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An one-pot two-step automated synthesis of [18F]T807 injection, its biodistribution in mice and monkeys, and a preliminary study in humans.
- Source :
-
PloS one [PLoS One] 2019 Jul 01; Vol. 14 (7), pp. e0217384. Date of Electronic Publication: 2019 Jul 01 (Print Publication: 2019). - Publication Year :
- 2019
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Abstract
- [18F]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 [18F]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/μmol. The quality of [18F]T807 synthesized by this method met the U.S. Pharmacopoeia (USP) criteria. The stability test showed that the [18F]T807 injection was stable at room temperature for up to 4 h after the end of synthesis (EOS). The estimated effective dose of the [18F]T807 injection extrapolated from monkeys was 19 μSv/MBq (n = 2), while the estimated effective doses of the [18F]T807 injection extrapolated from fasted and non-fasted mice were 123 ± 27 (n = 3) and 94 ± 19 (n = 4) μSv/MBq, respectively. This one-pot two-step automated method produced the [18F]T807 injection with high reproducibility and high quality. PET imaging and radiation dosimetry evaluation in mice and Formosan rock monkeys suggested that the [18F]T807 injection synthesized by this method is suitable for use in human PET imaging studies. Thus, this method could fulfill the demand for the [18F]T807 injection in both preclinical and clinical studies of tauopathies, especially for nearby study sites without cyclotrons.<br />Competing Interests: The authors have declared that no competing interests exist.
- Subjects :
- Alzheimer Disease genetics
Alzheimer Disease pathology
Animals
Biological Availability
Carbolines blood
Carbolines pharmacokinetics
Contrast Media pharmacokinetics
Drug Evaluation, Preclinical
Gene Expression
Haplorhini
Humans
Injections, Intravenous
Macaca
Male
Mice
Mice, Inbred ICR
Middle Aged
Positron-Emission Tomography methods
Radiometry
Radiopharmaceuticals blood
Radiopharmaceuticals pharmacokinetics
Tissue Distribution
tau Proteins genetics
Alzheimer Disease diagnostic imaging
Carbolines chemical synthesis
Contrast Media chemical synthesis
Radiopharmaceuticals chemical synthesis
tau Proteins chemistry
Subjects
Details
- Language :
- English
- ISSN :
- 1932-6203
- Volume :
- 14
- Issue :
- 7
- Database :
- MEDLINE
- Journal :
- PloS one
- Publication Type :
- Academic Journal
- Accession number :
- 31260447
- Full Text :
- https://doi.org/10.1371/journal.pone.0217384