On the GMP production of [18]FUCB-H : Imaging neurotransmission

We herein describe the straightforward synthesis of a stable pyridyl(aryl)iodonium salt and its [18F]radiolabelling within a one-step, fully automated and cGMP compliant radi-osynthesis of [18F]UCB-H, a PET tracer for the imaging of Synaptic Vesicle glycoprotein 2A (SV2A). Over the course of one year, 40 automated productions provided 34±2% of injectable [18F]UCB-H from up to 7.7 Ci of [18F]fluoride in 50 minutes (uncorrected radiochemical yield. Specific Activity = 22±5 Ci/µmol). The successful implementation of our synthetic strategy within routine, high-activity and cGMP productions attests to its practicality and reliability for the production of large doses of [18F]UCB-H. In addition to enabling efficient and cost-effective clinical research on a range of neurological pathologies through the imaging of SV2A, this work further demonstrates the real value of iodonium salts in the cGMP 18F-PET tracer manufacturing industry and their ability to fulfill practical and regulatory requirements in that field.