Tracer library / [90Y]Y-DOTA-TOC
Structure of DOTA-TOC (unlabelled parent compound, from PubChem)
Unlabelled parent compoundPubChem CID 158782

[90Y]Y-DOTA-TOC

Also written as DOTATOC; Y-90-DOTATOC; DOTA-TOC
Radionuclide
Y-90 t½ 3843.6 min
Modality
Therapy
Production route
—
Stage
—
Syntheses indexed
6
MeningiomaNeuroendocrine neoplasmsPeptide receptor radionuclide therapyPheochromocytoma and paraganglioma

What it is

Compound class
DOTA-conjugated somatostatin analog (radiolabeled peptide, DOTATOC)
Target / mechanism
Somatostatin receptor (SSTR) targeting PMID 39142827
Clinical application
Peptide receptor radionuclide therapy (PRRT) for somatostatin receptor-expressing tumors, including neuroendocrine tumors, pheochromocytoma/paraganglioma, and meningioma PMID 35450421
Theranostic pair
[68Ga]Ga-DOTA-TOC

Published syntheses

ModuleCassettePurificationYield %RCP %Precursor / supplierSource
Manual synthesiscustom manifoldnone96.2 ± 4.9%>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 - an average radiochemical yield ... of 96.2 ± 4.9% (n = 77) ... for 90Y ... DOTATOC
ADD-2
Amercare
custom manifoldnone90.3 ± 5.6%>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 - the average RCYs were 90.3 ± 5.6% (n = 63) for 90Y-DOTATOC
Modular-Lab EAZY
Eckert & Ziegler
vendor cassetteSPE82.0 ± 8.4%>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) ... for 90Y- ... DOTATOC ... were achieved
Manual synthesis——96.2 ± 4.9>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. - The mean radiochemical yields for 90Y-DOTATOC were 96.2 ± 4.9%
ADD-2
Amercare
custom manifold—90.3 ± 5.6>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 - 90.3 ± 5.6%, and 82.0 ± 8.4%
Modular-Lab EAZY
Eckert & Ziegler
vendor cassetteSPE82.0 ± 8.4>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

