Jump to content

Odanacatib

From Wikipedia, the free encyclopedia

This is an old revision of this page, as edited by Fconaway (talk | contribs) at 01:50, 28 July 2012 (documentation needed, as these imply mismanagement). The present address (URL) is a permanent link to this revision, which may differ significantly from the current revision.

{{Drugbox | Verifiedfields = changed | verifiedrevid = 443444475 | IUPAC_name = N-(1-cyanocyclopropyl)-4-fluoro-N2-{(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl}-L-leucinamide | image = Odanacatib Structural Formulae V.1.svg

| tradename = | pregnancy_AU = | pregnancy_US = | pregnancy_category = | legal_AU = | legal_CA = | legal_UK = | legal_US = | legal_status = | routes_of_administration = oral

| bioavailability = | protein_bound = | metabolism = | elimination_half-life = | excretion =

| CAS_number_Ref =  checkY | CAS_number = 603139-19-1 | ATC_prefix = none | ATC_suffix = | ATC_supplemental = | PubChem = 10152654 | DrugBank_Ref =  checkY | DrugBank = | UNII_Ref =  checkY | UNII = N673F6W2VH | ChEMBL_Ref =  ☒N | ChEMBL = 481611

| chemical_formula = | C=25 | H=27 | F=4 | N=3 | O=3 | S=1 | molecular_weight = 525.56 g/mol | smiles = CC(C)(CC(C(=O)NC1(CC1)C#N)NC(C2=CC=C(C=C2)C3=CC=C(C=C3)S(=O)(=O)C)C(F)(F)F)F | 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 }} 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. As of November 2009, Merck is conducting phase III clinical trials.

The clinical trial for this compound has been stopped after a review showed it was highly effective and has a good safety profile. To keep this compound away from the public would be unethical, just for further study. It is expected Merck will apply for approval within the next 12 months. Some projections expect this drug will bring a billion a year in sales.[citation needed]

This drug was developed at Merck Frosst, as was Merck's block buster drug Singular. The Frosst research site was closed Oct 2010. According to Merck this was due to very low return on investment at this site, and none of the researcher chemists who created this drug currently work for Merck.[citation needed]

References

  1. ^ PMID 18685424
  2. ^ Gauthier JY, Chauret N, Cromlish W; et al. (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. {{cite journal}}: Explicit use of et al. in: |author= (help); Unknown parameter |month= ignored (help)CS1 maint: multiple names: authors list (link)