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Radiobromination of anti-HER2/neu/ErbB-2 monoclonal antibody using the p-isothiocyanatobenzene derivative of the [76Br]undecahydro-bromo-7,8-dicarba-nido-undecaborate(1-) ion
Uppsala University, Disciplinary Domain of Science and Technology, Chemistry, Department of Chemistry. Uppsala University, Disciplinary Domain of Science and Technology, Chemistry, Department of Biochemistry and Organic Chemistry, Organic Chemistry II.
Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Medicine, Department of Oncology, Radiology and Clinical Immunology, Biomedical Radiation Sciences. (Biomedicinsk strålningsvetenskap)
Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Medicine, Department of Surgical Sciences. (Urologi)
Uppsala University, Disciplinary Domain of Science and Technology, Chemistry, Department of Chemistry. Uppsala University, Disciplinary Domain of Science and Technology, Chemistry, Department of Biochemistry and Organic Chemistry, Organic Chemistry II.
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2004 (English)In: Nuclear Medicine and Biology, ISSN 0969-8051, E-ISSN 1872-9614, Vol. 31, no 4, 425-33 p.Article in journal (Refereed) Published
Abstract [en]

The monoclonal humanized anti-HER2 antibody trastuzumab was radiolabeled with the positron emitter (76)Br (T(1/2) =16.2 h). Indirect labeling was performed using the p-isothiocyanatobenzene derivative of the [(76)Br]undecahydro-bromo-7,8-dicarba-nido-undecaborate(1-) ((76)Br-NBI) as a precursor molecule. (76)Br-NBI was prepared by bromination of the 7-(p-isothiocyanato-phenyl)dodecahydro-7,8-dicarba-nido-undecaborate(1-) ion (NBI) with a yield of 93-95% using Chloramine-T (CAT) as an oxidant. Coupling of radiobrominated NBI to antibody was performed without intermediate purification, in an "one pot" reaction. An overall labeling yield of 55.7 +/- 4.8% (mean +/- maximum error) was achieved when 300 microg of antibody was labeled. The label was stable in vitro in physiological and denaturing conditions. In a cell binding test, trastuzumab remained immunoreactive after labeling.

Place, publisher, year, edition, pages
2004. Vol. 31, no 4, 425-33 p.
Keyword [en]
Antibodies; Monoclonal/*chemistry/immunology/*pharmacokinetics, Breast Neoplasms/immunology/*metabolism/radionuclide imaging, Bromine Radioisotopes/*chemistry/immunology/*pharmacokinetics, Cell Line; Tumor, Drug Stability, Humans, Isotope Labeling/*methods, Radioimmunodetection/methods, Radiopharmaceuticals/chemical synthesis/chemistry/pharmacokinetics, Receptor; erbB-2/immunology/*metabolism, Research Support; Non-U.S. Gov't
National Category
Organic Chemistry
Identifiers
URN: urn:nbn:se:uu:diva-72941DOI: 10.1016/j.nucmedbio.2003.11.007PubMedID: 15093812OAI: oai:DiVA.org:uu-72941DiVA: diva2:100852
Available from: 2005-06-21 Created: 2005-06-21 Last updated: 2017-12-14Bibliographically approved

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Persson, MikaelMalmström, Per-UnoSjöberg, StefanTolmachev, Vladimir

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