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. 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
  2. Intraarterial Peptide Receptor Radionuclide Therapy Using 90Y-DOTATOC for Hepatic Metastases of Neuroendocrine Tumors.
    2021 · J Nucl Med · Prospective
  3. Inflammation-Based Index and 68Ga-DOTATOC PET-Derived Uptake and Volumetric Parameters Predict Outcome in Neuroendocrine Tumor Patients Treated with 90Y-DOTATOC.
    2020 · J Nucl Med · Prospective · Phase II
  4. 90Y-DOTATOC Dosimetry-Based Personalized Peptide Receptor Radionuclide Therapy.
    2018 · J Nucl Med · Prospective · Phase II
  5. Tumor response and clinical benefit in neuroendocrine tumors after 7.4 GBq (90)Y-DOTATOC.
    2002 · J Nucl Med · Prospective · Phase II
  6. Analysis of outcome in patients with different primary localisation of neuroendocrine tumors after PRRT. 10 years single institution experience.
    2026 · Hell J Nucl Med · Retrospective
  7. Tumour-absorbed dose and efficacy of peptide receptor radionuclide therapy with [90Y]Y-DOTATOC in patients with refractory meningioma: a single-centre experience.
    2026 · Eur J Nucl Med Mol Imaging · Retrospective
  8. Peptide Receptor Radionuclide Therapy Is Effective for Clinical Control of Symptomatic Metastatic Insulinoma: A Long-Term Retrospective Analysis.
    2024 · J Nucl Med · Retrospective
  9. Retrospective study of peptide receptor radionuclide therapy for Japanese patients with advanced neuroendocrine tumors.
    2021 · J Hepatobiliary Pancreat Sci · Retrospective
  10. Twelve-Year Follow-up After Peptide Receptor Radionuclide Therapy.
    2019 · J Nucl Med · Retrospective
Show all 51 clinical studies
  1. Peptide Receptor Radionuclide Therapy in Grade 3 Neuroendocrine Neoplasms: Safety and Survival Analysis in 69 Patients.
    2019 · J Nucl Med · Retrospective
  2. Peptide receptor radioligand therapy is an effective treatment for the long-term stabilization of malignant gastrinomas.
    2011 · Cancer · Retrospective
  3. Receptor radionuclide therapy with 90Y-DOTATOC in patients with medullary thyroid carcinomas.
    2004 · Cancer Biother Radiopharm · Retrospective
  4. Long-term Efficacy, Survival, and Toxicity of Peptide Receptor Radionuclide Therapy in Patients With Refractory Meningioma.
    2025 · Clin Nucl Med · Clinical study
  5. Peptide Receptor Radionuclide Therapy in Advanced Refractory Meningiomas: Efficacy and Toxicity in a Long Follow-up.
    2024 · J Nucl Med · Clinical study
  6. Repeat Peptide Receptor Radionuclide Therapy in Neuroendocrine Tumors: A NET Center of Excellence Experience.
    2024 · J Gastrointest Cancer · Clinical study
  7. Addition of 131I-MIBG to PRRT (90Y-DOTATOC) for Personalized Treatment of Selected Patients with Neuroendocrine Tumors.
    2021 · J Nucl Med · Clinical study · Phase I
  8. 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
  9. Treatment With 90Y/177Lu-DOTATOC in Patients With Metastatic Adrenocortical Carcinoma Expressing Somatostatin Receptors.
    2020 · J Clin Endocrinol Metab · Clinical study
  10. DNA damage in human whole blood caused by radiopharmaceuticals evaluated by the comet assay.
    2019 · Mutagenesis · Clinical study
  11. Effectiveness of radiolabelled somatostatin analogues (90Y-DOTATOC and 177Lu-DOTATATE) in patients with metastatic neuroendocrine tumours: a single centre experience in Mexico.
    2017 · Rev Esp Med Nucl Imagen Mol · Clinical study
  12. The prognostic and predictive value of sstr2-immunohistochemistry and sstr2-targeted imaging in neuroendocrine tumors.
    2017 · Eur J Nucl Med Mol Imaging · Clinical study
  13. Cerenkov and radioluminescence imaging of brain tumor specimens during neurosurgery.
    2016 · J Biomed Opt · Clinical study
  14. Dynamic 68Ga-DOTATOC PET/CT and static image in NET patients. Correlation of parameters during PRRT.
    2016 · Nuklearmedizin · Clinical study
  15. 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
  16. 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
  17. 90Y-DOTATOC as a Therapeutic Option for Complex Recurrent or Progressive Meningiomas.
    2015 · J Nucl Med · Clinical study
  18. Impairment of lymphocyte function following yttrium-90 DOTATOC therapy.
    2015 · Cancer Immunol Immunother · Clinical study
  19. Toward radioguided surgery with β- decays: uptake of a somatostatin analogue, DOTATOC, in meningioma and high-grade glioma.
    2015 · J Nucl Med · Clinical study
  20. Peptide receptor radionuclide therapy of differentiated thyroid cancer: efficacy and toxicity.
