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Proteolix, Inc. Drug Candidate, PR-957, Prevents Disease Progression in Rheumatoid Arthritis Models by Selective Inhibition of the Immunoproteasome
Date:6/15/2009

Findings Published in Nature Medicine Suggest Broad Implications for the Treatment of Inflammatory and Autoimmune Disorders

SOUTH SAN FRANCISCO, Calif., June 15 /PRNewswire/ -- Proteolix, Inc. announced that in an article published today in Nature Medicine, Proteolix's selective immunoproteasome inhibitor PR-957 was shown to block disease progression in mouse models of rheumatoid arthritis in a dose-dependent manner and to completely eliminate visible signs of disease at the highest dose. The anti-inflammatory effect induced by PR-957 was rapid and long-lasting, lowering expression of multiple inflammatory mediators, including TNF-a and IL-6. Disease regression was evident 24 hours after dosing and a complete amelioration of disease was achieved with a single dose. When compared to anti-TNF-a therapy (etanercept), PR-957 mediated a more rapid resolution of clinical symptoms, including joint inflammation, and was more effective than etanercept in a model of aggressive arthritis.

These data were published in the June 14, 2009 online edition of Nature Medicine and will be published in the upcoming July 2009 print edition in an article titled: A Selective Inhibitor of the Immunoproteasome Subunit LMP7 Blocks Cytokine Production and Attenuates Progression of Experimental Arthritis. The authors of the article included members of the laboratory of Dr. Marcus Groettrup at the University of Constance (Konstanz, Germany) and researchers, led by Dr. Christopher Kirk, at Proteolix, Inc. (South San Francisco, CA), where the drug candidate was discovered and developed.

PR-957 is the first highly selective, small molecule inhibitor of the immunoproteasome. The proteasome is an intracellular complex present in most cells that mediates the degradation of intracellular proteins, including key components of pathways that contribute to cancer cell growth and immune signaling. It is a proven and val
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SOURCE Proteolix, Inc.
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