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

Tobey J. Betthauser, Paul A. Ellison, Dhanabalan Murali, Patrick J. Lao, Todd E. Barnhart, Shozo Furumoto, Nobuyuki Okamura, Sterling C. Johnson, Jonathan W. Engle, Robert J. Nickles, Bradley T. Christian

Research output: Contribution to journalArticlepeer-review

5 Citations (Scopus)

Abstract

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 7 min at 110 °C with radiochemical yields proportional to precursor mass (0.1–0.5 mg). 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 86 min producing formulated product suitable for human research use.

Original languageEnglish
Pages (from-to)230-237
Number of pages8
JournalApplied Radiation and Isotopes
Volume130
DOIs
Publication statusPublished - 2017 Dec

Keywords

  • Alzheimer's disease
  • Automation
  • Formulation
  • Positron emission tomography
  • Radiochemical stability
  • Radiochemistry
  • THK
  • USP

ASJC Scopus subject areas

  • Radiation

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