Labeling monoclonal antibodies and F(ab')2 fragments with the alpha-particle-emitting nuclide astatine-211: preservation of immunoreactivity and in vivo localizing capacity

Proc Natl Acad Sci U S A. 1989 Sep;86(18):7149-53. doi: 10.1073/pnas.86.18.7149.


alpha-Particles such as those emitted by 211At may be advantageous for radioimmunotherapy since they are radiation of high linear energy transfer, depositing high energy over a short distance. Here we describe a strategy for labeling monoclonal antibodies and F(ab')2 fragments with 211At by means of the bifunctional reagent N-succinimidyl 3-(trimethylstannyl)benzoate. An intact antibody, 81C6, and the F(ab')2 fragment of Me1-14 (both reactive with human gliomas) were labeled with 211At in high yield and with a specific activity of up to 4 mCi/mg in a time frame compatible with the 7.2-hr half-life of 211At. Quantitative in vivo binding assays demonstrated that radioastatination was accomplished with maintenance of high specific binding and affinity. Comparison of the biodistribution of 211At-labeled Me1-14 F(ab')2 to that of a nonspecific antibody fragment labeled with 211At and 131I in athymic mice bearing D-54 MG human glioma xenografts demonstrated selective and specific targeting of 211At-labeled antibody in this human tumor model.

Publication types

  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Animals
  • Antibodies, Monoclonal*
  • Antigen-Antibody Complex / analysis
  • Astatine*
  • Cell Line
  • Epitopes / analysis
  • Glioma / analysis
  • Humans
  • Immunoglobulin Fab Fragments*
  • Immunoglobulin G
  • Liver / analysis
  • Mice
  • Mice, Nude
  • Neoplasm Proteins / analysis*
  • Neoplasm Transplantation
  • Organ Specificity
  • Proteins / analysis*
  • Proteins / immunology
  • Radioisotope Dilution Technique
  • Rats
  • Tenascin
  • Transplantation, Heterologous
  • Tumor Cells, Cultured / analysis


  • Antibodies, Monoclonal
  • Antigen-Antibody Complex
  • Epitopes
  • Immunoglobulin Fab Fragments
  • Immunoglobulin G
  • Neoplasm Proteins
  • Proteins
  • Tenascin
  • Astatine