Odanacatib is a potent, selective, and neutral cathepsin K inhibitor. Odanacatib is more selective in whole cell assays than the other Cat K inhibitors balicatib and relacatib.
In vivo
As an orally active, potent, and selective CatK inhibitor, odanacatib (ODN) exhibits robust and sustained suppression of bone resorption biomarkers (CTx and NTx/Cr) at weekly doses > or = 25 mg and daily doses > or = 2.5 mg. With the 50-mg dose of odanacatib, lumbar spine and total-hip BMD increased 5.5% and 3.2%, respectively, whereas BMD at these sites was essentially unchanged with placebo (-0.2% and -0.9%).