| Title: |
Preclinical evaluation of [68Ga]Ga-AAZTA-FAPI-46: a novel PET tracer for targeting fibroblast activation protein (FAP) |
| Authors: |
Rizzo R.; Rainone P.; Stefania R.; Belloli S.; Valtorta S.; Coliva A.; Maspero M.; Avalle L.; Capozza M.; Moresco R. M.; D'Alessandria C.; Terreno E. |
| Contributors: |
Rizzo, R; Rainone, P; Stefania, R; Belloli, S; Valtorta, S; Coliva, A; Maspero, M; Avalle, L; Capozza, M; Moresco, R; D'Alessandria, C; Terreno, E |
| Publisher Information: |
Springer Science and Business Media Deutschland GmbH; DE |
| Publication Year: |
2025 |
| Collection: |
Università degli Studi di Milano-Bicocca: BOA (Bicocca Open Archive) |
| Subject Terms: |
AAZTA; FAP; FAPI-46; GALLIUM-68; PET |
| Description: |
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 35min 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. |
| Document Type: |
article in journal/newspaper |
| File Description: |
ELETTRONICO |
| Language: |
English |
| Relation: |
info:eu-repo/semantics/altIdentifier/pmid/40762892; info:eu-repo/semantics/altIdentifier/wos/WOS:001544108700002; volume:10; issue:1; journal:EJNMMI RADIOPHARMACY AND CHEMISTRY; https://hdl.handle.net/10281/579197 |
| DOI: |
10.1186/s41181-025-00375-2 |
| Availability: |
https://hdl.handle.net/10281/579197; https://doi.org/10.1186/s41181-025-00375-2 |
| Rights: |
info:eu-repo/semantics/openAccess ; license:Creative Commons ; license uri:http://creativecommons.org/licenses/by/4.0/ |
| Accession Number: |
edsbas.995BD40B |
| Database: |
BASE |