An One-Pot Two-Step Automated Synthesis Of [F-18]T807 Injection, Its Biodistribution In Mice And Monkeys, And A Preliminary Study In Humans

[F-18]T807 is a potent tau protein imaging agent. In order to fulfill the demand from preclinical and clinical studies, we developed an automated one-pot two-step synthesis of this potent tau imaging agent and studied its stability, and dosimetry in mice and monkeys. We also conducted a preliminary study of this imaging agent in humans. Using this one-pot two-step method, the radiochemical yield (RCY) of [F-18]T807 was 20.5 +/- 6.1% (n = 15) at the end of bombardment (EOB) in a synthesis time of 70 +/- 5 min. The chemical and radiochemical purities were >90% and the specific activities were 151 +/- 52 GBq/pmol. The quality of [F-18]T807 synthesized by this method met the U.S. Pharmacopoeia (USP) criteria. The stability test showed that the [F-18]T807 injection was stable at room temperature for up to 4 h after the end of synthesis (EOS). The estimated effective dose of the [F-18]T807 injection extrapolated from monkeys was 19 pSv/MBq (n = 2), while the estimated effective doses of the [F-18]T807 injection extrapolated from fasted and non-fasted mice were 123 +/- 27 (n = 3) and 94 +/- 19 (n = 4) pSv/MBq, respectively. This one-pot two-step automated method produced the [F-18] T807 injection with high reproducibility and high quality. PET imaging and radiation dosimetry evaluation in mice and Formosan rock monkeys suggested that the [F-18]T807 injection synthesized by this method is suitable for use in human PET imaging studies. Thus, this method could fulfill the demand for the [F-18]T807 injection in both preclinical and clinical studies of tauopathies, especially for nearby study sites without cyclotrons.