About Cathepsin S & Autoimmune Diseases

Cathepsin S is overexpressed in certain human autoimmune diseases which makes it an excellent therapeutic target. Genetic and pharmacologic inhibition of cathepsin S results in amelioration of disease in pharmacology models.

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Cathepsin S inhibitor: VBY-891

VBY-891 is a next generation cathepsin S inhibitor. It is structurally distinct from the other cathepsin S inhibitors, VBY-129, VBY-036 and VBY-285.

VBY-891 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 is orally bioavailable and suitable for once-daily dosing in man. Virobay has initiated IND enabling activities for VBY-891.