2. Academic Validation
  3. First-in-class pan caspase inhibitor developed for the treatment of liver disease

First-in-class pan caspase inhibitor developed for the treatment of liver disease

  • J Med Chem. 2005 Nov 3;48(22):6779-82. doi: 10.1021/jm050307e.
Steven D Linton 1,  Teresa Aja,  Robert A Armstrong,  Xu Bai,  Long-Shiuh Chen,  Ning Chen,  Brett Ching,  Patricia Contreras,  Jose-Luis Diaz,  Craig D Fisher,  Lawrence C Fritz,  Patricia Gladstone,  Todd Groessl,  Xin Gu,  Julia Herrmann,  Brad P Hirakawa,  Niel C Hoglen,  Kathy G Jahangiri,  Vincent J Kalish,  Donald S Karanewsky,  Lalitha Kodandapani,  Joseph Krebs,  Jeff McQuiston,  Steven P Meduna,  Kip Nalley,  Edward D Robinson,  Robert O Sayers,  Kristen Sebring,  Alfred P Spada,  Robert J Ternansky,  Kevin J Tomaselli,  Brett R Ullman,  Karen L Valentino,  Suzanne Weeks,  David Winn,  Joe C Wu,  Pauline Yeo,  Cheng-zhi Zhang
Affiliations

Affiliation

  • 1 Idun Pharmaceuticals, 9380 Judicial Drive, San Diego, CA 92121, USA. slinton@idun.com
PMID: 16250635 DOI: 10.1021/jm050307e
Abstract

A series of oxamyl dipeptides were optimized for pan Caspase inhibition, anti-apoptotic cellular activity and in vivo efficacy. This structure-activity relationship study focused on the P4 oxamides and warhead moieties. Primarily on the basis of in vitro data, inhibitors were selected for study in a murine model of alpha-Fas-induced liver injury. IDN-6556 (1) was further profiled in additional in vivo models and pharmacokinetic studies. This first-in-class Caspase Inhibitor is now the subject of two Phase II clinical trials, evaluating its safety and efficacy for use in liver disease.

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