An anti-siglec-8 antibody depletes sputum eosinophils from asthmatic subjects and inhibits lung mast cells

Clin Exp Allergy. 2020 Aug;50(8):904-914. doi: 10.1111/cea.13681. Epub 2020 Jul 8.

Abstract

Background: Sialic acid-binding immunoglobulin-like lectin (Siglec)-8 is expressed on mast cells and eosinophils, but information about Siglec-8 expression and function in the lung is limited. A humanized antibody, AK002, targeting Siglec-8 is undergoing development for treatment of diseases associated with mast cell and eosinophil-driven inflammation.

Objective: To characterize Siglec-8 expression in the airway in asthma and determine whether antibodies that target Siglec-8 (S8mAbs) can decrease airway eosinophils in asthma or inhibit lung mast cell activation.

Methods: Gene expression profiling and flow cytometry were used to characterize Siglec-8 expression in sputum cells from stable asthma. An antibody-dependent cellular cytotoxicity (ADCC) assay was used to determine whether an S8mAb can decrease eosinophils in sputum from asthma patients ex vivo. A mast cell activation assay was used to determine whether an S8mAb can inhibit mast cell activation in human lung tissue ex vivo.

Results: Gene expression for Siglec-8 is increased in sputum cells in asthma and correlates with gene expression for eosinophils and mast cells. Gene expression for Siglec-8 is inversely and significantly correlated with measures of airflow obstruction in asthma patients. Siglec-8 is prominently expressed on the surface of eosinophils and mast cells in sputum. S8mAbs decrease eosinophils in sputum from patients with asthma and inhibit FcεR1-activated mast cells in lung tissues.

Conclusions and clinical relevance: Siglec-8 is highly expressed on eosinophils and mast cells in asthmatic sputum and targeting Siglec-8 with an antibody is a plausible strategy to decrease sputum eosinophils and inhibit lung mast cells in asthma.

Keywords: asthma; basic immunology; basophil; eosinophils; mast cells.

Publication types

  • Research Support, N.I.H., Extramural

MeSH terms

  • Adult
  • Anti-Asthmatic Agents / pharmacology*
  • Antibodies, Monoclonal, Humanized / pharmacology*
  • Antibody-Dependent Cell Cytotoxicity / drug effects
  • Antigens, CD / genetics
  • Antigens, CD / immunology
  • Antigens, CD / metabolism
  • Antigens, Differentiation, B-Lymphocyte / genetics
  • Antigens, Differentiation, B-Lymphocyte / immunology
  • Antigens, Differentiation, B-Lymphocyte / metabolism
  • Apoptosis / drug effects
  • Asthma / drug therapy*
  • Asthma / immunology
  • Asthma / metabolism
  • Case-Control Studies
  • Cells, Cultured
  • Eosinophils / drug effects*
  • Eosinophils / immunology
  • Eosinophils / metabolism
  • Female
  • Humans
  • Lectins / antagonists & inhibitors*
  • Lectins / genetics
  • Lectins / immunology
  • Lectins / metabolism
  • Lung / drug effects*
  • Lung / immunology
  • Lung / metabolism
  • Male
  • Mast Cells / drug effects*
  • Mast Cells / immunology
  • Mast Cells / metabolism
  • Middle Aged
  • Receptors, IgE / genetics
  • Receptors, IgE / metabolism
  • Sputum / cytology
  • Young Adult

Substances

  • AK002
  • Anti-Asthmatic Agents
  • Antibodies, Monoclonal, Humanized
  • Antigens, CD
  • Antigens, Differentiation, B-Lymphocyte
  • Lectins
  • Receptors, IgE
  • SIGLEC8 protein, human