Camostat mesilate | Serine protease inhibitor/antiviral/anti-inflammatory

Camostat mesilate (59721-29-8) is a serine protease inhibitor inhibiting plasmin, kallikrein, thrombin as well as trypsin, which attenuates pancreatic fibrosis.¹ Reduces weight gain and improves metabolism in obese rodent models.² In clinical use (in Japan) for pancreatitis.³ Inhibits influenza virus replication in human tracheal epithelial cells.⁴ Reduces infection of Calu-3 lung cells by SARS-CoV-2 (responsible for COVID-19) via inhibition of the serine protease TMPRSS2 required for viral spike protein priming.⁵

References/Citations:

1) Gibo et al. (2005), Camostat mesylate attenuates pancreatic fibrosis via inhibition of monocytes and pancreatic stellate cells activity; Lab Invest., 85 75
2) Albarazanji et al. (2019), Intestinal serine protease inhibition increases FGF21 and improves metabolism in obese mice.; Am. J. Physiol. Gastrointest. Liver Physiol., 316 G653
3) Ueda et al. (2015), The serine protease inhibitor camostat mesylate attenuates the progression of chronic kidney disease through its antioxidant effects; Nephron, 129 223
4) Yamaya et al. (2015), The serine protease inhibitor camostat inhibits influenza virus replication and cytokine production in primary cultures of human tracheal epithelial cells; Pulm. Pharmacol. Ther., 33 66
5) Hoffmann et al. (2020), SARS-CoV-2 Cell Entry Depends on ACE2 and TMPRSS2 and Is Blocked by a Clinically Proven Protease Inhibitor; Cell, 181 271