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Gallium 68

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https://www.readbyqxmd.com/read/28075350/hydroxypyridinone-chelators-from-iron-scavenging-to-radiopharmaceuticals-for-pet-imaging-with-gallium-68
#1
REVIEW
Ruslan Cusnir, Cinzia Imberti, Robert C Hider, Philip J Blower, Michelle T Ma
Derivatives of 3,4-hydroxypyridinones have been extensively studied for in vivo Fe(3+) sequestration. Deferiprone, a 1,2-dimethyl-3,4-hydroxypyridinone, is now routinely used for clinical treatment of iron overload disease. Hexadentate tris(3,4-hydroxypyridinone) ligands (THP) complex Fe(3+) at very low iron concentrations, and their high affinities for oxophilic trivalent metal ions have led to their development for new applications as bifunctional chelators for the positron emitting radiometal, (68)Ga(3+), which is clinically used for molecular imaging in positron emission tomography (PET)...
January 8, 2017: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/28034291/radiopharmaceuticals-for-diagnosis-and-therapy-of-neuroendocrine-differentiated-prostate-cancer
#2
Giampiero Giovacchini, Elisabetta Giovannini, Mattia Riondato, Andrea Ciarmiello
Neuroendocrine differentiation of prostate cancer (PCa) is a relatively frequent event, generally understudied, that carries important prognostic information. It is most frequently observed during the advanced stages of disease, when PCa has lost its sensitivity to androgen deprivation therapy or to chemotherapy, moderate to diffuse bone metastatic spread dominates the imaging scenario and it is responsible for painful clinical symptomatology. However, evidences indicate that neuroendocrine differentiation is a progressive phenomenon that starts at the very early part of the pathogenesis of cancer transformation contributing to it...
December 29, 2016: Current Radiopharmaceuticals
https://www.readbyqxmd.com/read/28026127/well-differentiated-bronchial-neuroendocrine-tumors-clinical-management-and-outcomes-in-105-patients
#3
Marinos Pericleous, Anna Karpathakis, Christos Toumpanakis, Heather Lumgair, Jonathan Reiner, Laura Marelli, Christina Thirlwell, Martyn E Caplin
INTRODUCTION: Bronchial neuroendocrine tumors (NETs) are rare tumors representing approximately 20%-30% of all neuroendocrine tumors and 2%-3% of all adult lung cancers. Here, they present a large case series of well-differentiated bronchial NETs with the aim of investigating the behavior of these tumors and long-term outcomes. METHODS: A retrospective review was performed of 105 patients with bronchial NETs managed in a tertiary referral center in the period between January 1998 and January 2012...
December 27, 2016: Clinical Respiratory Journal
https://www.readbyqxmd.com/read/27989179/dipicolinate-complexes-of-gallium-iii-and-lanthanum-iii
#4
David M Weekes, Caterina F Ramogida, Maria de Guadalupe Jaraquemada-Peláez, Brian O Patrick, Chirag Apte, Thomas I Kostelnik, Jacqueline F Cawthray, Lisa Murphy, Chris Orvig
Three dipicolinic acid amine-derived compounds functionalized with a carboxylate (H3dpaa), phosphonate (H4dppa), and bisphosphonate (H7dpbpa), as well as their nonfunctionalized analogue (H2dpa), were successfully synthesized and characterized. The 1:1 lanthanum(III) complexes of H2dpa, H3dpaa, and H4dppa, the 1:2 lanthanum(III) complex of H2dpa, and the 1:1 gallium(III) complex of H3dpaa were characterized, including via X-ray crystallography for [La4(dppa)4(H2O)2] and [Ga(dpaa)(H2O)]. H2dpa, H3dpaa, and H4dppa were evaluated for their thermodynamic stability with lanthanum(III) via potentiometric and either UV-vis spectrophotometric (H3dpaa) or NMR spectrometric (H2dpa and H4dppa) titrations, which showed that the carboxylate (H3dpaa) and phosphonate (H4dppa) containing ligands enhanced the lanthanum(III) complex stability by 3-4 orders of magnitude relative to the unfunctionalized ligand (comparing log βML and pM values) at physiological pH...
