Cathepsins are a family of proteases that have been implicated in many diseases.
Virobay compounds are highly potent, orally active and drug-like; addressing common problems in the design of cathepsin inhibitors.

Extracellular matrix remodeling plays an important role in COPD. As a secreted protease, cathepsin S degrades matrix proteins. Cathepsin S is expressed at high levels in lung tissue from smokers and in the BAL fluid of patients with COPD. Genetic (cathepsin S -/- mice) and/or pharmacological inhibition of cathepsin S is protective in mouse models of COPD. Cathepsin S is a novel and interesting target for potential treatment of COPD.
Extracellular matrix remodeling plays an important role in cardiovascular diseases such as atherosclerosis. As secreted proteases, cathepsin S and cathepsin K can degrade matrix proteins. Both cathepsins are expressed at high levels in human atherosclerotic plaques. LDL deficient mice or apo-E deficient mice that are also deficient in either cathespsin develop markedly less atherosclerosis. Cathepsin S and/or cathepsin K are novel and interesting targets for potential treatment of cardiovascular disease.