Tracers / [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
- 4
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
- Typical injected activity
- ~370-378 MBq (healthy volunteers 377.8 +/- 14.0 MBq, range 340-397) PMID 28336780 / DOI 10.2967/jnumed.116.189126
- Uptake time
- Brain PET acquired 50-60 min after injection PMID 31191427 / DOI 10.3389/fneur.2019.00503
Reported in the literature. Not a dosing recommendation.
Published syntheses
| Module | Cassette | Purification | Yield % | RCP % | Precursor / supplier | Source |
|---|---|---|---|---|---|---|
| ELIXYS FLEX/CHEM Sofie Biosciences | vendor cassette | HPLC+SPE | 23%, 48%, and 55% yes | 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. |
| — | — | — | — | — | — | 27355840 2016 PLoS One |
| In-house / custom built | custom manifold | — | — | >95% | — | 34912209 2021 Front Aging Neurosci manufactured at the Cyclotron and Radioisotope Center of Tohoku University using a semiautomated system developed in-house |
| — | — | HPLC | 21 ± 3.5% no | — | 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% |
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
- —
- USP monograph
- —
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
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Get in touchNotes
Off-target MAO-B binding is a known limitation.