Tailoring the pharmacokinetics and positron emission tomography imaging properties of anti-carcinoembryonic antigen single-chain Fv-Fc antibody fragments

Cancer Res. 2005 Jan 15;65(2):622-31.

Abstract

Antibody fragments are recognized as promising vehicles for delivery of imaging and therapeutic agents to tumor sites in vivo. The serum persistence of IgG1 and fragments with intact Fc region is controlled by the protective neonatal Fc receptor (FcRn) receptor. To modulate the half-life of engineered antibodies, we have mutated the Fc-FcRn binding site of chimeric anti-carcinoembryonic antigen (CEA) antibodies produced in a single-chain Fv-Fc format. The anti-CEA T84.66 single-chain Fv-Fc format wild-type and five mutants (I253A, H310A, H435Q, H435R, and H310A/H435Q, Kabat numbering system) expressed well in mammalian cell culture. After purification and characterization, effective in vitro antigen binding was shown by competition ELISA. Biodistribution studies in BALB/c mice using (125)I- and (131)I-labeled fragments revealed blood clearance rates from slowest to fastest as follows: wild-type > H435R > H435Q > I253A > H310A > H310A/H435Q. The terminal half-lives of the mutants ranged from 83.4 to 7.96 hours, whereas that of the wild-type was approximately 12 days. Additionally, (124)I-labeled wild-type, H435Q, I253A, H310A, and H310A/H435Q variants were evaluated in LS174T xenografted athymic mice by small animal positron emission tomography imaging, revealing localization to the CEA-positive xenografts. The slow clearing wild-type and H435Q constructs required longer to localize to the tumor and clear from the circulation. The I253A and H310A fragments showed intermediate behavior, whereas the H310A/H435Q variant quickly localized to the tumor site, rapidly cleared from the animal circulation and produced clear images. Thus, attenuating the Fc-FcRn interaction provides a way of controlling the antibody fragment serum half-life without compromising expression and tumor targeting.

Publication types

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

MeSH terms

  • Animals
  • Carcinoembryonic Antigen / immunology*
  • Carcinoembryonic Antigen / metabolism
  • Cell Line, Tumor
  • Colorectal Neoplasms / diagnostic imaging
  • Colorectal Neoplasms / metabolism
  • Female
  • Humans
  • Immunoconjugates / pharmacokinetics*
  • Immunoglobulin Fragments / biosynthesis
  • Immunoglobulin Fragments / isolation & purification
  • Immunoglobulin Fragments / metabolism*
  • Iodine Radioisotopes / pharmacokinetics*
  • Mice
  • Mice, Inbred BALB C
  • Mice, Nude
  • Multiple Myeloma / metabolism
  • Positron-Emission Tomography
  • Radiopharmaceuticals / pharmacokinetics*
  • Tissue Distribution
  • Transplantation, Heterologous

Substances

  • Carcinoembryonic Antigen
  • Immunoconjugates
  • Immunoglobulin Fragments
  • Iodine Radioisotopes
  • Radiopharmaceuticals