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Gallium 68

Surbhi Prakash, Puja Panwar Hazari, Virendra Kumar Meena, Anil Kumar Mishra
A new S-alkylated cysteine-derivatized tumor targeting agent, 2,2'-(12-(2-((2-acetamido-2-carboxyethyl)thio)acetamido)-11,13-dioxo-1,4,7,10-tetraazacyclotridecane-4,7-diyl)diacetic acid was developed for positron emission tomography (PET) imaging. N -Acetyl cysteine (NAC) was conjugated to ATRIDAT as a specific targeting agent toward L-type and ASC amino acid transporter systems in the oncogenic cells. NAC was attached via S-alkylation to prevent its incorporation at undesired recognition sites affecting the signal-to-noise ratio...
June 30, 2018: ACS Omega
Erik de Blois, Rory M S de Zanger, Elisabeth Oehlke, Ho Sze Chan, Wouter A P Breeman
INTRODUCTION: 68 Ga-radiopharmaceuticals are common in the field of Nuclear Medicine to visualize receptor-mediated processes. In contrast to straightforward labeling procedures for clinical applications, preclinical in vitro and in vivo applications are hampered for reasons like e.g. volume restriction, activity concentration, molar activity and osmolality. Therefore, we developed a semi-automatic system specifically to overcome these problems. A difficulty appeared unexpectedly, as intrinsic trace metals derived from eluate (Zn, Fe and Cu) are concentrated as well in amounts that influence radiochemical yield and thus lower molar activity...
June 27, 2018: Nuclear Medicine and Biology
Alexander Wurzer, Julia Pollmann, Alexander Schmidt, Dominik Reich, Hans-Jürgen Wester, Johannes Notni
Radiopharmaceuticals targeting the enzyme prostate-specific membrane antigen (PSMA; synonyms: glutamate carboxypeptidase II, NAALADase; EC have recently emerged as powerful agents for diagnosis and therapy (theranostics) of prostate carcinoma (PCa). The radiation doses for therapeutic application of such compounds are limited by substantial uptakes in kidneys and salivary glands, with excess doses reportedly leading to radiotoxicity-related adverse effects, such as kidney insufficiency or xenostomia...
July 16, 2018: Molecular Pharmaceutics
Xiaozhu Wang, María de Guadalupe Jaraquemada-Peláez, Yang Cao, Jinhe Pan, Kuo-Shyan Lin, Brian O Patrick, Chris Orvig
An acyclic hexadentate oxine-derived chelating ligand, H2 hox, was investigated as an alternative to current chelators for 68 Ga. The straightforward preparation of H2 hox, involving only one or two steps, obviates the synthetic challenges associated with many reported 68 Ga chelators; it forms a Ga3+ complex of great stability (log K = 34.4) with a remarkably high gallium scavenging ability (pGa3+ = -log[Ga3+ free ] = 28.3, ([Ga3+ ] = 1 μM; [L x- ] = 10 μM; pH 7.4, and 25 °C)). Moreover, H2 hox coordinates 68 Ga quantitatively in 5 min at room temperature in ligand concentrations as low as 1 × 10-7 M, achieving an unprecedented high molar activity of 11 ± 1 mCi/nmol (407 ± 3...
July 10, 2018: Inorganic Chemistry
Stefan A Koerber, Leon Will, Clemens Kratochwil, Matthias F Haefner, Henrik Rathke, Christophe Kremer, Jonas Merkle, Klaus Herfarth, Klaus Kopka, Peter L Choyke, Tim Holland-Letz, Uwe Haberkorn, Juergen Debus, Frederik L Giesel
The present study analyzed the impact of Gallium-68 (68 Ga)-labeled prostate-specific membrane antigen-HBED-CC (68 Ga-PSMA-11) positron-emission tomography (PET)/computed tomography (CT) on radiotherapeutic management in a large cohort of men with primary or recurrent disease. Methods: This study investigated 121 men with carcinoma of the prostate who underwent 68 Ga-PSMA-11 PET/CT as well as conventional imaging. 50 patients were treatment naive, 11 had persistent prostate-specific antigen (PSA) soon after surgery and 60 presented with recurrent PSA following definitive therapy...
