Publications [#330227] of Michael J. Therien

Papers Published

1. 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, The discovery of odanacatib (MK-0822), a selective inhibitor of cathepsin K., Bioorganic & medicinal chemistry letters, vol. 18 no. 3 (February, 2008), pp. 923-928 [doi]
   (last updated on 2026/01/18)

   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.