Tracers / [18F]Dolutegravir
[18F]Dolutegravir
Also written as [18F]Dolutegravir; [F-18]Dolutegravir
- Radionuclide
- F-18 t½ 109.77 min
- Modality
- PET
- Production route
- —
- Stage
- first-in-human (suitable for human applications)
- 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
- —
Regulatory status
- FDA
- —
- EMA (centralised)
- —
- Other approvals
- —
- Brand names
- —
Clinical use
- Typical injected activity
- —
- Uptake time
- —
Reported in the literature. Not a dosing recommendation.
Published syntheses
| Module | Cassette | Purification | Yield % | RCP % | Precursor / supplier | Source |
|---|---|---|---|---|---|---|
| TRACERlab FX N Pro GE HealthCare | fixed tubing | HPLC+SPE | 5.1 ± 0.8% no | >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 cassette | HPLC+SPE | 20 ± 5% yes | ≥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 |
Need this precursor?We can point you to suppliers for [18F]Dolutegravir, or handle the enquiry for you.
Get in touchQuality control Preliminary — inferred from compound class
- Ph. Eur. monograph
- —
- USP monograph
- —
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
Setting up quality control?We can help you scope the equipment needed to release [18F]Dolutegravir.
Get in touchNotes
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.'.