Tracer library / [177Lu]Lu-DOTA-TOC
[177Lu]Lu-DOTA-TOC
Also written as [177Lu]Lu-DOTATOC; [Lu-177]Lu-DOTATOC; DOTA-TOC; DOTATOC; edotreotide; Lu-177 DOTATOC
- Radionuclide
- Lu-177 t½ 9585 min
- Modality
- Therapy
- Production route
- —
- Stage
- —
- Syntheses indexed
- 11
What it is
- Compound class
- DOTA-conjugated somatostatin analog peptide (DOTA-TOC)
- Target / mechanism
- Somatostatin receptor (SSTR) targeting agonist PMID 32859703
- Clinical application
- Peptide receptor radionuclide therapy (PRRT) for neuroendocrine tumors PMID 40148509
- Theranostic pair
- [68Ga]Ga-DOTA-TOC
Published syntheses
| Module | Cassette | Purification | Yield % | RCP % | Precursor / supplier | Source |
|---|---|---|---|---|---|---|
| Modular-Lab EAZY Eckert & Ziegler | vendor cassette | none | 93.4 ± 3.9 | 99.7 ± 0.2 radio-HPLC | DOTA-TOC ABX | 37233924 2023 EJNMMI Radiopharm Chem ModularLab EAZY (Eckert & Ziegler Eurotope GmbH, Berlin, Germany) - we achieved an improved balanced radiochemical yield of 93.4 ± 3.9% with a decreased precursor load of 10–17 µg |
| Manual synthesis | custom manifold | none | 98.3 ± 0.6% | >99% TLC, >97% HPLC | DOTATOC Gamma Servizi s.r.l., Pavia, Italy | 29097938 2017 Contrast Media Mol Imaging a manually assembled system consisting of tubes, valves, and syringes - 98.3 ± 0.6% (n = 43) for ... 177Lu-DOTATOC |
| ADD-2 Amercare | custom manifold | none | 90.8 ± 8.3% | >98% | DOTATOC Gamma Servizi s.r.l., Pavia, Italy | 29097938 2017 Contrast Media Mol Imaging The radiolabelling was performed by using an ADD-2 (Amercare, Thame, UK), a prototype of a semiautomatic dose dispenser device - 90.8 ± 8.3% (n = 88) for 177Lu-DOTATOC |
| Modular-Lab EAZY Eckert & Ziegler | vendor cassette | SPE | 83.1 ± 5.7% | >97% | DOTATOC Gamma Servizi s.r.l., Pavia, Italy | 29097938 2017 Contrast Media Mol Imaging Modular-Lab Eazy automatic synthesizer, disposable cassettes (C0-YDOTAPEP-CM, C0-LUDOTAPEP-CM, C0-YDOTAPSMA-CM, and C0-LUDOTAPSMA-CM), hardware, and reagent kits were supplied by Eckert & Ziegler Eurotope GmbH (Berlin, Germany) - 83.1 ± 5.7% (n = 26) for ... 177Lu-DOTATOC, respectively, were achieved |
| Manual synthesis | — | — | — | >95% | DOTATOC ABX | 40147849 2025 J Nucl Med Radiolabeling of the DOTA compounds was done at 85°C for 25 min, using ascorbic acid buffer and no-carrier-added [177Lu]LuCl3 |
| Modular-Lab EAZY Eckert & Ziegler | vendor cassette | none | 93.4 ± 3.9 | 99.7 ± 0.2 | DOTA-TOC ABX | 37233924 2023 EJNMMI Radiopharm Chem All three radiopharmaceuticals were successfully synthesized in high radiochemical purities and yields on the ML Eazy. - we achieved an improved balanced radiochemical yield of 93.4 ± 3.9% with a decreased precursor load of 10–17 µg |
| Manual synthesis | — | — | — | ≥ 98% | DOTATOC | 34625828 2022 Eur J Nucl Med Mol Imaging Radiolabeling and quality control of the SST analogues were performed as previously reported [43]. |
| Manual synthesis | — | — | 98.3 ± 0.6 | >99% TLC, >97% HPLC | DOTATOC Gamma Servizi s.r.l., Pavia, Italy | 29097938 2017 Contrast Media Mol Imaging Manual labelling was carried out using telescopic tongs and dedicated poly(methyl methacrylate) (PMMA) shielding for syringes and vials. - for 177Lu-DOTATOC they were 98.3% ± 0.6 |
| ADD-2 Amercare | custom manifold | — | 90.8 ± 8.3 | >98% | DOTATOC Gamma Servizi s.r.l., Pavia, Italy | 29097938 2017 Contrast Media Mol Imaging The radiolabelling was performed by using an ADD-2 (Amercare, Thame, UK), a prototype of a semiautomatic dose dispenser device - 90.8% ± 8.3, and 83.1 ± 5.7% |
| Modular-Lab EAZY Eckert & Ziegler | vendor cassette | SPE | 83.1 ± 5.7 | >97% | DOTATOC Gamma Servizi s.r.l., Pavia, Italy | 29097938 2017 Contrast Media Mol Imaging Modular-Lab Eazy automatic synthesizer, disposable cassettes (C0-YDOTAPEP-CM, C0-LUDOTAPEP-CM, C0-YDOTAPSMA-CM, and C0-LUDOTAPSMA-CM), hardware, and reagent kits were supplied by Eckert & Ziegler Eurotope GmbH (Berlin, Germany). - average RCYs of 82.0 ± 8.4% (n = 24) and 83.1 ± 5.7% (n = 26) for 90Y- and 177Lu-DOTATOC, respectively |
