptake, but rather expanding the tracer applicability.</p>

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Preclinical evaluation of [68Ga]Ga-AAZTA-FAPI-46: a novel PET tracer for targeting fibroblast activation protein (FAP)

  • 期刊论文

  • 出版模式：

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  • 发表日期：

    2025年8月5日

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  • Rebecca Rizzo,
  • Paolo Rainone,
  • Rachele Stefania,
  • Sara Belloli,
  • Silvia Valtorta,
  • Angela Coliva,
  • Marco Maspero,
  • Lidia Avalle,
  • Martina Capozza,
  • Rosa Maria Moresco,
  • Calogero D’Alessandria,
  • Enzo Terreno

摘要

Background

The aim of this work was to demonstrate the suitability of AAZTA chelator conjugated to a FAPI-46-derived FAP inhibitor and labelled with gallium-68 as a potential PET tracer.

Results

Gallium-68 radiolabelling was achieved with high radiochemical yield at room temperature. The new tracer was stable in different media, showing specific binding to FAP-protein both in vitro and in vivo, and a suitable biodistribution and clearance. High tumor uptake of the tracer (1.01 ± 0.12 SUV 35 min p.i.) was found in 4T1-tumor bearing mice, and blocking experiments demonstrated the high target specificity.

Conclusion

The substitution of the DOTA chelator with the AAZTA ligand on FAPI-46 moiety allowed a fast radiolabelling at room temperature of the PET tracer without influencing the biodistribution properties, such as clearance and FAP-mediated tumor uptake, but rather expanding the tracer applicability.