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PSMA Gallium

Alexander Solle, Carsten Wanke, Lilli Geworski
Ga-68-labeled radiotracers, particularly used for the detection of neuroendocrine tumors by means of Ga-68-DOTA-TATE or -DOTA-TOC or for the diagnosis of prostate cancer by means of Ga-68-labeled antigens (Ga 68-PSMA), become increasingly important. In addition to the high sensitivity and specificity of these radiopharmaceuticals, the short-lived radionuclide Ga-68 offers almost ideal nuclear characteristics for use in PET. Ga-68 is obtained from a germanium-gallium-generator system, so that the availability of Ga-68-labeled radiotracers is independent of an on-site-cyclotron regardless of the short half-life of Ga-68 of about 68minutes...
July 15, 2016: Zeitschrift Für Medizinische Physik
V Schreiter, C Reimann, D Geisel, N F Schreiter
The new tracer Gallium-68 prostate-specific membrane antigen (Ga-68 PSMA) yields new promising options for the PET/CT diagnosis of prostate cancer (PCa) and its metastases. To overcome limitations of hybrid imaging, known from the use of choline derivatives, seems to be possible with the use of Ga-68 PSMA for PCa. The benefits of hybrid imaging with Ga-68 PSMA for PCa compared to choline derivatives shall be discussed in this article based on an overview of the current literature. Key Points: • Ga-68 PSMA PET/CT can achieve higher detection rates of PCa lesions than PET/CT performed with choline derivatives• The new tracer Ga-68 PSMA has the advantage of high specificity, independence of PSA-level and low nonspecific tracer uptake in surrounding tissue• The new tracer Ga-68 PSMA seems very suitable for MR-PET diagnostic Citation Format: • Schreiter V, Reimann C, Geisel D et al...
June 14, 2016: RöFo: Fortschritte Auf Dem Gebiete der Röntgenstrahlen und der Nuklearmedizin
Krishan Kant Agarwal, Madhavi Tripathi, Rajeev Kumar, Chandrasekhar Bal
We describe the imaging features of a metastatic superscan on gallium-68 Glu-NH-CO-NH-Lys-(Ahx)-[Ga-68(HBED-CC)], abbreviated as gallium-68-prostate-specific membrane antigen ((68)Ga-PSMA) positron emission tomography/computed tomography (PET/CT) imaging. (68)Ga-PSMA is novel radiotracer undergoing evaluation for PET/CT imaging of prostate carcinoma. This patient had a superscan of metastases on conventional bone scintigraphy and was referred for (68)Ga-PSMA PET/CT to evaluate the feasibility of (177)Lu-PSMA therapy...
April 2016: Indian Journal of Nuclear Medicine: IJNM: the Official Journal of the Society of Nuclear Medicine, India
Matthias Eiber, Gregor Weirich, Konstantin Holzapfel, Michael Souvatzoglou, Bernhard Haller, Isabel Rauscher, Ambros J Beer, Hans-Jürgen Wester, Juergen Gschwend, Markus Schwaiger, Tobias Maurer
BACKGROUND: Ligands of the prostate-specific membrane antigen (PSMA) show promising results in positron emission tomography (PET) imaging of prostate cancer (PCa). OBJECTIVE: To compare the diagnostic performance of simultaneous gallium 68 ((68)Ga)-PSMA HBED-CC PET/magnetic resonance imaging (MRI) for localization of primary PCa with multiparametric magnetic resonance imaging (mpMRI) and PET alone. DESIGN, SETTING, AND PARTICIPANTS: We performed (68)Ga-PSMA HBED-CC PET/MRI in 66 men with biopsy-proven PCa...
January 18, 2016: European Urology
Bhavan Prasad Rai, Richard Paul Baum, Amit Patel, Robert Hughes, Roberto Alonzi, Tim Lane, Jim Adshead, Nikhil Vasdev
The role of positron emission tomography (PET) with (68)Gallium (Ga)-labeled prostate-specific membrane antigen (PSMA) imaging for prostate cancer is gaining prominence. Current imaging strategies, despite having progressed significantly, have limitations, in particular their ability to diagnose metastatic lymph node involvement. Preliminary results of PET with (68)Ga-labeled PSMA have shown encouraging results, particularly in the recurrent prostate cancer setting. Furthermore, the ability of PET with (68)Ga-labeled PSMA of playing a dual diagnostic and therapeutic setting (theranostics) is currently being investigated as well...
