Automated sulfur-[18F]fluoride exchange radiolabelling of a prostate specific membrane antigen (PSMA) targeted ligand using the GE FASTlab™ cassette-based platform

Sulfur-[F-18]fluoride exchange radiochemistry is a rapid and convenient method for incorporating fluorine-18 into biologically active molecules. We report a fully automated radiolabelling procedure for the synthesis of a [F-18]SO3F-bearing prostate specific membrane antigen (PSMA) targeted ligand ([F-18](5)) using the GE FASTLab (TM) cassette-based platform in a 25.0 +/- 2.6% radiochemical yield (decay corrected). Uptake in vitro and in vivo correlated with PSMA expression, and the radioligand exhibited favourable biodistribution and pharmacokinetic profiles.

Automated summary

Sulfur-[F-18]fluoride exchange radiochemistry is a rapid and convenient method for incorporating fluorine-18 into biologically active molecules. We reported a fully automated radiolabelling procedure using the GE FASTLab(TM) cassette-based platform to synthesize a [F-18]SO3F-bearing prostate specific membrane antigen (PSMA) targeted ligand ([F-18](5)), which showed favorable biodistribution and pharmacokinetic profiles correlated with PSMA expression.