[18F]MEL050 as a melanin-targeted PET tracer: fully automated radiosynthesis and comparison to 18F-FDG for the detection of pigmented melanoma in mice primary subcutaneous tumors and pulmonary metastases
Melanoma is a highly malignant cutaneous tumor of melanin-producing cells. MEL050 is a synthetic benzamide-derived molecule that specifically binds to melanin with high affinity. Our aim was to implement a fully automated radiosynthesis of [18F]MEL050, using for the first time, the AllInOne ™ synthesis module (Trasis), and to evaluate the potential of [18F]MEL050 for the detection of pigmented melanoma in mice primary subcutaneous tumors and pulmonary metastases, and to compare it with that of [18F]FDG. (Source: Nuclear Medicine and Biology)
Source: Nuclear Medicine and Biology - August 22, 2016 Category: Nuclear Medicine Authors: Nathalie Rizzo-Padoin, Michael Chaussard, Nicolas Vignal, Ewa Kotula, Vadim Tsoupko-Sitnikov, Sofia Vaz, Fortune Hontonnou, Wang-Qing Liu, Jean-Luc Poyet, Michel Vidal, Pascal Merlet, Benoit Hosten, Laure Sarda-Mantel Source Type: research
Radioligand Therapy with 177Lu-PSMA-617 of metastatic prostate cancer has already been arrived in clinical use
Dear Editor. (Source: Nuclear Medicine and Biology)
Source: Nuclear Medicine and Biology - August 12, 2016 Category: Nuclear Medicine Authors: Hojjat Ahmadzadehfar, Markus Essler, Michael Sch äfers, Kambiz Rahbar Source Type: research
Formulation of clinical-scale 177Lu-PSMA-617: From laboratory to clinics
Dear Editor, (Source: Nuclear Medicine and Biology)
Source: Nuclear Medicine and Biology - August 12, 2016 Category: Nuclear Medicine Authors: Tapas Das, Mohini Bhadwal, Sharmila Banerjee Source Type: research
Iodinated benzimidazole PARP radiotracer for evaluating PARP1/2 expression in vitro and in vivo
PARP inhibitors (PARPi) have the potential to impact cancer therapy in a selective patient population; however, despite current patient selection methods clinical trials have shown mixed response rates. It is therefore clinically useful to determine which patients will respond prior to receiving PARPi therapy. One essential biomarker is to measure the level of PARP enzyme expression in tumors. Small molecule radiotracers have been developed to accurately quantify PARP-1 expression in vitro and in vivo. (Source: Nuclear Medicine and Biology)
Source: Nuclear Medicine and Biology - August 11, 2016 Category: Nuclear Medicine Authors: Redmond-Craig Anderson, Mehran Makvandi, Kuiying Xu, Brian P. Lieberman, Chenbo Zeng, Daniel A. Pryma, Robert H. Mach Source Type: research
Radiolabeled Enzyme Inhibitors and Binding Agents Targeting PSMA: Effective Theranostic Tools for Imaging and Therapy of Prostate Cancer
Because of the broad incidence, morbidity and mortality associated with prostate-derived cancer, the development of more effective new technologies continues to be an important goal for the accurate detection and treatment of localized prostate cancer, lymphatic involvement and metastases. Prostate-specific membrane antigen (PSMA; Glycoprotein II) is expressed in high levels on prostate-derived cells and is an important target for visualization and treatment of prostate cancer. Radiolabeled peptide targeting technologies have rapidly evolved over the last decade and have focused on the successful development of radiolabele...
