Xing Haiqun, Shi Ximin, Dong Chengyan, Wang Xuezhu, Jin Xiaona, Dang Yonghong, Zhu Wenjia, Yao Shaobo, Li Fang, Huo Li
Abstract
ObjectiveTo prepare 68Ga-fibroblast activation protein inhibitor (FAPI)-04, and evaluate its biodistribution and imaging characteristics in animals and healthy volunteers, in order to investigate the clinical translation potential.
Methods68Ga-FAPI-04 was synthesized by a manual method and its radiolabeling yield, radiochemical purity, and stability (in vivo and in vitro) were analyzed. ICR mice (n=16) were scarified at 5, 30, 60 and 120 min postinjection of 68Ga-FAPI-04 (1.11 MBq) to measure radioactive counts in main organs. The dynamic mircoPET imaging was acquired for 60 min on 3 ICR mice, and tumor imaging capabilities were examined with nude mice bearing HepG2 tumors. Furthermore, 2 healthy volunteers (1 male with age of 64 years, 1 female with age of 56 years) were recruited for the investigation of probe biodistribution in humans. A serial whole-body dynamic PET/CT scan was performed immediately following injection.
Results68Ga-FAPI-04 was synthesized within 20 min with the radiochemical yield of (68.7±4.0)% (decay corrected). The radiochemical purities of 68Ga-FAPI-04 were over 99% and the products were stable for 180 min in vitro and for 90 min in blood. 68Ga-FAPI-04 was mainly cleared through urinary tracts, while other organs only showed mild tracer accumulation. MicroPET imaging showed high uptake of 68Ga-FAPI-04 in the tumor tissue of mice, and the ratio of tumor/liver was 2.14±0.01 (35 min). The PET/CT imaging results of healthy volunteers revealed 68Ga-FAPI-04 could be quickly cleared.
Conclusion68Ga-FAPI-04 has many advantages for PET imaging, such as easy labeling, good stability, quick clearance and low background signals in the liver, which can be used as an attractive PET tracer for detection hepatocellular carcinoma.
Key words:
Serine proteinase inhibitors; Isotope labeling; Gallium; Liver neoplasms; Positron-emission tomography; Mice
Contributor Information
Xing Haiqun
Department of Nuclear Medicine, Peking Union Medical College Hospital, Peking Union Medical College, Chinese Academy of Medical Sciences
Beijing Key Laboratory of Molecular Targeted Diagnosis and Therapy in Nuclear Medicine, Beijing 100730, China
Shi Ximin
Department of Nuclear Medicine, Peking Union Medical College Hospital, Peking Union Medical College, Chinese Academy of Medical Sciences
Beijing Key Laboratory of Molecular Targeted Diagnosis and Therapy in Nuclear Medicine, Beijing 100730, China
Dong Chengyan
GE Healthcare China, Beijing 100176, China
Wang Xuezhu
Department of Nuclear Medicine, Peking Union Medical College Hospital, Peking Union Medical College, Chinese Academy of Medical Sciences
Beijing Key Laboratory of Molecular Targeted Diagnosis and Therapy in Nuclear Medicine, Beijing 100730, China
Jin Xiaona
Department of Nuclear Medicine, Peking Union Medical College Hospital, Peking Union Medical College, Chinese Academy of Medical Sciences
Beijing Key Laboratory of Molecular Targeted Diagnosis and Therapy in Nuclear Medicine, Beijing 100730, China
Dang Yonghong
Department of Nuclear Medicine, Peking Union Medical College Hospital, Peking Union Medical College, Chinese Academy of Medical Sciences
Beijing Key Laboratory of Molecular Targeted Diagnosis and Therapy in Nuclear Medicine, Beijing 100730, China
Zhu Wenjia
Department of Nuclear Medicine, Peking Union Medical College Hospital, Peking Union Medical College, Chinese Academy of Medical Sciences
Beijing Key Laboratory of Molecular Targeted Diagnosis and Therapy in Nuclear Medicine, Beijing 100730, China
Yao Shaobo
Department of PET/CT Diagnostic, Tianjin Medical University General Hospital, Tianjin 300052, China
Li Fang
Department of Nuclear Medicine, Peking Union Medical College Hospital, Peking Union Medical College, Chinese Academy of Medical Sciences
Beijing Key Laboratory of Molecular Targeted Diagnosis and Therapy in Nuclear Medicine, Beijing 100730, China
Huo Li
Department of Nuclear Medicine, Peking Union Medical College Hospital, Peking Union Medical College, Chinese Academy of Medical Sciences
Beijing Key Laboratory of Molecular Targeted Diagnosis and Therapy in Nuclear Medicine, Beijing 100730, China
