Camostat (mesylate)

Camostat is a protease inhibitor.^1,2 It inhibits trypsin (K_i = 1 nM), as well as various inflammatory proteases, including plasmin, kallikrein, and thrombin. Camostat (50 µM) inhibits entry of vesicular stomatitis virus (VSV) particles pseudotyped with severe acute respiratory syndrome coronavirus (SARS-CoV) and SARS-CoV-2 spike glycoprotein in Calu-3 cells and primary human lung epithelial cells.³ It reduces the number of SARS-CoV-2 genomic equivalents, a marker of infection, in Calu-3 cells. Camostat inhibits sodium channel function in human airway epithelial cells (IC₅₀ = 50 nM) and enhances mucociliary clearance in sheep.⁴ Dietary administration of camostat (1 mg/kg) inhibits the production of TNF-α and chemokine (C-C motif) ligand 2 (CCL2) by monocytes, as well as proliferation of pancreatic stellate cells in a rat model of pancreatic fibrosis.²

WARNING This product is not for human or veterinary use.

1. Coote, K., Atherton-Watson, H.C., Sugar, R., et al. Camostat attenuates airway epithelial sodium channel function in vivo through the inhibition of a channel-activating protease. J. Pharmacol. Exp. Ther. 329(2), 764-774 (2009).

2. Gibo, J., Ito, T., Kawabe, K., et al. Camostat mesilate attenuates pancreatic fibrosis via inhibition of monocytes and pancreatic stellate cells activity. Lab Invest. 85(1), 75-89 (2005).

3. Hoffmann, M., Kleine-Weber, H., Schroeder, S., et al. SARS-CoV-2 cell entry depends on ACE2 and TMPRSS2 and is blocked by a clinically proven protease inhibitor. Cell 181(2), 271-280 (2020).

4. Maianti, J.P., McFedries, A., Foda, Z.H., et al. Anti-diabetic activity of insulin-degrading enzyme inhibitors mediated by multiple hormones. Nature 511(7507), 94-98 (2014).

Barile, E., Baggio, C., Gambini, L., et al. Potential therapeutic targeting of coronavirus spike glycoprotein priming. Molecules 25(10), E2424 (2020).