Tracers / [18F]FLT

[18F]FLT

Also written as 3'-deoxy-3'-[18F]fluorothymidine; [18F]FLT; [18F]Fluorothymidine; [F-18]FLT; [F-18]Fluorothymidine; F-18 FLT; FLT
Radionuclide
F-18 t½ 109.7 min
Modality
PET
Production route
Cyclotron liquid target
Stage
Clinical research
Syntheses indexed
22

What it is

Compound class
Nucleoside analogue
Target / mechanism
Phosphorylation by thymidine kinase 1 (TK1) and intracellular trapping (thymidine salvage pathway); marker of cell proliferation PMID 9809561 / DOI 10.1038/3337; PMID 18523066 / DOI 10.2967/jnumed.107.046391
Clinical application
Proliferation imaging; treatment response PMID 38247994 / DOI 10.3390/hematolrep16010004
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=fluorothymidine
EMA (centralised)
Other approvals
Brand names

Clinical use

Typical injected activity
Uptake time
~40-60 min post-injection (summed dynamic images) PMID 32047966 / DOI 10.1007/s00259-020-04704-2

Reported in the literature. Not a dosing recommendation.

Published syntheses

ModuleCassettePurificationYield %RCP %Precursor / supplierSource
TRACERlab FX N Pro
GE HealthCare
fixed tubingSPE16 ± 2%
yes
>99%3-N-Boc-5′-O-dimethoxytrityl-3′-O-nosyl-thymidine (I)
Toronto Research Chemicals
36500417
2022 Molecules
GE TRACERlab FX N Pro synthesis module — [18F]FLT was obtained in radiochemical yield of 16 ± 2% (decay-corrected)
In-house / custom builtcustom manifoldSPE63±5%
yes
>99%3-N-Boc-5′-O-dimethoxytrityl-3′-O-nosyl-thymidine (DMTr-Boc-nosyl precursor)
ABX
24365651
2014 J Nucl Med
electrowetting on dielectric (EWOD) microfluidic radiosynthesizer, previously developed in our group — an overall decay-corrected radiochemical yield of 63±5% (n=5)
TRACERlab FX FN
GE HealthCare
custom manifoldHPLC23%
no
Boc-Boc-Nosyl FLT precursor
Siemens Molecular Imaging and Biomarker Research
21769163
2011 J Labelled Comp Radiopharm
General Electric Medical Systems (GEMS) TracerLab FXFN automated synthesis modules — the yield of [18F]FLT using this method is 23% (non-decay corrected, n = 5)
TRACERlab FX FN
GE HealthCare
custom manifoldHPLC4.2%
no
2,3′-anhydro-cyclic precursor
ABX
21769163
2011 J Labelled Comp Radiopharm
the Tracerlab synthesis module was used in the original "out-of-the-box" configuration illustrated in Figure 3 — the yield of [18F]FLT using this method is 4.2% (non-decay corrected, n = 25)
Bioscan
vendor cassetteSPE16-39%
yes
>99%3-N-Boc-5'-O-dimethoxytrityl-3'-O-nosyl-thymidine
ABX
25531913
2015 Appl Radiat Isot
Bioscan Coincidence GE FDG reaction module (Fairfield, CT) — we could obtain [18F]FLT in 16–39% decay-corrected radiochemical yield
TRACERlab FX FN
GE HealthCare
HPLC≤8.1%
yes
90-99%2,3'-anhydro-5'-O-benzoyl-2'-deoxythymidine
ABX
25531913
2015 Appl Radiat Isot
GE TRA-CERlab FXF-N reaction module (hereafter TRACERlab module) — led to decay-corrected radiochemical yields no greater than 8.1%
In-house / custom built
in-house
custom manifold7%
yes
73FLT precursor (3-N-Boc-5′-O-dimethoxytrityl-3′-O-nosyl-thymidine)
ABX
23999726
2013 Molecules
For automated radiosynthesis we used custom-made radiosynthesis robot controlled by LabView software. — The corresponding yields of FLT were only 7% and 5%
29470664
2018 Anal Bioanal Chem
HPLC29520821
2018 J Labelled Comp Radiopharm
70-90%21989864
2012 Nuklearmedizin
