Introduction of five potentially metabolizable linking groups between 111In-cyclohexyl EDTA derivatives and F(ab′)2 fragments of anti-carcinoembryonic antigen antibody-II. Comparative pharmacokinetics and biodistribution in human colorectal carcinoma-bearing nude mice

A. Faivre-chauvet, J. F. Gestin, R. C. Mease, C. Sai-maurel, P. Thédrez, M. Slinkin, G. E. Meinken, S. C. Srivastava, J. F. Chatal

Research output: Contribution to journalArticle

Abstract

The five linker-containing immunoconjugates described in the preceding paper were labeled with 111In and tested for their biodistribution, pharmacokinetics and immunoscintigraphic imaging properties in tumor-xenografted nude mice. The results were compared with DTPADA and CDTAMA for reference. Results showed that, for immunoscintigraphy, the derivatives in decreasing order of effectiveness were: aliphatic (tumor/liver > 4.5 and tumor/kidney > 6.5 at 96 h), thioether (tumor/liver > 3 and tumor/kidney > 1.2 at 24 h), ethylene glycol succinate (tumor/liver > 1.7 and tumor/kidney > 0.5 at 24 h) and disulfide (tumor/liver > 0.5 and tumor/kidney > 0.6 at 96 h). Pharmacokinetic results were complementary with those of the biodistribution studies and provide a basis for the study of in vivo metabolic mechanisms of linker-immunoconjugates. Indium-111-labeled linker-immunoconjugates appear promising for tumor imaging with better contrast than what is obtained with the use of the conventional 111In-DTPA dianhydride chelate.

Original languageEnglish (US)
Pages (from-to)763-771
Number of pages9
JournalNuclear Medicine and Biology
Volume20
Issue number6
DOIs
StatePublished - Aug 1993
Externally publishedYes

ASJC Scopus subject areas

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

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