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

作　　者：任超 黄政海 王源 贾琛皓 霍力 REN Chao;HUANG Zhenghai;WANG Yuan;JIA Chenhao;HUO Li(Department of Nuclear Medicine, Peking Union Medical College Hospital, Chinese Academy of Medical Sciences and PekingUnion Medical College,Beijing Key Laboratory of Molecular Targeted Diagnosis and Therapy in Nuclear Medicine,Beijing 100730, China;HTA Co., Ltd., Beijing 102413, China)

机构地区：[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,北京100730 [2]原子高科股份有限公司,北京102413

出　　处：《标记免疫分析与临床》2021年第5期842-846,共5页Labeled Immunoassays and Clinical Medicine

基　　金：中国医学科学院医学与健康科技创新工程(编号:2018-I2M-3-001)。

摘　　要：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.

关 键 词：^(18)F-flortaucipir 正电子发射体层扫描 合成 TAU蛋白 

分 类 号：R817[医药卫生—影像医学与核医学]