In vitro and in vivo pharmacology and pharmacokinetics of a human engineered monoclonal antibody to epithelial cell adhesion molecule

Neoplasia. 2003 Mar-Apr;5(2):146-54. doi: 10.1016/s1476-5586(03)80006-4.

Abstract

ING-1(heMAb), a Human Engineered monoclonal antibody to epithelial cell adhesion molecule (Ep-CAM), was evaluated for its in vitro and in vivo activity. The dissociation constant of ING-1(heMAb) for binding to Ep-CAM on HT-29 human colon tumor cells was 2 to 5 nM, similar to chimeric ING-1. In antibody-dependent cellular cytotoxicity and complement-dependent cytotoxicity assays, ING-1(heMAb) caused a concentration-dependent lysis of BT-20 breast, MCF-7 breast, HT-29 colon, and CACO-2 colon tumor cells, with maximum cytolysis at approximately 1 microg/ml. After an intravenous injection in rats, plasma ING-1(heMAb) levels declined with an alpha half-life of 8 to 11 hours, and a beta half-life of 20 days, typical of an IgG in a species without the target for ING-1. In nude mice with human HT-29 colon tumors, plasma ING-1(heMAb) levels declined more rapidly than in non-tumor-bearing mice, suggesting an enhanced clearance via the tumor-associated human Ep-CAM. In nude mice, intravenous treatments with ING-1(heMAb) twice a week for 3 weeks significantly suppressed the growth of human HT-29 colon and PC-3 prostate tumors in a dose-dependent manner, with 1.0 mg/kg providing the greatest benefit. These results indicate that Human Engineered ING-1(heMAb) is a high-affinity antibody with potent in vitro activity that targets and suppresses the growth of human tumors in vivo.

MeSH terms

  • Animals
  • Antibodies, Monoclonal / chemistry*
  • Antigens, Neoplasm / chemistry*
  • Antigens, Neoplasm / immunology
  • Cell Adhesion
  • Cell Adhesion Molecules / chemistry*
  • Cell Adhesion Molecules / immunology
  • Cell Line, Tumor
  • Dose-Response Relationship, Drug
  • Enzyme-Linked Immunosorbent Assay
  • Epithelial Cell Adhesion Molecule
  • Humans
  • Immunoglobulin G / chemistry
  • Kinetics
  • Male
  • Mice
  • Mice, Nude
  • Neoplasm Transplantation
  • Protein Binding
  • Rats
  • Time Factors

Substances

  • Antibodies, Monoclonal
  • Antigens, Neoplasm
  • Cell Adhesion Molecules
  • Epithelial Cell Adhesion Molecule
  • ING-1 monoclonal antibody, human
  • Immunoglobulin G