Novel NSAIDs

The Medical Need

Non Steroidal Anti-Inflammatory Drugs (NSAIDs) such as aspirin, ibuprofen, and naproxen, are among the most widely used drugs in the world. NSAIDs have been successfully prescribed for years and even decades for pain and inflammation, as in the treatment of osteoarthritis, which affects 20 million Americans.

NSAIDs comprise a $10 billion worldwide market. Despite their widespread use, the upper gastrointestinal (GI) adverse events caused by NSAID use are responsible for 107,000 hospitalizations and 17,000 deaths annually in the U.S.

For additional information on NSAIDs and their side effects, click here.

Medinox's Approach

Medinox's scientists have discovered proprietary chemical groups that can be attached to known NSAIDs to make them safer. In Medinox's NSAID program, a known NSAID is joined to a proprietary protective group which results in a new chemical entity that is less damaging to the stomach and intestinal lining. In the stomach and the intestine, the protective group remains intact and does not damage the GI system. When it is absorbed into the circulation, the conjugate is cleaved, freeing the NSAID so that it can perform its anti-inflammatory activities (see figure below). In animal studies, Medinox's novel NSAIDs have delivered the equivalent therapeutic benefits as their parent NSAIDs, but produce substantially fewer GI side effects.

Medinox's NSAIDs are based on conventional NSAIDs with proven clinical efficacy. With their improved safety and potential to provide cardioprotective benefits through COX-1 inhibition, our NSAIDs have the potential to be attractive therapeutic alternatives to currently available NSAIDs.

MX-1094 is an NSAID prodrug which is being developed to improve the GI safety profile of naproxen, an existing and well characterized pharmaceutical product. In December 2002 we concluded a Phase I trial of MX-1094 which was designed to demonstrate safety and evaluate the pharmacokinetics of MX-1094 in human volunteers. Because we observed a good safety profile in this study, we plan to advance development to a small-scale Phase II trial in Europe beginning early 2004.