Preclinical and clinical translation research of 68Ga-labeled fibroblast activation protein inhibitor for PET imaging
10.3760/cma.j.cn321828-20191101-00249
- VernacularTitle:68Ga标记成纤维细胞活化蛋白抑制剂的临床前实验及初步临床转化研究
- Author:
Haiqun XING
1
;
Ximin SHI
;
Chengyan DONG
;
Xuezhu WANG
;
Xiaona JIN
;
Yonghong DANG
;
Wenjia ZHU
;
Shaobo YAO
;
Fang LI
;
Li HUO
Author Information
1. 中国医学科学院、北京协和医学院北京协和医院核医学科、核医学分子靶向诊疗北京市重点实验室 100730
- From:
Chinese Journal of Nuclear Medicine and Molecular Imaging
2020;40(8):480-485
- CountryChina
- Language:Chinese
-
Abstract:
Objective:To 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. Methods:68Ga-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. Results:68Ga-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. Conclusion:68Ga-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.
