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

Karl Johan Winberg, Mikael Persson, Per Uno Malmström, Stefan Sjöberg, Vladimir Tolmachev

Research output: Contribution to journalArticlepeer-review

44 Citations (Scopus)

Abstract

The monoclonal humanized anti-HER2 antibody trastuzumab was radiolabeled with the positron emitter 76Br (T12 =16.2 h). Indirect labeling was performed using the p-isothiocyanatobenzene derivative of the [76Br]undecahydro-bromo-7,8-dicarba-nido-undecaborate(1-) ( 76Br-NBI) as a precursor molecule. 76Br-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 μg 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.

Original languageEnglish
Pages (from-to)425-433
Number of pages9
JournalNuclear Medicine and Biology
Volume31
Issue number4
DOIs
Publication statusPublished - May 2004
Externally publishedYes

Keywords

  • Bromine-76
  • Monoclonal antibodies
  • nido-Carborate derivatives
  • Prosthetic group
  • Radiobromination
  • Trautzumab

ASJC Scopus subject areas

  • Molecular Medicine
  • Radiology Nuclear Medicine and imaging
  • Cancer Research

Fingerprint Dive into the research topics of 'Radiobromination of anti-HER2/neu/ErbB-2 monoclonal antibody using the p-isothiocyanatobenzene derivative of the [<sup>76</sup>Br]undecahydro-bromo-7, 8-dicarba-nido-undecaborate(1-) ion'. Together they form a unique fingerprint.

Cite this