CTS-1027

CTS-1027 is an orally bioavailable small molecule inhibitor of matrix metalloproteinases (MMPs), specifically designed as a hydroxamic acid derivative. It potently inhibits several MMPs including MMP-2, MMP-3, MMP-8, MMP-9, MMP-12, MMP-13 and MMP-14 with high selectivity over other proteinases such as caspases and minimal activity against MMP1 and MMP7[1][3][4][5][6]. The drug was originally developed by Roche for osteoarthritis but was later licensed to Conatus Pharmaceuticals for investigation in liver fibrosis associated with hepatitis C virus infection[3]. Mechanistically, CTS-1027 reduces extracellular matrix degradation by inhibiting key enzymes involved in tissue remodeling and fibrogenesis. Preclinical studies demonstrated its ability to reduce hepatocyte apoptosis and hepatic fibrogenesis in models of liver injury[1][5]. Clinical development was discontinued due to laboratory abnormalities and adverse events observed in some trial participants[3].

Other names

DB08490DB-08490DB 08490