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    Bioorg Med Chem Lett. 2008 Feb 1;18(3):923-8. Epub 2008 Jan 15.

    The discovery of odanacatib (MK-0822), a selective inhibitor of cathepsin K.

    Source

    Merck Frosst Centre for Therapeutic Research, 16711 TransCanada Hwy, Kirkland, Que., Canada.

    Abstract

    Odanacatib is a potent, selective, and neutral cathepsin K inhibitor which was developed to address the metabolic liabilities of the Cat K inhibitor L-873724. Substituting P1 and modifying the P2 side chain led to a metabolically robust inhibitor with a long half-life in preclinical species. Odanacatib was more selective in whole cell assays than the published Cat K inhibitors balicatib and relacatib. Evaluation in dermal fibroblast culture showed minimal intracellular collagen accumulation relative to less selective Cat K inhibitors.

    PMID:
    18226527
    [PubMed - indexed for MEDLINE]

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