New Bifunctional Chelators for 225Ac and 227Th Radioimmunotherapy
نویسندگان
چکیده
منابع مشابه
Experimental α-particle radioimmunotherapy of breast cancer using 227Th-labeled p-benzyl-DOTA-trastuzumab
BACKGROUND The aim of the present study was to explore the biodistribution, normal tissue toxicity, and therapeutic efficacy of the internalizing low-dose rate alpha-particle-emitting radioimmunoconjugate 227Th-trastuzumab in mice with HER2-expressing breast cancer xenografts. METHODS Biodistribution of 227Th-trastuzumab and 227Th-rituximab in nude mice bearing SKBR-3 xenografts were determin...
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Targeted α therapy holds tremendous potential as a cancer treatment: it offers the possibility of delivering a highly cytotoxic dose to targeted cells while minimizing damage to surrounding healthy tissue. The metallic α-generating radioisotopes 225Ac and 227Th are promising radionuclides for therapeutic use, provided adequate chelation and targeting. Here we demonstrate a new chelating platfor...
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6-Hydrazinonicotinic acid (HYNIC, 1) is a well-established bifunctional technetium-binding ligand often used to synthesise bioconjugates for radiolabelling with Tc-99m. It is capable of efficient capture of technetium at extremely low concentrations, but the structure of the labelled complexes is heterogeneous and incompletely understood. In particular, it is of interest to determine whether, a...
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1Molecular Pharmacology and Chemistry Program, Sloan Kettering Institute, Memorial Sloan-Kettering Cancer Center, New York, New York; 2Weill Cornell Medical College, New York, New York; 3Department of Radiology, Memorial Sloan-Kettering Cancer Center, New York, New York; 4Department of Medicine, Memorial Sloan-Kettering Cancer Center, New York, New York; 5Department of Psychiatry and Behavioral...
متن کاملMaleimido-functionalized NOTA derivatives as bifunctional chelators for site-specific radiolabeling.
Two basic and simple synthetic routes for mono- and bis-maleimide bearing 1,4,7-triazacyclononane-N,N',N''-triacetic acid (NOTA) chelators as new bifunctional chelators are described. The syntheses are characterized by their simplicity and short reaction times, as well as practical purification methods and acceptable to very good chemical yields. The usefulness of these two synthetic pathways i...
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ژورنال
عنوان ژورنال: Journal of Medical Imaging and Radiation Sciences
سال: 2019
ISSN: 1939-8654
DOI: 10.1016/j.jmir.2019.03.086