Tracer library / [18F]Dolutegravir
Structure of Dolutegravir (unlabelled parent compound, from PubChem)
Unlabelled parent compoundPubChem CID 54726191

[18F]Dolutegravir

Also written as [18F]Dolutegravir; [F-18]Dolutegravir
Radionuclide
F-18 t½ 109.77 min
Modality
PET
Production route
—
Stage
Clinical research
Syntheses indexed
3

What it is

Compound class
Antiretroviral drug (integrase strand transfer inhibitor, dolutegravir analogue)
Target / mechanism
—
Clinical application
PET imaging of antiretroviral drug biodistribution and pharmacokinetics at HIV-1 reservoirs/sanctuary sites PMID 35631413
Theranostic pair
—

Published syntheses

ModuleCassettePurificationYield %RCP %Precursor / supplierSource
TRACERlab FX N Pro
GE HealthCare
fixed tubingHPLC+SPE5.1 ± 0.8%
not corrected
>99%2-fluoro-4-nitrobenzonitrile
Herceptin, Roche, Mississauga, ON
35631413
2022 Pharmaceuticals (Basel)
the automation was carried out using a TRACERlab® FX N Pro (GE Healthcare, Chicago, IL, USA) module - afforded ready-to-inject [18F]DTG in 5.1 ± 0.8% (n = 10) decay-corrected radiochemical yield within 95 min
AllinOne (AiO)
Trasis
vendor cassetteHPLC+SPE20 ± 5%
decay-corrected
≥99%compound 2 (trimethyltin precursor)39398184
2024 ACS Omega
the whole process was automated on a kit-based AllInOne synthesizer for clinical applications - Ready-to-inject [18F]DTG was obtained in 20 ± 5% (n = 12) decay-corrected radiochemical yield within 90 min
TRACERlab FX N Pro
GE HealthCare
——29%
conversion, not isolated RCY
—compound 2 (trimethyltin precursor)39398184
2024 ACS Omega
Optimization of the reaction conditions ... was performed on a TRACERlab FX N Pro module - reducing the quantity of 2 to 2 mg resulted in a 29% conversion

Precursor

Common precursor
—
Suppliers seen in the literature
—
Cited suppliers in indexed syntheses
Herceptin, Roche, Mississauga
Typical final purification
—

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Quality control Preliminary - inferred from compound class

Ph. Eur. monograph
not verified No Ph. Eur. check is recorded for this entry.
USP monograph
not verified No USP check is recorded for this entry.
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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Notes

Added from reverse module search (stage 6); 2 article(s) with F-18. Stage set/updated at stage 23 from PMID 39398184: '[18F]DTG (∼2 GBq) was obtained with a molar activity of 59 ± 2 GBq/μmol at the time of injection and was suitable for human applications.'. | Stage 30 (2026-09-18): Stage was 'first-in-human (suitable for human applications)'; normalised to 'Clinical research', original wording kept here.
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