ArticleEuropean journal of nuclear medicine and molecular imaging2012
Comprehensive evaluation of a somatostatin-based radiolabelled antagonist for diagnostic imaging and radionuclide therapy.
Article in European journal of nuclear medicine and molecular imaging, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 14 papers.
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Who cites it
14 citing papers in PubMed, 45 citations in OpenAlex.
- Controversies in NEN: An ENETS position statement on the interchangeability of somatostatin receptor PET tracers.Journal of neuroendocrinology · 2026Review
- Peptide Radioligands in Cancer Theranostics: Agonists and Antagonists.Pharmaceuticals (Basel, Switzerland) · 2023Review
- [Pharmaceutics · 2023Article
- Radiolabeled Somatostatin Analogs-A Continuously Evolving Class of Radiopharmaceuticals.Cancers · 2022Review
- Alpha-peptide receptor radionuclide therapy using actinium-225 labeled somatostatin receptor agonists and antagonists.Frontiers in medicine · 2022Review
- Preclinical study of a newAsia Oceania journal of nuclear medicine & biology · 2020Article
- The tetraamine chelator outperforms HYNIC in a new technetium-99m-labelled somatostatin receptor 2 antagonist.EJNMMI research · 2018Article
- Guideline for PET/CT imaging of neuroendocrine neoplasms withEuropean journal of nuclear medicine and molecular imaging · 2017Article
- Current Status of Radiopharmaceuticals for the Theranostics of Neuroendocrine Neoplasms.Pharmaceuticals (Basel, Switzerland) · 2017Review
- Functional Imaging of Paragangliomas with an Emphasis on Von Hippel-Lindau-Associated Disease: A Mini Review.Journal of kidney cancer and VHL · 2017Review
- [Theranostics · 2017Article
- Peptide receptor radionuclide therapy: focus on bronchial neuroendocrine tumors.Tumour biology : the journal of the International Society for Oncodevelopmental Biology and Medicine · 2016Review
- Peptide receptor radionuclide therapy using radiolabeled somatostatin analogs: focus on future developments.Clinical and translational imaging · 2014Review
- Peptide receptor targeting in cancer: the somatostatin paradigm.International journal of peptides · 2013Article
Corrections and comments
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Authors and funding
6 authors at 5 institutions in 4 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
purposeTargeting of tumours positive for somatostatin receptors (sst) with radiolabelled peptides is of interest for tumour localization, staging, therapy follow-up and targeted radionuclide therapy. The peptides used clinically are exclusively agonists, but recently we have shown that the radiolabelled somatostatin-based antagonist (111)In-DOTA-sst2-ANT may be preferable to agonists. However, a comprehensive study of this radiolabelled antagonist to determine its significance was lacking. The present report describes the evaluation of this novel antagonist labelled with (111)In and (177)Lu in three different tumour models.
methodsRadiopeptide binding, internalization and dissociation studies were performed using cells expressing HEK293-rsst(2). Biodistribution studies were performed in HEK293-rsst(2), HEK293-hsst(2) and HEK293-rsst(3) xenografted mice.
resultsSaturation binding analysis confirmed earlier IC(50) data for (111/nat)In-DOTA-sst2-ANT and showed similar affinity of (177/nat)Lu-DOTA-sst2-ANT for the sst(2). Only low internalization was found in cell culture (6.68 ± 0.06 % at 4 h), which was not unexpected for an antagonist, and this could be further reduced by the addition of sucrose. No internalization was observed in HEK293 cells not expressing sst. Both results indicate that the internalization was specific. (111)In-DOTA-sst2-ANT and (177)Lu-DOTA-sst2-ANT were shown to target tumour xenografts expressing the rat and the human sst(2) receptor with no differences in their uptake or pharmacokinetics. The uptake in rsst(2) and hsst(2) was high (about 30 %IA/g 4 h after injection) and surprisingly long-lasting (about 20-23 %IA/g 24 h after injection). Kidney uptake was blocked by approximately 50 % by lysine or Gelofusine.
conclusionThese results indicate that radiolabelled somatostatin-based antagonists may be superior to corresponding agonists. The long tumour retention time of (177)Lu-DOTA-sst2-ANT indicates that this new class of compounds is of relevance not only in diagnostic imaging but also in targeted radionuclide therapy of sst-positive tumours.
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