Odanacatib
Odanacatib Uses, Dosage, Side Effects, Food Interaction and all others data.
Odanacatib is an inhibiter of cathepsin K which was originally developed be Merck & Co as a new treatment for osteoporosis . The drug made it to phase III trials before abandoned due to increased stroke.
Increases bone mineral density and reduces risk of fractures in osteoporosis .
Trade Name | Odanacatib |
Generic | Odanacatib |
Odanacatib Other Names | Odanacatib |
Type | |
Formula | C25H27F4N3O3S |
Weight | Average: 525.56 Monoisotopic: 525.170925567 |
Protein binding | 97.5% bound to plasma proteins . |
Groups | Investigational |
Therapeutic Class | |
Manufacturer | |
Available Country | |
Last Updated: | September 19, 2023 at 7:00 am |
Uses
Investigated for use/treatment in osteoporosis .
How Odanacatib works
Odanacatib inhibits cathepsin K, likely by binding to its active site . Cathepsin K is a cysteine protease enzyme which is secreted by osteoclasts . Cathepsin K is responsible for the breakdown of collagen in the bone matrix as part of bone resorption. The inhibition of this enzyme results in decreased bone resorption without affecting bone deposition resulting in increased bone mineral density. This increased bone mineral density strengthens the bone which leads to fewer fractures in osteoporosis.
Toxicity
Odanacatib was found to increase the risk of stroke . No further toxicological studies have been performed.
Volume of Distribution
100L
Elimination Route
Tmax of 2-6h . The absolute bioavailabilities observed with 30mg and 50 mg doses are 70% and 30% respectively. When taken with high fat meals the 50mg dose's bioavailability increases to 49% and tmax increases to 10.5h .
Half Life
Apparent half life observed to be 87.3-94.7h .
Clearance
Total clearance of 0.8L/h .
Elimination Route
16.9% excreted in urine. 74.5% excreted in feces.
Innovators Monograph
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