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Odanacatib is a small molecule inhibitor of cathepsin K developed by Merck & Co for the treatment of osteoporosis and bone metastasis. Cathepsin K is a cysteine protease secreted by osteoclasts that plays a key role in the breakdown of collagen in bone matrix during bone resorption. By selectively inhibiting cathepsin K at its active site, odanacatib decreases bone resorption without affecting bone formation. This results in increased bone mineral density and reduced risk of fractures in patients with osteoporosis. Odanacatib was investigated primarily as an oral once-weekly therapy for postmenopausal women with osteoporosis and showed significant increases in BMD and reduction in fracture risk during clinical trials. However, development was discontinued after phase III due to an observed increased risk of stroke[1][3][4][5][7].
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