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Proteolix Presents Preclinical Data for Oral Proteasome Inhibitor PR-047 at the 50th Annual Meeting of the American Society of Hematology
Date:12/8/2008

Lead Oral Candidate Demonstrates Proteasome Inhibition and Anti-Tumor Activity

SOUTH SAN FRANCISCO, Calif., Dec. 8 /PRNewswire/ -- Proteolix, Inc., today announced results from a series of in vitro and in vivo studies designed to characterize PR-047, the company's oral proteasome inhibitor. These data were presented today in a poster titled "Preclinical Pharmacology and In Vitro Characterization of PR-047, An Oral Inhibitor of the 20S Proteasome" (Abstract # 3671) at the 50th Annual Meeting of the American Society of Hematology (ASH). PR-047 is the first oral compound in a new class of highly specific proteasome inhibitors. Carfilzomib, the lead compound in this class, will be the subject of two oral presentations of Phase 2 data on Tuesday, December 9th. PR-047 was designed by Proteolix scientists to combine the pharmacological properties of carfilzomib with the convenience of oral dosing.

Researchers evaluated PR-047's mechanism, bioavailability and activity in a series of preclinicalstudies. Like carfilzomib, PR-047 was shown to target the chymotrypsin-like activity of the proteasome and induce tumor cell death across multiple human cell lines. Oral administration of PR-047 in rodents and monkeys resulted in rapid and prolonged dose-dependent inhibition of the proteasome. Furthermore, significant proteasome inhibition was achieved at doses well below the maximum-tolerated dose even when administered over five consecutive days, suggesting that repeated daily dosing may be feasible with this molecule. Administration of PR-047 resulted in consistent anti-tumor responses in hematological and solid tumor xenograft models at doses below the maximum-tolerated dose.

"We are pleased by the preclinical data achieved to date with PR-047, which demonstrates a promising combination of proteasome inhibition, anti-tumor activity, bioavailability and tolerability," said Mark
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SOURCE Proteolix, Inc.
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