Balicatib

Balicatib (AAE581) is a potent, orally active and selective cathepsin K inhibitor with IC₅₀ values of 22, 61, 48, 2900 nM for cathepsin K, cathepsin B, cathepsin L, cathepsin S, respectively. Balicatib inhibits bone turnover, decreases bone formation rates. Balicatib has the potential for the research of osteoporosis^[1][2]. In Vitro: Balicatib (0-10 µM) shows less than 1.5-fold accumulation of Type I collagen at concentrations up to 10 µM in human dermal fibroblasts^[2]. In Vivo: Balicatib (0, 3, 10, 50 mg/kg; Oral gavage; twice daily for 18 months) partially prevented ovariectomyinduced changes in bone mass, inhibited bone turnover at most sites, and had an stimulatory effect on periosteal bone formation in cynomolgus monkeys^[1].