Camostat mesilate

Camostat mesylate is a broad spectrum protease inhibitor useful in the treatment of chronic pancreatitis.

Crystalline Solid

Ono (Japan)

Orally active, non-peptide proteolitic enzyme inhibitor with anti-trypsin and anti-plasmin activities, related structurally to gabexate. Protease inhibitor

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.

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+).

FOIPAN

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.

Desiccate at RT

Camostat Mesylate, also known as Foipan or FOY 305, is a synthetic serine protease inhibitor that is often used to treat pancreatitis pain. Camostat Mesylate attenuates airway epithelial sodium channel function by inhibiting channel-activating proteases with an IC50 of 50 nM. Camostat Mesylate inhibition of trypsin decreased food intake, body weight, blood glucose, liver weight, and lipidosis and increased FGF21 expression in obese mice.Camostat Mesylate is an effective inhibitor of TMPRSS2, a serine protease used by SARS-CoV-2/COVID-19 for viral S-protein priming and cell entry. Pre-treatment of human lung cancer cells with 100 μM Camostat Mesylate significantly reduced COVID-19 viral entry.

[1] JUNYA GIBO. Camostat mesilate attenuates pancreatic fibrosis via inhibition of monocytes and pancreatic stellate cells activity[J]. Laboratory Investigation, 2004, 85 1: 75-89. DOI:10.1038/labinvest.3700203
[2] KAMAL ALBARAZANJI. Intestinal serine protease inhibition increases FGF21 and improves metabolism in obese mice.[J]. American journal of physiology. Gastrointestinal and liver physiology, 2019, 316 5: G653-G667. DOI:10.1152/ajpgi.00404.2018
[3] MIKI UEDA. The serine protease inhibitor camostat mesilate attenuates the progression of chronic kidney disease through its antioxidant effects.[J]. Nephron, 2015, 129 3: 223-232. DOI:10.1159/000375308
[4] MUTSUO YAMAYA . The serine protease inhibitor camostat inhibits influenza virus replication and cytokine production in primary cultures of human tracheal epithelial cells[J]. Pulmonary pharmacology & therapeutics, 2015, 33: Pages 66-74. DOI:10.1016/j.pupt.2015.07.001
[5] MARKUS HOFFMANN. SARS-CoV-2 Cell Entry Depends on ACE2 and TMPRSS2 and Is Blocked by a Clinically Proven Protease Inhibitor.[J]. Cell, 2020: 271-280.e8. DOI:10.1016/j.cell.2020.02.052