Mechanism of antitumor activity of a single-chain interleukin-12 IgG3 antibody fusion protein (mscIL-12.her2.IgG3)

J Interferon Cytokine Res. 2001 Sep;21(9):709-20. doi: 10.1089/107999001753124444.

Abstract

We have constructed an antibody interleukin-12 (IL-12) fusion protein (mscIL-12.her2.IgG3) that demonstrates significant antitumor activity against the murine carcinoma CT26-expressing human HER2/neu. We now report that this antitumor activity is dose dependent and comparable to or better than recombinant murine IL-12 (rMuIL-12) using subcutaneous and metastatic models of disease. The antitumor activity of mscIL-12.her2.IgG3 is reduced in Rag2 knockout mice, suggesting that T cells play a role in tumor rejection. In SCID-beige mice, the antitumor activity is further reduced, suggesting that natural killer (NK) cells or macrophages or both are also important. The isotype of the antibody response to HER2/neu is consistent with a switch from a Th2 to a Th1 immune response and the infiltration of mononuclear cell in tumors from mice treated with mscIL-12.her2.IgG3. Immunohistochemistry reveals that mscIL-12.her2.IgG3 is antiangiogenic. Thus, the mechanism of the antitumor activity exhibited by mscIL-12.her2.IgG3 is highly complex and involves a combination of T and NK cell activity, a switch to a Th1 immune response, and antiantiogenic activity. This is the first study comparing the in vivo antitumor activity of an antibody-IL-12 fusion protein and free IL-12. Our results suggest that antibody-IL-12 fusion proteins may be useful for the treatment of human cancer.

Publication types

  • Comparative Study
  • 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

  • Angiogenesis Inhibitors / therapeutic use*
  • Animals
  • Antibodies, Neoplasm / genetics
  • Antibodies, Neoplasm / immunology
  • Antibodies, Neoplasm / therapeutic use*
  • CD3 Complex / metabolism
  • DNA-Binding Proteins / genetics
  • Female
  • Genes, erbB-2 / immunology
  • Humans
  • Immunoglobulin G / immunology
  • Interleukin-12 / genetics
  • Interleukin-12 / immunology
  • Interleukin-12 / therapeutic use*
  • Killer Cells, Natural / immunology
  • Liver / immunology
  • Lung Neoplasms / drug therapy*
  • Lung Neoplasms / secondary
  • Macrophages / immunology
  • Mice
  • Mice, Inbred BALB C
  • Mice, Knockout
  • Mice, SCID
  • Nuclear Proteins
  • Recombinant Fusion Proteins / genetics
  • Recombinant Fusion Proteins / immunology
  • Recombinant Fusion Proteins / therapeutic use*
  • T-Lymphocytes / immunology
  • Th1 Cells / immunology
  • Tissue Distribution

Substances

  • Angiogenesis Inhibitors
  • Antibodies, Neoplasm
  • CD3 Complex
  • DNA-Binding Proteins
  • Immunoglobulin G
  • Nuclear Proteins
  • RAG2 protein, human
  • Rag2 protein, mouse
  • Recombinant Fusion Proteins
  • V(D)J recombination activating protein 2
  • Interleukin-12