Nafamostat mesylate is a synthetic serine protease inhibitor, which inhibits various enzyme systems such as coagulation and fibrinolytic systems, the kallikrein–kinin system, the complement system, and the activation of protease-activated receptors. It also inhibits lipopolysaccharide-induced nitric oxide production, apoptosis, and interleukin (IL)-6 and IL-8 levels in cultured human trophoblasts. Moreover, it has been shown to act as an antioxidant in TNF-a-induced ROS production. It is sometimes used for the treatment of disseminated intravascular coagulation (DIC) and acute respiratory distress syndrome (ARDS), and it was usually used as an anticoagulant in extracorporeal circulation such as continuous renal replacement therapy (CRRT) of patients with chronic renal failure in Asian countries.
Recently, Nafamostat mesylate as a serine protease inhibitor prevents the fusion of the envelope of the SARS-CoV-2 with host cell surface membranes by inhibiting transmembrane serine protease 2(TMPRSS2), a human cell surface serine protease. Nafamostat mesylate might have a potential antiviral activity.
Here we review recent studies that showed possible roles of Nafamostat mesylate in COVID-19. The therapeutic potential of Nafamostat mesylate in relation to the pathogenesis of COVID-19 are also discussed. It is thought that these findings could provide a basis for the use of Nafamostat mesylate as a potential therapeutic for COVID-19 in human in the situation with no definite treatment for COVID-19 established.
Nafamostat mesylate, COVID-19, SARS-CoV-2, Anti-inflammation, Anticoagulation, Antiviral effect