About Cathepsin S and VBY-036
Cathepsin S is a member of the cysteine protease family of cathepsin inhibitors that catalyzes proteolytic cleavage of membrane-bound fractalkine from the surface of neurons to release soluble fractalkine. Fractalkine is a potent chemokine that stimulates the recruitment of inflammatory cells to the sites of neuronal damage and activates microglia. Microglia are macrophage-like cells that are implicated as key drivers in the pathogenesis of chronic neuropathic pain syndromes. In model systems, cathepsin S mediated microglial activation is essential in the development of pain. The inhibition of cathepsin S results in a reduction in pain, as well as prevention of pain in preclinical models of chemotherapy-induced neuropathic pain and diabetic neuropathy.
VBY-036 is an optimized cathepsin S inhibitor that is a potent, competitive and reversible inhibitor of cathepsin S. It has picomolar inhibitory potency against the isolated cathepsin S enzyme and nanomolar activity in cellular assays. VBY-036 is also highly selective against related human cathepsins as well as other enzymes, and sustained cathepsin S inhibition after oral dosing has been demonstrated in vivo through the use of a biomarker. The compound has been tested in pre-clinical studies and is now entering the next phase - a phase 1 clinical trial in healthy human volunteers. The VBY-036 program is a novel approach to the treatment of pain and may result in a safe and effective oral therapeutic for an important unmet medical need.
About Virobay, Inc.
Founded in 2006, Virobay is a leader in the design, synthesis and development of small molecule inhibitors of cysteine proteases, a class of enzymes that are key mediators in a variety of diseases, including autoimmunity, neuropath
|SOURCE Virobay, Inc.|
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