September 2016: Urology
Tobias Maurer, Jürgen E Gschwend, Isabel Rauscher, Michael Souvatzoglou, Bernhard Haller, Gregor Weirich, Hans-Jürgen Wester, Matthias Heck, Hubert Kübler, Ambros J Beer, Markus Schwaiger, Matthias Eiber
PURPOSE: Current standard imaging techniques are insufficient to reliably detect lymph node metastases in prostate cancer. Recently ligands of PSMA (prostate specific membrane antigen) were introduced in PET (positron emission tomography) of prostate cancer. Thus the aims of this retrospective analysis were to 1) investigate the diagnostic efficacy of (68)Ga-PSMA-PET imaging for lymph node staging in patients with prostate cancer scheduled for radical prostatectomy and 2) compare it to morphological imaging (computerized tomography and magnetic resonance tomography) with histopathological evaluation as the standard of reference...
May 2016: Journal of Urology
W Phillip Law, Frank Fiumara, William Fong, Kenneth A Miles
Gallium-68 (Ga-68) labelled prostate-specific membrane antigen (PSMA) imaging by positron emission tomography (PET) has emerged as a promising tool for staging of prostate cancer and restaging of disease in recurrence or biochemical failure after definitive treatment of prostate cancer. Ga-68 PSMA PET produces high target-to-background images of prostate cancer and its metastases which are reflective of the significant overexpression of PSMA in these cells and greatly facilitates tumour detection. However, relatively little is known about the PSMA expression of benign neoplasms and non-prostate epithelial malignancies...
August 2016: Journal of Medical Imaging and Radiation Oncology
Thomas Ebenhan, Mariza Vorster, Biljana Marjanovic-Painter, Judith Wagener, Janine Suthiram, Moshe Modiselle, Brenda Mokaleng, Jan Rijn Zeevaart, Mike Sathekge
Prostate-specific membrane antigen (PSMA), a type II glycoprotein, is highly expressed in almost all prostate cancers. By playing such a universal role in the disease, PSMA provides a target for diagnostic imaging of prostate cancer using positron emission tomography/computed tomography (PET/CT). The PSMA-targeting ligand Glu-NH-CO-NH-Lys-(Ahx)-HBED-CC (DKFZ-PSMA-11) has superior imaging properties and allows for highly-specific complexation of the generator-based radioisotope Gallium-68 ((68)Ga). However, only module-based radiolabeling procedures are currently available...
2015: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
Lars Budäus, Sami-Ramzi Leyh-Bannurah, Georg Salomon, Uwe Michl, Hans Heinzer, Hartwig Huland, Markus Graefen, Thomas Steuber, Clemens Rosenbaum
UNLABELLED: Prostate-specific membrane antigen (PSMA) overexpression theoretically enables targeting of prostate cancer (PCa) metastases using gallium Ga 68 ((68)Ga)-labeled PSMA ligands for positron emission tomography/computed tomography (PET/CT) imaging. Promising detection rates have been reported when using this approach for functional imaging of recurrent PCa; however, until now, the diagnostic accuracy of (68)Ga-PSMA PET/CT for preoperatively identifying lymph node metastases (LNMs) had not been assessed...
March 2016: European Urology
Martina Weineisen, Jakub Simecek, Margret Schottelius, Markus Schwaiger, Hans-Jürgen Wester
BACKGROUND: Due to its high expression in prostate cancer, PSMA (prostate-specific membrane antigen) represents an ideal target for both diagnostic imaging and endoradiotherapeutic approaches. Based on a previously published highly specific PSMA ligand ([(68)Ga]DOTA-FFK(Sub-KuE)), we developed a corresponding metabolically stable 1,4,7,10-tetraazacyclododececane,1-(glutaric acid)-4,7,10-triacetic acid (DOTAGA) construct for theranostic treatment of prostate cancer. METHODS: All ligands were synthesized by a combined solid phase and solution phase synthesis strategy...
