Tracers / [177Lu]Lu-DOTA-MGS5
[177Lu]Lu-DOTA-MGS5
Also written as [177Lu]Lu-DOTA-MGS5; [Lu-177]Lu-DOTA-MGS5
- Radionuclide
- Lu-177 t½ 9585 min
- Modality
- Therapy
- Production route
- —
- Stage
- first therapeutic clinical trial initiation / first-in-patient therapy
- Syntheses indexed
- 10
What it is
- Compound class
- DOTA-conjugated minigastrin analog peptide (CCK2R-targeting)
- Target / mechanism
- Cholecystokinin-2 receptor (CCK2R) targeting peptide analog PMID 30530828
- Clinical application
- Peptide receptor radionuclide therapy (PRRT) targeting CCK2R-expressing tumors, including small cell lung cancer PMID 41599245
- 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 |
|---|---|---|---|---|---|---|
| Modular-Lab PharmTracer Eckert & Ziegler | vendor cassette | — | — | 98.1 ± 0.6% | DOTA-MGS5 | 39643727 2025 Eur J Nucl Med Mol Imaging synthesized using a Modular-Lab PharmTracer® (Eckert & Ziegler Eurotrope GmbH, Berlin, Germany) |
| — | — | HPLC | >95% | >95% | DOTA-γ-MGS5 | 37421545 2023 EJNMMI Res |
| — | — | HPLC | >95% | >95% | DOTA-MGS5 | 37421545 2023 EJNMMI Res |
| Manual synthesis | — | HPLC | >95% | >90% | DOTA-MGS5 | 42707991 2026 Theranostics Each ligand was combined with varying activity of [177Lu]LuCl3 in ammonium acetate buffer (0.4 M, pH 5.0, 250 μL) and heated at 95 °C for 30 min to yield the corresponding ¹⁷⁷Lu-labeled radioligand. — radiochemical yield (> 95%) |
| Modular-Lab PharmTracer Eckert & Ziegler | — | — | — | 97.9 ± 0.2% | DOTA-MGS5 | 41599245 2026 Pharmaceutics using an automated synthesis module (Modular-Lab PharmTracer®; Eckert & Ziegler Eurotrope GmbH, Berlin, Germany) following a previously published method |
| Modular-Lab PharmTracer Eckert & Ziegler | vendor cassette | — | — | 98.1 ± 0.6% | DOTA-MGS5 | 39643727 2025 Eur J Nucl Med Mol Imaging synthesized using a Modular-Lab PharmTracer® (Eckert & Ziegler Eurotrope GmbH, Berlin, Germany) |
| Manual synthesis | — | SPE | — | — | DOTA-[(N-Me)1Nal8]MGS5 | 37052226 2023 Pharmaceuticals (Basel) For DOTA-[(N-Me)1Nal8]MGS5, radiolabeling was performed with gallium-68 (10–20 μg, 50−300 MBq) and lutetium-177 (10–20 μg, 50−250 MBq) using previously published protocols [19]. |
| Manual synthesis | — | SPE | — | ≥95% | DOTA-MGS5 piCHEM, Raaba-Grambach, Austria | 36986657 2023 Pharmaceutics Radiolabeling with lutetium-177 was carried out using 2–10 µg of DOTA-conjugate, ~50–350 MBq of ≤150 µL [177Lu]LuCl3 solution and a >1.2-fold volume of a 0.4 M sodium acetate/0.24 M gentisic acid solution with pH 5 |
| — | — | SPE | — | >99% | DOTA-DGlu-Pro-Tyr-Gly-Trp-(N-Me)Nle-Asp-1Nal-NH2 piCHEM, Raaba-Grambach, Austria | 33049999 2020 Molecules |
| — | — | — | — | — | DOTA-MGS5 | 30530828 2019 J Nucl Med |
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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); radiometal tracer -> metal impurities (rule); Lu-177 preparation -> Lu-177m content (rule); therapeutic radiopharmaceutical -> osmolality (rule); receptor ligand with a saturable target -> molar activity (rule)
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 [177Lu]Lu-DOTA-MGS5.
Get in touchNotes
Added from reverse module search (stage 6); 1 article(s) with Lu-177. Stage set/updated at stage 23 from PMID 41599245: 'the first PRRT with [177Lu]Lu-DOTA-MGS5 was conducted in a patient with extensive disease SCLC (ED-SCLC)'.