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FAPI-04 PET/CT Using [F-18]AlF Labeling Strategy: Automatic Synthesis, Quality Control, and In Vivo Assessment in Patient

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机构: [1]Radiation Oncology Key Laboratory of Sichuan Province, Sichuan Cancer Hospital, Chengdu, China [2]Institute of Isotope, China Institute of Atomic Energy, Beijing, China
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关键词: fibroblast activation protein inhibitor (FAPI)-PET fibroblast activation protein inhibitor automatic synthesis PET molecular imaging cancer associated fibroblasts invasive ductal carcinoma

摘要:
Ga-68 labeled FAPI is the current standard for FAPI-PET, but its batch activity is limited. [F-18]AlF-NOTA-FAPI-04 is a promising alternative combining the advantages of a chelator-based radiolabeling method with the unique properties of fluorine-18. The objective of this study was to develop a quick automatic method for synthesis of [F-18]AlF-NOTA-FAPI-04 using a AllinOne synthesis system, and perform PET imaging with [F-18]AlF-NOTA-FAPI-04 on patients. [F-18]AlF-NOTA-FAPI-04 was produced, and its quality control was conducted by HPLC equipped with a radioactive detector. [F-18]AlF-NOTA-FAPI-04 PET/CT imaging was performed in normal BALB/c mice (n = 3) and 4T1 breast cancer models (n = 3) to determine its biodistribution. Then [F-18]AlF-NOTA-FAPI-04 and F-18-fluorodeoxyglucose (FDG) PET/CT imaging were performed in an invasive ductal carcinoma patient (female, 54 years old). The synthesis time of [F-18]AlF-NOTA-FAPI-04 was about 25 min, and the radiochemical yield was 26.4 +/- 1.5% (attenuation correction, n = 10). The radiochemical purity was above 99.0% and was above 98.0% after 6 h. The product was colorless transparent solution with pH value of 7.0-7.5, and the specific activity was 49.41 +/- 3.19 GBq/mu mol. PET/CT imaging in mice showed that physiological uptake of [F-18]AlF-NOTA-FAPI-04 was mainly in the biliary system and bladder, and [F-18]AlF-NOTA-FAPI-04 highly concentrated in tumor xenografts. PET/CT imaging in the patient showed that [F-18]AlF-NOTA-FAPI-04 obtained high tumor background ratio (TBR) value of 8.44 in segment V and VI, while TBR value was 2.55 by F-18-FDG. [F-18]AlF-NOTA-FAPI-04 could be synthesized with high radiochemical yield and batch production by AllinOne module and show excellent diagnosis performance in cancer patients.

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基金编号: 2019YJ0574 2020YFS0421

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出版当年[2021]版:
大类 | 3 区 医学
小类 | 3 区 肿瘤学
最新[2023]版:
大类 | 3 区 医学
小类 | 3 区 肿瘤学
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Q2 ONCOLOGY
最新[2023]版:
Q2 ONCOLOGY

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第一作者机构: [1]Radiation Oncology Key Laboratory of Sichuan Province, Sichuan Cancer Hospital, Chengdu, China [2]Institute of Isotope, China Institute of Atomic Energy, Beijing, China
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