Odanacatib (also known as MK-0822) is a potent, neutral, and selective inhibitor of human/rabbit cathepsin K that may be applied to the management of bone metastases and osteoporosis. With IC50s of 0.2 nM/1 nM, it inhibits cathepsin K (human/rabbit) and shows good selectivity against off-target cathepsins B, L, and S. Odanacatib binds to cathepsin K specifically and inhibits its activity. This may reduce bone resorption, improve bone mineral density, and reverse osteoporotic changes. Approximately 16,000 postmenopausal osteoporosis patients are participating in a phase III trial to assess the potential of odanacatib to reduce fracture risk.
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