Tracers / [18F]FETrp

[18F]FETrp

Also written as [18F]FETrp; [F-18]FETrp; F-18 FETrp; FETrp; fluoroethyltryptophan
Radionuclide
F-18 t½ 109.7 min
Modality
PET
Production route
Cyclotron liquid target
Stage
Research
Syntheses indexed
5

What it is

Compound class
Amino acid
Target / mechanism
Amino-acid transporters and the IDO-mediated kynurenine pathway of tryptophan metabolism PMID 30815792 / DOI 10.1007/s11307-019-01327-4
Clinical application
PET imaging of cancer via dual targeting of amino-acid transporters and the IDO/kynurenine tryptophan-metabolism pathway (brain tumours, neuroendocrine tumours; preclinical + patient studies) PMID 30815792 / DOI 10.1007/s11307-019-01327-4; PMID 38012510 / DOI 10.1007/s11307-023-01877-8
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=fluoroethyltryptophan
EMA (centralised)
Other approvals
Brand names

Clinical use

Typical injected activity
5.2 MBq/kg (0.14 mCi/kg) in patients PMID 38012510 / DOI 10.1007/s11307-023-01877-8
Uptake time
Dynamic imaging from injection; brain-tumour SUV peaks ~90 min p.i.; whole-body multi-pass scans 0-60 min PMID 38012510 / DOI 10.1007/s11307-023-01877-8; PMID 32123231 / DOI 10.1038/s41598-020-60728-6

Reported in the literature. Not a dosing recommendation.

Published syntheses

ModuleCassettePurificationYield %RCP %Precursor / supplierSource
Synthra RNplus
Synthra
custom manifoldHPLC+SPE6.0 ± 0.3%
yes
96–97%tert-Butyl Nα-(tert-butoxycarbonyl)-1-(2-(tosyloxy)ethyl)-L-tryptophanate
Affinity Research Chemical Inc, Wilmington, DE, USA
37118900
2023 J Labelled Comp Radiopharm
Synthra RNPlus research module — The radiochemical yields were 6.0 ± 0.3% (decay corrected to EOB).
Raytest SynChrom
Elysia-Raytest
custom manifoldHPLC+SPE55.2 ± 7.5%
yes
99.9%(S)-3 tosylate precursor38564046
2024 EJNMMI Radiopharm Chem
fully automated on a SynChrom R&D EVOI module — to produce the radiotracer in 55.2 ± 7.5% radiochemical yield
19.0 ± 7.0
yes
over 99 %N-boc-1-(2-tosylethyl) tryptophan tert-butyl ester27815661
2017 Mol Imaging Biol
in a GE Tracerlab FX-N module — 19.0 ± 7.0 and 9.0 ± 3.0 % (n = 3) decay-corrected yield
9.0 ± 3.0
yes
over 99 %N-boc-1-(2-tosylethyl) tryptophan tert-butyl ester27815661
2017 Mol Imaging Biol
in a GE Tracerlab FX-N module — 19.0 ± 7.0 and 9.0 ± 3.0 % (n = 3) decay-corrected yield
about 12%
no
above 95%1,3-di(4-methylphenylsulfonyloxy)propane12798378
2003 Appl Radiat Isot

Precursor

Common precursor
(S)-tert-butyl 2-((tert-butoxycarbonyl)amino)-3-(1-(2-(tosyloxy)ethyl)-1H-indol-3-yl)propanoate (Boc/tBu-protected 1-(2-tosyloxyethyl)indole precursor) PMID 32123231 / DOI 10.1038/s41598-020-60728-6
Suppliers seen in the literature
Affinity Research Chemicals Inc (Wilmington, DE, USA)
Cited suppliers in indexed syntheses
Affinity Research Chemical Inc
Typical final purification
HPLC

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Quality control Preliminary — inferred from compound class

Ph. Eur. monograph
USP monograph
AppearancepHRCP HPLCRCP TLCHPLC UVRadionuclidic (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)

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

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