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Stephen Thompson, Melissa E Rodnick, Jenelle Stauff, Janna Arteaga, Timothy J Desmond, Peter J H Scott, Benjamin L Viglianti
Radiolabeled erythrocytes have multiple applications in nuclear medicine, including blood pool imaging. Historically they have been labeled with SPECT radionuclides. A PET blood pool imaging agent is highly desirable as it would improve clinical applications with better image quality and resolution, higher sensitivity, and dynamic scanning capabilities. With the coming of age of modern 68 Ge/68 Ga generator systems, gallium-68 is now widely accessible. In this paper we describe an updated method for the preparation of 68 Ga-labeled erythrocytes and their preliminary use in rodent blood pool imaging...
March 1, 2018: MedChemComm
Parul Thakral, Ishita Sen, Vineet Pant, Santosh Kumar Gupta, Sugandha Dureja, Jyotsna Kumari, Sunil Kumar, Pallavi Un, Vindhya Malasani
OBJECTIVE: Two radiosensitizing chemotherapeutic drugs, capecitabine (CAP) and temozolomide (TEM), are administered concurrently to enhance the therapeutic efficacy of peptide receptor radionuclide therapy (PRRT). This study aims to assess the biodistribution and normal-organ and tumor radiation dosimetry for Lu-177 DOTATATE administered concurrently with CAP/TEM. METHODS: 20 patients with non-resectable histologically confirmed gastroenteropancreatic neuroendocrine tumors with normal kidney function, a normal haematological profile and somatostatin receptor expression of the tumor lesions, as scintigraphically assessed by a Ga-68 DOTANOC scan, were included in two groups-case group (n = 10) and control group (n = 10)...
July 27, 2018: British Journal of Radiology
Stefanie Felicitas Färber, Alexander Wurzer, Florian Reichart, Roswitha Beck, Horst Kessler, Hans-Jürgen Wester, Johannes Notni
The epithelial integrin αvβ6 is expressed by many malignant carcinoma cell types, including pancreatic cancer, and thus represents a promising target for radionuclide therapy. The peptide cyclo(FRGDLAFp( N Me)K) was decorated with different chelators (DOTPI, DOTAGA, and DOTA). The Lu(III) complexes of these conjugates exhibited comparable αvβ6 integrin affinities (IC50 ranging from 0.3 to 0.8 nM) and good selectivities against other integrins (IC50 for αvβ8 >43 nM; for α5β1 >238 nM; and for αvβ3, αvβ5, and αIIbβ3 >1000 nM)...
February 28, 2018: ACS Omega
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...
September 4, 2018: Molecular Pharmaceutics
Julian M Rogasch, Hannes Cash, Sebastian Zschaeck, Sefer Elezkurtaj, Winfried Brenner, Bernd Hamm, Marcus Makowski, Holger Amthauer, Christian Furth, Alexander D J Baur
PURPOSE: To evaluate the accuracy of clinical parameters and established pre-treatment risk stratification systems for prostate cancer (PCa) in predicting PSMA-positive metastases in men undergoing Ga-68-PSMA PET/CT as initial staging examination. MATERIALS AND METHODS: A retrospective analysis in 108 consecutive treatment-naïve patients with biopsy-proven PCa undergoing Ga-68-PSMA PET/CT (median age, 72 years [range, 49-82 years]) was performed. Prediction of PSMA-positive metastases by serum PSA, clinical T stage (cT), ISUP group, percentage of positive biopsy cores, and derived risk scores (D'Amico risk classification system, Roach [RF], Yale formula [YF], and Briganti nomogram [BN]) was examined with ROC analysis...
July 5, 2018: Prostate
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
Yan Huo, Lei Kang, Xiaoxi Pang, Haoyuan Shen, Ping Yan, Chunli Zhang, Xuhe Liao, Xueqi Chen, Rongfu Wang
PURPOSE: Tc-99m- and I-131-labeled arginine-arginine-leucine (RRL) peptides have shown the feasibility of tumor imaging in our previous studies. However, there have been no reports using RRL peptide for positron emission tomography (PET) imaging. In this study, RRL was radiolabeled with Ga-68 under optimized reaction conditions to develop a better specific and effective tumor imaging agent. PROCEDURES: RRL was synthesized and conjugated to a bifunctional chelating agent (DOTA-NHS), then radiolabeled with Ga-68...
