Tracer library / [177Lu]Lu-DOTA-LM3
[177Lu]Lu-DOTA-LM3
Also written as [Lu-177]Lu-DOTA-LM3; Lu-177-DOTA-LM3
- Radionuclide
- Lu-177 t½ 9584.6 min
- Modality
- Therapy
- Production route
- —
- Stage
- Clinical research
- Syntheses indexed
- 6
What it is
- Compound class
- Somatostatin receptor (SST2) antagonist peptide, DOTA-conjugated (DOTA-LM3)
- Target / mechanism
- Somatostatin receptor subtype 2 (SST2) antagonist PMID 40591088
- Clinical application
- Peptide receptor radionuclide therapy (PRRT) for metastatic neuroendocrine neoplasms PMID 33674401
- Theranostic pair
- —
Published syntheses
| Module | Cassette | Purification | Yield % | RCP % | Precursor / supplier | Source |
|---|---|---|---|---|---|---|
| Manual synthesis | — | none | >99% | >95% | DOTA-LM3 | 40591088 2025 EJNMMI Radiopharm Chem The 177Lu-DOTA-conjugates were obtained by incubating 3 nmol of the corresponding DOTA-conjugate in 250 µL of ammonium acetate buffer (0.4 M, pH 5.0) with [177Lu]LuCl3 (40–120 MBq, depending on the planned experiment) for 30 min at 95 °C. - Radiochemical yield (non-isolated product, estimated by radio-HPLC) was > 99% |
| Manual synthesis | — | none | >99% | >95% | DOTA-[2Pal3]-LM3 | 40591088 2025 EJNMMI Radiopharm Chem The 177Lu-DOTA-conjugates were obtained by incubating 3 nmol of the corresponding DOTA-conjugate in 250 µL of ammonium acetate buffer (0.4 M, pH 5.0) with [177Lu]LuCl3 (40–120 MBq, depending on the planned experiment) for 30 min at 95 °C. - Radiochemical yield (non-isolated product, estimated by radio-HPLC) was > 99% |
| Manual synthesis | — | none | >99% | >95% | DOTA-[3Pal3]-LM3 | 40591088 2025 EJNMMI Radiopharm Chem The 177Lu-DOTA-conjugates were obtained by incubating 3 nmol of the corresponding DOTA-conjugate in 250 µL of ammonium acetate buffer (0.4 M, pH 5.0) with [177Lu]LuCl3 (40–120 MBq, depending on the planned experiment) for 30 min at 95 °C. - Radiochemical yield (non-isolated product, estimated by radio-HPLC) was > 99% |
| Manual synthesis | — | none | >99% | >95% | DOTA-[4Pal3]-LM3 | 40591088 2025 EJNMMI Radiopharm Chem The 177Lu-DOTA-conjugates were obtained by incubating 3 nmol of the corresponding DOTA-conjugate in 250 µL of ammonium acetate buffer (0.4 M, pH 5.0) with [177Lu]LuCl3 (40–120 MBq, depending on the planned experiment) for 30 min at 95 °C. - Radiochemical yield (non-isolated product, estimated by radio-HPLC) was > 99% |
| Manual synthesis | — | none | — | >98% | DOTA-LM3 CSBio, California, US | 39046521 2024 Eur J Nucl Med Mol Imaging DOTA-LM3 (CSBio, Silicon Valley Menlo Park, California, United States) and DOTATATE (Bachem, Bubendorf, Switzerland) were labeled with terbium-161 or lutetium-177 at a molar activity of up to 100 MBq/nmol using standard labeling conditions as previously reported |
| — | — | — | — | ≥ 98% | DOTA-LM3 | 34625828 2022 Eur J Nucl Med Mol Imaging |
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.
- First-in-Humans Study of the SSTR Antagonist 177Lu-DOTA-LM3 for Peptide Receptor Radionuclide Therapy in Patients with Metastatic Neuroendocrine Neoplasms: Dosimetry, Safety, and Efficacy.2021 · J Nucl Med · Clinical study
- Successful Intra-arterial Peptide Receptor Radionuclide Therapy of DOTATOC-Negative High-Grade Liver Metastases of a Pancreatic Neuroendocrine Neoplasm Using 177Lu-DOTA-LM3: A Somatostatin Receptor Antagonist.2020 · Clin Nucl Med · Clinical study
- Superior NET Targeting by Switch From Agonist to Antagonist-mediated Somatostatin Receptor Theranostics Allowing Successful (LM3-based) PRRT of Otherwise Precluded mNET: Intraindividual Proof-of-concept.2026 · Clin Nucl Med · Case report
- TANDEM Peptide Receptor Radionuclide Therapy Using [ 225 Ac]Ac-/[ 177 Lu]Lu-DOTA-LM3 in a Patient With Parotid Gland Metastasis From Pancreatic Neuroendocrine Neoplasm.2025 · Clin Nucl Med · Case report
Precursor
- Common precursor
- —
- Suppliers seen in the literature
- —
- Cited suppliers in indexed syntheses
- CSBio
- Typical final purification
- —
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Added at stage 21 from therapy-discovered.xlsx (bulk PubMed search by isotope/therapy-type/known-agent, not individually researched yet) -- 9 articles found. Target/mechanism, clinical application, indications, approval and precursor fields still need per-agent research and are intentionally left empty. Stage set/updated at stage 23 from PMID 33674401: 'First-in-Humans Study of the SSTR Antagonist 177Lu-DOTA-LM3 for Peptide Receptor Radionuclide Therapy in Patients with Metastatic Neuroendocrine Neoplasms: Dosimetry, Safety, and Efficacy.'. | Stage 30 (2026-09-18): Stage was 'first-in-human'; normalised to 'Clinical research', original wording kept here.