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

Zixuan Yang; Chris Barnes; Juozas Domarkas; Joanna Koch-Paszkowski; John Wright; Ala Amgheib; Isaline Renard; Ruisi Fu; Stephen Archibald; Eric O. Aboagye; Louis Allott

doi:10.1039/D3RE00307H

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

Zixuan Yang,^b Chris Barnes,^b Juozas Domarkas,^a Joanna Koch-Paszkowski,^a John Wright,^a Ala Amgheib,^b Isaline Renard,

^a Ruisi Fu,^b Stephen Archibald,

^a Eric O. Aboagye

*^b and Louis Allott

*^a

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* Corresponding authors

^a Centre for Biomedicine and Positron Emission Tomography Research Centre, Hull York Medical School and University of Hull, Cottingham Road, Hull, UK
E-mail: louis.allott@hull.ac.uk

^b Comprehensive Cancer imaging Centre, Faculty of Medicine, Department of Surgery and Cancer, Imperial College London, Hammersmith Hospital, Du Cane Road, London, UK
E-mail: eric.aboagye@imperial.ac.uk

Abstract

Sulfur-[¹⁸F]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 [¹⁸F]SO₃F-bearing prostate specific membrane antigen (PSMA) targeted ligand ([¹⁸F]5) using the GE FASTLab™ 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.

Reaction Chemistry & Engineering

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

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

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