Development of an automated, GMP compliant FASTlabTM radiosynthesis of [18F]GE ‐179 for the clinical study of activated NMDA receptors

We describe the development of a process using the GE FASTlabTM radiosynthesis platform coupled with HPLC purification. The radiosynthesis is a two ‐step process, involving the nucleophilic fluorination of ethylene ditosylate, 11, followed by alkylation to the deprotonated thiol precursor,N‐(2‐chloro‐5‐thiophenol)‐N’‐(3‐thiomethylphenyl)‐N’‐methyl guanidine, 8.The crude product was purified by semi ‐preparative HPLC to give the formulated product in an activity yield (AY) of 7 ± 2% (n = 15) with a total synthesis time of 120 minutes. The radioactive concentration (RAC) and radiochemical purity (RCP) were 328 ± 77 MBq/mL and 96.5 ± 1% respectively and the total chemical content was 2 ± 1 μg. The final formulation volume was 14 mL.The previously described radiosynthesis of [18F]GE ‐179 was successfully modified to deliver an process on the FASTlabTM that allows the manufacture of a GMP quality product from high starting radioactivitity (up to 80 GBq) and delivers a product suitable for clinical use.
Source: Journal of Labelled Compounds and Radiopharmaceuticals - Category: Biochemistry Authors: Tags: RESEARCH ARTICLE Source Type: research