Cathepsin K is a protease released by osteoclasts, which is involved in the destruction of collagen fibers that form the organic phase of the bone matrix, and plays a key role in bone resorption. Odanacatib is a selective inhibitor of cathepsin K, which blocks bone remodeling by inhibiting resorption. Phase II trials have shown that odanacatib is a potent antiresorptive agent and does not significantly reduce biochemical markers of bone formation during long-term treatment of postmenopausal women. This increases the bone mineral density that is comparable with the most powerful antiresorptive agents. Odanacatib has a generally favorable tolerability and safety profile. Currently, only Phase II studies have been reported and its efficacy in reducing fractures has not been demonstrated. The adverse effects are reversible and disappear after discontinuation. If this antifracture efficacy can be shown, odanacatib could be a a safe, efficacious option for the treatment of osteoporosis.
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