December 2014: EJNMMI Research
Joshua J Morigi, Phillip D Stricker, Pim J van Leeuwen, Reuben Tang, Bao Ho, Quoc Nguyen, George Hruby, Gerald Fogarty, Raj Jagavkar, Andrew Kneebone, Adam Hickey, Stefano Fanti, Lisa Tarlinton, Louise Emmett
UNLABELLED: In prostate cancer with biochemical failure after therapy, current imaging techniques have a low detection rate at the prostate-specific antigen (PSA) levels at which targeted salvage therapy is effective. (11)C-choline and (18)F-fluoromethylcholine, though widely used, have poor sensitivity at low PSA levels. (68)Ga-PSMA (Glu-NH-CO-NH-Lys-(Ahx)-[(68)Ga-N,N'-bis[2-hydroxy-5-(carboxyethyl)benzyl]ethylenediamine-N,N'-diacetic acid]) has shown promising results in retrospective trials...
August 2015: Journal of Nuclear Medicine: Official Publication, Society of Nuclear Medicine
Martina Weineisen, Margret Schottelius, Jakub Simecek, Richard P Baum, Akin Yildiz, Seval Beykan, Harshad R Kulkarni, Michael Lassmann, Ingo Klette, Matthias Eiber, Markus Schwaiger, Hans-Jürgen Wester
UNLABELLED: On the basis of the high and consistent expression of prostate-specific membrane antigen (PSMA) in metastatic prostate cancer (PC), the goal of this study was the development, preclinical evaluation, and first proof-of-concept investigation of a PSMA inhibitor for imaging and therapy (PSMA I&T) for (68)Ga-based PET and (177)Lu-based endoradiotherapeutic treatment in patients with metastatic and castration-resistant disease. METHODS: PSMA I&T was synthesized in a combined solid phase and solution chemistry strategy...
August 2015: Journal of Nuclear Medicine: Official Publication, Society of Nuclear Medicine
Markus Dietlein, Carsten Kobe, Georg Kuhnert, Simone Stockter, Thomas Fischer, Klaus Schomäcker, Matthias Schmidt, Felix Dietlein, Boris D Zlatopolskiy, Philipp Krapf, Raphael Richarz, Stephan Neubauer, Alexander Drzezga, Bernd Neumaier
PURPOSE: Gallium-68 (Ga-68)-labeled tracers for imaging expression of the prostate-specific membrane antigen (PSMA) such as the [(68)Ga]Ga-PSMA-HBED-CC have already demonstrated high potential for the detection of recurrent prostate cancer. However, compared to Ga-68, a labeling with fluorine-18 (F-18) would offer advantages with respect to availability, production amount, and image resolution. [(18)F]DCFPyL is a promising F-18-labeled candidate for PSMA-positron emission tomography (PET) imaging that has been recently introduced...
August 2015: Molecular Imaging and Biology: MIB: the Official Publication of the Academy of Molecular Imaging
Mehmet Onur Demirkol, Ömer Acar, Burcu Uçar, Sultan Rana Ramazanoğlu, Yeşim Sağlıcan, Tarık Esen
BACKGROUND: There is an ongoing need for an accurate imaging modality which can be used for staging purposes, metastatic evaluation, predicting biologic aggresiveness and investigating recurrent disease in prostate cancer. Prostate specific membrane antigen, given its favorable molecular characteristics, holds a promise as an ideal target for prostate cancer-specific nuclear imaging. In this study, we evaluated our initial results of PSMA based PET/CT imaging in prostate cancer. METHODS: A total of 22 patients with a median age and serum PSA level of 68 years and 4...
May 2015: Prostate
Matthias Eiber, Stephan G Nekolla, Tobias Maurer, Gregor Weirich, Hans-Jürgen Wester, Markus Schwaiger
Current imaging procedures for prostate cancer including positron emission tomography (PET) exhibit considerable limitations and are not always able to meet the diagnostic needs. Recently, a (68)Gallium-labeled ligand of the prostate-specific membrane antigen ((68)Ga-PSMA) has been introduced in PET-imaging of prostate cancer with first promising results. Due to relatively exclusive expression of PSMA in prostatic tissue as well as increased expression in prostate cancer, 68 Ga-PSMA was reported to exhibit a favorable lesion to background ratio...