December 19, 2016: Inorganic Chemistry
https://www.readbyqxmd.com/read/27981835/radiolabeled-selective-matrix-metalloproteinase-13-mmp-13-inhibitors-radio-syntheses-and-in-vitro-and-first-in-vivo-evaluation
#5
Verena Hugenberg, Stefan Wagner, Klaus Kopka, Michael Schäfers, Robert C Schuit, Albert D Windhorst, Sven Hermann
The noninvasive imaging of MMP activity in vivo could have a high impact in basic research as well as in clinical applications. This approach can be established using radiolabeled MMP inhibitors (MMPIs) as tracers for the detection of activated MMPs by means of PET. However, the complexity of diseases associated with dysregulated MMP expression necessitates the imaging of distinct MMPs or MMP subgroups to distinguish their individual role in specific diseases. To this end, selective and potent MMP-13 inhibitors based on a N,N'-bis(benzyl)pyrimidine-4,6-dicarboxamide core have been synthesized and successfully radiolabeled with carbon-11, fluorine-18, and gallium-68...
December 16, 2016: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/27980050/in-vivo-pet-imaging-of-the-cancer-integrin-%C3%AE-v%C3%AE-6-using-gallium-68-labelled-cyclic-rgd-nonapeptides
#6
Johannes Notni, Dominik Reich, Oleg V Maltsev, Tobias G Kapp, Katja Steiger, Frauke Hoffmann, Irene Esposito, Wilko Weichert, Horst Kessler, Hans-Jürgen Wester
: Expression of the cellular transmembrane receptor αvβ6 integrin is essentially restricted to malignant epithelial cells in carcinomas of a broad variety of lineages, while it is virtually absent in normal adult tissues. Thus, it is a highly attractive target for tumor imaging and therapy. Furthermore, αvβ6 integrin plays an important role for the epithelial-mesenchymal interaction and the development of fibrosis. METHODS: On the basis of the Gallium-68 chelators TRAP (triazacyclononane-triphosphinate) and NODAGA, we synthesized mono- di- and trimeric conjugates of the αvβ6 integrinselective peptide cyclo(FRGDLAFp(NMe)K) via click chemistry (CuAAC)...
December 15, 2016: Journal of Nuclear Medicine: Official Publication, Society of Nuclear Medicine
https://www.readbyqxmd.com/read/27966893/enhancing-pet-signal-at-target-tissue-in-vivo-dendritic-and-multimeric-tris-hydroxypyridinone-conjugates-for-molecular-imaging-of-%C3%AE-v%C3%AE-3-integrin-expression-with-gallium-68
#7
Cinzia Imberti, Samantha Y A Terry, Carleen Cullinane, Fiona Clarke, Georgina H Cornish, Nisha K Ramakrishnan, Peter Roselt, Andrew P Cope, Rodney J Hicks, Philip J Blower, Michelle T Ma
Tris(hydroxypyridinone) chelators conjugated to peptides can rapidly complex the positron-emitting isotope gallium-68 ((68)Ga) under mild conditions, and the resulting radiotracers can delineate peptide receptor expression at sites of diseased tissue in vivo. We have synthesized a dendritic bifunctional chelator containing nine 1,6-dimethyl-3-hydroxypyridin-4-one groups (SCN-HP9) that can coordinate up to three Ga(3+) ions. This derivative has been conjugated to a trimeric peptide (RGD3) containing three peptide groups that target the αvβ3 integrin receptor...
