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-036 is a next generation cathepsin S inhibitor. It is structurally distinct from the other cathepsin S inhibitors, VBY-129, VBY-891 and VBY-285.
VBY-036 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-036 is very selective against other human cathepsins (B, F, L and K). Sustained cathepsin S inhibition after oral dosing has been demonstrated in vivo through the use of a biomarker. VBY-036 shows potent inhibitory activity in models of autoimmunity and neuropathic pain.
VBY-036 is orally bioavailable and suitable for once-daily dosing in man.