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

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

  • Bioorg Med Chem Lett. 2008 Feb 1;18(3):923-8. doi: 10.1016/j.bmcl.2007.12.047.
Jacques Yves Gauthier 1,  Nathalie Chauret,  Wanda Cromlish,  Sylvie Desmarais,  Le T Duong,  Jean-Pierre Falgueyret,  Donald B Kimmel,  Sonia Lamontagne,  Serge Léger,  Tammy LeRiche,  Chun Sing Li,  Frédéric Massé,  Daniel J McKay,  Deborah A Nicoll-Griffith,  Renata M Oballa,  James T Palmer,  M David Percival,  Denis Riendeau,  Joel Robichaud,  Gideon A Rodan,  Sevgi B Rodan,  Carmai Seto,  Michel Thérien,  Vouy-Linh Truong,  Michael C Venuti,  Gregg Wesolowski,  Robert N Young,  Robert Zamboni,  W Cameron Black
Affiliations

Affiliation

  • 1 Merck Frosst Centre for Therapeutic Research, 16711 TransCanada Hwy, Kirkland, Que., Canada.
PMID: 18226527 DOI: 10.1016/j.bmcl.2007.12.047
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.

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