Odanacatib

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Odanacatib

Odanacatib is a selective inhibitor of cathepsin K, an enzyme involved in the breakdown of bone in the body. It was developed by Merck & Co. for the treatment of osteoporosis and bone metastases. However, development was discontinued in 2016 due to concerns about its side effect profile.

History

Merck & Co. began developing odanacatib in the early 2000s as a potential treatment for osteoporosis. The drug works by inhibiting cathepsin K, an enzyme that breaks down collagen in bones. By inhibiting this enzyme, odanacatib was designed to slow the rate of bone loss in patients with osteoporosis.

In 2014, Merck announced positive results from a Phase III clinical trial of odanacatib. The trial found that the drug significantly reduced the risk of hip fractures and other types of fractures in postmenopausal women with osteoporosis. However, the trial also found an increased risk of stroke in patients taking odanacatib.

In 2016, Merck announced that it was discontinuing development of odanacatib due to concerns about the drug's side effect profile. The decision was based on an analysis of long-term data from the Phase III trial, which showed an increased risk of stroke and other cardiovascular events in patients taking the drug.

Mechanism of Action

Odanacatib inhibits cathepsin K, a lysosomal enzyme that plays a key role in the breakdown of bone. Cathepsin K is produced by osteoclasts, cells that break down bone tissue. By inhibiting cathepsin K, odanacatib reduces the activity of osteoclasts, slowing the rate of bone loss.

Clinical Trials

Odanacatib underwent several clinical trials to evaluate its safety and efficacy in treating osteoporosis. The most significant of these was a Phase III trial involving more than 16,000 postmenopausal women with osteoporosis. The trial found that odanacatib significantly reduced the risk of hip fractures and other types of fractures. However, the trial also found an increased risk of stroke and other cardiovascular events in patients taking the drug.

Side Effects

The most common side effects of odanacatib include nausea, vomiting, abdominal pain, and diarrhea. The drug has also been associated with an increased risk of stroke and other cardiovascular events.

Discontinuation

In 2016, Merck announced that it was discontinuing development of odanacatib due to concerns about the drug's side effect profile. The decision was based on an analysis of long-term data from the Phase III trial, which showed an increased risk of stroke and other cardiovascular events in patients taking the drug.