Cathepsin S plays a key role in the pathology of autoimmune disease and in the maintenance of neuropathic pain. Genetic and pharmacologic inhibition of cathepsin S results in amelioration of disease in pharmacology models.
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 shows potent inhibitory activity in models of autoimmunity and neuropathic pain.
VBY-891 is orally bioavailable and suitable for once-daily dosing in man. Virobay has initiated IND enabling activities for VBY-891.