Caspase inhibitor for sepsis?
Tuesday January 8, 8:04 am Eastern Time
Press Release
SOURCE: Vertex Pharmaceuticals Incorporated
Vertex Pharmaceuticals Advances New Drug Candidate, VX-799, Into Development to Treat Sepsis
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Caspases and Vertex Drug Discovery
VX-799 has been demonstrated to be a highly potent inhibitor in various cell assays that use many distinct stimuli to trigger apoptosis, including hypoxia, serum deprivation, receptor mediated and spontaneous apoptosis. VX- 799 has shown significant therapeutic potential in an apoptosis-dependent model of organ failure and several models of bacterially induced sepsis. Based on these and other research results, VX-799 is now being evaluated as a drug candidate for the treatment of sepsis.
To increase the pace of drug discovery for structurally similar targets in protein families such as caspases, Vertex has pioneered gene family-based drug discovery. This approach leverages the physical, chemical and biological similarity among related target proteins to enable more efficient drug design. Vertex has conducted extensive research into the role of caspases in disease, and has pioneered the design of small molecule inhibitors directed at caspases. As part of its drug discovery efforts in the caspase protein family, Vertex has determined the three-dimensional atomic structure of several caspases and numerous caspase/inhibitor co-complexes. Vertex has also identified the physiological role of specific caspases using gene-targeting approaches.
Previously, the Company's successful design and optimization of inhibitors of the inflammation target caspase-1 (ICE) has produced orally-active compounds, including pralnacasan (VX-740), a compound in clinical development with Aventis, and VX-765, in preclinical development. VX-799 is the first drug candidate to be advanced as part of Vertex's research efforts targeting caspases involved in apoptosis. VX-799 was discovered by researchers at Vertex's Oxford, U.K. site. Under an agreement begun in 2000, Serono S.A. holds an option to develop and commercialize VX-799 in Europe and as part of a joint venture with Vertex in North America. Taisho holds the option to develop and commercialize VX-799 in Japan and certain Asian markets. |