July 5, 2018: Journal of Nuclear Medicine: Official Publication, Society of Nuclear Medicine
Ludwike W M van Kalmthout, Marnix G E H Lam, Bart de Keizer, Gerard C Krijger, Tessa F T Ververs, Rememrt de Roos, Arthur J A T Braat
BACKGROUND: External cooling of the salivary glands is advised to prevent xerostomia in lutetium-177-PSMA treatment for advanced prostate cancer. Since evidence addressing this subject is sparse, this study aims to determine impact of icepacks application on uptake in salivary glands. Eighty-nine patients referred for gallium-68-PSMA PET/CT for (re)staging of prostate cancer were prospectively included. Twenty-four patients were scanned with unilateral (solely left-sided) icepacks; 20 with bilateral icepacks; 45 without icepacks...
July 3, 2018: EJNMMI Research
Kristen M Anderson, Christopher V Barback, Zhengtao Qin, David J Hall, Carl K Hoh, David R Vera, Michael T McHale
Molecular imaging with a fluorescent version of Tilmanocept may permit an accurate and facile detection of sentinel nodes of endometrial cancer. Tilmanocept accumulates in sentinel lymph nodes (SLN) by binding to a cell surface receptor unique to macrophages and dendritic cells. Four female Yorkshire pigs underwent cervical stromal injection of IRDye800-Tilmanocept, a molecular imaging agent tagged with near-infrared fluorescent dye and radiolabeled with gallium-68 and technetium-99m. PET/CT scans 1.5 hours post-injection provided pre-operative SLN mapping...
2018: PloS One
Rakhee Vatsa, Abhiram Gopalajois Ashwathanarayana, Jaya Shukla, Shashank Singh, Priya Bhusari, Rajender Kumar, Harmandeep Singh, Bhagwant Rai Mittal
The gamut of gallium labeled radiopharmaceuticals contributes to augmented variety in molecular imaging approach for in vivo identification of tumor characteristics. The spectrum ranges from somatostatin receptor based target-specific imaging agents, to those used for tumor imaging based on specific receptor types extending into ones used for therapeutic monitoring. The versatility of gallium chemistry provides the needed advantage for imaging which is further exploited in clinical practice influences the specificity of tumor imaging...
July 2018: Indian Journal of Nuclear Medicine: IJNM: the Official Journal of the Society of Nuclear Medicine, India
Frédéric Arsenault, Jean-Mathieu Beauregard, Frédéric Pouliot
PURPOSE OF REVIEW: In recent years, major advances in molecular imaging of prostate cancers (PCa) were made with the development and clinical validation of highly accurate PET tracers to stage and restage the disease. Prostate-specific membrane antigen (PSMA) is a transmembrane protein highly expressed in PCa, and its expression has led to the development of PSMA-binding radiopharmaceuticals for molecular imaging or radioligand therapy (RLT). We herein review the recent literature published on diagnostic and therapeutic (i...
June 22, 2018: Current Opinion in Supportive and Palliative Care
Marina Lledos, Vincenzo Mirabello, Sophia Sarpaki, Haobo Ge, Hubert J Smugowski, Laurence Carroll, Eric O Aboagye, Franklin I Aigbirhio, Stanley W Botchway, Jonathan R Dilworth, David G Calatayud, Pawel K Plucinski, Gareth J Price, Sofia I Pascu
Molecular imaging has become a powerful technique in preclinical and clinical research aiming towards the diagnosis of many diseases. In this work, we address the synthetic challenges in achieving lab-scale, batch-to-batch reproducible copper-64- and gallium-68-radiolabelled metal nanoparticles (MNPs) for cellular imaging purposes. Composite NPs incorporating magnetic iron oxide cores with luminescent quantum dots were simultaneously encapsulated within a thin silica shell, yielding water-dispersible, biocompatible and luminescent NPs...
