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Proteolix Announces Positive Data From Two Ongoing Phase 2 Clinical Trials of Carfilzomib in Multiple Myeloma at the 50th Annual Meeting of the American Society of Hematology
Date:12/9/2008

al Targets of Proteasome Inhibitors Bortezomib and Carfilzomib (Abstract #2657) and The Selective Proteasome Inhibitor Carfilzomib is Well Tolerated in Experimental Animals with Dose Intensive Administration (Abstract #2765).

Carfilzomib acts by inhibiting the proteasome with a high degree of selectivity and is structurally and mechanistically distinct from bortezomib. Preclinical studies designed to assess and compare the off-target activity of bortezomib and carfilzomib indicate that carfilzomib has minimal activity on proteases other than the proteasome. In contrast, bortezomib targets several serine proteases including Cathepsin G, an enzyme whose inhibition may play a role in neuropathic pain. Proteolix researchers believe that these observations may translate into a different and possibly superior safety profile for carfilzomib as compared to bortezomib. In support of this notion, chronic administration of carfilzomib is well tolerated in rats and monkeys with no signs of the significant behavioral and histological neurotoxicities that have been described for bortezomib.

About Multiple Myeloma

According to the American Cancer Society, in 2008, approximately 19,900 new cases of multiple myeloma will be diagnosed in the United States. Newly diagnosed patients have treatment options that include combination chemotherapeutic agents and stem cell transplantation. While many patients respond to treatment, most eventually relapse and require subsequent treatment. Few patients are ultimately cured of their disease.

About Carfilzomib

Carfilzomib is the first in a new class of highly specific proteasome inhibitors. Carfilzomib produces specific and sustained inhibition of the proteasome, leading to apoptosis in cancer cells with minimal off-target effects. In Phase 1 and Phase 2 clinical trials, carfilzomib has demonstrated single-agent activity in hematologic and solid
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SOURCE Proteolix, Inc.
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