Tracers / [18F]FMISO

[18F]FMISO

Also written as 1H-1-(3-[18F]fluoro-2-hydroxypropyl)-2-nitroimidazole; [18F]Fluoromisonidazole; [18F]FMISO; [F-18]Fluoromisonidazole; [F-18]FMISO; F-18 Fluoromisonidazole; F-18 FMISO
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
Nitroimidazole
Target / mechanism
Bioreductive trapping: after cell entry the 2-nitroimidazole nitro group is reduced and, under hypoxia, binds irreversibly to intracellular macromolecules (re-oxidised and washed out under normoxia) PMID 29212283 / DOI 10.18632/oncotarget.21662
Clinical application
Tumour hypoxia; radiotherapy planning PMID 29212283 / DOI 10.18632/oncotarget.21662
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=fluoromisonidazole
EMA (centralised)
Other approvals
Brand names

Clinical use

Typical injected activity
Uptake time
120-240 min post-injection (commonly ~2 h) PMID 29212283 / DOI 10.18632/oncotarget.21662

Reported in the literature. Not a dosing recommendation.

Published syntheses

ModuleCassettePurificationYield %RCP %Precursor / supplierSource
Manual synthesiscustom manifoldSPE78
yes
NITTP (1-(2ʹ-nitro-1ʹ-imidazolyl)-2-O-tetrahydropyranyl-3-O-tosyl-propanediol)40113734
2025 EJNMMI Radiopharm Chem
following modified non-automated protocols similar to those reported in the literature — the overall corrected radiochemical yield (RCY) was estimated to be 78%
FASTlab
GE HealthCare
vendor cassetteSPE49 ± 7% (n = 30)
yes
99.9%NITTP
ABX
36897480
2023 EJNMMI Radiopharm Chem
a FASTlab1 radiosynthesizer (GE HealthCare) was used — The radiochemical yield of [18F]FMISO using original cassettes for FASTlab was 49 ± 7% (n = 30) within 48 min synthesis time.
FASTlab
GE HealthCare
custom manifoldSPE39 ± 11% (n = 19)
yes
99.8%NITTP
ABX
36897480
2023 EJNMMI Radiopharm Chem
a FASTlab1 radiosynthesizer (GE HealthCare) was used — The radiochemical yield of [18F]FMISO obtained with in-house prepared cassettes and 10 mg (23.5 µmol) NITTP precursor was 39 ± 11% (n = 19), which is somewhat lower in comparison with the original cassettes.
In-house / custom built
in-house
custom manifoldHPLC26 ± 7.5
yes
99 ± 0.502-nitroimidazole (6)
ABX
34245396
2021 EJNMMI Radiopharm Chem
An automated multi-purpose synthesizer developed in-house was used for all the radiosynthetic runs in this study (Supplemental information: Fig. S1, Fukumura et al. 2007). — The radiochemical yield of [18F]FMISO based on the cyclotron-produced [18F]F− at the end of the synthesis (EOS) was 26 ± 7.5 % (n = 8).
> 95%1-(2′-nitro-1′-imidazolyl)-2-O-tetrahydropyranyl-3-O-toluenesulphonylpropanediol31278504
2019 EJNMMI Res
In-house / custom built
Siemens
custom manifoldHPLC38% ± 2%
yes
≥99%NITTP22871433
2012 Appl Radiat Isot
a fourth generation microfluidic prototype instrument (P-IV instrument) developed at Siemens Molecular Imaging — Radiochemical yields for [18F] FMISO based on starting [18F] activity was 38% ± 2%
41807884
2026 Mol Diagn Ther
SPE56%>99.5%34613615
2022 J Labelled Comp Radiopharm
[18 F]FMISO was synthesized using a TracerLab FX-FDG module — in 56% radiochemical yield
HPLC29520821
2018 J Labelled Comp Radiopharm
>97%enantiopure epoxides25595134
2015 Nucl Med Biol
using custom-made automation module
>97%enantiopure epoxides25595134
2015 Nucl Med Biol
using custom-made automation module
SPE25.1 ± 5.0%
no
1-(2'-nitro-1'-imidazolyl)-2-O-tetra-hydropyranyl-3-O-toluenesulfonyl propanediol (NITTP)24339013
