Odanacatib (MK-0822) is a selective and reversible inhibitor of cathepsin K (CatK). The cathepsin K inhibitor odanacatib (MK-0822) was shown to increase bone mineral density (BMD) and maintained normal bone strength at the spine in ovariectomized (OVX) rhesus monkeys. Odanacatib increased femoral neck (FN) BMD by 11% and 15% (p < 0.07) and ultimate load by 25% (p < 0.05) and 30% (p < 0.01) versus vehicle. Moreover, Odanacatib stimulated long-term FN and PF periosteal BFR by 3.5-fold and 6-fold with the 30 mg/kg dose versus vehicle, respectively. Odanacatib reduces bone turnover and increases bone mass in the lumbar spine of skeletally mature ovariectomized rhesus monkeys. Odanacatib was more selective than the published Cat K inhibitors balicatib and relacatib. Odanacatib (MK 0822) is currently in Phase II clinical trials.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||DMSO 100 mg/mL|
Odanacatib treatment increases hip bone mass and cortical thickness by preserving endocortical bone formation and stimulating periosteal bone formation in the ovariectomized adult rhesus monkey.
Cusick T, et al. J Bone Miner Res. 2012 Mar;27(3):524-37. PMID: 22113921.
Odanacatib in the treatment of postmenopausal women with low bone mineral density: three-year continued therapy and resolution of effect.
Eisman JA, et al. J Bone Miner Res. 2011 Feb;26(2):242-51. PMID: 20740685.
The discovery of odanacatib (MK-0822), a selective inhibitor of cathepsin K.
Gauthier JY, et al. Bioorg Med Chem Lett. 2008 Feb 1;18(3):923-8. PMID: 18226527.
|Related Cathepsin Products|
N-Ethylmaleimide (NEM) is a cysteine protease inhibitor.
CA-074 Me is a membrane-permeable derivative of CA-074 and acts as an irreversible cathepsin B inhibitor.
UK-371804 is a potent and selective urokinase-type plasmogen activator (uPA) inhibitor with excellent enzyme potency (Ki=10 nM) and selectivity profile (4000-fold versus tPA and 2700-fold versus plasmin).
Leupeptin hemisulfate is a reversible inhibitor of trypsin-like and cysteine proteases such as calpain.
Balicatib is a potent and selective inhibitor of cathepsin K; 10-100-fold more potent in cell-based enzyme occupancy assays than against cathepsin B, L, and S.
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