COX-2 inhibitors compared and contrasted

Expert Opin Pharmacother. 2001 Nov;2(11):1859-76. doi: 10.1517/14656566.2.11.1859.


Non-steroidal anti-inflammatory drugs (NSAIDs) are the principal drug treatments for inflammation, pain and fever. They act primarily by inhibiting prostaglandin (PG) synthesis but this can cause adverse events (AEs). Since the discovery of two PG synthesising enzymes, COX-1 and COX-2, and the substantial evidence that sparing COX-1 is advantageous for gastric safety, great interest has focused on selective COX-2 inhibitors. Much of the impetus has come from the most recently developed compounds celecoxib and rofecoxib, which have shown spectacular sales growth. However, the older drugs etodolac, nimesulide and meloxicam, made before COX-2 was discovered, are also COX-1-sparing and have good GI safety and therapeutic activities. These five compounds show similarities and differences that are discussed in relation to aspects that include their uses, efficacy, actions and safety.

Publication types

  • Comparative Study
  • Review

MeSH terms

  • Animals
  • Arthritis, Rheumatoid / drug therapy
  • Cyclooxygenase 2
  • Cyclooxygenase 2 Inhibitors
  • Cyclooxygenase Inhibitors / adverse effects
  • Cyclooxygenase Inhibitors / chemistry
  • Cyclooxygenase Inhibitors / economics
  • Cyclooxygenase Inhibitors / pharmacokinetics
  • Cyclooxygenase Inhibitors / therapeutic use*
  • Humans
  • Isoenzymes / antagonists & inhibitors*
  • Membrane Proteins
  • Pain / drug therapy
  • Prostaglandin Antagonists / pharmacology
  • Prostaglandin-Endoperoxide Synthases
  • Terminology as Topic


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