2013 J Labelled Comp Radiopharm
automatic synthesis using GE TRACERlab MX — Non-decay-corrected radiochemical yields of 25.1 ± 5.0% and 13.3 ± 5.1% (n = 3) were achieved after solid-phase extraction purification using automatic synthesis with GE TRACERlab MX and KHCO3 at concentrations of 14.1 and 33.0 µmol, respectively
SPE13.3 ± 5.1%
no
1-(2'-nitro-1'-imidazolyl)-2-O-tetra-hydropyranyl-3-O-toluenesulfonyl propanediol (NITTP)24339013
2013 J Labelled Comp Radiopharm
automatic synthesis using GE TRACERlab MX — Non-decay-corrected radiochemical yields of 25.1 ± 5.0% and 13.3 ± 5.1% (n = 3) were achieved after solid-phase extraction purification using automatic synthesis with GE TRACERlab MX and KHCO3 at concentrations of 14.1 and 33.0 µmol, respectively
80% for protected [18F]FMISO22001413
2012 Appl Radiat Isot
The substitutions were carried out in a microfluidic reaction flow cell — 80% for protected [(18)F]FMISO
SPE37.49+/-1.68%
no
>95%1-(2'-nitro-1'-imidazolyl)-2-O-tetrahydropyranyl-3-O-toluenesulphonylpropanediol (NITTP)20493720
2010 Appl Radiat Isot
using a modified nuclear interface synthesis module — The maximum overall radiochemical yield obtained was 37.49+/-1.68% with 10mg NITTP (n=3, without any decay correction)
30±5%
no
>97%17379530
2007 Appl Radiat Isot
using a Scanditronix Anatech RB III robotic system — an uncorrected radiochemical yield of 30+/-5% at end of synthesis (EOS)
HPLC58.5±3.5%
yes
1-(2'-nitro-1'-imidazolyl)-2-O-tetrahydrofuranyl-3-O-toluenesulfonylpropanediol16253816
2005 Nucl Med Biol
Fully automated synthesis of [18F]fluoromisonidazole using a conventional [18F]FDG module. — [18F]FMISO was obtained with high end-of-synthesis (EOS) radiochemical yields of 58.5+/-3.5% for 60.0+/-5.2 min with high-performance liquid chromatography (HPLC) purification
HPLC+SPE54.5±2.8%
yes
1-(2'-nitro-1'-imidazolyl)-2-O-tetrahydrofuranyl-3-O-toluenesulfonylpropanediol16253816
2005 Nucl Med Biol
Fully automated synthesis of [18F]fluoromisonidazole using a conventional [18F]FDG module. — the EOS radiochemical yields were 54.5+/-2.8% (337+/-25 GBq/micromol) for 70.0+/-3.8 min
SPEgreater than 40%
no
greater than 95%1-(2'-nitro-1'-imidazolyl)-2-O-tetrahydropyranyl-3-O-toluenesulphonylpropanediol15982586
2005 Nucl Med Biol
using a modified commercial Tracerlab FX(F-N) synthesis module — The overall radiochemical yield with no decay correction was greater than 40%
55-80%8358398
1993 Appl Radiat Isot
One-step radiolabeling and rapid protection group removal provided 55-80% yield in 50 min. — 55-80% yield in 50 min
40%[18F]fluoride2738663
1989 J Nucl Med
99±127562785
2016 Curr Radiopharm
the novel fully automated platform of the BG75 system

Precursor

Common precursor
NITTP (1-(2'-nitro-1'-imidazolyl)-2-O-tetrahydropyranyl-3-O-toluenesulfonylpropanediol) PMID 35697954 / DOI 10.1186/s41181-022-00165-0
Suppliers seen in the literature
ABX advanced biochemical compounds (Radeberg, Germany) (precursor NITTP)
Cited suppliers in indexed syntheses
ABX
Typical final purification
SPE

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Quality control Pharmacopoeial monograph

Ph. Eur. monograph
2459
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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Notes

Reference hypoxia tracer since 1986; slow kinetics require late imaging.