Cancer and cyclooxygenase-2 (COX-2) inhibition

Curr Pharm Des. 2004;10(6):627-34. doi: 10.2174/1381612043453126.


Prior to the discovery of cyclooxygenase-2 (COX-2), a beneficial association was shown between chronic usage of non steroidal anti-inflammatory drugs (NSAIDs), that non-selectively inhibit both cyclooxygenase-1 (COX-1) and COX-2, and prevention of colorectal cancer. The cloning of COX-2 allowed the development of enzyme inhibitors that selectively inhibit COX-2 and also facilitated the expression profiling of COX-2 in many cancer tissues. COX-2 selective inhibitors have shown efficacy in vitro and in vivo in several animal cancer models and in limited human clinical trials. The potency of COX-2 inhibitors in vivo can be attributed to the inhibition of the enzyme in the tumor as well as in stromal cells, resulting in reduction of carcinogen production, anti-proliferative and pro-apoptopic actions within the tumor and anti-angiogenic and pro-immune surveillance activities in endothelial and myeloid cells. The combination of COX-2 inhibitor with standard cancer chemotherapeutic and/or radiation may provide additional therapeutic paradigms in the treatment of various human cancers.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Animals
  • Antineoplastic Agents / therapeutic use
  • Combined Modality Therapy
  • Cyclooxygenase 2
  • Cyclooxygenase 2 Inhibitors
  • Cyclooxygenase Inhibitors / therapeutic use*
  • Drug Administration Schedule
  • Humans
  • Isoenzymes / antagonists & inhibitors
  • Isoenzymes / genetics
  • Membrane Proteins
  • Neoplasms / drug therapy*
  • Neoplasms / enzymology
  • Neoplasms / prevention & control*
  • Prostaglandin-Endoperoxide Synthases / genetics


  • Antineoplastic Agents
  • Cyclooxygenase 2 Inhibitors
  • Cyclooxygenase Inhibitors
  • Isoenzymes
  • Membrane Proteins
  • Cyclooxygenase 2
  • PTGS2 protein, human
  • Prostaglandin-Endoperoxide Synthases