August 2015: Abdominal Imaging
Benjamin Baur, Christoph Solbach, Elena Andreolli, Gordon Winter, Hans-Jürgen Machulla, Sven N Reske
Since prostate-specific membrane antigen (PSMA) has been identified as a diagnostic target for prostate cancer, many urea-based small PSMA-targeting molecules were developed. First, the clinical application of these Ga-68 labelled compounds in positron emission tomography (PET) showed their diagnostic potential. Besides, the therapy of prostate cancer is a demanding field, and the use of radiometals with PSMA bearing ligands is a valid approach. In this work, we describe the synthesis of a new PSMA ligand, CHX-A''-DTPA-DUPA-Pep, the subsequent labelling with Ga-68, Lu-177 and Y-90 and the first in vitro characterization...
2014: Pharmaceuticals
Johannes Notni, Jakub Šimeček, Hans-Jürgen Wester
Given the wide application of positron emission tomography (PET), positron-emitting metal radionuclides have received much attention recently. Of these, gallium-68 has become particularly popular, as it is the only PET nuclide commercially available from radionuclide generators, therefore allowing local production of PET radiotracers independent of an on-site cyclotron. Hence, interest in optimized bifunctional chelators for the elaboration of (68) Ga-labeled bioconjugates has been rekindled as well, resulting in the development of improved triazacyclononane-triphosphinate (TRAP) ligand structures...
June 2014: ChemMedChem
Ali Afshar-Oromieh, Christian M Zechmann, Anna Malcher, Matthias Eder, Michael Eisenhut, Heinz G Linhart, Tim Holland-Letz, Boris A Hadaschik, Frederik L Giesel, Jürgen Debus, Uwe Haberkorn
PURPOSE: Positron emission tomography (PET) with choline tracers has found widespread use for the diagnosis of prostate cancer (PC). However, choline metabolism is not increased in a considerable number of cases, whereas prostate-specific membrane antigen (PSMA) is overexpressed in most PCs. Therefore, a (68)Ga-labelled PSMA ligand could be superior to choline tracers by obtaining a high contrast. The aim of this study was to compare such a novel tracer with standard choline-based PET/CT...
January 2014: European Journal of Nuclear Medicine and Molecular Imaging
A Afshar-Oromieh, A Malcher, M Eder, M Eisenhut, H G Linhart, B A Hadaschik, T Holland-Letz, F L Giesel, C Kratochwil, S Haufe, U Haberkorn, C M Zechmann
PURPOSE: Prostate-specific membrane antigen (PSMA) is a cell surface protein with high expression in prostate carcinoma (PC) cells. Recently, procedures have been developed to label PSMA ligands with (68)Ga, (99m)Tc and (123/124/131)I. Our initial experience with Glu-NH-CO-NH-Lys-(Ahx)-[(68)Ga(HBED-CC)]((68)Ga-PSMA) suggests that this novel tracer can detect PC relapses and metastases with high contrast. The aim of this study was to investigate its biodistribution in normal tissues and tumour lesions...
April 2013: European Journal of Nuclear Medicine and Molecular Imaging
Matthias Eder, Martin Schäfer, Ulrike Bauder-Wüst, William-Edmund Hull, Carmen Wängler, Walter Mier, Uwe Haberkorn, Michael Eisenhut
Urea-based inhibitors of the prostate-specific membrane antigen (PSMA) represent low-molecular-weight pepidomimetics showing the ability to image PSMA-expressing prostate tumors. The highly efficient, acyclic Ga(III) chelator N,N'-bis [2-hydroxy-5-(carboxyethyl)benzyl] ethylenediamine-N,N'- diacetic acid (HBED-CC) was introduced as a lipophilic side chain into the hydrophilic pharmacophore Glu-NH-CO-NH-Lys which was found favorable to interact with the PSMA "active binding site". This report describes the syntheses, in vitro binding analyses, and biodistribution data of the radiogallium labeled PSMA inhibitor Glu-NH-CO-NH-Lys(Ahx)-HBED-CC in comparison to the corresponding DOTA conjugate...
April 18, 2012: Bioconjugate Chemistry
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