Cox-2-selective inhibitors: the new super aspirins.

Nonsteroidal anti-inflammatory drugs (NSAIDs) such as aspirin or ibuprofen are commonly used for the occasional headache or fever or to reduce soreness and inflammation resulting from work or exercise. However, many individuals who have rheumatoid arthritis and osteoarthritis depend on these drugs to reduce pain and to restore sufficient flexibility in inflamed joints to permit normal day-to-day activities. Until now, the beneficial effects of NSAIDs have come with a price; about 1% of chronic users per year develop ulcers or other serious gastrointestinal complications (Chase, 1998). Because of the widespread use of NSAIDs, these toxicities are one of the most prevalent drug-associated health risks. In December 1998, the first in a new family of cyclooxygenase-2 isozyme (Cox-2) inhibitors, celecoxib (SC58635; Celebrex), was approved. These second-generation NSAIDs, which preferentially inhibit Cox-2, promise to have the same anti-inflammatory, antipyretic, and analgesic activities as current NSAIDs. However, unlike present-day NSAIDs, which also inhibit prostaglandin synthesis by Cox-1 in the stomach lining, Cox-2-selective inhibitors are not expected to cause the gastrointestinal complications that last year hospitalized an estimated 76,000 NSAID users in the United States. In an NSAID market that amounted to $1.9 billion in prescription sales in America in 1997, estimates from Wall Street are that worldwide sales of the first Cox-2 inhibitors could eventually reach $1 to $3 billion annually (Chase, 1998).