December 14, 2016: Bioconjugate Chemistry
https://www.readbyqxmd.com/read/27956089/outcome-analysis-of-first-line-somatostatin-analog-treatment-in-metastatic-pulmonary-neuroendocrine-tumors-and-prognostic-significance-of-18-fdg-pet-ct
#8
Alberto Bongiovanni, Federica Recine, Nada Riva, Flavia Foca, Chiara Liverani, Laura Mercatali, Silvia Nicolini, Federica Pieri, Dino Amadori, Toni Ibrahim
INTRODUCTION: Pulmonary carcinoids (PCs) are classed according to the World Health Organization 2004 classification as typical or atypical carcinoids. Owing to their rarity, no dedicated clinical trials with somatostatin analogs (SSAs) have been carried out on primary PCs. PATIENTS AND METHODS: From January 2007 to December 2015, 30 patients with metastatic PCs underwent first-line SSA treatment (20 with octreotide long-acting repeatable 30 mg and 10 with lanreotide 120 mg every 28 days)...
November 21, 2016: Clinical Lung Cancer
https://www.readbyqxmd.com/read/27910132/a-simple-method-for-preparation-of-pure-68-ga-acetate-precursor-for-formulation-of-radiopharmaceuticals-physicochemical-characteristics-of-the-68-ga-eluate-of-the-sno2-based-68-ge-68-ga-column-generator
#9
Sankha Chattopadhyay, Md Neyar Alam, Madhu Smita, Umesh Kumar, Sujata Saha Das, Luna Barua
Gallium-68 radioisotope is an excellent source in clinical positron emission tomography application due to its ease of availability from germanium-68 ((68) Ge)/gallium-68 ((68) Ga) generator having a shelf life of 1 year. In this paper, a modified method for purification of the primary eluate of (68) Ge-(68) Ga generator by using a small cation exchange resin (Dowex-50) column has been described. The breakthrough of (68) Ge before and after purification of (68) Ga eluate was 0.014% and 0.00027%, respectively...
December 1, 2016: Journal of Labelled Compounds & Radiopharmaceuticals
https://www.readbyqxmd.com/read/27904870/preclinical-study-of-68-ga-dotatoc-biodistribution-assessment-in-syrian-rats-and-evaluation-of-absorbed-dose-in-human-organs
#10
Mojdeh Naderi, Samaneh Zolghadri, Hassan Yousefnia, Ali Ramazani, Amir Reza Jalilian
OBJECTIVES: Gallium-68 DOTA-DPhe(1)-Tyr(3)-Octreotide ((68)Ga-DOTATOC) has been applied by several European centers for the treatment of a variety of human malignancies. Nevertheless, definitive dosimetric data are yet unavailable. According to the Society of Nuclear Medicine and Molecular Imaging, researchers are investigating the safety and efficacy of this radiotracer to meet Food and Drug Administration requirements. The aim of this study was to introduce the optimized procedure for (68)Ga-DOTATOC preparation, using a novel germanium-68 ((68)Ge)/(68)Ga generator in Iran and evaluate the absorbed doses in numerous organs with high accuracy...
2016: Asia Oceania Journal of Nuclear Medicine & Biology
https://www.readbyqxmd.com/read/27887852/morphological-and-functional-imaging-of-neck-paragangliomas
#11
J-P Guichard, N Fakhry, J Franc, P Herman, C-A Righini, D Taieb
OBJECTIVE: To review the optimal techniques for localization and characterization of neck paragangliomas (PGL). MATERIAL AND METHODS: Systematic review of the literature from the PubMed/Medline database. RESULTS: Neck PGL are hypervascular tumours essentially arising from paraganglionic tissue situated at the carotid bifurcation (carotid body) and along the vagus nerve. Morphological and functional imaging are indicated to confirm the diagnosis, identify multifocal disease and for local and regional staging...
