Tracers / [18F]TFB

[18F]TFB

Also written as [18F]BF4; [18F]BF4-; [18F]Tetrafluoroborate; [18F]TFB; [F-18]BF4; [F-18]Tetrafluoroborate; [F-18]TFB
Radionuclide
F-18 t½ 109.7 min
Modality
PET
Production route
Cyclotron liquid target
Stage
Clinical research
Syntheses indexed
4

What it is

Compound class
Inorganic anion
Target / mechanism
Sodium/iodide symporter (NIS) substrate PMID 29080017 / DOI 10.1186/s13550-017-0337-5
Clinical application
Imaging of NIS expression (thyroid; NIS as a reporter gene) PMID 29080017 / DOI 10.1186/s13550-017-0337-5
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=fluorotetrafluoroborate
EMA (centralised)
Other approvals
Brand names

Clinical use

Typical injected activity
333-407 MBq in healthy volunteers PMID 29080017 / DOI 10.1186/s13550-017-0337-5
Uptake time
Dynamic + whole-body static PET/CT over 4 h post-injection (dosimetry) PMID 29080017 / DOI 10.1186/s13550-017-0337-5

Reported in the literature. Not a dosing recommendation.

Published syntheses

ModuleCassettePurificationYield %RCP %Precursor / supplierSource
Synthra
custom manifoldSPE41.0% (range 30.2–56.0%)98.4 ± 1.5%boron trifluoride-methanol complex
Sigma-Aldrich
36512196
2022 EJNMMI Radiopharm Chem
customised SYNTHRA module (Synthra GmbH, Germany) — These conditions ... provided RCY 41.0% (range 30.2–56.0%) and Am in the range of 33.9–216.7 GBq/µmol at EOS
TRACERlab FX FN
GE HealthCare
vendor cassetteSPE50 (26)98 (1)boron trifluoride acetonitrile complex
Sigma-Aldrich
36512196
2022 EJNMMI Radiopharm Chem
TRACERLAB FXFN (GE Healthcare) — FXFN (n = 5)CH3CN1/30035 (30)50(26)98 (1)39.8 (2.1–99.3)1.13
SPE14.2% ± 1.2%97.5% ± 0.95%15-Crown-5 and boron trifluoride diethyl etherate
Sigma-Aldrich
36458201
2022 Mol Ther Oncolytics
BF4−32248325
2020 Eur J Nucl Med Mol Imaging

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Quality control Preliminary — inferred from compound class

Ph. Eur. monograph
USP monograph
AppearancepHRCP HPLCRCP TLCHPLC cond.Radionuclidic (HPGe)Half-lifeActivityEndotoxins (LAL)SterilityFilter integrity
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); STAGE 17.4 recheck by compound class ('Inorganic anion'): HPLC UV -> HPLC cond. (tetrafluoroborate (BF4-) -- a simple inorganic anion with no UV chromophore at all, same category as fluoride/chloride/phosphate/sulfate)

Tests listed by reference only. Monograph texts are copyrighted and are not reproduced here. How these are derived

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Notes

Labelled by isotopic exchange on boron rather than by nucleophilic substitution.