Immunomodulatory drug CC-4047 is a cell-type and stimulus-selective transcriptional inhibitor of cyclooxygenase 2

J Clin Immunol. 2007 Mar;27(2):210-20. doi: 10.1007/s10875-007-9070-6. Epub 2007 Feb 17.

Abstract

COX2 (prostaglandin G/H synthase, PTGS2) is a well-validated target in the fields of both oncology and inflammation. Despite their significant toxicity profile, non-steroidal anti-inflammatory drugs (NSAIDs) have become standard of care in the treatment of many COX2-mediated inflammatory conditions. In this report, we show that one IMiDs((R)) immunomodulatory drug, CC-4047, can reduce the levels of COX2 and the production of prostaglandins (PG) in human LPS-stimulated monocytes. The inhibition of COX2 by CC-4047 occurs at the level of gene transcription, by reducing the LPS-stimulated transcriptional activity at the COX2 gene. Because it is a transcriptional rather than an enzymatic inhibitor of COX2, CC-4047 inhibition of PG production is not susceptible to competition by exogenous arachadonic acid (AA). The distinct mechanisms of action allow CC-4047 and a COX2-selective NSAID to work additively to block PG secretion from monocytes. CC-4047 does not, however, block COX2 induction in or prostacyclin secretion from IL-1beta stimulated human umbilical vein endothelial cells (HUVEC) cells, nor does it inhibit COX1 in either monocytes or HUVEC cells. CC-4047 also inhibits COX2 and PG production in monocytes derived from patients with sickle cell disease (SCD). Taken together, the data in this manuscript suggest CC-4047 will provide important anti-inflammatory benefit to patients and will improve the safety of NSAIDs in the treatment of SCD or other inflammatory conditions.

MeSH terms

  • Anemia, Sickle Cell / metabolism
  • Anti-Inflammatory Agents, Non-Steroidal / pharmacology
  • Blotting, Western
  • Cyclooxygenase 2 / drug effects*
  • Cyclooxygenase 2 Inhibitors / pharmacology*
  • Drug Synergism
  • Gene Expression / drug effects
  • Humans
  • Immunologic Factors / pharmacology*
  • Immunoprecipitation
  • Lipopolysaccharides / pharmacology
  • Membrane Proteins / drug effects*
  • Monocytes / drug effects
  • Monocytes / metabolism
  • Nitrobenzenes / pharmacology
  • Prostaglandins / metabolism
  • Reverse Transcriptase Polymerase Chain Reaction
  • Sulfonamides / pharmacology
  • Thalidomide / analogs & derivatives*
  • Thalidomide / pharmacology
  • Transcription, Genetic / drug effects*

Substances

  • Anti-Inflammatory Agents, Non-Steroidal
  • Cyclooxygenase 2 Inhibitors
  • Immunologic Factors
  • Lipopolysaccharides
  • Membrane Proteins
  • Nitrobenzenes
  • Prostaglandins
  • Sulfonamides
  • N-(2-cyclohexyloxy-4-nitrophenyl)methanesulfonamide
  • Thalidomide
  • pomalidomide
  • Cyclooxygenase 2
  • PTGS2 protein, human