Tracer library / [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
7
Prostate cancerBreast cancerReceptor expression phenotyping

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
[111In]In-RM2

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
—

Published syntheses

ModuleCassettePurificationYield %RCP %Precursor / supplierSource
——nonequantitative>95%RM240890559
2025 EJNMMI Res
——nonequantitative>95%[Hse7]RM240890559
2025 EJNMMI Res
——nonequantitative>95%[Bta8]RM240890559
2025 EJNMMI Res
Manual synthesis——>90%>95%RM239563828
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 ± 0.67DOTA-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
Kit-based preparation
Life Molecular Imaging
vendor cassettenone81.1 ± 1.1%
not corrected
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)
——SPE48.9 ± 12.9%
not corrected
99.4 ± 0.4%RM234452121
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)

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. Prospective head-to-head comparison of [68Ga]Ga-RM2 PET/CT and [68Ga]Ga-PSMA-617 PET/CT in newly diagnosed patients with intermediate-risk localized prostate cancer.
    2026 · Eur J Nucl Med Mol Imaging · Prospective
  2. Clinical impact of [68Ga]Ga-RM2 positron emission tomography imaging on staging and prognosis in estrogen receptor-positive breast cancer: A pilot study.
    2025 · Chin J Cancer Res · Prospective
  3. Modified PROMISE criteria for standardized interpretation of gastrin-releasing peptide receptor (GRPR)-targeted PET.
    2023 · Eur J Nucl Med Mol Imaging · Retrospective, prospective
  4. Comparison of 68Ga-PSMA-617 PET/CT and 68Ga-RM2 PET/CT in Patients with Localized Prostate Cancer Who Are Candidates for Radical Prostatectomy: A Prospective, Single-Arm, Single-Center, Phase II Study.
    2023 · J Nucl Med · Prospective · Phase II
  5. Physiological 68Ga-RM2 uptake in patients with biochemically recurrent prostate cancer: an atlas of semi-quantitative measurements.
    2020 · Eur J Nucl Med Mol Imaging · Prospective
  6. Prospective Study of the Radiolabeled GRPR Antagonist BAY86-7548 for Positron Emission Tomography/Computed Tomography Imaging of Newly Diagnosed Prostate Cancer.
    2019 · Eur Urol Oncol · Prospective
  7. Prospective Evaluation of 68Ga-RM2 PET/MRI in Patients with Biochemical Recurrence of Prostate Cancer and Negative Findings on Conventional Imaging.
    2018 · J Nucl Med · Prospective
  8. The Clinical Utility of 18F-Fluciclovine PET/CT in Biochemically Recurrent Prostate Cancer: an Academic Center Experience Post FDA Approval.
    2021 · Mol Imaging Biol · Retrospective
  9. Association between gastrin-releasing peptide receptor expression as assessed with [68Ga]Ga-RM2 PET/CT and histopathological tumor regression after neoadjuvant chemotherapy in primary breast cancer.
    2020 · Nucl Med Biol · Retrospective
  10. First-in-Human Serum Stability Studies of [177Lu]Lu-AMTG: A Step Toward Improved GRPR-Targeted Radiopharmaceutical Therapy.
    2025 · J Nucl Med · Clinical study
Show all 15 clinical studies
  1. Value of 68Ga-labeled bombesin antagonist (RM2) in the detection of primary prostate cancer comparing with [18F]fluoromethylcholine PET-CT and multiparametric MRI-a phase I/II study.
    2023 · Eur Radiol · Clinical study · Phase I/II
  2. PSMA- and GRPR-Targeted PET: Results from 50 Patients with Biochemically Recurrent Prostate Cancer.
    2021 · J Nucl Med · Clinical study
  3. 68Ga-RM2 PET in PSMA- positive and -negative prostate cancer patients.
    2019 · Nuklearmedizin · Clinical study
  4. Gastrin-releasing Peptide Receptor Imaging in Breast Cancer Using the Receptor Antagonist (68)Ga-RM2 And PET.
    2016 · Theranostics · Clinical study
  5. Pilot Comparison of ⁶⁸Ga-RM2 PET and ⁶⁸Ga-PSMA-11 PET in Patients with Biochemically Recurrent Prostate Cancer.
    2016 · J Nucl Med · Clinical study

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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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 integrityMolar activityMetal impuritiesGe-68 breakthrough
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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