Background:

Camostat Mesylate(FOY305; FOY-S980) is a trypsin-like protease inhibitorTarget: Trypsin-like proteaseCamostat mesilate (500 mM) inhibits generation of TGF-beta by suppressing plasmin activity and reduces the activity of TGF-beta, which blocks in vitro activation of HSCs [1]. Camostat mesilate (20 mM) combined with insulin results a significant hypoglycemic effect following large intestinal administration. Camostat mesilate (20 mM) is effective in reducing insulin degradation in both small and large intestinal homogenates of rats [2]. Camostat mesilate (2 mM) inhibits MCP-1 and TNF- production in activated rat monocytes. Camostat mesilate (2 mM) inhibits proliferation and MCP-1 production of cultured rat PSCs. Camostat mesilate (1 mg/g) prevents pancreatic atrophy and improves pancreatic exocrine function of rat chronic pancreatitis induced by DBTC. Camostat mesilate (1 mg/g) inhibits chronic inflammation and pancreatic fibrosis induced by DBTC. Camostat mesilate (1 mg/g) inhibits the development of pancreatic fibrosis and PSCs activation in the pancreas induced by DBTC. Camostat mesilate (1 mg/g) suppresses monocytes infiltration and inhibits MCP-1 expression both in serum and in pancreatic tissue [3].

参考文献:
[1]. Okuno, M., et al., Prevention of rat hepatic fibrosis by the protease inhibitor, camostat mesilate, via reduced generation of active TGF-beta. Gastroenterology, 2001. 120(7): p. 1784-800.
[2]. Yamamoto, A., et al., Effects of various protease inhibitors on the intestinal absorption and degradation of insulin in rats. Pharm Res, 1994. 11(10): p. 1496-500.
[3]. Gibo, J., et al., Camostat mesilate attenuates pancreatic fibrosis via inhibition of monocytes and pancreatic stellate cells activity. Lab Invest, 2005. 85(1): p. 75-89.