Tracers / [68Ga]Ga-RM2
[68Ga]Ga-RM2
Also written as [68Ga]Ga-RM2; [Ga-68]Ga-RM2; Ga-68 RM2; RM2
- Radionuclide
- Ga-68 t½ 67.7 min
- Modality
- PET
- Production route
- Generator
- Stage
- Clinical research
- Syntheses indexed
- 15
What it is
- Compound class
- Peptide (bombesin antagonist)
- Target / mechanism
- Gastrin-releasing peptide receptor (GRPR); bombesin-based antagonist PMID 40306971 / DOI 10.2967/jnumed.124.269132
- Clinical application
- GRPR-targeted PET imaging of prostate cancer (and other GRPR-expressing tumours such as breast cancer) PMID 40306971 / DOI 10.2967/jnumed.124.269132
- Theranostic pair
- <a href="/tracers/in111-rm2/">in111-rm2</a>
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=RM2+bombesin
- 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 |
|---|---|---|---|---|---|---|
| — | — | none | quantitative | more than 95% | RM2 | 40890559 2025 EJNMMI Res |
| — | — | none | quantitative | more than 95% | [Hse7]RM2 | 40890559 2025 EJNMMI Res |
| — | — | none | quantitative | more than 95% | [Bta8]RM2 | 40890559 2025 EJNMMI Res |
| — | — | — | — | — | — | 41229973 2025 Chin J Cancer Res |
| Manual synthesis | — | — | over 90% | above 95% | RM2 | 39563828 2024 ACS Med Chem Lett [68Ga]Ga, Hepes buffer (0.25 M), pH = 4.0, 95 °C, 30 min. — radiochemical yield was over 90% |
| Manual synthesis | — | SPE | <10% | 98.00 ± 0.67 | DOTA-RM2 Nanchang Tanzhen Biological Technology Co., Ltd., China | 37285007 2023 EJNMMI Res 20 µL (aqueous solution of 15 nmol) of X-RM2 was buffered with 500 µL of 0.05 M sodium acetate, then 110–200 MBq/mL 68GaCl3 eluted from the generator with 0.05 M HCl was added — the labelling yield of 68Ga-DOTA-RM2 was less than 10% under the same conditions or extended time |
| — | — | — | — | — | — | 36215569 2023 J Nucl Med |
| — | — | — | — | — | — | 35864350 2023 Eur Radiol |
| — | — | — | — | — | RM2 | 35744904 2022 Molecules |
| Kit-based preparation Life Molecular Imaging | vendor cassette | none | 81.1 ± 1.1% no | 96.7 ± 1.4% | RM2 acetate salt Life Molecular Imaging | 34452121 2021 Pharmaceutics The kit-based formulation of RM2 is suitable to disseminate GRP-R imaging and therapy to distant hospitals without complex radiochemistry equipment. — the higher radiolabeling yield obtained via the kit route (81.1 ± 1.1% vs. 48.9 ± 12.9% for the module; p < 0.0001, non-decay-corrected) |
| — | — | SPE | 48.9 ± 12.9% no | 99.4 ± 0.4% | RM2 | 34452121 2021 Pharmaceutics Conventionally prepared [68Ga]Ga-RM2 using an automated synthesizer was used as a comparator. — the higher radiolabeling yield obtained via the kit route (81.1 ± 1.1% vs. 48.9 ± 12.9% for the module; p < 0.0001, non-decay-corrected) |
| — | — | — | — | — | — | 33674398 2021 J Nucl Med |
| — | — | — | — | — | — | 41656418 2026 Eur J Nucl Med Mol Imaging |
| — | — | — | — | — | — | 41611483 2026 J Nucl Med |
| — | — | — | — | — | — | 40518457 2025 Eur J Nucl Med Mol Imaging |
Precursor
- Common precursor
- DOTA-conjugated GRPR-antagonist peptide RM2 (DOTA-Pip-D-Phe-Gln-Trp-Ala-Val-Gly-His-Sta-Leu-NH2) PMID 39760843 / DOI 10.1007/s13246-024-01510-0
- Suppliers seen in the literature
- —
- Cited suppliers in indexed syntheses
- Life Molecular Imaging, Nanchang Tanzhen Biological Technology Co., Ltd.
- 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
- —
How this set was arrived at. base set per Ph. Eur. general monograph 0125 (rule); radiometal tracer -> metal impurities (rule); Ga-68, generator production assumed (no synthesis data found) -> Ge-68 breakthrough (preliminary); 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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