Tracer library / [177Lu]Lu-DOTA-MGS5
Structure of DOTA-MGS5 (unlabelled parent compound, from PubChem)
Unlabelled parent compoundPubChem CID 162659624

[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
Clinical research
Syntheses indexed
8

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
—

Published syntheses

ModuleCassettePurificationYield %RCP %Precursor / supplierSource
Modular-Lab PharmTracer
Eckert & Ziegler
vendor cassette——98.1 ± 0.6%DOTA-MGS539643727
2025 Eur J Nucl Med Mol Imaging
synthesized using a Modular-Lab PharmTracer® (Eckert & Ziegler Eurotrope GmbH, Berlin, Germany)
——HPLC>95%>95%DOTA-γ-MGS537421545
2023 EJNMMI Res
——HPLC>95%>95%DOTA-MGS537421545
2023 EJNMMI Res
Manual synthesis—HPLC>95%>90%DOTA-MGS542707991
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
vendor cassette——98.1 ± 0.6%DOTA-MGS539643727
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]MGS537052226
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…DOTA-DGlu-Pro-Tyr-Gly-Trp-(N-Me)Nle-Asp-1Nal-NH2
piCHEM, Raaba-Grambach, Austria
33049999
2020 Molecules

Clinical literature

Clinical studies in the indexed corpus, ordered by design (multicentre, prospective, retrospective, others, case reports last) and then by year. Titles and links only, as published; this is not a summary of the evidence.

  1. Paving the Way for CCK2R-Targeted Peptide Receptor Radionuclide Therapy with [177Lu]Lu-DOTA-MGS5 in Patients with Small Cell Lung Cancer.
    2026 · Pharmaceutics · Clinical study

Precursor

Common precursor
—
Suppliers seen in the literature
—
Cited suppliers in indexed syntheses
piCHEM
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 HPLCHPLC UVRadionuclidic (HPGe)Half-lifeActivityEndotoxins (LAL)SterilityFilter integrityOsmolalityMolar activityMetal impuritiesLu-177m
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

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Notes

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)'. | Stage 30 (2026-09-18): Stage was 'first therapeutic clinical trial initiation / first-in-patient therapy'; normalised to 'Clinical research', original wording kept here.
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