November 22, 2016: European Annals of Otorhinolaryngology, Head and Neck Diseases
https://www.readbyqxmd.com/read/27876341/imaging-of-neuroendocrine-tumors-of-the-pancreas
#12
C Dromain, D Déandréis, J-Y Scoazec, D Goere, M Ducreux, E Baudin, L Tselikas
Pancreatic neuroendocrine tumors (PNETs) are rare and represent a heterogeneous disease. PNET can be functioning or non-functioning with different clinical presentations and different prognosis based on WHO and pTNM classifications. The role of imaging includes the localization of small functioning tumor, differentiation of these tumors from adenocarcinoma, identification of signs of malignancy and evaluation of extent. PNETs have a broad spectrum of appearance. On CT and MRI, most of functioning PNETs are well defined small tumors with intense and homogeneous enhancement on arterial and portal phases...
December 2016: Diagnostic and Interventional Imaging
https://www.readbyqxmd.com/read/27843513/bilateral-choroidal-metastases-from-endobronchial-carcinoid-treated-with-somatostatin-analogues
#13
Deborah De Bruyn, Jan Lamont, Erik Vanderstraeten, Simon Van Belle, Elise Platteau, Julie De Zaeytijd, Kristien P Hoornaert
OBJECTIVE: To describe a patient with bilateral multifocal choroidal metastases from an endobronchial carcinoid treated with a somatostatin analogue. METHOD: A 60-year-old woman presenting with photopsia in the left eye underwent an extensive ophthalmic examination, including fluorescein angiography, OCT and ultrasound. RESULTS: Fundoscopy revealed a small retinal tear in the left eye, for which she received laser treatment. In addition, choroidal masses were detected in both eyes...
2016: Open Ophthalmology Journal
https://www.readbyqxmd.com/read/27829184/inorganic-oxides-with-potential-application-in-the-preparation-of-a-68-ge-68-ga-generator-system
#14
E Romero, M A Morcillo
The ion exchange properties of some tin and titanium oxides with potential application in the development of a (68)Ge/(68)Ga generator were determined. The best potential candidates, SnO2 and calcined SnO2, were further characterized by powder X-Ray Diffraction (XRD), Scanning Electron Microscopy (SEM) and Brunauer-Emmett-Teller (BET) surface area analysis and its radiation stability was also determined. Two (68)Ge/(68)Ga pilot generators (1.85MBq) based on SnO2 and calcined SnO2 were developed and evaluated over 100 and 200 elution cycles respectively, using as eluent different concentrations of HCl...
January 2017: Applied Radiation and Isotopes
https://www.readbyqxmd.com/read/27819034/quantification-of-%C3%AE-cell-mass-in-intramuscular-islet-grafts-using-radiolabeled-exendin-4
#15
Daniel Espes, Ramkumar Selvaraju, Irina Velikyan, Martin Krajcovic, Per-Ola Carlsson, Olof Eriksson
BACKGROUND: There is an increasing interest in alternative implantation sites to the liver for islet transplantation. Intramuscular implantation has even been tested clinically. Possibilities to monitor β-cell mass would be of huge importance not only for the understanding of islet engraftment but also for the decision of changing the immunosuppressive regime. We have therefore evaluated the feasibility of quantifying intramuscular β-cell mass using the radiolabeled glucagon like peptide-1 receptor agonist DO3A-VS-Cys(40)-Exendin-4...
August 2016: Transplantation Direct
https://www.readbyqxmd.com/read/27805844/localization-of-insulinoma-using-68-ga-dotatate-pet-ct-scan
#16
Pavel Nockel, Bruna Babic, Corina Millo, Peter Herscovitch, Dhaval Patel, Naris Nilubol, Samira Sadowski, Craig Cochran, Phillip Gorden, Electron Kebebew
CONTEXT: The reliable localization of insulinoma is critical for the successful surgical treatment. OBJECTIVE: This study compared the accuracy of (68)Gallium (Ga)-DOTATATE PET/CT to anatomic imaging modalities, selective arterial secretagogue injection (SASI), and intraoperative ultrasound (IOUS) and palpation for localizing insulinoma in patients who were biochemically cured. DESIGN, SETTING, AND PATIENTS: We conducted a retrospective analysis of 31 patients who had an insulinoma confirmed on histology and were biochemically cured...
