Diagnosis and therapy are walking together on radiopeptides’ avenue

Mansi, Luigi; Virgolini, Irene

doi:10.1007/s00259-011-1762-8

Cited by 18 publications

(9 citation statements)

References 27 publications

(31 reference statements)

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“…Similarly, a favourable cost/effective result may be obtained using radioactive complexes concentrating on the basis of a mechanical and non-functional mechanism. This is the case for alternative routes of administration such as by using radiolabelled microspheres for intra-arterial therapy of liver neoplasms or radiocolloids for intra-articular synovectomy [49]. However, as a result of using radionuclide therapy radiotracers with a high molecular weight and/or by using biologically active molecules such as antibodies there exists more potential for complexity and unfavourable pharmacokinetics.…”

Section: The Radionuclide Therapy Scenario: From Radio-iodine To Radimentioning

confidence: 99%

Radionuclide Antibody-Conjugates, a Targeted Therapy Towards Cancer

Kitson¹,

Cuccurullo²,

Moody³

et al. 2013

CRP

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Targeted alpha therapy (TAT) is an investigational procedure which utilises monoclonal antibodies (mAbs), peptide conjugates and/or other chemical compounds. These bio-vectors are able to transport a dose of alpha particles to destroy cancer cells. Radionuclide antibody-conjugates (RACs), labelled with beta emitters, have already been used in humans. More recently, TAT has been introduced to treat oncological diseases mainly leukaemia and lymphoma. Encouraging results have also been obtained in solid neoplasms with the administration of anti-tenascin. This chimeric antibody labelled with astatine-211 was delivered in patients with recurrent brain tumours into a surgically created cavity. Conversely, a clinical trial using a standard TAT approach to treat patients with metastatic melanoma, observed the shrinkage of the solid tumour mass. This response in melanoma may lead to an alternative mechanism for TAT, called tumour-antivascular- alpha-therapy (TAVAT), and forms the basis of a novel approach to the treatment of cancer disease states. In this paper, we will concentrate mainly on the application of TAT using antibodies. In particular, an investigation into the major general features connected with the use of alpha emitters in cancer therapy will be discussed. The prospective role of TAT with RACs will also be outlined briefly, especially focussing on the most important therapeutic strategies to date based on antibodies radiolabelled with beta emitters.

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Section: The Radionuclide Therapy Scenario: From Radio-iodine To Radimentioning

confidence: 99%

Radionuclide Antibody-Conjugates, a Targeted Therapy Towards Cancer

Kitson¹,

Cuccurullo²,

Moody³

et al. 2013

CRP

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“…The aim of this short review is to assemble recently available information on the physiological roles of somatostatin and similar substances, on modern concepts on receptors, and on binding modulators, in order to attempt to arrive at a new level of interpretation that will put a new light on scintigraphic and binding data. These data should also be a guiding complement for new peptide tracers being developed [ 3 ].…”

Section: The Settingmentioning

confidence: 99%

Reflections on the theory of "silver bullet" octreotide tracers: implications for ligand-receptor interactions in the age of peptides, heterodimers, receptor mosaics, truncated receptors, and multifractal analysis

Moncayo

2011

EJNMMI Research

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The classical attitude of Nuclear Medicine practitioners on matters of peptide-receptor interactions has maintained an intrinsic monogamic character since many years. New advances in the field of biochemistry and even in clinical Nuclear Medicine have challenged this type of thinking, which prompted me to work on this review. The central issue of this paper will be the use of somatostatin analogs, i.e., octreotide, in clinical imaging procedures as well as in relation to neuroendocirne tumors. Newly described characteristics of G-protein coupled receptors such as the formation of receptor mosaics will be discussed. A small section will enumerate the regulatory processes found in the cell membrane. Possible new interpretations, other than tumor detection, based on imaging procedures with somatostatin analogs will be presented. The readers will be taken to situations such as inflammation, nociception, mechanosensing, chemosensing, fibrosis, taste, and vascularity where somatostatin is involved. Thyroid-associated orbitopathy will be used as a model for the development of multi-agent therapeutics. The final graphical summary depicts the multifactorial properties of ligand binding.

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“…Additionally, it has been revealed that the evaluation of remnant liver function can help to discriminate different stages of alcoholic liver cirrhosis [ 10 ] and could be used to differentiate areas of steatosis, fibrosis, and cholestasis [ 11 ]. Moreover, control of liver status before and during peptide receptor radionuclide therapy (PRRT) [ 12 ] could lead to an optimized patient management. Furthermore, patients who are potentially suitable for selective internal radiation therapy (SIRT) [ 13 ] may also benefit from such a diagnostic method, allowing stratifying patients according to their peri-interventional risk.…”

Section: Introductionmentioning

confidence: 99%

[68Ga]NOTA-Galactosyl Human Serum Albumin: a Tracer for Liver Function Imaging with Improved Stability

et al. 2017

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PurposeNon-invasive techniques allowing quantitative determination of the functional liver mass are of great interest for patient management in a variety of clinical settings. Recently, we presented [68Ga]DTPA-GSA to target the hepatic asialoglycoprotein receptor for this purpose. Here, we introduce [68Ga]NOTA-GSA to improve metabolic stability of the radiopharmaceutical and compare the imaging properties with [68Ga]DTPA-GSA.ProceduresLabeling of the compounds was carried out at room temperature using 1.9 M sodium acetate as buffer. For quality control, thin-layer, high-performance liquid, and size exclusion chromatographies were used. Metabolic stability was studied in rat and human serums. For in vivo evaluation, Fischer rats were scanned by positron emission tomography and magnetic resonance imaging and subsequently sacrificed for biodistribution studies. Time activity curves (TACs) for heart and liver were generated and corresponding parameters (T50, T90, LHL15, HH15) were calculated.Results[68Ga]NOTA-GSA can be produced in high radiochemical yield and purity (>95 %) within 15 min. Stability studies revealed almost no metabolite formation over the 2-h observation period. Analysis of the TACs showed comparable results for most of the investigated parameters. The only significant difference was found in the T90 value, where [68Ga]NOTA-GSA showed slower uptake in comparison with 68Ga-DTPA-GSA (123 ± 10 vs. 89 ± 3 s, p < 0.01).Conclusions[68Ga]NOTA-GSA showed a significant increase of the metabolic stability and in most organs lower background activity. However, comparison of LHL15 and HH15 indicates that the increased stability did not further improve the diagnostic value. Thus, [68Ga]NOTA-GSA and [68Ga]DTPA-GSA can be used equivalent for imaging hepatic function with positron emission tomography.

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Diagnosis and therapy are walking together on radiopeptides’ avenue

Cited by 18 publications

References 27 publications

Radionuclide Antibody-Conjugates, a Targeted Therapy Towards Cancer

Radionuclide Antibody-Conjugates, a Targeted Therapy Towards Cancer

Reflections on the theory of "silver bullet" octreotide tracers: implications for ligand-receptor interactions in the age of peptides, heterodimers, receptor mosaics, truncated receptors, and multifractal analysis

[68Ga]NOTA-Galactosyl Human Serum Albumin: a Tracer for Liver Function Imaging with Improved Stability

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