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Journal of Labelled Compounds & Radiopharmaceuticals

Wen-Ting K Tsai, Anna M Wu
The exquisite specificity of antibodies and antibody fragments renders them excellent agents for targeted delivery of radionuclides. Radiolabeled antibodies and fragments have been successfully used for molecular imaging and radioimmunotherapy (RIT) of cell-surface targets in oncology and immunology. Protein engineering has been employed for antibody humanization essential for clinical applications, as well as optimization of important characteristics including pharmacokinetics, biodistribution, and clearance...
March 14, 2018: Journal of Labelled Compounds & Radiopharmaceuticals
Syed Qaiser Shah, Gul-E-Raana, Ghias Uddin
This investigation aimed to modify finasteride (1) to finasteride dithiocarbamate (2) for subsequent synthesis of the rhenium analogue (3) and [99m Tc]tricarbonyl complexes (4), to assess its prostate cancer (PCa) targeting potential in a rat model. To validate the identity of (4), reference (3) has been synthesized using fac-[Net4 ]2 [ReBr3 (CO)3 ] precursor and characterized by1 H-NMR,13 C-NMR , ESI-MS and elemental analysis. The analogue (4) was synthesized using fac-[99m Tc(H2 O)3 (CO)3 ]+ precursor and its structure was confirmed by comparative HPLC using (3) as a reference...
March 13, 2018: Journal of Labelled Compounds & Radiopharmaceuticals
Babak Behnam Azad, Daniel P Holt, Hayden T Ravert, Andrew G Horti, Robert F Dannals
In this concise practitioner protocol, the radiochemical synthesis of [18 F]FNDP suitable for human PET studies is described and the results from validation productions are presented. The high specific activity radiotracer product is prepared as a sterile, apyrogenic solution that conforms to current Good Manufacturing Practice (cGMP) requirements.
March 12, 2018: Journal of Labelled Compounds & Radiopharmaceuticals
Mark D Bartholomä
While radioimmunotherapy (RIT) for the treatment of hematological malignancies such as indolent B-cell lymphoma has proven quite successful, clinical results of RIT in solid tumors have only been moderate in the past. The reasons were manifold and can be mostly attributed to the different biological properties of solid tumors vs. hematological cancers. Furthermore, the slow clearance of the radiolabelled antibody prevents the use of radiation doses necessary to achieve clinical responses. The long biological half-life of radioimmunoconjugates results in high background levels and is the main reason for radiation related toxicities...
March 9, 2018: Journal of Labelled Compounds & Radiopharmaceuticals
Ren Iwata, Claudio Pascali, Kazunori Terasaki, Yoichi Ishikawa, Shozo Furumoto, Kazuhiko Yanai
High specific activity is often a significant requirement for radiopharmaceuticals. To achieve that with18 F-labeled probes, it is mandatory to start from no-carrier-added fluoride and to reduce to a minimum the amount of precursor in order to decrease the presence of any pseudo-carrier. In the present study a feasible and efficient method for microscale one-pot radiosynthesis of18 F-labeled probes is described. It allows a substantial reduction in precursor, solvent and reagents, thus reducing also possible side reaction in the case of base-sensitive precursors...
March 8, 2018: Journal of Labelled Compounds & Radiopharmaceuticals
D Hesk, D Koharski, P McNamara, P Royster, S Saluja, V Truong, K Voronin
SCH 430765 and SCH 500496 are potent and selective antagonists of the NPY5 receptor. NPY5 receptor antagonists have the potential for the treatment of obesity. [35 S]SCH 500946 was prepared for a competition binding assay which led to the identification of SCH 430765. Three distinct isotopically labelled forms of SCH 430765 were synthesized. [3 H]SCH 430765 was prepared for a preliminary ADME evaluation of the compound and [14 C]SCH 430765 for more definitive ADME work. In addition [13 C2, 2 H4 ]SCH 430765 was prepared as an internal standard for a LC-MS bioanalytical method...
March 1, 2018: Journal of Labelled Compounds & Radiopharmaceuticals
Suresh Subramanian, K V Vimalnath, Ashutosh Dash
Hepatocellular carcinoma (HCC) or liver cancer is an increasingly prevalent and highly morbid disease with critical significance in the Asian and African sub-continents. Among the various therapies currently employed in the clinic to combat the global menace of HCC, radio-embolization with suitable therapeutic isotopes is an effective targeted approach. In the Indian context, the significant cost and logistical disadvantage of imported radio-embolic formulations for HCC therapy make it essential to develop more feasible indigenous alternatives - using locally available radioisotopes and microspheric carriers - that can serve the nuclear medicine community...
