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Virobay and LEO Pharma Initiate a Phase 1 Trial of VBY-891, a Compound Intended for Oral Treatment of Psoriasis
Date:3/18/2013

pand and improve treatment options for patients and this is an important example of our commitment to meeting patient needs. To the best of our knowledge, the VBY-891 compound has the potential to be the first in class on the market," said Kim Kjøller, Senior Vice President, Global Development, LEO Pharma.

Background

About Cathepsin S and VBY-891

Cathepsin S is a member of the cysteine protease family of cathepsin inhibitors that catalyzes the final proteolytic step in the processing of invariant chain in specific antigen presenting cells. This step is essential in the maturation and loading of MHC Class II with antigenic peptides and subsequent activation of CD4+ T cells. Continuous presentation of antigenic self-peptides is thought to be involved in the maintenance of chronic disease in autoimmune disorders, including psoriasis. Inhibition of cathepsin S is likely to result in a reduction in antigen presentation without an impact on innate immunity.

VBY-891 is a next generation cathepsin S inhibitor that is a potent, competitive and reversible inhibitor of purified cathepsin S. It has picomolar inhibitory potency against the cathepsin S enzyme and nanomolar inhibitory potency in cellular assays. VBY-891 is also highly selective against human cathepsins L, B, F and K. Sustained cathepsin S inhibition after oral dosing has been demonstrated in vivo through the use of a biomarker. VBY-891 shows potent inhibitory activity in models of autoimmunity and neuropathic pain. Therefore, inhibition of cathepsin S may have therapeutic potential across a range of dermatological conditions.

About the collaboration

The multi-million dollar collaboration between Virobay Inc. and LEO Pharma A/S was entered in 2012 when LEO Pharma in-licensed the promising compound from Virobay. The collaboration agreement involves up-front payment to Virobay of USD 7m, followed by milestone payments totalling up to USD 300m and tiered
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SOURCE Virobay, Inc. and LEO Pharma A/S
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