    2015 · Arch Immunol Ther Exp (Warsz) · Clinical study
  21. Differentiated thyroid cancer: a new perspective with radiolabeled somatostatin analogues for imaging and treatment of patients.
    2014 · Thyroid · Clinical study
  22. 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
  23. Neuroendocrine tumor liver metastases: use of dynamic contrast-enhanced MR imaging to monitor and predict radiolabeled octreotide therapy response.
    2012 · Radiology · Clinical study
  24. Hepatic arterial infusion enhances DOTATOC radiopeptide therapy in patients with neuroendocrine liver metastases.
    2011 · Endocr Relat Cancer · Clinical study
  25. Peptide receptor radionuclide therapy with (90)Y-DOTATOC in recurrent meningioma.
    2009 · Eur J Nucl Med Mol Imaging · Clinical study
  26. Radiolabeled DOTATOC in patients with advanced paraganglioma and pheochromocytoma.
    2008 · Q J Nucl Med Mol Imaging · Clinical study
  27. Three-year recurrence-free survival in a patient with recurrent medulloblastoma after resection, high-dose chemotherapy, and intrathecal Yttrium-90-labeled DOTA0-D-Phe1-Tyr3-octreotide radiopeptide brachytherapy.
    2005 · Cancer · Clinical study
  28. Targeted radiotherapy for small cell lung cancer using 90Yttrium-DOTATOC, an Yttrium-labelled somatostatin analogue: a pilot trial.
    2004 · Lung Cancer · Clinical study
  29. Receptor-mediated radionuclide therapy with 90Y-DOTATOC in association with amino acid infusion: a phase I study.
    2003 · Eur J Nucl Med Mol Imaging · Clinical study · Phase I
  30. 90Y-DOTA-D-Phe1-Try3-octreotide in therapy of neuroendocrine malignancies.
    2002 · Biopolymers · Clinical study
  31. Local injection of the 90Y-labelled peptidic vector DOTATOC to control gliomas of WHO grades II and III: an extended pilot study.
    2002 · Eur J Nucl Med Mol Imaging · Clinical study
  32. Preliminary data on biodistribution and dosimetry for therapy planning of somatostatin receptor positive tumours: comparison of (86)Y-DOTATOC and (111)In-DTPA-octreotide.
    2001 · Eur J Nucl Med · Clinical study
  33. The clinical value of [90Y-DOTA]-D-Phe1-Tyr3-octreotide (90Y-DOTATOC) in the treatment of neuroendocrine tumours: a clinical phase II study.
    2001 · Ann Oncol · Clinical study · Phase II
  34. Radiopeptide transmitted internal irradiation of non-iodophil thyroid cancer and conventionally untreatable medullary thyroid cancer using.
    2001 · Nucl Med Commun · Clinical study
  35. Exceptional results in neuroendocrine-metastases-caused paraplegia treated with [90Y-DOTA]-D-Phe1-Tyr3-octreotide (90Y-DOTATOC), a radiolabelled somatostatin analogue.
    2000 · Clin Oncol (R Coll Radiol) · Clinical study
  36. Receptor-mediated radionuclide therapy with 90Y-DOTA-D-Phe1-Tyr3-Octreotide: preliminary report in cancer patients.
    1999 · Cancer Biother Radiopharm · Clinical study
  37. Locoregional regulatory peptide receptor targeting with the diffusible somatostatin analogue 90Y-labeled DOTA0-D-Phe1-Tyr3-octreotide (DOTATOC): a pilot study in human gliomas.
    1999 · Clin Cancer Res · Clinical study
  38. Metastatic Nasopharyngeal Carcinoma Treated With Intraarterial Combined With Intravenous Peptide Receptor Radionuclide Therapy.
    2019 · Clin Nucl Med · Case report
  39. Significant impact of transient deterioration of renal function on dosimetry in PRRT.
    2013 · Ann Nucl Med · Case report
  40. Successful targeted radiotherapy with 90Y-DOTATOC in a patient with Merkel cell carcinoma. A Case Report.
    2004 · Oncology · Case report
  41. Successful diffusible brachytherapy (dBT) of a progressive low-grade astrocytoma using the locally injected peptidic vector and somatostatin analogue [90Y]-DOTA0-D-Phe1-Tyr3-octreotide (DOTATOC).
    2001 · Swiss Med Wkly · Case report

Precursor

Common precursor
—
Suppliers seen in the literature
—
Cited suppliers in indexed syntheses
Gamma Servizi s.r.l.
Typical final purification
—

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Notes

Added at stage 21 from therapy-discovered.xlsx (bulk PubMed search by isotope/therapy-type/known-agent, not individually researched yet) -- 38 articles found. Target/mechanism, clinical application, indications, approval and precursor fields still need per-agent research and are intentionally left empty. Diagnostic pair signal at discovery: YES - Ga-68. | Stage 28: added indication(s) onc-ppgl from consolidated missing-rubric review.
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