Sivelestat is an inhibitor of neutrophil elastase that exhibits cardioprotective, anti-inflammatory, and anticancer activities. In vitro, sivelestat decreases superoxide dismutase (SOD) adduct formation and in vivo, it decreases SOD levels, resulting in a decrease in myocardial infarction size and improvement in left ventricular contractility. In other cellular models, sivelestat decreases induction of iNOS and production of NO and also prevents activation of NF-κB and expression of the IL-1 receptor. Sivelestat inhibits contraction of tracheal and bronchial rings, decreasing airway hyperresponsiveness. Additionally, this compound inhibits release of TGF-α, PDGF-AA, PDGF-BB, and VEGF in esophageal carcinoma cells, inhibiting cell invasion and proliferation.