Therapeutic Radiometals: Worldwide Scientific Literature Trend Analysis (2008–2018)

Uccelli, Licia; Martini, Petra; Cittanti, Corrado; Carnevale, Aldo; Missiroli, Loretta; Giganti, Melchiore; Bartolomei, Mirco; Boschi, Alessandra

doi:10.3390/molecules24030640

Cited by 24 publications

(16 citation statements)

References 32 publications

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“…Brought directly to the cancer cell, the radiation emitted by the radioactive decay causes irreversible ionization of the cell’s DNA, which induces its apoptosis. The main isotopes used today are iodine-131, yttrium-90, lutetium-177 and, to a lesser extent, rhenium-188 [ 158 ]. As mentioned earlier, the purpose of the DOTA-SSA design was to work with a chelating cavity capable of complexing radioelements for imaging or therapy.…”

Section: Targeting Of Somatostatin Receptors With Radiopharmaceutimentioning

confidence: 99%

“…In a theranostic perspective, other β-emitting nuclides could have a potential interest—such as 47 Sc (T 1/2 = 3.35 d, E βmax = 600.8 keV), 67 Cu (T 1/2 = 2.58 d, E βmax = 577 keV), and 161 Tb (T 1/2 = 6.91 d, E βmax = 593 keV)—to be coupled with 44 Sc, 64 Cu, and 152 Tb/ 155 Tb respectively [ 129 , 158 , 189 ]. To date, no 67 Cu-labeled somatostatin analogs have been described so far, and only very preliminary studies have been described with [ 161 Tb]-DTPA-Octreotide and [ 47 Sc]-DOTATOC [ 190 , 191 ].…”

Section: Targeting Of Somatostatin Receptors With Radiopharmaceutimentioning

confidence: 99%

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Overview of Radiolabeled Somatostatin Analogs for Cancer Imaging and Therapy

et al. 2020

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Identified in 1973, somatostatin (SST) is a cyclic hormone peptide with a short biological half-life. Somatostatin receptors (SSTRs) are widely expressed in the whole body, with five subtypes described. The interaction between SST and its receptors leads to the internalization of the ligand–receptor complex and triggers different cellular signaling pathways. Interestingly, the expression of SSTRs is significantly enhanced in many solid tumors, especially gastro-entero-pancreatic neuroendocrine tumors (GEP-NET). Thus, somatostatin analogs (SSAs) have been developed to improve the stability of the endogenous ligand and so extend its half-life. Radiolabeled analogs have been developed with several radioelements such as indium-111, technetium-99 m, and recently gallium-68, fluorine-18, and copper-64, to visualize the distribution of receptor overexpression in tumors. Internal metabolic radiotherapy is also used as a therapeutic strategy (e.g., using yttrium-90, lutetium-177, and actinium-225). With some radiopharmaceuticals now used in clinical practice, somatostatin analogs developed for imaging and therapy are an example of the concept of personalized medicine with a theranostic approach. Here, we review the development of these analogs, from the well-established and authorized ones to the most recently developed radiotracers, which have better pharmacokinetic properties and demonstrate increased efficacy and safety, as well as the search for new clinical indications.

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Section: Targeting Of Somatostatin Receptors With Radiopharmaceutimentioning

confidence: 99%

Section: Targeting Of Somatostatin Receptors With Radiopharmaceutimentioning

confidence: 99%

Overview of Radiolabeled Somatostatin Analogs for Cancer Imaging and Therapy

et al. 2020

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“…An amount of 1 mL of freshly prepared 90 Y-hinokitiol (45)(46)(47)(48)(49)(50)(51)(52)(53)(54)(55)(56)(57)(58)(59)(60)(61)(62)(63)(64) in Lipiodol phase was taken with a syringe and put into a 12-mL flat bottom glass vial, containing 10 mL of physiological serum (previously weighed), and the vial was closed. Activity in the vial was measured with the dose calibrator.…”

Section: Over Time Release In the Aqueous Phasementioning

confidence: 99%

Labeling of Hinokitiol with 90Y for Potential Radionuclide Therapy of Hepatocellular Carcinoma

et al. 2021

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Hepatocellular carcinoma (HCC), the most common form of primary liver tumors, is the fifth cancer in the world in terms of incidence, and third in terms of mortality. Despite significant advances in the treatment of HCC, its prognosis remains bleak. Transarterial radioembolization with radiolabeled microspheres and Lipiodol has demonstrated significant effectiveness. Here we present a new, simple radiolabeling of Lipiodol with Yttrium-90, for the potential treatment of HCC.

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“…However, advances are not limited to wider use of these established radionuclides, research on theranostics also was stimulated by investigation of alternative radionuclides to improve therapeutic efficacy, to adapt the physical half-life to the target under investigation or to improve the "matched pair" concept, i.e., eliminating differences in chemistry between a diagnostic and therapeutic radionuclide (6,7). A high interest emerged in the use of alpha emitters, to a great extent driven by the impressive results of using Actinium-225 labeled PSMA ligands, even when 177 Lu-analogs had failed (8) with an ever increasing number of publications on radionuclide production, preclinical and clinical results (9).…”

Section: Introductionmentioning

confidence: 99%

Emerging Radionuclides in a Regulatory Framework for Medicinal Products – How Do They Fit?

2021

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Recent years have seen the establishment of several radionuclides as medicinal products in particular in the setting of theranostics and PET. [177Lu]Lutetium Chloride or [64Cu]Copper Chloride have received marketing authorization as radionuclide precursor, [68Ga]Gallium Chloride has received regulatory approval in the form of different 68Ge/68Ga generators. This is a formal requirement by the EU directive 2001/83, even though for some of these radionuclide precursors no licensed kit is available that can be combined to obtain a final radiopharmaceuticals, as it is the case for Technetium-99m. In view of several highly promising, especially metallic radionuclides for theranostic applications in a wider sense, the strict regulatory environment poses the risk of slowing down development, in particular for radionuclide producers that want to provide innovative radionuclides for clinical research purposes, which is the basis for their further establishment. In this paper we address the regulatory framework for novel radionuclides within the EU, the current challenges in particular related to clinical translation and potential options to support translational development within Europe and worldwide.

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Therapeutic Radiometals: Worldwide Scientific Literature Trend Analysis (2008–2018)

Cited by 24 publications

References 32 publications

Overview of Radiolabeled Somatostatin Analogs for Cancer Imaging and Therapy

Overview of Radiolabeled Somatostatin Analogs for Cancer Imaging and Therapy

Labeling of Hinokitiol with 90Y for Potential Radionuclide Therapy of Hepatocellular Carcinoma

Emerging Radionuclides in a Regulatory Framework for Medicinal Products – How Do They Fit?

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