Tracers / [18F]FAZA
[18F]FAZA
Also written as [18F]FAZA; [18F]fluoroazomycinarabinoside; [F-18]FAZA; [F-18]fluoroazomycinarabinoside; F-18 FAZA; FAZA
- Radionuclide
- F-18 t½ 109.77 min
- Modality
- PET
- Production route
- —
- Stage
- —
- Syntheses indexed
- 4
What it is
- Compound class
- Radiolabelled 2-nitroimidazole (azomycin arabinoside derivative)
- Target / mechanism
- Hypoxic cells — bioreductive (nitroreductase-mediated) trapping under low oxygen tension PMID 15632040
- Clinical application
- Tumour-hypoxia PET imaging (head and neck, lung, prostate, rectal cancers) PMID 24152663
- Theranostic pair
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Regulatory status
- FDA
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- EMA (centralised)
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- Other approvals
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- Brand names
- —
Clinical use
- Typical injected activity
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- Uptake time
- —
Reported in the literature. Not a dosing recommendation.
Published syntheses
| Module | Cassette | Purification | Yield % | RCP % | Precursor / supplier | Source |
|---|---|---|---|---|---|---|
| TRACERlab FX FN GE HealthCare | custom manifold | HPLC | 4.8% no | — | FAZA precursor Prof. Friedrich Hammerschmidt (Universität Wien, Austria) and Prof. Hans-Jürgen Machulla, Steinbeis Transfer Center Radiopharmacy, Germany | 21769163 2011 J Labelled Comp Radiopharm the Tracerlab synthesis module was used in the original "out-of-the-box" configuration illustrated in Figure 3 — Typical yield of [18F]FAZA prepared using this method is 4.8% (non-decay corrected, n = 25). |
| — | — | — | 70-90% | — | — | 21989864 2012 Nuklearmedizin |
| — | — | SPE | 21.98±1.40% no | >95% | 1-(2,3-di-O-acetyl-5-O-tosyl-alpha-D-arabinofuranosyl)-2-nitroimidazole | 20478712 2010 Appl Radiat Isot [(18)F]FAZA was prepared via a one-pot, two-step synthesis using a nuclear interface nucleophilic synthesis module. — The overall radiochemical yield obtained was 21.98+/-1.40% (n=5, without decay correction) |
| — | — | — | 52.4±5.3% yes | — | 2.5mg (5.2 μmol) of the precursor | 21420304 2011 Appl Radiat Isot a modified NIRS original synthesis system for clinical use — a high radiochemical yield of 52.4±5.3% (decay-corrected, n=8) |
Precursor
- Common precursor
- FAZA precursor PMID 21769163 (DOI 10.1002/jlcr.1865)
- Suppliers seen in the literature
- academic (Univ. Wien / Steinbeis Transfer Center Radiopharmacy)
- Cited suppliers in indexed syntheses
- Prof. Friedrich Hammerschmidt (Universität Wien, Austria) and Prof. Hans-Jürgen Machulla
- Typical final purification
- HPLC (semi-preparative)
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Get in touchQuality control Preliminary — inferred from compound class
- Ph. Eur. monograph
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- USP monograph
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How this set was arrived at. base set per Ph. Eur. general monograph 0125 (rule); organic solvent confirmed in synthesis data (PMID 21769163) -> GC residual solvents; 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
Setting up quality control?We can help you scope the equipment needed to release [18F]FAZA.
Get in touchNotes
Added from reverse module search (stage 6); 7 article(s) with F-18.