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

被引：43
作者：
Jiang, Xiao [1 ,2 ]
Wang, Xiaoxiong [1 ]
Shen, Taipeng [1 ]
Yao, Yutang [1 ]
Chen, Meihua [1 ]
Li, Zeng [1 ]
Li, Xiuli [1 ]
Shen, Jiaqi [1 ]
Kou, Ying [1 ]
Chen, Shirong [1 ]
Zhou, Xing [1 ]
Luo, Zhifu [2 ]
Cheng, Zhuzhong [1 ]
机构：
[1] Sichuan Canc Hosp, Radiat Oncol Key Lab Sichuan Prov, Chengdu, Peoples R China
[2] China Inst Atom Energy, Inst Isotope, Beijing, Peoples R China
来源：
FRONTIERS IN ONCOLOGY | 2021年 / 11卷
关键词：
fibroblast activation protein inhibitor (FAPI)-PET; fibroblast activation protein inhibitor; automatic synthesis; PET molecular imaging; cancer associated fibroblasts; invasive ductal carcinoma;
D O I：
10.3389/fonc.2021.649148
中图分类号：
R73 [肿瘤学];
学科分类号：
100214 ;
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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页数：9
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