|
Oxaprozin (4,5-diphenyl-2-oxazolepropionic acid) is an achiral non steroidal anti-inflammatory drug (NSAID) belonging to the class of the propionic acid derivatives.
Moreover, oxaprozin showed other important pharmacological activities, such as the inhibition of the release of TNF-α and of the Nuclear Factor-κB translocation to DNA that is implicated in the amplification of the inflammatory response. Oxaprozin has dual hepatic metabolic processes (oxidative and coniugative), dual (renal and faecal) elimination pathways that may reduce the risk of disproportionate drug accumulation and toxicity when the drug is used in the elderly and compromised patients. Furthermore its long elimination half-life (about 50-60 hours) allows a once a day administration. Oxaprozin has shown to reach an high concentration in synovial fluid and tissue, in comparison with other NSAIDs. The clinical efficacy of oxaprozin in the management of signs and symptoms of osteoarthritis, adult rheumatoid arthritis, ankylosing spondylitis, soft tissue disorders and gout is well documented by a large number of controlled clinical trials versus other NSAIDs. Oxaprozin 1200mg/day has shown an efficacy equal or even superior in comparison with usual dosage of aspirin, ibuprofen, indomethacin, nabumetone, naproxen, piroxicam, diclofenac. Oxaprozin is well tolerated. Mild gastrointestinal complaints (e.g. nausea, diarrhoea, constipation, gastralgia and occasionally vomiting) are, as with other NSAIDs, the most frequently occurring adverse events with oxaprozin. Helsinn holds the oxaprozin exclusive worldwide licensing rights, excluding USA, Canada and Japan. Oxaprozin was first launched in Italy in 2000 and then in Chile and Germany (2002), followed by Greece and Czech Republic, Bulgaria (2003) and recently in Lithuania (2004). It will be launched in several other European and Latin American countries within 2004 Oxaprozin is presently available on the market under the following trademarks: Dayrun®, Danoprox®, Duraprox®, Flusyd®, Walix®.
|