June 18, 2018: Molecular Imaging and Biology: MIB: the Official Publication of the Academy of Molecular Imaging
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
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
Licia Uccelli, Alessandra Boschi, Corrado Cittanti, Petra Martini, Luca Lodi, Elisa Zappaterra, Simona Romani, Samanta Zaccaria, Davide Cecconi, Ilaria Rambaldi, Ivan Santi, Stefano Panareo, Melchiore Giganti, Mirco Bartolomei
BACKGROUND AND OBJECTIVE: Gallium-68 is a PET isotope available in each nuclear medicine departments, even those not equipped with a cyclotron, since it is easily obtained by eluting compact and transportable generator system. The preparation of Ga-68 DOTA-labeled compounds is performed by remotely controlled automated systems developed in order to ensure production efficiency, reproducibility of the results, fast reaction time, to facilitate the synthesis and minimize the radiation exposure...
2018: Current Radiopharmaceuticals
Michael S Hofman, Declan G Murphy, Scott G Williams, Tatenda Nzenza, Alan Herschtal, Richard De Abreu Lourenco, Dale L Bailey, Ray Budd, Rodney J Hicks, Roslyn J Francis, Nathan Lawrentschuk
BACKGROUND: Accurate staging of patients with prostate cancer (PCa) is important for therapeutic decision-making. Relapse after surgery or radiotherapy of curative intent is not uncommon and, in part, represents a failure of staging with current diagnostic imaging techniques to detect disease spread. Prostate-specific membrane antigen (PSMA) positron-emission tomography (PET)/computed tomography (CT) is a new whole-body scanning technique that enables visualization of PCa with high contrast...
May 3, 2018: BJU International
Ismet Sarikaya, Abdelhamid H Elgazzar, Mahmoud A Alfeeli, Ali Sarikaya
Gallium-68 prostate-specific membrane antigen (Ga-68 PSMA) ligand (HBED-CC) is a new promising positron emission tomography (PET) tracer for prostate cancer. Intense renal parenchymal uptake is a physiologic finding on Ga-68 PSMA ligand PET images. Evaluation of kidneys in low intensity demonstrates excellent distribution of this radiotracer in renal parenchyma with excellent image quality and resolution. In this article, we present the Ga-68 PSMA ligand PET renal images of four patients with prostate cancer...
April 2018: World Journal of Nuclear Medicine
Mariza Vorster, M R Modiselle, C S Corbett, I O Lawal, John R Buscombe, Mike M Sathekge
Neuroendocrine tumors (NETs) are a diverse group of tumors that often present late due to nonspecific symptoms. These tumors frequently express somatostatin receptors (SSRs), which allows for positron emission tomography/computed tomography (PET/CT) imaging with Ga-68-DOTATATE. In eligible patients, this may then be followed by peptide receptor radionuclide therapy (PRRT). Here, we report our initial results and experience with PRRT in a developing country, as one of the first groups to provide this therapy in South Africa...
April 2018: World Journal of Nuclear Medicine
Caiqin Zhang, Yong Zhao, Ningning Zhao, Dengxu Tan, He Zhang, Xue Chen, Hai Zhang, Jiaze An, Changhong Shi, Mengbin Li
Combining near-infrared fluorescence (NIRF) and nuclear imaging techniques provides a novel approach for hepatocellular carcinoma (HCC) diagnosis. Here, we report the synthesis and characteristics of a dual-modality NIRF optical/positron emission tomography (PET) imaging probe using heptamethine carbocyanine dye and verify its feasibility in both nude mice and rabbits with orthotopic xenograft liver cancer. This dye, MHI-148, is an effective cancer-specific NIRF imaging agent and shows preferential uptake and retention in liver cancer...
