Nuclear Techniques ›› 2020, Vol. 43 ›› Issue (8): 80301-080301.doi: 10.11889/j.0253-3219.2020.hjs.43.080301

• NUCLEAR CHEMISTRY, RADIOCHEMISTRY, RADIOPHARMACEUTICALS AND NUCLEAR MEDICINE • Previous Articles     Next Articles

Automated preparation of neuroinflammation imaging tracer 18F-PBR06

Hongwen QIAO1,Ze LI1,Shu'an CHEN1,Zhigang LIANG1,2,Jie LU1,3   

  1. 1.Department of Nuclear Medicine, Xuanwu Hospital Capital Medical University, Beijing 100053, China
    2.Information Center, Xuanwu Hospital Capital Medical University, Beijing 100053, China
    3.Department of Radiology, Xuanwu Hospital Capital Medical University, Beijing 100053, China
  • Received:2020-04-13 Revised:2020-06-23 Online:2020-08-15 Published:2020-08-12
  • About author:QIAO Hongwen, male, born in 1986, graduated from Beijing Normal University with a doctoral degree in 2012, Chemist, technician, focusing on radiochemistry
  • Supported by:
    National Natural Science Foundation of China(81701726);the National Key Research and Development Program of China

Abstract: Background

The 18 kDa translocator protein (TSPO) is an important neuroinflammatory imaging target for neurological diseases. 18F-PBR06 is a second-generation TSPO targeting agent with suitable biological properties, which has been used for human imaging.

Purpose

The study aims to promote the application of the imaging tracer 18F-PBR06 in research and clinical studies.

Methods

The disposable cassette system and process sequence for the Neptis Perform synthesizer was developed to produce 18F-PBR06. The quality control inspection method and specification for the product were established with reference to the Chinese Pharmacopoeia (2015 edition). The safety of the product was confirmed by the abnormal toxicity test following the requirements of the Chinese Pharmacopoeia (2015 edition). The biodistribution of the product was evaluated with normal mice. Based on the above research, the preliminary study of 18F-PBR06 PET imaging on healthy controls and patients with multiple sclerosis was performed.

Results

18F-PBR06 is successfully prepared with a radiochemical yield of (32±5)% (decay corrected, n=20), radiochemical purity >99%, specific activity >111 GBq?μmol-1, and total time is (54±2) min (n=20). The product quality control tests and abnormal toxicity inspection are in compliance with the requirements of the Chinese Pharmacopoeia. The biodistribution study shows that high uptake is found in the organs of high densities of TSPO, including lung, kidney, spleen and heart. Preliminary PET/CT imaging research results show that the radioactive uptake in thalamus and pons of multiple sclerosis patient brain is significantly higher than that of health controls, and the white matter uptake is moderately increased.

Conclusions

The above results prove that 18F-PBR06 can be prepared through the process developed in this study. The product meets the requirements of research and clinical applications. This study makes favorable preparations for further clinical neuroinflammation PET imaging studies.

Key words: Neuroinflammation, PET imaging, 18F-PBR06, Automated preparation, Multiple sclerosis

CLC Number: 

  • TL92+3