Description
Camostat mesylate is a broad spectrum protease inhibitor useful in the treatment
of chronic pancreatitis.
Chemical Properties
Crystalline Solid
Uses
Orally active, non-peptide proteolitic enzyme inhibitor with anti-trypsin and anti-plasmin activities, related structurally to gabexate. Protease inhibitor
Uses
It is used as a protease and Trypsin inhibitor. Furthermore it was found that this water induction and bicarbonate secretion increase was achieved via direct regulation of ductular cells of the dog pancreas. Other studies have shown Camostat mesylate to suppress spinal Fos expression in the rat, which is a marker for neuronal activation. In addition it was shown that this compound may prevent or depress pancreatitis-induced referred allodynia/hyperalgesia in rat models. Camostat mesylate has also demonstrated the ability to prevent Trypsin attack of microspheres, which causes the degradation product N-benzoyl-dl-arginine. Camostat mesylate is an inhibitor of KLK, plasminogen, Prothrombin and Trypsin.
Definition
ChEBI: Camostat mesylate is a methanesulfonate (mesylate) salt prepared from equimolar amounts of camostat and methanesulfonic acid. It is a serine protease inhibitor approved and marketed in Japan in 1985 for the alleviation of acute symptoms associated with chronic pancreatitis. In 1994, it was approved for the treatment of postoperative reflux esophagitis. It has a role as an anticoronaviral agent, an anti-inflammatory agent, an antifibrinolytic drug, an antihypertensive agent, an antineoplastic agent, an antiviral agent and a serine protease inhibitor. It contains a camostat(1+).
Biological Activity
Orally active protease inhibitor. Known to inhibit trypsin and various inflammatory proteases including plasmin, kallikrein and thrombin. Suppresses pancreatitis-induced pain in rats following oral administration.
References
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
