Tracer library / [18F]THK5351
[18F]THK5351
Also written as [18F]THK-5351; [18F]THK5351; [F-18]THK-5351; [F-18]THK5351; F-18 THK-5351; F-18 THK5351; F-18-THK5351
- Radionuclide
- F-18 t½ 109.7 min
- Modality
- PET
- Production route
- Cyclotron liquid target
- Stage
- Research
- Syntheses indexed
- 2
What it is
- Compound class
- Arylquinoline
- Target / mechanism
- Aggregated tau (neurofibrillary tangles); substantial off-target binding to monoamine oxidase-B (MAO-B) PMID 28359327 / DOI 10.1186/s13195-017-0253-y; PMID 29752516 / DOI 10.1007/s00259-018-4012-5
- Clinical application
- Investigated for tau imaging in Alzheimer disease and other tauopathies (interpretation confounded by MAO-B binding) PMID 28359327 / DOI 10.1186/s13195-017-0253-y
- Theranostic pair
- —
Regulatory status
- FDA
- No Drugs@FDA / openFDA drug registry — no approved application found; search: https://www.accessdata.fda.gov/scripts/cder/daf/index.cfm?event=BasicSearch.process&searchTerm=THK5351
- EMA (centralised)
- —
- Other approvals
- —
- Brand names
- —
Clinical use
Published syntheses
| Module | Cassette | Purification | Yield % | RCP % | Precursor / supplier | Source |
|---|---|---|---|---|---|---|
| ELIXYS FLEX/CHEM Sofie | vendor cassette | HPLC+SPE | 23% 48%, and 55% decay-corrected | 99.98% ± 0.04% | THK-5352 Tohoku University | 29031087 2017 Appl Radiat Isot an automated radiosynthesis routine (ELIXYS, Sofie Biosciences) - [18F]THK-5351 decay-corrected radiochemical yields post-HPLC purification were 23%, 48%, and 55%, using precursor masses of 0.1, 0.2, and 0.5 mg, respectively. |
| TRACERlab FX FN GE HealthCare | — | HPLC | 21 ± 3.5% not corrected | — | O-THP protected tosyl precursor | 27859483 2017 J Labelled Comp Radiopharm the use of a commercially available radiosynthesis module, the GE TRACERlab™ FXFN - an uncorrected radiochemical yield of 21 ± 3.5% |
Clinical literature
Clinical studies in the indexed corpus, ordered by design (multicentre, prospective, retrospective, others, case reports last) and then by year. Titles and links only, as published; this is not a summary of the evidence.
- 18F-THK5351 Positron Emission Tomography Imaging in Neurodegenerative Tauopathies.2021 · Front Aging Neurosci · Clinical study
- Dynamic PET Measures of Tau Accumulation in Cognitively Normal Older Adults and Alzheimer's Disease Patients Measured Using [18F] THK-5351.2016 · PLoS One · Clinical study
Precursor
- Common precursor
- OTHP-protected tosylate precursor THK-5352 ((S)-2-(2-methylaminopyrid-5-yl)-6-[[2-(tetrahydro-2H-pyran-2-yloxy)-3-tosyloxy]propoxy]quinoline); nucleophilic [18F]fluorination then acid hydrolysis PMID 29031087 / DOI 10.1016/j.apradiso.2017.10.002
- Suppliers seen in the literature
- Synthesised and supplied by Tohoku University (Japan)
- Cited suppliers in indexed syntheses
- Tohoku University
- Typical final purification
- SPE
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Get in touchQuality control Preliminary - inferred from compound class
- Ph. Eur. monograph
- not verified No Ph. Eur. check is recorded for this entry.
- USP monograph
- not verified No USP check is recorded for this entry.
How this set was arrived at. base set per Ph. Eur. general monograph 0125 (rule); organic-phase radiosynthesis assumed from isotope/compound class, no synthesis data confirming it -> GC residual solvents (preliminary); conventional nucleophilic 18F-fluorination assumed from isotope/compound class, no synthesis data confirming K222 use -> Kryptofix test (preliminary)
Tests listed by reference only. Monograph texts are copyrighted and are not reproduced here. How these are derived
Setting up quality control?We can help you scope the equipment needed to release [18F]THK5351.
Get in touchNotes
Off-target MAO-B binding is a known limitation.