Cyclooxygenase-2 inhibitors: a new class of anti-inflammatory agents that spare the gastrointestinal tract.
The NSAIDs are potent anti-inflammatory and analgesic agents. It is now believed that the NSAIDs exert their therapeutic activity through the inhibition of COX-2 at the site of inflammation. Unfortunately, these compounds are equally capable of inhibiting constitutively expressed COX-1 in tissues such as the gastrointestinal tract and kidney, which results in serious, mechanism-based toxicities that limit the drug's therapeutic utility. With the identification of selective COX-2 inhibitors, alternatives to traditional NSAID therapy should be available that will provide clinical usefulness with reduced toxicity.
Masferrer
J L
JL
Inflammatory Diseases Research, G.D. Searle at Monsanto Corporation, St. Louis, Missouri, USA.
Isakson
P C
PC
Seibert
K
K
D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000494:pharmacology*; D051546:Cyclooxygenase 2; D052246:Cyclooxygenase 2 Inhibitors; D016861:Cyclooxygenase Inhibitors / Q000494:pharmacology*; D004064:Digestive System / Q000187:drug effects* / Q000201:enzymology; D005767:Gastrointestinal Diseases / Q000188:drug therapy / Q000201:enzymology; D006801:Humans; D007527:Isoenzymes / Q000096:biosynthesis / Q000187:drug effects*; D008565:Membrane Proteins; D010544:Peroxidases / Q000096:biosynthesis / Q000187:drug effects*; D011451:Prostaglandin-Endoperoxide Synthases / Q000096:biosynthesis / Q000187:drug effects*
D000894:Anti-Inflammatory Agents, Non-Steroidal; D052246:Cyclooxygenase 2 Inhibitors; D016861:Cyclooxygenase Inhibitors; D007527:Isoenzymes; D008565:Membrane Proteins; D010544:Peroxidases; D051546:Cyclooxygenase 2; C496540:PTGS2 protein, human; D011451:Prostaglandin-Endoperoxide Synthases