Preclinical evaluation and pilot clinical study of[18F]AlF-labeled FAPI-tracer for PET imaging of ca

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In recent years,fibroblast activation protein(FAP)has emerged as an attractive target for the diag-nosis and radiotherapy of cancers using FAP-specific radioligands.Herein,we aimed to design a novel 18F-labeled FAP tracer([18F]A1F-P-FAPI)for FAP imaging and evaluated its potential for clinical application.The[18F]A1F-P-FAPI novel tracer was prepared in an automated manner within 42 min with a non-decay cor-rected radiochemical yield of 32±6%(n=8).Among A549-FAP cells,[1 8F]A1F-P-FAPI demonstrated spe-cific uptake,rapid internalization,and low cellular efflux.Compared to the patent tracer[18F]FAPI-42,[18F]A1F-P-FAPI exhibited lower levels of cellular efflux in the A549-FAP cells and higher stability in vivo.Micro-PET imaging in the A549-FAP tumor model indicated higher specific tumor uptake of[18F]A1F-P-FAPI(7.0±1.0%ID/g)compared to patent tracers[18F]FAPI-42(3.2±0.6%ID/g)and[68Ga]Ga-FAPI-04(2.7±0.5%ID/g).Furthermore,in an initial diagnostic application in a patient with nasopharyngeal cancer,[18F]A1F-P-FAPI and[18F]FDG PET/CT showed comparable results for both primary tumors and lymph node metastases.These results suggest that[18F]A1F-P-FAPI can be conveniently prepared,with promising charac-teristics in the preclinical evaluation.The feasibility of FAP imaging was demonstrated using PET studies.
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