Clinical implications of somatostatin-receptor scintigraphy in ophthalmic Graves' disease

Colao, Annamaria; Pivonello, Rosario; Lastoria, Secondo; Faggiano, Antongiulio; Ferone, Diego; Lombardi, Gaetano; Fenzi, Gianfranco

doi:10.1530/eje.0.143s035

Cited by 9 publications

(32 citation statements)

References 39 publications

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“…The internalized receptor-ligand complexes are first found in endosomes, and later part of the radioactivity may be seen in the nucleus and also in mitochondria [according to one report only (577)]. The selection of the radioisotopes depends on the purpose of the targeting: for diagnostic applications, isotopes emitting g-radiation are necessary, such as 99m Tc, 111 In, or positron-emitters (e.g., 68 Ga), which also lead to g-radiation. For therapeutic application, short-range a-emitters (rare) or b-emitters (more frequent) are selected or, alternatively, isotopes that emit Auger electrons.…”

Section: Principles Of Tumor Targeting With Radiopeptidesmentioning

confidence: 99%

“…Incorporation of 111 In, 67/68 Ga, 64 Cu, and 86 Y into peptides requires a chelator, and for 18 F, a prosthetic group is necessary. 123/124 I can be inserted by direct labeling, and this is also possible for 99m Tc if the peptide contains a disulfide bond (Fig.…”

Section: Radioisotopes For In Vivo Tumor Targetingmentioning

confidence: 99%

“…Cyclotron-produced 123 I reveals good imaging results but is costly and not readily available. Similarly, 111 In is cyclotron-produced and has limited availability at high costs, yields good scintigraphy, and can be used for acquiring delayed images. However, it produces a relatively high radiation burden to patients.…”

Section: Radioisotopes For In Vivo Tumor Targetingmentioning

confidence: 99%

“…4) to [Tyr 3 ]-octreotide via reductive alkylation of [Tyr 3 , Lys(Boc) 5 ]-octreotide with glyoxylic acid, followed by conjugation of the N-terminally generated carboxy group of [Tyr 3 ]-octreotide to 1-( p-aminobenzyl)-pentakis-butyloxy-DTPA and deprotection with TFA (507,515). The serum stability for both 111 In-and 90 Y-labeled [DTPA(PABz)-D-Phe 1 , Tyr 3 ]-octreotide was clearly increased, but a relatively high accumulation in nontumor tissues (adrenals, pancreas, kidneys) limited its application for internal radiotherapy, most likely due to the increased lipophilicity of the peptide (507,515). Recently, alternative DTPA-derived chelators (374), DTPA linked to octreotide via metabolizable linkers (506), or modified DTPA-peptide structures have been tested.…”

Section: Reprintsmentioning

confidence: 99%

“…Not only did radiolabeled SRIF peptides serve as models for the development of new concepts for radiopeptide targeting (569) it was also the SRIF analogue octreotide labeled with 111 In which was first registered radiopharmaceutical (OctreoScan Õ ) for tumor scintigraphy in 1991 (31) and has since then been further developed for therapeutic application using 90 Y as radionuclide (OctreoTher Õ ) (504).…”

Section: Introductionmentioning

confidence: 99%

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Receptor-Mediated Tumor Targeting with Radiopeptides. Part 1. General Concepts and Methods: Applications to Somatostatin Receptor-Expressing Tumors

Eberlé

Mild

Froidevaux

2004

Journal of Receptors and Signal Transduction

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Radiolabeled peptides have become important tools in nuclear oncology, both as diagnostics and more recently also as therapeutics. They represent a distinct sector of the molecular targeting approach, which in many areas of therapy will implement the old "magic bullet" concept by specifically directing the therapeutic agent to the site of action. In this three-part review, we present a comprehensive overview of the literature on receptor-mediated tumor targeting with the different radiopeptides currently studied. Part I summarizes the general concepts and methods of targeting, the selection of radioisotopes, chelators, and the criteria of peptide ligand development. Then, the >400 studies on the application to somatostatin/somatostatin-release inhibiting factor receptor-mediated tumor localization and treatment will be reviewed, demonstrating that peptide radiopharmaceuticals have gained an important position in clinical medicine.

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Section: Principles Of Tumor Targeting With Radiopeptidesmentioning

confidence: 99%

Section: Radioisotopes For In Vivo Tumor Targetingmentioning

confidence: 99%

Section: Radioisotopes For In Vivo Tumor Targetingmentioning

confidence: 99%

Section: Reprintsmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

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Receptor-Mediated Tumor Targeting with Radiopeptides. Part 1. General Concepts and Methods: Applications to Somatostatin Receptor-Expressing Tumors

Eberlé

Mild

Froidevaux

2004

Journal of Receptors and Signal Transduction

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Nuclear Medicine Imaging of Infections and Inflammation of Central Nervous System and of the Head and Neck Structures

Signore¹,

Lanzolla²,

Lauri³

2021

Radionuclide Imaging of Infection and Inflammation

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Slow-release lanreotide in Graves’ ophthalmopathy: A double-blind randomized, placebo-controlled clinical trial

Chang

Liao

2006

J Endocrinol Invest

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SS analogs are an attractive alternative in treating Graves' ophthalmopathy (GO). Most of the previous studies were uncontrolled and enrolled few patients. The present study was conducted as a larger scale, prospective, randomized controlled study to determine the effectiveness of a slow-release formulation of lanreotide in GO. Sixty patients with active GO received an im injection every two weeks of either lanreotide 30 mg or placebo for 12 weeks. They were then followed and further treated in the traditional way if necessary. The Clinical Activity Score (CAS) was the primary efficacy criterion. Proptosis, diplopia, corneal erosion or ulcer, visual acuity, extraocular muscle movement and intraocular pressure were also evaluated. At the end of the 12 weeks, the mean CAS was not significantly decreased in the lanreotide group compared to the placebo group. The overall mean difference of proptosis between these two groups also did not reach significance at 12 weeks. Only diplopia at downward gaze had significant improvement for the lanreotide- treated group vs placebo group (p = 0.03). No differences were observed between the two groups compared to other outcome measures. During the 24-month follow-up after the clinical trial, 14 patients received eye surgery in the placebo group compared with 10 patients in the lanreotide group (p = 0.29). Six patients received methylprednisolone pulse therapy in the placebo group and two patients in the lanreotide group (p = 0.25). In conclusion, lanreotide treatment had no significant effects on GO compared with placebo.

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Clinical implications of somatostatin-receptor scintigraphy in ophthalmic Graves' disease

Cited by 9 publications

References 39 publications

Receptor-Mediated Tumor Targeting with Radiopeptides. Part 1. General Concepts and Methods: Applications to Somatostatin Receptor-Expressing Tumors

Receptor-Mediated Tumor Targeting with Radiopeptides. Part 1. General Concepts and Methods: Applications to Somatostatin Receptor-Expressing Tumors

Nuclear Medicine Imaging of Infections and Inflammation of Central Nervous System and of the Head and Neck Structures

Slow-release lanreotide in Graves’ ophthalmopathy: A double-blind randomized, placebo-controlled clinical trial

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