tau蛋白PET显像剂^(18)F-flortaucipir的自动化合成及初步临床验证

Automated Synthesis and Preliminary Clinical Validation of ^(18)F-flortaucipir for Tau Protein PET Imaging

目的使用TRACERlab^(TM)FX2 N型氟多功能合成模块合成器自动化合成tau蛋白正电子显像剂^(18)F-flortaucipir,并研究其临床应用。方法在TRACERlab^(TM) FX2 N型合成器上,前体与氟(^(18)F)离子发生亲核反应后,依次经过在线溶剂交换、高效液相色谱法(high performance liquid chromatography,HPLC)分离及固相萃取后获得^(18)F-flortaucipir,进行药物质量控制和临床应用。结果^(18)F-flortaucipir合成时间为70min,不校正合成效率为(22.27±5.27)%(n=10),产品放射性化学纯度大于95%,并在阿尔茨海默病(Alzheimer’s disease,AD)患者脑部病变区明显摄取。结论TRACERlabTM FX2 N型合成器生产^(18)F-flortaucipir方法具有合成速度快、步骤少、自动化程度高的优点,可在临床上广泛应用。

Objective The tau protein imaging agent^(18)F-flortaucipir was synthesized automatically using TRACERlab^(TM) FX2 N radiosynthesis module and its clinical application was studied.Methods^(18)F-flortaucipir was produced by on-line solvent exchange,high performance liquid chromatography(HPLC)and solid phase extraction after nucleophilic reaction between the precursor and[^(18)F]Fluoride on TRACERlab^(TM) FX2 N radiosynthesis module.Results The synthesis duration of^(18)F-flortaucipir was 70 min,while the no-corrected productive rate of radiochemistry was(22.27±5.27)%(n=10).The radiochemistry purity was over 95%,and the uptake was clearly in the brain lesions of Alzheimer’s disease patient.Conclusion The methodology of^(18)F-flortaucipir by TRACERlabTM FX2 N radiosynthesis module offers the advantage of faster synthesis in relatively fewer steps,which can facilitate a broad clinical applications.