An anti-CD20-IL-2 immunocytokine is highly efficacious in a SCID mouse model of established human B lymphoma

Blood. 2005 May 15;105(10):3972-8. doi: 10.1182/blood-2004-09-3533. Epub 2005 Feb 3.

Abstract

We have engineered an anti-CD20-interleukin 2 (IL-2) immunocytokine (ICK) based on the Leu16 anti-CD20 antibody and have deimmunized both the variable (V) regions as well as the junction between the heavy (H) chain constant region and IL-2. Mutations were made to remove potential T-cell epitopes identified by in silico binding to major histocompatibility complex (MHC) class II molecules. The resulting immunocytokine, DI-Leu16-IL-2, retained full anti-CD20 activity as assessed by fluorescence-activated cell-sorting (FACS) analysis, and had enhanced antibody-dependent cellular cytotoxicity (ADCC) effector function relative to the DI-Leu16 antibody or control anti-CD20 antibody (rituximab). In a severe combined immunodeficient (SCID) mouse model of disseminated, residual lymphoma, anti-CD20-IL-2 immunocytokines based on Leu16 were far more effective at a dose of 0.25 mg/kg than anti-CD20 antibody given at 25/mg/kg, despite a shorter half-life of the ICK. Anti-CD20-IL-2 was also far more effective than a control ICK targeted to an antigen with greatly reduced expression on Daudi tumor cells, or various combinations of anti-CD20 antibodies and IL-2. Antitumor activity of DI-Leu16-IL-2 was shown to partially but not entirely depend on Fc receptor (R) binding, suggesting that ADCC and targeting of IL-2 both play roles in the mechanism of tumor clearance. Based on these animal models, DI-Leu16-IL-2 could offer therapeutic potential for patients with CD20 positive lymphoma. Clinical trials are currently under development.

MeSH terms

  • Animals
  • Antibodies / immunology
  • Antibodies, Monoclonal / immunology
  • Antibodies, Monoclonal / therapeutic use
  • Antibodies, Monoclonal, Murine-Derived
  • Antigens, CD20 / immunology*
  • Apoptosis
  • Cell Line, Tumor
  • Disease Models, Animal*
  • Humans
  • Immunotherapy*
  • Interleukin-2 / immunology*
  • Lymphoma, B-Cell / drug therapy*
  • Lymphoma, B-Cell / immunology*
  • Mice
  • Mice, Inbred BALB C
  • Mice, SCID
  • Neoplasm Metastasis
  • Neoplasm, Residual / drug therapy
  • Neoplasm, Residual / immunology
  • Rituximab
  • Survival Rate
  • Xenograft Model Antitumor Assays

Substances

  • Antibodies
  • Antibodies, Monoclonal
  • Antibodies, Monoclonal, Murine-Derived
  • Antigens, CD20
  • Interleukin-2
  • Rituximab