Astatinated trastuzumab, aputative agent for radionuclide immunotherapy of ErbB2-expressing tumours

Mikael I. Persson, L. Gedda, H. J. Jensen, H. Lundqvist, P. U. Malmström, V. Tolmachev

Research output: Contribution to journalArticlepeer-review

21 Citations (Scopus)


The anti-ErbB2 antibody trastuzumab is used for the treatment of patients with advanced breast cancer, resulting in a response rate of 40-60%. Coupling with a cytotoxic nuclide, e.g. α-emitting 211At, may further increase tumour response. The tumour-targeting properties of trastuzumab, astatinated using N-succinimidyl-para-(tri-n-methylstannyl)-benzoate, were evaluated and compared with those of radioiodinated trastuzumab in this study. We found that astatinated trastuzumab retains high specificity towards ErbB2. While the immunoreactive fraction of radioiodinated trastuzumab was higher than that of astatinated trastuzumab (76±9% versus 54±28%), both radioconjugates showed high affinity (KD 0.75±0.16 nM versus 1.8±0.3 nM). A growth inhibition study indicated a dose-dependent cell deactivation, in which approximately 74 cell-associated astatine decays per cell gave a survival fraction of 4.5±0.8×10-4. Results of a comparative animal study on normal mice gave no indication that astatination would have any adverse effects on the biodistribution of the antibody. In conclusion, the results of the study suggest that astatinated trastuzumab is a promising candidate for treating ErbB2-expressing tumours.

Original languageEnglish
Pages (from-to)673-680
Number of pages8
JournalOncology Reports
Issue number3
Publication statusPublished - Mar 2006
Externally publishedYes


  • Astatine
  • Cancer
  • ErbB-2
  • Radioimmunotherapy
  • Targeting

ASJC Scopus subject areas

  • Oncology
  • Cancer Research

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