The results of the first phase III clinical trials for the new osteoarthritis drug licofelone, have shown comparable efficacy to conventional NSAIDs but with excellent gastrointestinal (GI) and general tolerability. These results are similar to those achieved in the original development of COX-2 inhibitors; however, the action of licofelone should also avoid the possible disadvantages of COX-2 inhibitors and may therefore offer additional benefits for the treatment of osteoarthritis (OA).
According to data presented at the 2002 European League Against Rheumatism (EULAR) congress in Stockholm, licofelone inhibits both 5-LOX and COX enzymes in the inflammatory pathway and appears in theory, and now in clinical trials, to offer benefits over selective COX-2 inhibitors in the treatment of osteoarthritis. The most recent data presented by Professor Jean-Yves Reginster, of the University of Liege, Belgium, show licofelone to be as effective as the traditional NSAID, naproxen and with excellent GI and general tolerability.
“The trials in which we were involved start to show that our expectations for the benefits of 5-LOX/ COX inhibitors in treating osteoarthritis are well founded. Licofelone appears to offer comparable efficacy to the highly effective treatment naproxen, but with excellent GI, renal, hepatic and general tolerability,” Reginster said.
Current treatment options for the inflammation and pain of osteoarthritis include conventional NSAIDs (such as the naproxen used in this study) and selective COX-2 inhibitors. Conventional NSAIDs effectively inhibit the COX-1 and COX-2 pathway, but have a high risk of adverse GI events. Selective COX-2 inhibitors have remained the main focus of research due to their early success and major pharmaceutical backing. Currently available COX-2 inhibitors have also demonstrated a reduction in gastrointestinal effects compared with the traditional NSAIDs.
However, it is now becoming clear that some COX-2 inhibitors may also be associated with an increased risk of GI events, and it is now being suggested, through the development of licofelone, that the balanced inhibition of the 5-LOX and COX pathways may provide a new alternative with an optimal benefit/risk ratio.
Professor Stefan Laufer, University of Tuebingen, Germany who is the researcher credited with discovering licofelone commented, “An extensive, published, pre-clinical program has demonstrated the anti-inflammatory and analgesic efficacy of licofelone. These results are now being confirmed in phase III studies, the first of which have been presented today. Licofelone has passed the stage of being interesting research and has now become a real potential alternative in optimizing the future treatment of osteoarthritis. We look forward to seeing the next available data which we hope will further support these findings and allow the companies involved to make a license submission to support the availability of the treatment for clinicians use as soon as possible.”