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Relacatib is a potent, orally bioavailable small molecule inhibitor of cathepsin K, a cysteine protease highly expressed in osteoclasts and implicated in bone resorption. It also inhibits cathepsins L and V with high potency. Relacatib was developed for the treatment of osteoporosis, osteoarthritis, bone metastases, and potentially other disorders involving excessive bone degradation. The drug has demonstrated inhibition of endogenous cathepsin K activity in human osteoclasts and suppression of human osteoclast-mediated bone resorption both in vitro and in vivo (notably in cynomolgus monkeys). Clinical development reached phase II trials for osteoporosis but did not progress to approval[1][2][3][4][5][6].
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