High molar activity [18F]tetrafluoroborate synthesis for sodium iodide symporter imaging by PET

EJNMMI Radiopharmacy and Chemistry

Methodology

Piotr Dzien¹  Agata Mackintosh¹  Gavin Brown¹  Gaurav Malviya¹  Dmitry Soloviev¹  David Lewis² 

[1] Cancer Research UK Beatson Institute, Garscube Estate, Switchback Road, G61 1BD, Glasgow, UK;Cancer Research UK Beatson Institute, Garscube Estate, Switchback Road, G61 1BD, Glasgow, UK;School of Cancer Sciences, University of Glasgow, Garscube Estate, Switchback Road, G611QH, Glasgow, UK;

关键词: NIS;    Reporter gene imaging;    Tetrafluoroborate;    Fluorine-18;    Positron emission tomography;    Sodium iodide symporter;   

DOI  :  10.1186/s41181-022-00185-w

 received in 2022-11-04, accepted in 2022-12-02,  发布年份 2022

来源: Springer

【 摘 要 】

BackgroundSodium iodide symporter (NIS) imaging by positron emission tomography (PET) is gaining traction in nuclear medicine, with an increasing number of human studies being published using fluorine-18 radiolabelled tetrafluoroborate ([18F]TFB). Clinical success of any radiotracer relies heavily on its accessibility, which in turn depends on the availability of robust radiolabelling procedures providing a radiotracer in large quantities and of high radiopharmaceutical quality.ResultsHere we publish an improved radiolabelling method and quality control procedures for high molar activity [18F]TFB. The use of ammonium hydroxide for [18F]fluoride elution, commercially available boron trifluoride-methanol complex dissolved in acetonitrile as precursor and removal of unreacted [18F]fluoride on Florisil solid-phase extraction cartridges resulted in the reliable production of [18F]TFB on SYNTHRA and TRACERLAB FXFN automated synthesizers with radiochemical yields in excess of 30%, radiochemical purities in excess of 98% and molar activities in the range of 34–217 GBq/µmol at the end of synthesis. PET scanning of a mouse lung tumour model carrying a NIS reporter gene rendered images of high quality and improved sensitivity.ConclusionsA novel automated radiosynthesis procedure for [18F]tetrafluoroborate has been developed that provides the radiotracer with high molar activity, suitable for preclinical imaging of NIS reporter gene.

【 授权许可】

CC BY   
© The Author(s) 2022

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