Licofelone: A Novel Non-Steriodal Anti-Inflammatory Drug (NSAID) in Arthritis

Arthritis refers to different medical conditions associated with disorder of the primary structures that determine joint functions such as bones, cartilage and synovial membranes. Drug discovery and delivery to retard the degeneration of joint tissues are challenging. Current treatments of different arthritis involves administration of ideal non-steroidal anti-inflammatory drugs (NSAIDs) but are frequently associated with adverse reactions, related to inhibition of cyclo-oxygenase (COX) in tissues where prostaglandins exert physiological effects, such as gastric mucosal defense and renal homeostasis. As a consequence, the interest for novel approaches has re-emerged. New therapeutic options, still under clinical evaluation, are represented as dual COX and 5-lipooxygenase (5-LOX) inhibitors. These are expected to possess clinical advantages over the selective inhibitors of COX enzyme. One of the most promising compounds belonging to this category, licofelone, a competitive inhibitor of 5-lipoxygenase, cyclooxygenase (COX-1 and COX-2), is currently in clinical development for the treatment of osteoarthritis (OA). Licofelone decreases the production of pro-inflammatory leukotrienes and prostaglandins which are involved in the pathophysiology of OA and in gastrointestinal (GI) damage induced by NSAIDs and have the potential to combine good analgesic and anti-inflammatory effects with excellent GI tolerability. The emerging clinical data for licofelone indicate that it is an effective and well-tolerated therapy which could be suitable for the long-term treatment of patients with OA. This review focuses upon the gastrointestinal (GI) safety of selective COX-2 inhibitors and of novel therapeutic strategies, in comparison with traditional NSAIDs.