Preparation, characterization, and biological evaluation of a streptavidin-chimeric t84.66 conjugate for antibody pretargeting

Cancer Biother Radiopharm. 2007 Oct;22(5):654-64. doi: 10.1089/cbr.2007.343-S.

Abstract

In order to develop a new system for the antibody pretargeting of carcinoembryonic antigen (CEA)-positive cancers, a streptavidin (SA) conjugate of the monoclonal antibody (mAb) chimeric, T84.66, was synthesized and characterized. Antibody disulfide bonds were reduced with 1,4-dithiothreitol, and the resulting thiols were reacted with succinimidyl 4-(N-maleimidomethyl)cyclohexane-1-carboxylate-derivatized streptavidin (SMCC-SA). The desired SA-cT84.66 conjugate was purified by iminobiotin affinity chromatography and size-exclusion high-performance liquid chromatography (HPLC). The molecular weight of the SA-cT84.66 conjugate (210 kDa) and immounoreactivity (100%) were confirmed by size-exclusion HPLC, and the conjugate bound three equivalents of (111)In-DOTA-biotin. SA-cT84.66-pretargeted (111)In-DOTA-biotin was evaluated in nude mice bearing LS174T human colon carcinoma xenografts. Tumor uptake of (111)In-DOTA-biotin peaked at 3.32% injected dose per gram after 15 minutes. Clearance from blood and normal organs was extremely rapid, and tumor-to-blood ratios were >20:1 after 24 hours. The specific tumor targeting and rapid whole-body clearance of SA-cT84.66-pretargeted (111)In-DOTA-biotin indicated that this system is promising for the imaging and therapy of CEA-positive cancers.

Publication types

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

MeSH terms

  • Animals
  • Biotin / analogs & derivatives
  • Biotin / chemistry
  • Carcinoembryonic Antigen / immunology*
  • Cell Line, Tumor
  • Chromatography, High Pressure Liquid
  • Colonic Neoplasms / metabolism*
  • Colonic Neoplasms / pathology
  • Colonic Neoplasms / radiotherapy
  • Humans
  • Immunotoxins / chemistry*
  • Immunotoxins / immunology
  • Immunotoxins / pharmacokinetics*
  • Indium Radioisotopes / chemistry
  • Indium Radioisotopes / pharmacokinetics
  • Maleimides / chemistry
  • Mice
  • Mice, Nude
  • Molecular Structure
  • Organometallic Compounds / chemistry
  • Radioimmunotherapy / methods
  • Streptavidin / chemistry
  • Tissue Distribution
  • Xenograft Model Antitumor Assays

Substances

  • Carcinoembryonic Antigen
  • DOTA-biotin
  • Immunotoxins
  • Indium Radioisotopes
  • Maleimides
  • Organometallic Compounds
  • Biotin
  • Streptavidin