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Review
. 2011 Jun 14;7(8):447-56.
doi: 10.1038/nrrheum.2011.77.

Cathepsin K: its skeletal actions and role as a therapeutic target in osteoporosis

Aline G Costa  1 , Natalie E Cusano, Barbara C Silva, Serge Cremers, John P Bilezikian
Affiliations
Review

Cathepsin K: its skeletal actions and role as a therapeutic target in osteoporosis

Aline G Costa et al. Nat Rev Rheumatol. .

Abstract

Bone remodeling consists of two phases--bone resorption and bone formation--that are normally balanced. When bone resorption exceeds bone formation, pathologic processes, such as osteoporosis, can result. Cathepsin K is a member of the papain family of cysteine proteases that is highly expressed by activated osteoclasts. Cathepsin K readily degrades type I collagen, the major component of the organic bone matrix. With such a major role in the initial process of bone resorption, cathepsin K has become a therapeutic target in osteoporosis. The antiresorptive properties of cathepsin K inhibitors have been studied in phase I and phase II clinical trials. Phase III studies are currently underway for odanacatib, a selective cathepsin K inhibitor.

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