| Modular-Lab EAZY Eckert & Ziegler | vendor cassette | SPE | 90.1 ± 0.8 | >99% TLC, >98% HPLC | PSMA-617 Gamma Servizi s.r.l., Pavia, Italy | 29097938 2017 Contrast Media Mol Imaging Modular-Lab Eazy automatic synthesizer, disposable cassettes (C0-YDOTAPEP-CM, C0-LUDOTAPEP-CM, C0-YDOTAPSMA-CM, and C0-LUDOTAPSMA-CM), hardware, and reagent kits were supplied by Eckert & Ziegler Eurotope GmbH (Berlin, Germany). - average RCYs of 76.4 ± 2.2% (n = 5) and 90.1 ± 0.8% (n = 5), for yttrium-90 and lutetium-177, respectively, were achieved |
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.
- Targeted β--Particle Plus Conversion and Auger-Electron Therapy with 161Tb-Labeled Somatostatin Receptor Antagonist DOTA-LM3: A Phase 0 Study.2026 · J Nucl Med · Prospective · Phase 0
- Radiolabeled Somatostatin Receptor Antagonist Versus Agonist for Peptide Receptor Radionuclide Therapy in Patients with Therapy-Resistant Meningioma: PROMENADE Phase 0 Study.2024 · J Nucl Med · Prospective · Phase 0
- Glucose Metabolism Modification Induced by Radioligand Therapy with [177Lu]Lu/[90Y]Y-DOTATOC in Advanced Neuroendocrine Neoplasms: A Prospective Pilot Study within FENET-2016 Trial.2022 · Pharmaceutics · Prospective · Phase II
- Radiolabelled somatostatin receptor antagonist versus agonist for peptide receptor radionuclide therapy in patients with metastatic pheochromocytoma or paraganglioma: a retrospective pilot study.2026 · Eur J Nucl Med Mol Imaging · Retrospective
- Multimodal Deep Learning for Prediction of Progression-Free Survival in Patients with Neuroendocrine Tumors Undergoing 177Lu-Based Peptide Receptor Radionuclide Therapy.2026 · Cancers (Basel) · Retrospective
- SSTR-directed peptide receptor radionuclide therapy for recurrent meningiomas: analysis of safety, efficacy and prognostic factors.2025 · Eur J Nucl Med Mol Imaging · Retrospective
- Beyond similarities: overall survival and prognostic insights from [¹⁷⁷Lu]Lu-DOTATOC therapy in neuroendocrine tumors.2025 · Eur J Nucl Med Mol Imaging · Retrospective
- Peptide Receptor Radionuclide Therapy Is Effective for Clinical Control of Symptomatic Metastatic Insulinoma: A Long-Term Retrospective Analysis.2024 · J Nucl Med · Retrospective
- Comparison of Choi, RECIST and Somatostatin Receptor PET/CT Based Criteria for the Evaluation of Response and Response Prediction to PRRT.2022 · Pharmaceutics · Retrospective
- Retrospective study of peptide receptor radionuclide therapy for Japanese patients with advanced neuroendocrine tumors.2021 · J Hepatobiliary Pancreat Sci · Retrospective
Show all 36 clinical studies
- Peptide Receptor Radionuclide Therapy in Grade 3 Neuroendocrine Neoplasms: Safety and Survival Analysis in 69 Patients.2019 · J Nucl Med · Retrospective
- [(177)Lu-DOTA](0)-D-Phe(1)-Tyr(3)-Octreotide ((177)Lu-DOTATOC) For Peptide Receptor Radiotherapy in Patients with Advanced Neuroendocrine Tumours: A Phase-II Study.2016 · Theranostics · Retrospective
- Peptide receptor radioligand therapy is an effective treatment for the long-term stabilization of malignant gastrinomas.2011 · Cancer · Retrospective
- Long-term Efficacy, Survival, and Toxicity of Peptide Receptor Radionuclide Therapy in Patients With Refractory Meningioma.2025 · Clin Nucl Med · Clinical study
- A Randomized clinical trial evaluating the impact on survival and quality of life of 177Lutetium[Lu]-edotreotide versus everolimus in patients with neuroendocrine tumors of the lung and thymus: the LEVEL study (GETNE T-2217).2025 · BMC Cancer · Clinical study
- Safety and Efficacy of Para-Aminohippurate Coinfusion for Renal Protection During Peptide Receptor Radiotherapy in Patients with Neuroendocrine Tumors.2024 · J Nucl Med · Clinical study
