Rizzo Rebecca, Rainone Paolo, Stefania Rachele, Belloli Sara, Valtorta Silvia, Coliva Angela, Maspero Marco, Avalle Lidia, Capozza Martina, Moresco Rosa Maria, D'Alessandria Calogero, Terreno Enzo
Center for Biotechnology and Translational Medicine, University of Turin, Piazza Nizza 44/bis, Turin, 10126, Italy.
Nuclear Medicine and PET Cyclotron Unit, IRCCS Ospedale San Raffaele, Milano, Italy.
EJNMMI Radiopharm Chem. 2025 Aug 5;10(1):51. doi: 10.1186/s41181-025-00375-2.
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.
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.
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.
本研究的目的是证明与FAPI-46衍生的FAP抑制剂偶联并标记有镓-68的AAZTA螯合剂作为潜在PET示踪剂的适用性。
在室温下以高放射化学产率实现了镓-68放射性标记。新的示踪剂在不同介质中稳定，在体外和体内均显示出与FAP蛋白的特异性结合，以及合适的生物分布和清除率。在荷4T1肿瘤小鼠中发现示踪剂的肿瘤摄取率高（注射后35分钟为1.01±0.12 SUV），阻断实验证明了高靶标特异性。
在FAPI-46部分用AAZTA配体替代DOTA螯合剂，使得PET示踪剂在室温下能够快速进行放射性标记，而不会影响生物分布特性，如清除率和FAP介导的肿瘤摄取，反而扩大了示踪剂的适用性。
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