Odanacatib
Odanacatib (INN;[1] codenamed MK-0822) is an investigational treatment for osteoporosis and bone metastasis.[2] It is an inhibitor of cathepsin K,[3] an enzyme involved in bone resorption.
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| Other names | (2S)-N-(1-Cyanocyclopropyl)-4-fluoro-4-methyl-2-{[(1S)-2,2,2-trifluoro-1-{4'-(methanesulfonyl)-[1,1'-biphenyl]-4-yl}ethyl]amino}pentanamide |
| Routes of administration | By mouth |
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| ECHA InfoCard | 100.207.747  |
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| Formula | C25H27F4N3O3S |
| Molar mass | 525.56 g·mol−1 |
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The drug was developed by Merck & Co. The phase III clinical trial for this medicine was stopped early after a review showed it was highly effective and had a good safety profile. Merck announced in 2014 that it would apply for regulatory approval in 2015.[4]
In 2016, Merck discontinued development of odanacatib and announced it would not seek regulatory approval after analysis discovered an increased risk of stroke.[5]
This drug was developed at Merck Frosst in Montreal.
References
- "International Nonproprietary Names for Pharmaceutical Substances (INN). Recommended International Nonproprietary names: List 60" (PDF). World Health Organization. 2008. p. 239. Retrieved 11 November 2016.
- Le Gall, C. L.; Bonnelye, E.; Clézardin, P. (2008). "Cathepsin K inhibitors as treatment of bone metastasis". Current Opinion in Supportive and Palliative Care. 2 (3): 218–22. doi:10.1097/SPC.0b013e32830baea9. PMID 18685424. S2CID 5834581.
- Gauthier JY, Chauret N, Cromlish W, et al. (February 2008). "The discovery of odanacatib (MK-0822), a selective inhibitor of cathepsin K". Bioorg. Med. Chem. Lett. 18 (3): 923–8. doi:10.1016/j.bmcl.2007.12.047. PMID 18226527.
- https://www.reuters.com/article/2014/09/15/us-merck-osteoporosis-idUSKBN0HA1Y820140915
- "Merck Provides Update on Odanacatib Development Program". Business Wire. 2016-09-02. Archived from the original on 2016-09-03. Retrieved 2016-09-30.
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