November 2, 2016: Journal of Clinical Endocrinology and Metabolism
https://www.readbyqxmd.com/read/27804868/gallium-68-in-medical-imaging
#17
Lucia Martiniova, Louis De Palatis, Elba Etchebehere, Gregory Ravizzini
Over the past several years, Positron Emission Tomography (PET) imaging agents labeled with 68Gallium (68Ga) have undergone a significant increase in clinical utilization. 68Ga is conveniently produced from a germanium-68/gallium-68 (68Ge/68Ga) generator. Because of the compact size and ease of use of the generator, 68Ga labeled compounds may be more cost-effective than PET radioisotopes that are cyclotron-produced. The convenient half-life of 68Ga (T1/2=68 min) provides sufficient radioactivity for various PET imaging applications, while delivering acceptable radiation doses to patients...
October 28, 2016: Current Radiopharmaceuticals
https://www.readbyqxmd.com/read/27775994/the-role-of-68ga-dota-tate-pet-ct-scanning-in-the-evaluation-of-patients-with-multiple-myeloma-preliminary-results
#18
Kerim Sonmezoglu, Betul Vatankulu, Tugrul Elverdi, Resit Akyel, Melih E Erkan, Metin Halac, Meltem Ocak, Emre Demirci, Yildiz Aydin
OBJECTIVE: In this observational pilot study, we aimed to evaluate the role of gallium-68-labelled DOTA-TATE (Ga-TATE) PET/computed tomography (CT) scanning in patients with multiple myeloma (MM), considering previous promising results obtained from conventional somatostatin receptor scintigraphy with In pentetreotide. MATERIALS AND METHODS: Twenty-one patients with a diagnosis of MM were prospectively included in this study: eight patients were referred for initial staging and 13 patients for restaging purpose...
January 2017: Nuclear Medicine Communications
https://www.readbyqxmd.com/read/27771904/pilot-study-use-of-gallium-68-psma-pet-for-detection-of-metastatic-lesions-in-patients-with-renal-tumour
#19
Handoo Rhee, John Blazak, Chui Ming Tham, Keng Lim Ng, Benjamin Shepherd, Malcolm Lawson, John Preston, Ian Vela, Paul Thomas, Simon Wood
BACKGROUND: In this study, we prospectively evaluate the diagnostic potential of a gallium-68 (68Ga) prostate-specific membrane antigen (PSMA)-binding ligand and positron emission tomography (PET) in detecting metastatic lesions in patients with renal tumour. The secondary aim was to determine whether the findings would result in the alteration of patient management. RESULTS: Ten patients with renal lesion and potential metastatic disease on conventional imaging were recruited...
December 2016: EJNMMI Research
https://www.readbyqxmd.com/read/27743211/evaluation-of-a-flexible-nota-rgd-kit-solution-using-gallium-68-from-different-68-ge-68-ga-generators-pharmacokinetics-and-biodistribution-in-nonhuman-primates-and-demonstration-of-solitary-pulmonary-nodule-imaging-in-humans
#20
Thomas Ebenhan, Isabel Schoeman, Daniel D Rossouw, Anne Grobler, Biljana Marjanovic-Painter, Judith Wagener, Hendrik G Kruger, Mike M Sathekge, Jan Rijn Zeevaart
PURPOSE: Radiopharmaceuticals containing the motive tripeptide arginyl-glycyl-asparatic acid (RGD) are known to target ανβ3 integrins during tumor angiogenesis. A more generic kit radiolabeling procedure accommodating Ga-68 from different generators was developed for NOTA-RGD and evaluated for its versatile use and safety in subsequent in vivo applications. The [(68)Ga]NOTA-RGD kit was further verified for its expected biodistribution and pharmacokinetics in nonhuman primates and its clinical sensitivity to detect solitary pulmonary nodules (SPN) in cancer patients...
October 14, 2016: Molecular Imaging and Biology: MIB: the Official Publication of the Academy of Molecular Imaging
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