18F-THK5351: A Novel PET Radiotracer for Imaging Neurofibrillary Pathology in Alzheimer Disease
Open accessAbstract
UNLABELLED: Imaging of neurofibrillary pathology in the brain helps in diagnosing dementia, tracking disease progression, and evaluating the therapeutic efficacy of antidementia drugs. The radiotracers used in this imaging must be highly sensitive and specific for tau protein fibrils in the human brain. We developed a novel tau PET tracer, (18)F-THK5351, through compound optimization of arylquinoline derivatives. METHODS: The in vitro binding properties, pharmacokinetics, and safety of (18)F-THK5351 were investigated, and a clinical study on Alzheimer disease (AD) patients was performed. RESULTS: (18)F-THK5351 demonstrated higher binding affinity for hippocampal homogenates from AD brains and faster dissociation from white-matter tissue than did (18)F-THK5117. The THK5351 binding amount correlated with the amount of tau deposits in human brain samples. Autoradiography of brain sections revealed that THK5351 bound to neurofibrillary tangles selectively and with a higher signal-to-background ratio than did THK5117. THK5351 exhibited favorable pharmacokinetics and no defluorination in mice. In first-in-human PET studies in AD patients, (18)F-THK5351 demonstrated faster kinetics, higher contrast, and lower retention in subcortical white matter than(18)F-THK5117. CONCLUSION: (18)F-THK5351 is a useful PET tracer for the early detection of neurofibrillary pathology in AD patients.
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PET imaging was first established for amyloid and later for tau, and both are now in clinical use.
“PET imaging was first established for amyloid 145 and later for tau 146 , and both are now in clinical use.”
From Mental health care for older adults: recent advances and new directions in clinical practice and research (2022) · cites this paper as [146]
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References 36 · Cited by 330
- Authors
- Harada, R., Okamura, N., Furumoto, S., Furukawa, K., Ishiki, A., Tomita, N., Tago, T., Hiraoka, K., Watanuki, S., Shidahara, M., Miyake, M., Ishikawa, Y., Matsuda, R., Inami, A., Yoshikawa, T., Funaki, Y., Iwata, R., Tashiro, M., Yanai, K., Arai, H., & Kudo, Y.
- Affiliations
- Tohoku University (JP)
- ORCID
- Venue
- Journal of Nuclear Medicine
- Publisher
- Society of Nuclear Medicine
- Published
- 2015-11-05
- Volume
- 57
- Issue
- 2
- Pages
- 208-214
- ISSN
- 0161-5505 (ISSN-L)
- 2159-662X
- OpenAlex
- W2219920450
- Cited by
- 330
- References
- 36
- Citations by year
- 2026: 10 · 2025: 15 · 2024: 20 · 2023: 24 · 2022: 41 · 2021: 30 · 2020: 33 · 2019: 33 · 2018: 38 · 2017: 49 · 2016: 36 · 2015: 1
- FWCI
- 30.45
- Type
- journal article
- Language
- en
- Open access
- bronze
- doi.org
- Locations
- Journal of Nuclear Medicine (publishedVersion)
- PubMed (publishedVersion)
- Funders
- Japan Society for the Promotion of Science (25293259, 15K15268, 15K08127, 25670525, 16H05383, 15H04900, 26253016, 26830041)
- Topics
- Health Sciences › Medicine › Physiology › Alzheimer's disease research and treatments
- Health Sciences › Medicine › Psychiatry and Mental health › Dementia and Cognitive Impairment Research
- Health Sciences › Medicine › Radiology, Nuclear Medicine and Imaging › Radiopharmaceutical Chemistry and Applications
- Keywords
- 18F-THK5351, tau PET tracers, neurofibrillary pathology, Alzheimer's disease, neurofibrillary tangles, binding affinity, pharmacokinetics, hippocampus
- MeSH terms
- Alzheimer Disease, Aminopyridines, Animals, Autoradiography, Biotransformation, Brain, Hippocampus, Magnetic Resonance Imaging, Mice, Inbred ICR, Quinolines, Radiation Dosage, Tissue Distribution, Neurofibrillary Tangles, tau Proteins, Radiopharmaceuticals, Positron-Emission Tomography, Mice, White Matter
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