February 20, 2018: Journal of Labelled Compounds & Radiopharmaceuticals
Sudipta Chakraborty, K V Vimalnath, Jyothi Sharma, Priyalata Shetty, H D Sarma, Rubel Chakravarty, Deep Prakash, P K Sinha, Ashutosh Dash
Since the inception of radiation synovectomy, a host of radioactive colloids and microparticles incorporating suitable therapeutic radionuclides have been proposed for the treatment of arthritis. The present article reports the synthesis and evaluation of barium titanate microparticles as an innovative and effective carrier platform for lanthanide radionuclides in the preparation of therapeutic agents for treatment of arthritis. The material was synthesized by mechanochemical route and characterized by X-ray diffraction (XRD), scanning electron microscopy (SEM), surface area and particle size distribution analyses...
February 12, 2018: Journal of Labelled Compounds & Radiopharmaceuticals
Mallory Salvé, Hermane T Avohou, Jean-Christophe M Monbaliu, Pierre Lebrun, Christian Lemaire, Christian Damblon, Pascal de Tullio, Philippe Hubert, Roland Hustinx, André Luxen
This work reports on the development of amide bond bioconjugation for the production of -NOTA and -NODAGA PRGD2 using batch strategy and microfluidic reactor technology. The final radiolabelling step was fully optimized using Design of Experiments (DoE) and Design Space (DS) approaches, hence targeting robust labelling yields in routine. Optimal labelling conditions were defined in sodium acetate buffer as 168 μg/mL peptide concentration, 4.9 pH, 47.5 °C temperature and 12.5 min reaction time. Upon optimization, the Gallium-68 radiolabelling was fully automated...
February 12, 2018: Journal of Labelled Compounds & Radiopharmaceuticals
M H Sanad, A B Farag, Dina H Salama
No abstract text is available yet for this article.
February 12, 2018: Journal of Labelled Compounds & Radiopharmaceuticals
Lukas M Carter, Sophie Poty, Sai Kiran Sharma, Jason S Lewis
Intact antibodies and their truncated counterparts (e.g. Fab, scFv fragments) are generally exquisitely specific and selective vectors, enabling recognition of individual cancer-associated molecular phenotypes against a complex and dynamic biomolecular background. Complementary alignment of these advantages with unique properties of radionuclides is a defining paradigm in both radioimmunoimaging and radioimmunotherapy, which remain some of the most adept and promising tools for cancer diagnosis and treatment...
February 7, 2018: Journal of Labelled Compounds & Radiopharmaceuticals
Bachir Latli, Matt Hrapchak, Jolaine Savoie, Yongda Zhang, Carl A Busacca, Chris H Senanayake
No abstract text is available yet for this article.
February 6, 2018: Journal of Labelled Compounds & Radiopharmaceuticals
Jianjun Wang, Junping Ma, Qiuyu Zhao, Wenjiang Yang, Jinquan Xue, Yanhua Zhang, Yu Liu
This work reports the synthesis, radiolabeling and biological studies of 99m Tc-DTPA-colchicine dimer in tumor-bearing mice. The novel colchicine dimer was successfully synthesized by conjugation of DTPA to two colchicine biomolecules. The ligand could be labeled by 99m Tc in high yield to get 99m Tc-DTPA-colchicine dimer, which was hydrophilic and stable at room temperature. Biodistribution and imaging studies in tumor-bearing mice showed that 99m Tc-DTPA-colchicine dimer accumulated in the tumor with improved uptake and retention...
January 31, 2018: Journal of Labelled Compounds & Radiopharmaceuticals
Sara Westrøm, Marion Malenge, Ida Sofie Jorstad, Elisa Napoli, Øyvind S Bruland, Tina B Bønsdorff, Roy H Larsen
Internal therapy with α-emitters should be well suited for micrometastatic disease. Radium-224 emits multiple α-particles through its decay and has a convenient 3.6 days half-life. Despite its attractive properties, the use of 224 Ra has been limited to bone-seeking applications because it cannot be stably bound to a targeting molecule. Alternative delivery systems for 224 Ra are therefore of considerable interest. In this study, calcium carbonate (CaCO3 ) microparticles are proposed as carriers for 224 Ra, designed for local therapy of disseminated cancers in cavitary regions, such as peritoneal carcinomatosis...