April 2018: ChemNanoMat: Chemistry of Nanomaterials for Energy, Biology and More
Jyotsna Bhatt, Archana Mukherjee, Ajit Shinto, Kamaleshwaran Koramadai Karuppusamy, Aruna Korde, Mukesh Kumar, Haladhar Dev Sarma, Krishnamohan Repaka, Ashutosh Dash
INTRODUCTION: Gallium-68 based infection imaging agents are in demand to detect infection foci with high spatial resolution and sensitivity. In this study, Ubiquicidin derived octapeptide, UBI (31-38) conjugated with macrocyclic chelator NOTA was radiolabeled with 68 Ga to develop infection imaging agent. METHODS: Circular dichroism (CD) spectroscopy was performed to study conformational changes in UBI (31-38) and its NOTA conjugate in a "membrane like environment"...
May 4, 2018: Nuclear Medicine and Biology
Adrienn Vágner, Attila Forgács, Ernő Brücher, Imre Tóth, Alessandro Maiocchi, Alexander Wurzer, Hans-Jürgen Wester, Johannes Notni, Zsolt Baranyai
In order to rationalize the influence of FeIII contamination on labeling with the 68 Ga eluted from 68 Ge/68 Ga- g enerator, a detailed investigation was carried out on the equilibrium properties, formation and dissociation kinetics of GaIII - and FeIII -complexes of 1,4,7-triazacyclononane-1,4,7-tris(methylene[2-carboxyethylphosphinic acid]) (H6 TRAP). The stability and protonation constants of the [Fe(TRAP)]3- complex were determined by pH-potentiometry and spectrophotometry by following the competition reaction between the TRAP ligand and benzhydroxamic acid (0...
2018: Frontiers in Chemistry
Kristen A Wangerin, Lucia Baratto, Mohammad Mehdi Khalighi, Thomas A Hope, Praveen K Gulaka, Timothy W Deller, Andrei H Iagaru
OBJECTIVE: Gallium-68-labeled radiopharmaceuticals pose a challenge for scatter estimation because their targeted nature can produce high contrast in these regions of the kidneys and bladder. Even small errors in the scatter estimate can result in washout artifacts. Administration of diuretics can reduce these artifacts, but they may result in adverse events. Here, we investigated the ability of algorithmic modifications to mitigate washout artifacts and eliminate the need for diuretics or other interventions...
June 6, 2018: AJR. American Journal of Roentgenology
Anja Braune, Martin Scharffenberg, Anne Naumann, Thomas Bluth, Marcelo Gama de Abreu, Jörg Kotzerke
AIM: We compared 68 Gallium (68 Ga)- and fluorescence-labeled microspheres for measurement of pulmonary perfusion distribution in anesthetized pigs without lung injury. METHODS: In two mechanically ventilated pigs, the distribution of pulmonary perfusion was marked in vivo with 68 Ga- and fluorescence-labeled microspheres in supine and prone position. After each injection, the distribution of 68 Ga-labeled microspheres was measured in vivo with positron emission tomography/ computed tomography (PET/CT) in the position in which microspheres were injected and vice versa...
June 2018: Nuklearmedizin. Nuclear Medicine
Kay M Westenfelder, Beatrice Lentes, Julia Rackerseder, Nassir Navab, Jürgen E Gschwend, Matthias Eiber, Tobias Maurer
No abstract text is available yet for this article.
