Characterization of the radiosynthesis and purification of [18F]THK-5351, a PET ligand for neurofibrillary tau.

Betthauser, T., P. Ellison, D. Murali, P. Lao, T. Barnhart, S. Furumoto, N. Okamura, S. Johnson, J. Engle, R. Nickles, and B. Christian. “Characterization of the Radiosynthesis and Purification of [18F]THK-5351, a PET Ligand for Neurofibrillary Tau.”. Applied Radiation and Isotopes : Including Data, Instrumentation and Methods for Use in Agriculture, Industry and Medicine, Vol. 130, 2017, pp. 230-7.

This work characterizes the radiochemical synthesis, purification, and formulation of [18F]THK-5351, a tau PET radioligand, and develops an automated radiosynthesis routine (ELIXYS, Sofie Biosciences). Nucleophilic radiofluorination reaction was complete by 7min at 110°C with radiochemical yields proportional to precursor mass (0.1-0.5mg). Optimized HPLC purification produced radiotracer product with no chemical impurities observed on analytical HPLC in formulation. Automated radiosynthesis (ELIXYS), HPLC purification and formulation was completed in 86min producing formulated product suitable for human research use.

DOI: 10.1016/j.apradiso.2017.10.002

PubMed: 29031087