Somatostatin Receptors as Targets for Nuclear Medicine Imaging and Radionuclide Treatment

Maecke, Helmut R.; Reubi, Jean Claude

doi:10.2967/jnumed.110.084236

Cited by 108 publications

(78 citation statements)

References 22 publications

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“…Ga-DOTATATE PET/CT provides valuable information on somatostatin receptor status in this group of patients when peptide receptor radionuclide therapy (PRRT) is being considered as part of the multimodal management in metastatic PCC/PGL [40,41]. High detectability of somatostatin receptor expression lesions in metastatic PCC/ PGL provides the basis for consideration of PRRT as initial therapeutic strategy.…”

mentioning

confidence: 99%

Diagnostic Performance of 68Ga-DOTATATE PET/CT, 18F-FDG PET/CT and 131I-MIBG Scintigraphy in Mapping Metastatic Pheochromocytoma and Paraganglioma

Tan

Hussein²,

Saad

et al. 2015

Nucl Med Mol Imaging

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confidence: 99%

Diagnostic Performance of 68Ga-DOTATATE PET/CT, 18F-FDG PET/CT and 131I-MIBG Scintigraphy in Mapping Metastatic Pheochromocytoma and Paraganglioma

Tan

Hussein²,

Saad

et al. 2015

Nucl Med Mol Imaging

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“…The overexpression of somatostatin receptor on neuroendocrine tumors (NETs) has allowed tumor localization, staging, therapy follow-up, and targeted radionuclide therapy (3). Radiolabeled somatostatin analogs can be used to localize NETs with high specificity and sensitivity, translating into successful targeted radionuclide therapy or to PET imaging (4)(5)(6)(7). Although the overexpression of somatostatin has proven to be an important tool for the targeting of NETs, there are limitations since not all NETs express somatostatin (8).…”

mentioning

confidence: 99%

The Glucose-Dependent Insulinotropic Polypeptide Receptor: A Novel Target for Neuroendocrine Tumor Imaging—First Preclinical Studies

Gourni

Waser

Clerc³

et al. 2014

J Nucl Med

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A new family of peptide receptors, the incretin receptor family, overexpressed on many neuroendocrine tumors (NETs) is of great importance because it may enable the in vivo peptide-based receptor targeting of a category of NETs that does not express the somatostatin receptor. Impressive in vivo diagnostic data were published for glucagonlike peptide 1 receptor-targeting radiopeptides. Recently, promising in vitro data have appeared for the second member of the incretin family, the glucose-dependent insulinotropic polypeptide (GIP) receptor. This prompted us to develop and evaluate a new class of radioligands with the potential to be used for the in vivo targeting of GIP receptor-positive tumors. Methods: GIP(1-42) was modified C-terminally, and the truncated peptides showed high affinity toward GIP receptor for the GIP conjugates. Specific in vitro internalization was found, and almost the entire cellassociated activity was internalized (.90% of the cell-bound activity), supporting the agonist potency of the 111 In-EG4 and 68 Ga-EG4 were shown to specifically target INR1G9-hGIPr xenografts, with tumor uptake of 10.4% ± 2.2% and 17.0% ± 4.4% injected activity/g, 1 h after injection, respectively. Kidneys showed the highest uptake, which could be reduced by approximately 40%-50% with a modified-fluid-gelatin plasma substitute or an inhibitor of the serine protease dipeptidyl peptidase 4. The PET images clearly visualized the tumor. Conclusion: The evaluation of EG4 as a proof-ofprinciple radioligand indicated the feasibility of imaging GIP receptorpositive tumors. These results prompt us to continue the development of this family of radioligands for imaging of a broad spectrum of NETs.

