Cathepsin K is a member of the papain family of cysteine proteases which is associated with osteopetrosis, impaired resorption of bone matrix, impaired processing of thyroglobulin and reduced release of thyroid hormone. Balicatib is a very potent and selective inhibitor of human cathepsin K, with a Ki value of 0.7 nM. 140 postmenopausal women administered of AAE-581 once a day orally (10-50 mg per day) showed successful reduced bone resorption and improved bone formation[3]. Balicatib treatment for 18 months in female cynomolgus monkeys (orally twice daily by nasogastric intubation, 10/30/50 mg/kg/day) partially prevented ovariectomy-induced changes in bone mass and inhibited cancellous bone turnover[4].
作用机制
Balicatib targets to lysosomes by conjugating with poly(ethylene glycol) polymers.
Balicatib/巴利卡替 细胞实验
Cell Line
Concentration
Treated Time
Description
References
primary human trabecular meshwork (HTM) cells
10 µM
24 h
To investigate the effects of Balicatib on ECM protein expression in HTM cells. Results showed that Balicatib treatment significantly increased FN and COL1A expression.
Cells. 2021 Oct 24;10(11):2864
primary porcine trabecular meshwork (PTM) cells
10 µM
24 h
To evaluate the effects of Balicatib on cell viability and CTSK activity in PTM cells. Results showed that 10 µM Balicatib treatment did not significantly affect cell viability but significantly reduced CTSK activity.
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