Cathepsin K inhibitors prevent matrix-derived growth factor degradation by human osteoclasts.

The coupling between bone formation and resorption creates a therapeutic impasse in osteoporosis: antiresorptive therapy halts bone loss, but also inhibits bone formation, and therefore does not cure the condition. Surprisingly, recent preliminary reports suggest that inhibition of resorption by cathepsin K (CathK) inhibitors augments bone formation. Uniquely amongst resorption-inhibitors, CathK-inhibitors suppress degradation of the organic matrix of bone while allowing demineralization.