Tracers / [18F]FSPG
[18F]FSPG
Also written as (S)-4-(3-[18F]fluoropropyl)-L-glutamic acid; [18F]FSPG; [F-18]FSPG; BAY 94-9392; F-18 FSPG; FSPG
- Radionuclide
- F-18 t½ 109.7 min
- Modality
- PET
- Production route
- Cyclotron liquid target
- Stage
- Clinical research
- Syntheses indexed
- 9
What it is
- Compound class
- Amino acid
- Target / mechanism
- Cystine/glutamate antiporter (system xc-) PMID 36525163 / DOI 10.1007/s11307-022-01793-3
- Clinical application
- Oncology imaging; assessment of intracellular redox / oxidative-stress status PMID 36525163 / DOI 10.1007/s11307-022-01793-3
- 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=FSPG+glutamic+acid
- EMA (centralised)
- —
- Other approvals
- —
- Brand names
- —
Clinical use
- Typical injected activity
- ~300 MBq (299 +/- 23 MBq dosimetry study; 285-309 MBq in NSCLC/HNSCC cohorts) PMID 23568366 / DOI 10.2967/jnumed.112.112581; PMID 38611114 / DOI 10.3390/cancers16071437
- Uptake time
- Static PET ~45-60 min post-injection (dosimetry series acquired 5-240 min p.i.) PMID 26785040 / DOI 10.1148/radiol.2015142000; PMID 23568366 / DOI 10.2967/jnumed.112.112581
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 | SPE | 22.56 ± 0.97% no | 96.31 ± 0.62% | di-tert-butyl (2S,4S)-2-(3-((naphthalen-2 ylsulfonyl)oxy)propyl)-4 (tritylamino) pentanedioate ABX | 37461634 2023 Res Sq GE TRACERlab™ FXFN — The average non-decay-corrected radiochemical yield was 22.56 ± 0.97% with radiochemical purity of 96.31 ± 0.62% |
| FASTlab GE HealthCare | vendor cassette | SPE | 30.82 ± 1.60% no | 95.96 ± 0.70% | di-tert-butyl (2S,4S)-2-(3-((naphthalen-2 ylsulfonyl)oxy)propyl)-4 (tritylamino) pentanedioate ABX | 37461634 2023 Res Sq GE FASTlab™ — the average radiochemical yields was also observed to be significantly higher than from the TRACERlab counterpart, 30.82 ± 1.60% vs. 22.56 ± 0.97%, p < 0.0001 |
| AllinOne (AiO) Trasis | vendor cassette | SPE | 33.5 ± 4.9% | 96.8 ± 1.1% | [18F]FSPG precursor (naphthyltosylate precursor) ABX | 39821860 2025 EJNMMI Radiopharm Chem The automated synthesis module used in the study was the Trasis AIO™ (Trasis SA) — The optimised method provided [18F]FSPG in 33.5 ± 4.9% radiochemical yield in just 35 min when starting with 18–25 GBq. |
| FASTlab GE HealthCare | vendor cassette | SPE | 38.4 ± 2.6 % yes | >96 % | [18F]FSPG precursor 1 ABX | 34013395 2021 Mol Imaging Biol The automated radiosynthesis platform used in the study was the GE FASTlab™ (GE Healthcare) — The optimized protocol produced [18F]FSPG in 38.4 ± 2.6 % radiochemical yield |
| TRACERlab FX FN GE HealthCare | fixed tubing | SPE | 22.56 ± 0.97% no | 96.31 ± 0.62% | di-tert-butyl (2S,4S)-2-(3-((naphthalen-2 ylsulfonyl)oxy)propyl)-4 (tritylamino) pentanedioate ABX | 37486582 2023 EJNMMI Radiopharm Chem GE TRACERlab™ FXFN and FASTlab™, the most widely used synthesis modules for routine clinical radiopharmaceutical production — average radiochemical yields of 22.56 ± 0.97% |
| FASTlab GE HealthCare | vendor cassette | SPE | 30.82 ± 1.60% no | 95.96 ± 0.70% | di-tert-butyl (2S,4S)-2-(3-((naphthalen-2 ylsulfonyl)oxy)propyl)-4 (tritylamino) pentanedioate ABX | 37486582 2023 EJNMMI Radiopharm Chem FASTlab™, a cassette-based module, for easier adoption by other radiopharmaceutical manufacturing facilities — average radiochemical yields was also observed to be significantly higher than from the TRACERlab counterpart, 30.82 ± 1.60% versus 22.56 ± 0.97% |
| Synthra RNplus Synthra | custom manifold | HPLC+SPE | 39-43 yes | 95-97 | di-tert-butyl-(2S,4S)-2-(3-((naphthalen-2-ylsulfonyl)oxy)propyl)-4-(tritylamino)pentanedioate ABX | 36525163 2023 Mol Imaging Biol The radiosynthesis of [18F]FSPG was performed using a customised RNPlus Research automated radiosynthesis system (Synthra GmbH, Hamburg, Germany). — [18F]FSPG was produced typically in 39–43% radiochemical yield (decay corrected) from [18F]fluoride |
| — | — | — | — | — | — | 21750203 2011 Clin Cancer Res |
| — | — | SPE | — | — | — | 23568366 2013 J Nucl Med 18F-FSPG was prepared by a fully automated 2-step procedure and purified by a solid-phase extraction method. |
Precursor
- Common precursor
- Protected FSPG precursor with an aryl sulfonate (naphthalene-/4-nitrophenyl-sulfonate) leaving group; nucleophilic [18F]fluorination then acid/base deprotection PMID 34013395 / DOI 10.1007/s11307-021-01609-w; PMID 36525163 / DOI 10.1007/s11307-022-01793-3
- Suppliers seen in the literature
- ABX GmbH (Radeberg, Germany)
- Cited suppliers in indexed syntheses
- ABX
- Typical final purification
- SPE
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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-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 ('Amino acid'): HPLC UV -> HPLC cond. (non-aromatic glutamate analogue (4-[18F]fluoroglutamic acid) -- weak UV chromophore like glutamine/glutamic acid, not an aromatic amino acid like FET/FDOPA/FETrp/FTYR)
Tests listed by reference only. Monograph texts are copyrighted and are not reproduced here. How these are derived
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