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

Publication ,  Journal Article
Zalutsky, MR; Garg, PK; Friedman, HS; Bigner, DD
Published in: Proc Natl Acad Sci U S A
September 1989

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.

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Published In

Proc Natl Acad Sci U S A

DOI

ISSN

0027-8424

Publication Date

September 1989

Volume

86

Issue

18

Start / End Page

7149 / 7153

Location

United States

Related Subject Headings

  • Tumor Cells, Cultured
  • Transplantation, Heterologous
  • Tenascin
  • Rats
  • Radioisotope Dilution Technique
  • Proteins
  • Organ Specificity
  • Neoplasm Transplantation
  • Neoplasm Proteins
  • Mice, Nude
 

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Zalutsky, M. R., Garg, P. K., Friedman, H. S., & Bigner, D. D. (1989). 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, 86(18), 7149–7153. https://doi.org/10.1073/pnas.86.18.7149
Zalutsky, M. R., P. K. Garg, H. S. Friedman, and D. D. Bigner. “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 86, no. 18 (September 1989): 7149–53. https://doi.org/10.1073/pnas.86.18.7149.
Zalutsky, M. R., et al. “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, vol. 86, no. 18, Sept. 1989, pp. 7149–53. Pubmed, doi:10.1073/pnas.86.18.7149.
Journal cover image

Published In

Proc Natl Acad Sci U S A

DOI

ISSN

0027-8424

Publication Date

September 1989

Volume

86

Issue

18

Start / End Page

7149 / 7153

Location

United States

Related Subject Headings

  • Tumor Cells, Cultured
  • Transplantation, Heterologous
  • Tenascin
  • Rats
  • Radioisotope Dilution Technique
  • Proteins
  • Organ Specificity
  • Neoplasm Transplantation
  • Neoplasm Proteins
  • Mice, Nude