Abstract
68Ga labeled FAPI is the current standard for FAPI-PET, but its batch activity is limited. [18F]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 [18F]AlF-NOTA-FAPI-04 using a AllinOne synthesis system, and perform PET imaging with [18F]AlF-NOTA-FAPI-04 on patients. [18F]AlF-NOTA-FAPI-04 was produced, and its quality control was conducted by HPLC equipped with a radioactive detector. [18F]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 [18F]AlF-NOTA-FAPI-04 and 18F-fluorodeoxyglucose (FDG) PET/CT imaging were performed in an invasive ductal carcinoma patient (female, 54 years old). The synthesis time of [18F]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/μmol. PET/CT imaging in mice showed that physiological uptake of [18F]AlF-NOTA-FAPI-04 was mainly in the biliary system and bladder, and [18F]AlF-NOTA-FAPI-04 highly concentrated in tumor xenografts. PET/CT imaging in the patient showed that [18F]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 18F-FDG. [18F]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.
Highlights
Fibroblast activation protein (FAP) is a widely distributed antigen in epithelial tumor cells, and FAP is closely related to the formation and maintenance of epithelial cell interstitial state, multidrug resistance and immunosuppression [1,2,3]
Preliminary results show that FAP targeted positron emission molecular imaging probes accumulate in sarcoma, esophageal cancer, breast cancer, cholangiocarcinoma, and lung cancer with a standardized uptake value (SUV) over 12
The final product was confirmed by comparing product with NOTA-fibroblast activation protein inhibitor (FAPI)-04
Summary
Fibroblast activation protein (FAP) is a widely distributed antigen in epithelial tumor cells, and FAP is closely related to the formation and maintenance of epithelial cell interstitial state, multidrug resistance and immunosuppression [1,2,3]. FAP was expressed in 90% epithelial tumor tissues and Synthesis of [18F]AlF-FAPI-04. FAP is a broad-spectrum tumor target with strong specificity and good stability. Preliminary results show that FAP targeted positron emission molecular imaging probes accumulate in sarcoma, esophageal cancer, breast cancer, cholangiocarcinoma, and lung cancer with a standardized uptake value (SUV) over 12. FAP targeted positron emission molecular imaging probes have several advantages comparing with 18F-FDG such as unrelated to blood glucose, broader cancer spectrum, higher tumor to background ratio (higher than 3–6) and specificity. Molecular imaging probes targeting FAP are becoming a promising broad cancer spectrum PET tracer
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