freselestat

Freselestat is a reversible, nonpeptide small molecule inhibitor of human neutrophil elastase. It was developed by Ono Pharmaceutical for the potential treatment of inflammatory conditions such as chronic obstructive pulmonary disease (COPD), acute lung injury (ALI), systemic inflammatory response syndrome (SIRS), rheumatoid arthritis, and inflammatory bowel disease. Freselestat selectively inhibits neutrophil elastase activity without affecting other proteases like pancreatic elastase or trypsin. By inhibiting neutrophil elastase, it reduces interleukin 8 production and the formation of the complement membrane attack complex (C5b-9), thereby decreasing inflammation and tissue damage during conditions such as simulated extracorporeal circulation or acute lung injury. Despite promising preclinical results in reducing lung hemorrhage and neutrophil accumulation in animal models, clinical development was terminated due to abnormal variations in liver function observed during trials[1][3][5][6].

Other names

freselestat [INN]ono-6818ono6818ono 6818208848-19-5