January 29, 2018: Journal of Labelled Compounds & Radiopharmaceuticals
Sara Roslin, Kenneth Dahl, Patrik Nordeman
In this article we describe the carbon-11 (11 C, t1/2 = 20.4 min) labeling of benzyl alcohols, benzaldehydes and ketones using an efficient two-step synthesis in which 11 C-carbon monoxide is used in an initial palladium-mediated reaction to produce 11 C-benzoyl chloride as a key intermediate. In the second step, the obtained 11 C-benzoyl chloride is further treated with a metalloid reagent to furnish the final 11 C-labeled product. Benzyl alcohols were obtained in moderated to high non-isolated radiochemical yields (RCY, 35-90%) with lithium aluminium hydride or lithium aluminium deuteride as metalloid reagent...
January 26, 2018: Journal of Labelled Compounds & Radiopharmaceuticals
Xuran Zhang, Linyi You, Shuting Chen, Mengna Gao, Zhide Guo, Jin Du, Jie Lu, Xianzhong Zhang
The chemokine receptor 4 (CXCR4) has been an attractive molecular target for tumor imaging, since it is overexpressed in many tumor types and involved in tumor progression and metastasis. The purpose of this study is to examine the CXCR4 targeting properties of 99m Tc-labeled AMD3465, a small molecule antagonist of CXCR4. 99m Tc-AMD3465 was prepared in high yield (>95%) and stable in mice serum at least for 4 h. In vitro cell binding experiments were performed with CHO (Chinese hamster ovary), MCF-7 (breast cancer) and CHO-CXCR4 (CHO stably transfected to express CXCR4) cell lines...
January 25, 2018: Journal of Labelled Compounds & Radiopharmaceuticals
Eduardo Aluicio-Sarduy, Paul A Ellison, Todd E Barnhart, Weibo Cai, Robert Jerry Nickles, Jonathan W Engle
Recent advances in molecular characterization of tumors have made possible the emergence of new types of cancer therapies where the traditional cytotoxic drugs and nonspecific chemotherapy can be complemented with targeted molecular therapies. One of the main revolutionary treatments is the use of monoclonal antibodies (mAbs) that selectively target the disseminated tumor cells while sparing normal tissues. mAbs and related therapeutics can be efficiently radiolabeled with a wide range of radionuclides to facilitate preclinical and clinical studies...
January 17, 2018: Journal of Labelled Compounds & Radiopharmaceuticals
Brooke N McKnight, Nerissa T Viola-Villegas
Therapeutic monoclonal antibodies (mAbs) have been used in cancer treatment for 30 years, with around 24 mAb and mAb:drug conjugates approved by the FDA to date. Despite their specificity, efficacy has remained limited, which, in part, derails nascent initiatives towards precision medicine. An image-guided approach to reinforce treatment decisions using immune positron emission tomography (immunoPET) companion diagnostic is warranted. This review provides a general overview of current translational research using Zr-89 immunoPET and opportunities for utilizing and harnessing this tool to its full potential...
January 17, 2018: Journal of Labelled Compounds & Radiopharmaceuticals
Xiang Zhang, Ryan Dunlow, Burchelle N Blackman, Rolf E Swenson
Traditional radiosynthetic optimization faces the challenges of high radiation exposure, cost and inability to perform serial reactions due to tracer decay. To accelerate tracer development, we have developed a strategy to simulate radioactive 18 F-syntheses by using tracer-level (nanomolar) non-radioactive 19 F-reagents and LC-MS/MS analysis. The methodology was validated with fallypride synthesis under tracer-level 19 F-conditions, which showed reproducible and comparable results with radiosynthesis, and proved the feasibility of this process...
January 16, 2018: Journal of Labelled Compounds & Radiopharmaceuticals
Heinz H Coenen, Antony D Gee, Michael Adam, Gunnar Antoni, Cathy S Cutler, Yasuhisa Fujibayashi, Jae Min Jeong, Robert H Mach, Thomas L Mindt, Victor W Pike, Albert D Windhorst
No abstract text is available yet for this article.
January 13, 2018: Journal of Labelled Compounds & Radiopharmaceuticals
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