Description
Relacatib (SB-462795, GSK-462795) is a potent and orally bioavailable small molecule cathepsin inhibitor with Ki of 41, 68 and 53 pM for cathepsin K, L and V, respectively; displays 39-300-fold selectivity over other cathepsins; inhibits endogenous cathepsin K in situ in human osteoclasts and human osteoclast-mediated bone resorption with IC50 of 45nM and 70nM, respectively; inhibits bone resorption both in vitro in human tissue and in vivo in cynomolgus monkeys. Osteoporosis Phase 2 Discontinued