First-in-class pan caspase inhibitor developed for the treatment of liver disease.
J Med Chem
; 48(22): 6779-82, 2005 Nov 03.
Article
em En
| MEDLINE
| ID: mdl-16250635
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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Base de dados:
MEDLINE
Assunto principal:
Ácidos Pentanoicos
/
Inibidores de Caspase
/
Hepatopatias
Tipo de estudo:
Etiology_studies
Limite:
Adult
/
Animals
/
Humans
Idioma:
En
Ano de publicação:
2005
Tipo de documento:
Article