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Virobay, Inc. initiates a Phase 1 Trial of VBY-036, a compound intended for the treatment of neuropathic pain
Date:5/23/2013

therapy of dermatological diseases," said Robert Booth .

Background

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
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SOURCE Virobay, Inc.
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