[Preliminary data from PI for R788 for RA & ITP]
>>SOUTH SAN FRANCISCO, Calif., Feb. 22 /PRNewswire-FirstCall/ -- Rigel Pharmaceuticals, Inc. (Nasdaq: RIGL - News) today announced preliminary data from a Phase I double-blind, placebo controlled trial to investigate the safety and pharmacokinetics of R788, an oral syk kinase inhibitor, in combination with methotrexate in rheumatoid arthritis (RA) patients. The data demonstrated that R788 was well tolerated when given in combination with methotrexate and had no significant adverse pharmacokinetic interactions. The company also announced plans to initiate separate clinical efficacy studies with R788, in RA and in Immune Thrombocytopenic Purpura (ITP), in the second half of 2006.
"New, effective therapeutic options in RA are greatly needed since current treatments have potentially significant limitations," stated Elliott B. Grossbard, M.D., senior vice president of medical development at Rigel. "We are pursuing R788 in autoimmune diseases such as RA and ITP because it has been shown to be a potent and selective inhibitor of syk kinase, which may play a key role in autoimmune diseases."
The Phase I study enrolled patients verified to suffer from RA and who were receiving methotrexate treatment. There were no unanticipated adverse events and pharmacokinetic analysis suggests that there is no adverse interaction with the two agents.
About R788
R788 is a novel, oral syk kinase inhibitor that blocks the activation of mast cells, macrophages and B cells that promote swelling and an inflammatory response. It is being developed initially to treat RA. Phase I trial results have demonstrated that R788 is well-tolerated and showed good pharmaceutical properties. Earlier Phase I studies generated valuable pharmacokinetic/pharmacodynamic data establishing a strong correlation between drug plasma levels and the inhibition of the drug target. In preclinical studies, Rigel's compound greatly diminished the swelling and tissue destruction associated with RA. In addition, in a murine model of ITP, the drug increased platelet counts significantly.
Rheumatoid Arthritis: Current Treatments and Market Opportunity
Approximately 2.1 million people in the U.S. suffer from RA and the worldwide market for innovative RA drugs is projected to reach $10 billion by 2008. RA is a chronic inflammatory disease that affects multiple tissues, but typically produces its most pronounced symptoms in the joints. It is often progressive and debilitating, preventing people from living a symptom-free life. Ultimately the chronic inflammation of joints leads to the destruction of the soft tissue and erosion of the articular surfaces of the bone.
The current treatment options for RA have potentially significant side effects and other shortfalls, including gastrointestinal complications and kidney damage. Some RA patients currently receive multiple drugs depending on the extent and aggressiveness of the disease. Most RA patients require some form of DMARD -- including methotrexate, an anti-cancer agent, or TNF-blocking agents such as Enbrel®. The TNF-blocking agents only inhibit the inflammatory mediator TNF, and are all delivered via injection. Rigel believes that there is a significant opportunity for an oral DMARD that can be used earlier in the course of the disease, preventing its progression prior to major bone and cartilage destruction; this is the product goal for R788 in RA.<<
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