- Improving Overall Survival and Quality of Life in Patients with Prostate Cancer and Neuroendocrine Tumors Using 177Lu-iPSMA and 177Lu-DOTATOC: Experience after 905 Treatment Doses.2023 · Pharmaceutics · Clinical study
- 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
- Intraindividual comparison of [177Lu]Lu-DOTA-EB-TATE and [177Lu]Lu-DOTA-TOC.2021 · Eur J Nucl Med Mol Imaging · Clinical study
- A Rapid and Safe Infusion Protocol for 177Lu Peptide Receptor Radionuclide Therapy.2021 · J Nucl Med · Clinical study
- Dissimilar DNA Damage to Blood Lymphocytes After 177Lu-Labeled DOTATOC or Prostate-Specific Membrane Antigen Therapy.2021 · J Nucl Med · Clinical study
- 177Lu-DOTATOC Peptide Receptor Radionuclide Therapy in a Patient With Neuroendocrine Breast Carcinoma and Breast Invasive Ductal Carcinoma.2020 · Clin Nucl Med · Clinical study
- Ectopic Corticotropin-Releasing Hormone-Secreting Pancreatic Neuroendocrine Tumor: Excellent Response of Liver Metastases to Peptide Receptor Radionuclide Therapy as Demonstrated by 68Ga-DOTATOC and 18F-FDG PET/CT Imaging.2020 · Clin Nucl Med · Clinical study
- Treatment With 90Y/177Lu-DOTATOC in Patients With Metastatic Adrenocortical Carcinoma Expressing Somatostatin Receptors.2020 · J Clin Endocrinol Metab · Clinical study
- Peptide receptor radionuclide therapy for aggressive pituitary tumors: a monocentric experience.2019 · Endocr Connect · Clinical study
- The prognostic and predictive value of sstr2-immunohistochemistry and sstr2-targeted imaging in neuroendocrine tumors.2017 · Eur J Nucl Med Mol Imaging · Clinical study
- Semi-automatic 3D-volumetry of liver metastases from neuroendocrine tumors to improve combination therapy with 177Lu-DOTATOC and 90Y-DOTATOC.2016 · Diagn Interv Radiol · Clinical study
- Time Evolution of DOTATOC Uptake in Neuroendocrine Tumors in View of a Possible Application of Radioguided Surgery with β- Decay.2015 · J Nucl Med · Clinical study
- DNA damage in blood lymphocytes in patients after (177)Lu peptide receptor radionuclide therapy.2015 · Eur J Nucl Med Mol Imaging · Clinical study
- Impact of peptide receptor radionuclide therapy on the 68Ga-DOTATOC-PET/CT uptake in normal tissue.2013 · Q J Nucl Med Mol Imaging · Clinical study
- Radiolabeled somatostatin analogues therapy in advanced neuroendocrine tumors: a single centre experience.2012 · J Oncol · Clinical study
- PET SUV correlates with radionuclide uptake in peptide receptor therapy in meningioma.2012 · Eur J Nucl Med Mol Imaging · Clinical study
- Hepatic arterial infusion enhances DOTATOC radiopeptide therapy in patients with neuroendocrine liver metastases.2011 · Endocr Relat Cancer · Clinical study
- Radiolabeled DOTATOC in patients with advanced paraganglioma and pheochromocytoma.2008 · Q J Nucl Med Mol Imaging · Clinical study
- Metastatic Nasopharyngeal Carcinoma Treated With Intraarterial Combined With Intravenous Peptide Receptor Radionuclide Therapy.2019 · Clin Nucl Med · Case report
- Successful palliative peptide receptor radionuclide therapy for impending compression of vena cava due to unresectable liver metastasis of neuroendocrine tumor.2019 · EXCLI J · Case report
Precursor
- Common precursor
- —
- Suppliers seen in the literature
- —
- Cited suppliers in indexed syntheses
- ABX, Gamma Servizi s.r.l.
- Typical final purification
- —
Need this precursor?We can point you to suppliers for [177Lu]Lu-DOTA-TOC, or handle the enquiry for you.
Get in touchQuality control Derived from the published synthesis
- 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.
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-TOC.
Get in touchNotes
Added from reverse module search (stage 6); 3 article(s) with Lu-177. Compound class inferred from precursor name (not stated outright) -- PMID 37233924: 'DOTA-TOC (GMP quality, product no. 9702) was purchased from ABX, Radeberg, Germany'. | Stage 28: added indication(s) onc-ppgl from consolidated missing-rubric review.