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
2004 (English)In: Nuclear Medicine and Biology, ISSN 0969-8051, Vol. 31, no 4, 425-33 p.Article in journal (Refereed) Published
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.
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
IdentifiersURN: urn:nbn:se:uu:diva-72941DOI: 10.1016/j.nucmedbio.2003.11.007PubMedID: 15093812OAI: oai:DiVA.org:uu-72941DiVA: diva2:100852