Odanacatib (MK-0822) 603139-19-1

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Molecular Weight:

525.56 Odanacatib (MK 0822) is a potent, selective, and neutral inhibitor of cathepsin K (human/rabbit) with IC50 of 0.2 nM/1 nM, and demonstrated high selectivity versus off-target cathepsin B, L, S. Phase 3.






Biological Activity


In vitro, Odanacatib shows the high inhibitory activity and selectivity
on cathepsin K with IC50 values of 0.2 nM and 1 nM for human cathepsin K
and rabbit cathepsin K, respectively. Furthermore, Odanacatib also
shows similar potencies in whole human cell enzyme occupancy assays with
corrected IC50 of 5 nM. A recent study shows that
Odanacatib results in reduction of Osteoclast (OC) resorption activity
by interrupting intracellular vesicular trafficking.


In preclinical rats, Odanacatib (10 mg/kg) exhibits excellent pharmacokinetics with clearance (Cl: 2 mL kg-1 min-1), low volume of distribution (Vdss: 1.1 L kg-1), half-life (T1/2:
6 hours) and oral bioavailability (F: 8%), respectively. Besides,
Odanacatib also exhibits excellent metabolic stability in rat
hepatocytes with a 96% recovery of the parent identity.


Odanacatib (ODN) administrated by p.o. prevents bone loss in
ovariectomized (OVX) rabbits in a dose-related manner. Moreover,
Odanacatib (9 µM/day) leads to a significant increase in proximal femur
bone mineral density (BMD) (7.8%), femoral neck BMD (10.8%) and the
greater trochanter BMD (6.5%). In the estrogen-deficient,
skeletally mature rhesus monkeys, long-term treatment with Odanacatib
effectively inhibits bone turnover without reducing osteoclast number
and maintains normal biomechanical properties of the spine of OVX
nonhuman primates.

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Product Categories : Proteases > Cysteine Protease Inhibitor