Odanacatib

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Odanacatib
Odanacatib Structural Formulae V.1.svg
Systematic (IUPAC) name
N-(1-cyanocyclopropyl)-4-fluoro-N2-{(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl}-L-leucinamide
Clinical data
Routes of
administration
oral
Identifiers
CAS Number 603139-19-1 YesY
ATC code none
PubChem CID 10152654
IUPHAR/BPS 6478
ChemSpider 8328162 N
UNII N673F6W2VH YesY
ChEMBL CHEMBL481611 N
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
Chemical data
Formula C25H27F4N3O3S
Molar mass 525.56 g/mol
 NYesY (what is this?)  (verify)

Odanacatib (pINN; codenamed MK-0822) is an investigational treatment for osteoporosis and bone metastasis.[1] It is an inhibitor of cathepsin K,[2] 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,[3] but as of early 2016 there was no report of any application. In 2014 Cowen and Co predicted odanacatib will generate a billion USD per year in sales by 2020.[4]

This drug was developed at Merck Frosst in Montreal.

References[edit]

  1. ^ 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. 
  2. ^ 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. 
  3. ^ http://www.reuters.com/article/2014/09/15/us-merck-osteoporosis-idUSKBN0HA1Y820140915
  4. ^ "Merck to seek approval of osteoporosis drug, cites safety risks". Reuters. 2014-05-06.