SPE23.2+/-2.6%
yes
>97%3-N-t-butoxycarbonyl-1-[5'-O-(4,4'-dimethoxy triphenylmethyl)-2'-deoxy-3'-O-(4-nitrobenzenesulfonyl)-beta-d-threopentofuranosyl]thymine20451400
2010 Appl Radiat Isot
using PET-MF-2V-IT-I synthesis module — corrected radiochemical yield of 23.2+/-2.6% (n=6, uncorrected yield: 16-22%)
37.9%3-N-t-butoxycarbonyl-[5'-O-(4,4'-dimethoxytrityl)-2'-deoxy-3'-O-(4-nitrobenzenesulfonyl)-beta-D-threopentofuranosyl]thymine (thymidine derivative II)16129604
2006 Appl Radiat Isot
we modified 2-vessel [18F]FDG synthesis module (manufactured by CTI) to produce [18F]FLT — gave the best radiochemical yield (37.9%) when the reaction was carried out at 140 degrees C for 5 min
16203269
2005 Bull Cancer
HPLC50.5 +/- 5.2%
yes
15246372
2004 Nucl Med Biol
by modifying a commercial FDG synthesizer and its disposable fluid pathway — [18F]FLT was obtained with a yield of 50.5 +/- 5.2% (n = 28, decay corrected)
SPE9.95 ± 0.24%
yes
>99%3-N-Boc-5'-O-dimethoxytrityl-3'-O-nosyl-thymidine (BOC-Nosyl)35466460
2022 J Labelled Comp Radiopharm
in the general purpose TRACERlab FX modules — the decay corrected radiochemical yield (RCY) was 9.95 ± 0.24%
HPLC24±5%
yes
over 99%3-N-Boc-5'-O-dimethoxytrityl-3'-O-nosyl-thymidine (Boc-FLT)28612546
2017 Sichuan Da Xue Xue Bao Yi Xue Ban
CFN-MPS-200 automatic synthesis module — resulted in a radio chemical yield of (24±5)% (after attenuation correction, n =20)
54%
yes
27314451
2016 Nucl Med Biol
24692121
2014 J Labelled Comp Radiopharm
HPLC609922172393
2012 Nucl Med Biol
automated them on an Explora General Nucleophilic double-synthesis module — radiochemical yields of up to 60% within 70±10 min
HPLC60.2±5.2%(5'-O-DMTr-2'-deoxy-3'-O-nosyl-beta-D-threo-pentofuranosyl)-3-N-BOC-thymine17384949
2007 Eur J Nucl Med Mol Imaging
commercially available radiochemistry modules (TracerLab MX, GE Healthcare) — Automated synthesis with TBAHCO3 and 20 mg of precursor at 120 degrees C for 10 min of [18F]fluorination led to radiochemical yields of 60.2+/-5.2% after HPLC purification with an MX module (n=10)
HPLC19.8%3-N-Boc-1-[5-O-(4,4'-dimethoxytrityl)-3-O-nosyl-2-deoxy-beta-D-lyxofuranosyl]thymine11823132
2002 Nucl Med Biol
13%10773543
2000 Nucl Med Biol

Precursor

Common precursor
3-N-Boc-5'-O-dimethoxytrityl-3'-O-nosyl-thymidine (BOC-Nosyl) PMID 35466460 / DOI 10.1002/jlcr.3974
Suppliers seen in the literature
Cited suppliers in indexed syntheses
ABX, Siemens Molecular Imaging and Biomarker Research, Toronto Research Chemicals
Typical final purification
HPLC

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Quality control Pharmacopoeial monograph

Ph. Eur. monograph
2460
USP monograph
not verified — the USP-NF monograph index is subscription-only and no public confirmation was found
AppearancepHRCP HPLCHPLC UVResidual solvents (GC)KryptofixRadionuclidic (HPGe)Half-lifeActivityEndotoxins (LAL)SterilityFilter integrity
How this set was arrived at. Cross-checked against Ph. Eur. general monograph 0125 (base set), EANM validation guideline (PMC7016057) and cGRPP guidance (PMC7881071). Draft X-marks consistent with the base set; tracer-specific analytical tests follow the specific monograph where one exists.

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

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