Interferon-α suppressed granulocyte colony stimulating factor production is reversed by CL097, a TLR7/8 agonist

J Gastroenterol Hepatol. 2010 Dec;25(12):1883-90. doi: 10.1111/j.1440-1746.2010.06281.x.

Abstract

Background and aim: Neutropenia, a major side-effect of interferon-α (IFN-α) therapy can be effectively treated by the recombinant form of granulocyte colony stimulating factor (G-CSF), an important growth factor for neutrophils. We hypothesized that IFN-α might suppress G-CSF production by peripheral blood mononuclear cells (PBMCs), contributing to the development of neutropenia, and that a toll-like receptor (TLR) agonist might overcome this suppression.

Methods: Fifty-five patients who were receiving IFN-α/ribavirin combination therapy for chronic hepatitis C virus (HCV) infection were recruited. Absolute neutrophil counts (ANC), monocyte counts and treatment outcome data were recorded. G-CSF levels in the supernatants of PBMCs isolated from the patients and healthy controls were assessed by enzyme-linked immunosorbent assay following 18 h of culture in the absence or presence of IFN- α or the TLR7/8 agonist, CL097.

Results: Therapeutic IFN-α caused a significant reduction in neutrophil counts in all patients, with 15 patients requiring therapeutic G-CSF. The reduction in ANC over the course of IFN-α treatment was paralleled by a decrease in the ability of PBMCs to produce G-CSF. In vitro G-CSF production by PBMCs was suppressed in the presence of IFN-α; however, co-incubation with a TLR7/8 agonist significantly enhanced G-CSF secretion by cells obtained both from HCV patients and healthy controls.

Conclusions: Suppressed G-CSF production in the presence of IFN-α may contribute to IFN-α-induced neutropenia. However, a TLR7/8 agonist elicits G-CSF secretion even in the presence of IFN-α, suggesting a possible therapeutic role for TLR agonists in treatment of IFN-α-induced neutropenia.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adult
  • Aged
  • Antiviral Agents / therapeutic use*
  • Case-Control Studies
  • Cells, Cultured
  • Drug Therapy, Combination
  • Enzyme-Linked Immunosorbent Assay
  • Female
  • Granulocyte Colony-Stimulating Factor / metabolism*
  • Hepatitis C, Chronic / drug therapy*
  • Hepatitis C, Chronic / immunology
  • Humans
  • Imidazoles / therapeutic use*
  • Interferon alpha-2
  • Interferon-alpha / adverse effects
  • Interferon-alpha / therapeutic use*
  • Ireland
  • Leukocyte Count
  • Male
  • Middle Aged
  • Neutropenia / chemically induced
  • Neutropenia / drug therapy*
  • Neutropenia / immunology
  • Neutrophils / drug effects*
  • Neutrophils / immunology
  • Polyethylene Glycols / adverse effects
  • Polyethylene Glycols / therapeutic use*
  • Prospective Studies
  • Quinolines / therapeutic use*
  • Recombinant Proteins
  • Ribavirin / therapeutic use*
  • Time Factors
  • Toll-Like Receptor 7 / agonists*
  • Toll-Like Receptor 8 / agonists*
  • Treatment Outcome

Substances

  • Antiviral Agents
  • CL097 compound
  • Imidazoles
  • Interferon alpha-2
  • Interferon-alpha
  • Quinolines
  • Recombinant Proteins
  • TLR7 protein, human
  • TLR8 protein, human
  • Toll-Like Receptor 7
  • Toll-Like Receptor 8
  • Granulocyte Colony-Stimulating Factor
  • Polyethylene Glycols
  • Ribavirin
  • peginterferon alfa-2b
  • peginterferon alfa-2a