Source: Nuclear Medicine and Biology - August 10, 2016 Category: Nuclear Medicine Authors: M.R.A. Pillai, R. Nanabala, A. Joy, A. Sasikumar, F.F. (Russ) Knapp Source Type: research
Radiosynthesis and quality control of [11C]TASP457 as a clinically useful PET ligand for imaging of histamine H3 receptors in human brain
Recently, 6-[(1-cyclobutylpiperidin-4-yl)oxy]- 1-(6-[11C]methoxypyridin-3-yl)-3,4-dihydroquinolin-2(1H)-one ([11C]TASP457, [11C]2) has been developed as a novel PET ligand for histamine H3 receptors in brain. [11C]2 is potentially suitable for imaging H3 receptors in rat and monkey brains, which has motivated us to perform first-in-human study of [11C]2 for qualifying H3 receptors in human brain. In this paper, we report efficient radiosynthesis of [11C]2 to obtain sufficient radioactivity and high quality for clinical application. (Source: Nuclear Medicine and Biology)
Source: Nuclear Medicine and Biology - August 9, 2016 Category: Nuclear Medicine Authors: Masayuki Hanyu, Kazunori Kawamura, Makoto Takei, Kenji Furutsuka, Satoshi Shiomi, Tomoya Fujishiro, Masanao Ogawa, Nobuki Nengaki, Hiroki Hashimoto, Toshimitsu Fukumura, Ming-Rong Zhang Source Type: research
[18F]Fluoro-azomycin-2 ´-deoxy-β-d-ribofuranoside — A new imaging agent for tumor hypoxia in comparison with [18F]FAZA
Radiolabeled 2-nitroimidazoles (azomycins) are a prominent class of biomarkers for PET imaging of hypoxia. [18F]Fluoro-azomycin- α-arabinoside ([18F]FAZA) – already in clinical use – may be seen as α-configuration nucleoside, but enters cells only via diffusion and is not transported by cellular nucleoside transporters. To enhance image contrast in comparison to [18F]FAZA our objective was to 18F-radiolabel an azomycin- 2´-deoxyriboside with β-configuration ([18F]FAZDR, [18F]-β-8) to mimic nucleosides more closely and comparatively evaluate it versus [18F]FAZA. (Source: Nuclear Medicine and Biology)
Source: Nuclear Medicine and Biology - August 8, 2016 Category: Nuclear Medicine Authors: Anna Schweifer, Florian Maier, Walter Ehrlichmann, Denis Lamparter, Manfred Kneilling, Bernd J. Pichler, Friedrich Hammerschmidt, Gerald Reischl Source Type: research
Comparative evaluation of 4 and 6-carbon spacer conformationally flexible tetrahydroisoquinolinyl benzamide analogues for imaging the sigma-2 receptor status of solid tumors
Nine novel analogues were synthesized including a 6-carbon spacer analogue of ISO-1 (7). They have moderate binding affinity for sigma-2 ( σ2) receptors and high selectivity for σ2 receptors relative to sigma-1 (σ1) receptors. (Source: Nuclear Medicine and Biology)
Source: Nuclear Medicine and Biology - August 8, 2016 Category: Nuclear Medicine Authors: Iljung Lee, Brian P. Lieberman, Shihong Li, Catherine Hou, Mehran Makvandi, Robert H. Mach Source Type: research
[18F]Fluoro-azomycin-2 ´-deoxy-β-D-ribofuranoside – A new imaging agent for tumor hypoxia in comparison with [18F]FAZA
Radiolabeled 2-nitroimidazoles (azomycins) are a prominent class of biomarkers for PET imaging of hypoxia. [18F]Fluoro-azomycin- α-arabinoside ([18F]FAZA) - already in clinical use - may be seen as α-configuration nucleoside, but enters cells only via diffusion and is not transported by cellular nucleoside transporters. To enhance image contrast in comparison to [18F]FAZA our objective was to 18F-radiolabel an azomycin-2´- deoxyriboside with β-configuration ([18F]FAZDR, [18F]-β-8) to mimic nucleosides more closely and comparatively evaluate it versus [18F]FAZA. (Source: Nuclear Medicine and Biology)
Source: Nuclear Medicine and Biology - August 8, 2016 Category: Nuclear Medicine Authors: Anna Schweifer, Florian Maier, Walter Ehrlichmann, Denis Lamparter, Manfred Kneilling, Bernd J. Pichler, Friedrich Hammerschmidt, Gerald Reischl Source Type: research
