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

Published

Journal Article

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.

Full Text

Duke Authors

Cited Authors

  • Gauthier, JY; Chauret, N; Cromlish, W; Desmarais, S; Duong, LT; Falgueyret, J-P; Kimmel, DB; Lamontagne, S; Léger, S; LeRiche, T; Li, CS; Massé, F; McKay, DJ; Nicoll-Griffith, DA; Oballa, RM; Palmer, JT; Percival, MD; Riendeau, D; Robichaud, J; Rodan, GA; Rodan, SB; Seto, C; Thérien, M; Truong, V-L; Venuti, MC; Wesolowski, G; Young, RN; Zamboni, R; Black, WC

Published Date

  • February 2008

Published In

Volume / Issue

  • 18 / 3

Start / End Page

  • 923 - 928

PubMed ID

  • 18226527

Pubmed Central ID

  • 18226527

Electronic International Standard Serial Number (EISSN)

  • 1464-3405

International Standard Serial Number (ISSN)

  • 0960-894X

Digital Object Identifier (DOI)

  • 10.1016/j.bmcl.2007.12.047

Language

  • eng