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

BACKGROUND: Sodium 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 ([(18)F]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. RESULTS: Here we publish an improved radiolabelling method and quality control procedures for high molar activity [(18)F]TFB. The use of ammonium hydroxide for [(18)F]fluoride elution, commercially available boron trifluoride-methanol complex dissolved in acetonitrile as precursor and removal of unreacted [(18)F]fluoride on Florisil solid-phase extraction cartridges resulted in the reliable production of [(18)F]TFB on SYNTHRA and TRACERLAB FX(FN) 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. CONCLUSIONS: A novel automated radiosynthesis procedure for [(18)F]tetrafluoroborate has been developed that provides the radiotracer with high molar activity, suitable for preclinical imaging of NIS reporter gene.