![]() In an organ biodistribution study of patients, Al 18F-NOTA-FAPI showed a lower SUVmean than 2-fluoro-2-deoxy-D-glucose (2-FDG) in most organs, especially in the liver (1.1 ± 0.2 vs. In U87MG tumour-bearing mice, Al 18F-NOTA-FAPI showed good tumour detection efficacy based on the results of micro PET/CT imaging and biodistribution studies. The whole body effective dose of Al 18F-NOTA-FAPI was estimated to be 1.24E - 02 mSv/MBq, which was lower than several other FAPI probes ( 68Ga-FAPI-04, 68Ga-FAPI-46 and 68Ga-FAPI-74). The radiolabelling yield of Al 18F-NOTA-FAPI was 33.8 ± 3.2% using manual synthesis (n = 10), with a radiochemical purity over 99% and the specific activity of 9.3-55.5 MBq/nmol. After the approval of the ethical committee, the Al 18F-NOTA-FAPI probe was translated into the clinic for PET/CT imaging of the first 10 cancer patients. The biodistribution, pharmacokinetics, radiation dosimetry and tumour imaging efficacy of the Al 18F-NOTA-FAPI probe were researched in healthy Kunming (KM) and/or U87MG model mice. Cell uptake and competitive binding assays were completed with the U87MG and A549 cell lines to evaluate the affinity and specificity of the Al 18F-NOTA-FAPI probe. The radiolabelling procedure of Al 18F-NOTA-FAPI was optimized. The tumour detection efficacy of Al 18F-NOTA-FAPI was further validated in both preclinical and clinical translational studies. ![]() this study, a novel aluminium-fluoride (Al 18F)-labelled 1,4,7‑triazacyclononane-N,N',N″-triacetic acid (NOTA)-conjugated fibroblast activation protein inhibitor (FAPI) probe, named Al 18F-NOTA-FAPI, was developed for fibroblast activation protein (FAP)-targeted tumour imaging it could deliver hundreds of millicuries of radioactivity using automated synthesis. 5 Key Laboratory of Carcinogenesis and Translational Research, Ministry of Education/Beijing, NMPA Key Laboratory for Research and Evaluation of Radiopharmaceuticals, Department of Nuclear Medicine, Peking University Cancer Hospital & Institute, No. 4 Institute of Medical Technology, Peking University Health Science Center, Beijing, 100191, China.
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