Comparative Evaluation of 4 and 6-Carbon Spacer Conformationally-Flexible Tetrahydroisoquinolinyl Benzamide Analogues for Imaging the Sigma-2 Receptor Status of Solid Tumors
Nine novel analogues were synthesized including a 6-carbon spacer analogue of ISO-1 (7). They have moderate binding affinity for sigma-2 ( σ2) receptors and high selectivity for σ2 receptors relative to sigma-1 (σ1) receptors. (Source: Nuclear Medicine and Biology)
Source: Nuclear Medicine and Biology - August 8, 2016 Category: Nuclear Medicine Authors: Iljung Lee, Brian P. Lieberman, Shihong Li, Catherine Hou, Mehran Makvandi, Robert H. Mach Source Type: research
A DOTA based bisphosphonate with an albumin binding moiety for delayed body clearance for bone targeting
Radiolabelled bisphosphonates are commonly used in the diagnosis and therapy of bone metastases. Blood clearance of bisphosphonates is usually fast and only 30 –50% of the injected activity is retained in the skeleton, while most of the activity is excreted by the urinary tract. A longer blood circulation may enhance accumulation of bisphosphonate compounds in bone metastases. Therefore, a chemically modified macrocyclic bisphosphonate derivative with an additional human albumin binding entity was synthesized and pharmacokinetics of its complex was evaluated. (Source: Nuclear Medicine and Biology)
Source: Nuclear Medicine and Biology - July 31, 2016 Category: Nuclear Medicine Authors: Marian Meckel, Vojt ěch Kubíček, Petr Hermann, Matthias Miederer, Frank Rösch Source Type: research
Targeted therapy of osteosarcoma with radiolabeled monoclonal antibody to an insulin-like growth factor-2 receptor (IGF2R)
In this study we investigated a novel osteosarcoma therapy utilizing radioimmunotherapy (RIT) targeted to IGF2R, which is widely expressed in OS. (Source: Nuclear Medicine and Biology)
Source: Nuclear Medicine and Biology - July 29, 2016 Category: Nuclear Medicine Authors: David S. Geller, Jonathan Morris, Ekaterina Revskaya, Mani Kahn, Wendong Zhang, Sajida Piperdi, Amy Park, Pratistha Koirala, Hillary Guzik, Charles Hall, Bang Hoang, Rui Yang, Michael Roth, Jonathan Gill, Richard Gorlick, Ekaterina Dadachova Source Type: research
Efficient preparation of high-quality 64Cu for routine use
In this study, we propose a new separation method to produce high-quality 64Cu using a cation exchange column, as well as an automated separation system suitable for large-scale production. (Source: Nuclear Medicine and Biology)
Source: Nuclear Medicine and Biology - July 28, 2016 Category: Nuclear Medicine Authors: Tomoyuki Ohya, Kotaro Nagatsu, Hisashi Suzuki, Masami Fukada, Katsuyuki Minegishi, Masayuki Hanyu, Toshimitsu Fukumura, Ming-Rong Zhang Source Type: research
Paradoxical effects of Auger electron-emitting 111In-DTPA-NLS-CSL360 radioimmunoconjugates on hCD45+ cells in the bone marrow and spleen of leukemia-engrafted NOD/SCID or NRG mice
111In-DTPA-NLS-CSL360 radioimmunoconjugates (RIC) recognize the overexpression of the interleukin-3 receptor α-subchain (CD123) relative to the β-subchain (CD131) on leukemia stem cells (LSC). Our aim was to study Auger electron radioimmunotherapy (RIT) of acute myeloid leukemia (AML) with 111In-DTPA-NLS-CSL360 in non-obese diabetic severe combined immunodeficiency (NOD/SCID) mice or NOD-Rag1nullIL2rγnu ll (NRG) mice engrafted with CD123+ human AML-5 cells. (Source: Nuclear Medicine and Biology)
Source: Nuclear Medicine and Biology - July 20, 2016 Category: Nuclear Medicine Authors: Dane Bergstrom, Jeffrey V. Leyon, Arman Zereshkian, Conrad Chan, Zhongli Cai, Raymond M. Reilly Source Type: research
