The mechanistic and functional profile of the therapeutic anti-IgE antibody ligelizumab differs from omalizumab

Nat Commun. 2020 Jan 8;11(1):165. doi: 10.1038/s41467-019-13815-w.

Abstract

Targeting of immunoglobulin E (IgE) represents an interesting approach for the treatment of allergic disorders. A high-affinity monoclonal anti-IgE antibody, ligelizumab, has recently been developed to overcome some of the limitations associated with the clinical use of the therapeutic anti-IgE antibody, omalizumab. Here, we determine the molecular binding profile and functional modes-of-action of ligelizumab. We solve the crystal structure of ligelizumab bound to IgE, and report epitope differences between ligelizumab and omalizumab that contribute to their qualitatively distinct IgE-receptor inhibition profiles. While ligelizumab shows superior inhibition of IgE binding to FcεRI, basophil activation, IgE production by B cells and passive systemic anaphylaxis in an in vivo mouse model, ligelizumab is less potent in inhibiting IgE:CD23 interactions than omalizumab. Our data thus provide a structural and mechanistic foundation for understanding the efficient suppression of FcεRI-dependent allergic reactions by ligelizumab in vitro as well as in vivo.

Publication types

  • Comparative Study
  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Anti-Allergic Agents / administration & dosage*
  • Anti-Allergic Agents / chemistry
  • Antibodies, Anti-Idiotypic / administration & dosage*
  • Antibodies, Anti-Idiotypic / chemistry
  • Antibodies, Monoclonal, Humanized / administration & dosage*
  • B-Lymphocytes / drug effects
  • B-Lymphocytes / immunology
  • Basophils / drug effects
  • Basophils / immunology
  • Humans
  • Hypersensitivity / drug therapy*
  • Hypersensitivity / immunology
  • Immunoglobulin E / chemistry
  • Immunoglobulin E / immunology
  • Mice
  • Mice, Inbred C57BL
  • Mice, Transgenic
  • Omalizumab / administration & dosage*
  • Omalizumab / chemistry
  • Receptors, IgE / immunology

Substances

  • Anti-Allergic Agents
  • Antibodies, Anti-Idiotypic
  • Antibodies, Monoclonal, Humanized
  • Receptors, IgE
  • anti-IgE antibodies
  • Omalizumab
  • Immunoglobulin E
  • ligelizumab