Odanacatib

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Odanacatib
Odanacatib.svg
Clinical data
Routes of
administration
By mouth
ATC code
  • None
Legal status
Legal status
  • Development terminated
Identifiers
Synonyms (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
CAS Number
PubChem CID
IUPHAR/BPS
ChemSpider
UNII
KEGG
ChEMBL
ECHA InfoCard 100.207.747
Chemical and physical data
Formula C25H27F4N3O3S
Molar mass 525.56 g/mol
3D model (Jmol)
 NYesY (what is this?)  (verify)

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.

It is being developed by Merck & Co. The phase III clinical trial for this compound 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 2014 Cowen and Co predicted odanacatib will generate a billion US$ per year in sales by 2020.[5]

In 2016, Merck discontinued development of odanacatib and announced it would not seek regulatory approval after analysis discovered an increased risk of stroke.[6]

This drug was developed at Merck Frosst in Montreal.

References[edit]

  1. ^ "International Nonproprietary Names for Pharmaceutical Substances (INN). Recommended International Nonproprietary names: List 60" (PDF). World Health Organization. 2008. p. 239. Retrieved 11 November 2016. 
  2. ^ 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. PMID 18685424. doi:10.1097/SPC.0b013e32830baea9. 
  3. ^ 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. PMID 18226527. doi:10.1016/j.bmcl.2007.12.047. 
  4. ^ http://www.reuters.com/article/2014/09/15/us-merck-osteoporosis-idUSKBN0HA1Y820140915
  5. ^ "Merck to seek approval of osteoporosis drug, cites safety risks". Reuters. 2014-05-06. 
  6. ^ "Merck Provides Update on Odanacatib Development Program". Business Wire. 2016-09-02. Archived from the original on 2016-09-03. Retrieved 2016-09-30.