May 29, 2018: Clinical Genitourinary Cancer
Sanchit Sharma, Achintya D Singh, Surendra K Sharma, Madhavi Tripathi, Chandan J Das, Rajeev Kumar
INTRODUCTION: We evaluated the role of gallium-68-labeled [1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid]-1-Nal3-octreotide (Ga-DOTA-NOC) PET/CT in assessing sarcoidosis disease activity. PATIENTS AND METHODS: Patients diagnosed with sarcoidosis underwent Ga-DOTA-NOC-PET/CT. The maximum standardized uptake value (SUVmax) at the pathological site and in the descending thoracic aorta (reference standard, SUVmed) were assessed. A SUVmax/SUVmed ratio (disease activity score) of more than one was considered a marker of active disease and was compared with the clinical symptoms and serum angiotensin-converting enzyme and computed tomography (CT) scan...
May 30, 2018: Nuclear Medicine Communications
Dominik Summer, Christine Rangger, Maximilian Klingler, Peter Laverman, Gerben M Franssen, Beatrix E Lechner, Thomas Orasch, Hubertus Haas, Elisabeth von Guggenberg, Clemens Decristoforo
Cholecystokinin-2 receptors (CCK2R) are overexpressed in a variety of malignant diseases and therefore have gained certain attention for peptide receptor radionuclide imaging. Among extensive approaches to improve pharmacokinetics and metabolic stability of minigastrin (MG) based radioligands, the concept of multivalency for enhanced tumour targeting has not been investigated extensively. We therefore utilized fusarinine C (FSC) as chelating scaffold for novel mono-, di-, and trimeric bioconjugates for targeting CCK2R expression...
2018: Contrast Media & Molecular Imaging
Pardeep Kumar, Sushil K Tripathi, C P Chen, Eric Wickstrom, Mathew L Thakur
PURPOSE: In recent years, considerable progress has been made in the use of gallium-68 labeled receptor-specific peptides for imaging oncologic diseases. The objective was to examine the stability and pharmacokinetics of [68 Ga]NODAGA and DOTA-peptide conjugate targeting VPAC [combined for vasoactive intestinal peptide (VIP) and pituitary adenylate cyclase-activating peptide (PACAP)] receptors on tumor cells. PROCEDURES: A VPAC receptor-specific peptide was chosen as a model peptide and conjugated to NODAGA and DOTA via solid-phase synthesis...
May 25, 2018: Molecular Imaging and Biology: MIB: the Official Publication of the Academy of Molecular Imaging
Sonya Youngju Park, Claudia Zacharias, Caitlyn Harrison, Richard E Fan, Christian Kunder, Negin Hatami, Frederik Giesel, Pejman Ghanouni, Bruce Daniel, Andreas M Loening, Geoffrey A Sonn, Andrei Iagaru
Purpose To report the results of dual-time-point gallium 68 (68 Ga) prostate-specific membrane antigen (PSMA)-11 positron emission tomography (PET)/magnetic resonance (MR) imaging prior to prostatectomy in patients with intermediate- or high-risk cancer. Materials and Methods Thirty-three men who underwent conventional imaging as clinically indicated and who were scheduled for radical prostatectomy with pelvic lymph node dissection were recruited for this study. A mean dose of 4.1 mCi ± 0.7 (151.7 MBq ± 25...
May 16, 2018: Radiology
Sebastian Zschaeck, Fabian Lohaus, Marcus Beck, Gregor Habl, Stephanie Kroeze, Constantinos Zamboglou, Stefan Alexander Koerber, Jürgen Debus, Tobias Hölscher, Peter Wust, Ute Ganswindt, Alexander D J Baur, Klaus Zöphel, Nikola Cihoric, Matthias Guckenberger, Stephanie E Combs, Anca Ligia Grosu, Pirus Ghadjar, Claus Belka
68 Gallium prostate specific membrane antigen (PSMA) ligand positron emission tomography (PET) is an increasingly used imaging modality in prostate cancer, especially in cases of tumor recurrence after curative intended therapy. Owed to the novelty of the PSMA-targeting tracers, clinical evidence on the value of PSMA-PET is moderate but rapidly increasing. State of the art imaging is pivotal for radiotherapy treatment planning as it may affect dose prescription, target delineation and use of concomitant therapy...
May 11, 2018: Radiation Oncology
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