A highly potent inhibitor of cathepsin K (relacatib) reduces biomarkers of bone resorption both in vitro and in an acute model of elevated bone turnover in vivo in monkeys.

@article{Kumar2007AHP,
  title={A highly potent inhibitor of cathepsin K (relacatib) reduces biomarkers of bone resorption both in vitro and in an acute model of elevated bone turnover in vivo in monkeys.},
  author={S. Kiran Kumar and Lauren C Dare and Janice Vasko-Moser and Ian E. James and Simon M Blake and David J. Rickard and S M Hwang and Thaddeus A. Tomaszek and Dennis S. Yamashita and Robert W. Marquis and Hyun Jung Alvarez Oh and Jae Uk Jeong and Daniel F. Veber and Maxine Gowen and Michael W. Lark and George B Stroup},
  journal={Bone},
  year={2007},
  volume={40 1},
  pages={122-31}
}
Cathepsin K is an osteoclast-derived cysteine protease that has been implicated as playing a major role in bone resorption. A substantial body of evidence indicates that cathepsin K is critical in osteoclast-mediated bone resorption and suggests that its pharmacological inhibition should result in inhibition of bone resorption in vivo. Here we report the pharmacological characterization of SB-462795 (relacatib) as a potent and orally bioavailable small molecule inhibitor of cathepsin K that… CONTINUE READING
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