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“…In particular, somatostatin receptor tumor targeting currently constitutes a well-established method to image or to treat patients with somatostatin receptor-positive gastroenteropancreatic neuroendocrine tumors. 111 In-pentetreotide (OctreoScan; Covidien), for instance, has been widely used to visualize these types of tumors (4,5). Furthermore, in clinical studies, somatostatin receptor radionuclide therapy with patients with neuroendocrine tumors has given promising results (6).…”

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confidence: 99%

Evaluation of ¹⁷⁷Lu-DOTA-sst₂ Antagonist Versus ¹⁷⁷Lu-DOTA-sst₂ Agonist Binding in Human Cancers In Vitro

Cescato

Waser²,

Fani³

et al. 2011

J Nucl Med

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Somatostatin receptor targeting of neuroendocrine tumors using radiolabeled somatostatin agonists is today an established method to image and treat cancer patients. However, in a study using an animal tumor model, somatostatin receptor antagonists were shown to label sst 2 -and sst 3 -expressing tumors in vivo better than agonists, with comparable affinity even though they are not internalized into the tumor cell. In the present study, we evaluated the in vitro binding of the antagonist 177 Lu-DOTApNO 2 -Phe-c (DCys-Tyr-DTrp-Lys-Thr-Cys) DTyrNH 2 ( 177 Lu-DOTA-BASS) or the 177 Lu-DOTATATE agonist to sst 2 -expressing human tumor samples. Methods: Forty-eight sst 2 -positive human tumor tissue samples (9 ileal carcinoids, 10 pheochromocytomas, 7 breast carcinomas, 10 renal cell carcinomas, and 12 non-Hodgkin lymphomas) were analyzed by in vitro receptor autoradiography for the expression of sst 2 , comparing the binding capacity of 177 Lu-DOTA-BASS and 177 Lu-DOTATATE in successive tissue sections. The autoradiograms were quantitated using an electronic autoradiography detection system. Results: In all cases, the radiolabeled antagonist bound to more receptor sites than did the agonist. The mean ratios of the antagonist 177 Lu-DOTA-BASS to the agonist 177 Lu-DOTATATE were 4.2 6 0.5 in the 9 ileal carcinoids, 12 6 3 in the 10 pheochromocytomas, 11 6 4 in the 7 breast carcinomas, 5.1 6 0.6 in the 10 renal cell carcinomas, and 4.8 6 0.7 in the 12 non-Hodgkin lymphomas. Conclusion: The present in vitro human data, together with previous in vivo animal tumor data, are strong arguments indicating that sst 2 antagonists may be worth testing in vivo in patients in a wide range of tumors including nonneuroendocrine tumors.

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Somatostatin Receptors as Targets for Nuclear Medicine Imaging and Radionuclide Treatment

Cited by 108 publications

References 22 publications

Diagnostic Performance of 68Ga-DOTATATE PET/CT, 18F-FDG PET/CT and 131I-MIBG Scintigraphy in Mapping Metastatic Pheochromocytoma and Paraganglioma

Diagnostic Performance of 68Ga-DOTATATE PET/CT, 18F-FDG PET/CT and 131I-MIBG Scintigraphy in Mapping Metastatic Pheochromocytoma and Paraganglioma

The Glucose-Dependent Insulinotropic Polypeptide Receptor: A Novel Target for Neuroendocrine Tumor Imaging—First Preclinical Studies

Evaluation of ¹⁷⁷Lu-DOTA-sst₂ Antagonist Versus ¹⁷⁷Lu-DOTA-sst₂ Agonist Binding in Human Cancers In Vitro

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Somatostatin Receptors as Targets for Nuclear Medicine Imaging and Radionuclide Treatment

Cited by 108 publications

References 22 publications

Diagnostic Performance of 68Ga-DOTATATE PET/CT, 18F-FDG PET/CT and 131I-MIBG Scintigraphy in Mapping Metastatic Pheochromocytoma and Paraganglioma

Diagnostic Performance of 68Ga-DOTATATE PET/CT, 18F-FDG PET/CT and 131I-MIBG Scintigraphy in Mapping Metastatic Pheochromocytoma and Paraganglioma

The Glucose-Dependent Insulinotropic Polypeptide Receptor: A Novel Target for Neuroendocrine Tumor Imaging—First Preclinical Studies

Evaluation of 177Lu-DOTA-sst2 Antagonist Versus 177Lu-DOTA-sst2 Agonist Binding in Human Cancers In Vitro

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Evaluation of ¹⁷⁷Lu-DOTA-sst₂ Antagonist Versus ¹⁷⁷Lu-DOTA-sst₂ Agonist Binding in Human Cancers In Vitro