2018: Contrast Media & Molecular Imaging
Deidré Prince, Daniel Rossouw, Sietske Rubow
PURPOSE: The aim of this study was to optimize a radiolabeling method using cationic processed Ga-68 eluates from a SnO2 -based 68 Ge/68 Ga generator, followed by the development of DOTA-Tyr3 -Thre8 -octreotide (DOTATATE) kits. PROCEDURES: Diluted generator eluates were adsorbed on a SCX resin and desorbed with acidified 5 M NaCl solution. Optimized labeling conditions were determined by variation of pH, using 35 μg DOTATATE and sodium acetate buffer. DOTATATE kits were developed based on optimized radiolabeling conditions, were labeled, and evaluated...
April 23, 2018: Molecular Imaging and Biology: MIB: the Official Publication of the Academy of Molecular Imaging
Tiago Sampaio Vieira, Diogo Borges Faria, Fernando Azevedo Silva, Sérgio Barroso, Graça Fonseca, José Pereira Oliveira
No abstract text is available yet for this article.
July 2018: European Journal of Nuclear Medicine and Molecular Imaging
Mohammed Al-Qahtani, Yousif Al Malki, Hadeel Mutwali, Edward Helal-Neto, Ralph Santos-Oliveira
BACKGROUND AND OBJECTIVE: The future of medicine relies on the capability to forecast the future and in the development of new drugs. The same rationale is applied to radiopharmacy. In this direction the development of nano-radiopharmaceuticals represents the most effective glance of the future. METHODS: In this manuscript we developed an efficient, rapid and direct methodology to label ultrasmall polymeric nanoparticle (10 to 12 nm) and regular polymeric nanoparticles (200 to 210 nm), both obtained by double emulsion technique, with Ga-68 in order to promote the development of PETnanoradiopharmaceuticals...
2018: Current Radiopharmaceuticals
Sung-Hyun Moon, Mee Kyung Hong, Young Ju Kim, Yun-Sang Lee, Dong Soo Lee, June-Key Chung, Jae Min Jeong
Glu-Urea-Lys (GUL) derivatives have been reported as prostate-specific membrane antigen (PSMA) agent. We developed derivatives of GUL conjugated with NOTA or DOTA via a thiourea linker and tested their feasibility as PSMA imaging agents after labeling with 68 Ga. NOTA-GUL and DOTA-GUL were synthesized and labeled with 68 Ga using generator-eluted 68 GaCl3 in 0.1 M HCl in the presence of 1 M NaOAc at pH 5.5. The stabilities of 68 Ga-labeled compounds in human serum were tested at 37.5 °C. A competitive binding assay was performed using the PSMA-positive prostate cancer cell line 22Rv1 and [125 I]MIP-1072 (PSMA-specific binding agent) as a tracer...
May 15, 2018: Bioorganic & Medicinal Chemistry
Ismet Sarikaya, Abdelhamid H Elgazzar, Ali Sarikaya, Naheel Alnafisi, Saud Alenezi
On radionuclide somatostatin receptor imaging studies, the spleen shows high physiologic uptake. Reducing the intensity of the image settings helps to better assess the distribution of radiotracer in the spleen. In our routine studies, we incidentally recognized that 68 Ga-DOTANOC PET provides higher-resolution splenic images than 111 In-octreotide SPECT. Autoradiography and immunohistochemistry studies have shown that somatostatin receptors are located mainly in the red pulp of the spleen. The distribution of 68 Ga-DOTANOC in the spleen appears to correlate with the distribution of red pulp...
June 2018: Journal of Nuclear Medicine Technology
Mateusz Adam Synowiecki, Lars Rutger Perk, J Frank W Nijsen
The global network of cyclotrons has expanded rapidly over the last decade. The bulk of its industrial potential is composed of small medical cyclotrons with a proton energy below 20 MeV for radionuclides production. This review focuses on the recent developments of novel medical radionuclides produced by cyclotrons in the energy range of 3 MeV to 20 MeV. The production of the following medical radionuclides will be described based on available literature sources: Tc-99 m, I-123, I-124, Zr-89, Cu-64, Ga-67, Ga-68, In-111, Y-86 and Sc-44...
2018: EJNMMI Radiopharmacy and Chemistry
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