Evaluation of F-537-Tetrazine in a model for brain pretargeting imaging: comparison to N-(3-[18F] fluoro-5-(1,2,4,5-tetrazin-3-yl)benzyl)propan-1-amine

Shalgunov, V.; Broek, S.L. van den; Andersen, I.V.; Raval, N.R.; Schäfer, G.; Barz, M.; ... ; Battisti, U.M. (2024)

Article / Letter to editor

Brain pretargeted nuclear imaging for the diagnosis of various neurodegenerative diseases is a quickly developing field. The tetrazine ligation is currently the most explored approach to achieve this goal due to its remarkable properties. In this work, we evaluated the performance of F-537-Tetrazine, previously developed by Biogen, and N-(3-[¹⁸F]fluoro-5-(1,2,4,5-tetrazin-3-yl)benzyl)propan-1-amine, previously developed in our group, thereby allowing for the direct comparison of these two imaging probes. The evaluation included synthesis, radiolabeling and a comparison of the physicochemical properties of the compounds. Furthermore, their performance was evaluated by in vitro and in vivo pretargeting models. This study indicated that N-(3-[¹⁸F] fluoro-5-(1,2,4,5-tetrazin-3-yl)benzyl)propan-1-amine might be more suited for brain pretargeted imaging.

• All authors: Shalgunov, V.; Broek, S.L. van den; Andersen, I.V.; Raval, N.R.; Schäfer, G.; Barz, M.; Herth, M.M.; Battisti, U.M.
• Date: 2024-12-31
• Journal: Nuclear Medicine and Biology
• Volume: 128-129
• DOI: doi:10.1016/j.nucmedbio.2024.108877