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-129 is a potent, competitive and reversible inhibitor of purified cathepsin S. It is also highly selective against other human cathepsins (B, F, L, K and V). VBY-129 has potent activity in cellular assays and in animal models of disease.
A Phase 1 clinical trial of VBY-129 was completed which demonstrated sustained inhibition of cathepsin S after once daily oral dosing.