Details
| Stereochemistry | ACHIRAL |
| Molecular Formula | C20H22N4O5 |
| Molecular Weight | 398.4125 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
CN(C)C(=O)COC(=O)CC1=CC=C(OC(=O)C2=CC=C(NC(N)=N)C=C2)C=C1
InChI
InChIKey=XASIMHXSUQUHLV-UHFFFAOYSA-N
InChI=1S/C20H22N4O5/c1-24(2)17(25)12-28-18(26)11-13-3-9-16(10-4-13)29-19(27)14-5-7-15(8-6-14)23-20(21)22/h3-10H,11-12H2,1-2H3,(H4,21,22,23)
| Molecular Formula | C20H22N4O5 |
| Molecular Weight | 398.4125 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ACHIRAL |
| Additional Stereochemistry | |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Optical Activity | NONE |
Camostat mesilate (FOY-305) is a synthetic f low-molecular weight protease inhibitor. It is able to inhibit trypsin, prostasin, matriptase and plasma kallikrein. In addition camostat attenuates airway epithelial sodium channel function and enhances mucociliary clearance. Camostat mesilate tablets (FOIPAN®) are approved in Japan and used for the treatment of remission of acute symptoms of chronic pancreatitis and postoperative reflux esophagitis.
CNS Activity
Approval Year
PubMed
| Title | Date | PubMed |
|---|---|---|
| New orally active serine protease inhibitors. | 1995 Jul 7 |
|
| Acceleration of ulcer healing by cholecystokinin (CCK): role of CCK-A receptors, somatostatin, nitric oxide and sensory nerves. | 1999 Jun 30 |
|
| Preparation and characterization of biodegradable or enteric-coated microspheres containing the protease inhibitor camostat. | 2001 Feb |
|
| Different effects of oral administration of synthetic trypsin inhibitor on the pancreas between cholecystokinin-A receptor gene knockout mice and wild type mice. | 2002 Jul |
|
| Estimation of bioavailability of salmon calcitonin from the hypocalcemic effect in rats (II): effect of protease inhibitor on the pharmacokinetic-pharmacodynamic relationship after intranasal administration. | 2003 |
|
| CCK-58 is the only detectable endocrine form of cholecystokinin in rat. | 2003 Aug |
|
| Circulating ethanol does not stimulate pancreatic secretion in conscious rats. | 2003 Nov |
|
| Differential mechanism and site of action of CCK on the pancreatic secretion and growth in rats. | 2003 Oct |
|
| Calcineurin mediates pancreatic growth in protease inhibitor-treated mice. | 2004 May |
|
| Preventive and therapeutic effects of the protease inhibitor camostat on pancreatic fibrosis and atrophy in CCK-1 receptor-deficient rats. | 2005 Jan |
|
| Camostat, an oral trypsin inhibitor, reduces pancreatic fibrosis induced by repeated administration of a superoxide dismutase inhibitor in rats. | 2005 Jun |
|
| Synthetic protease inhibitor camostat prevents and reverses dyslipidemia, insulin secretory defects, and histological abnormalities of the pancreas in genetically obese and diabetic rats. | 2005 May |
|
| Calcineurin-dependent and calcineurin-independent signal transduction pathways activated as part of pancreatic growth. | 2006 Apr |
|
| [Effects of Chinese herbal medicines on spontaneous chronic pancreatitis in rats and the pathological relationships between formulas and syndromes]. | 2006 Jul |
|
| Activation of the mTOR signalling pathway is required for pancreatic growth in protease-inhibitor-fed mice. | 2006 Jun 15 |
|
| Effects of the cholecystokinin A receptor antagonist loxiglumide on the proliferation and cell cycle time of pancreatic acinar cells in rats. | 2006 Mar |
|
| Strategies of development of antiviral agents directed against influenza virus replication. | 2007 |
|
| Pancreatic diabetes in a follow-up survey of chronic pancreatitis in Japan. | 2007 Apr |
|
| [Fibrosis markers in heavy alcohol drinkers]. | 2007 Aug |
|
| Induction of early response genes in trypsin inhibitor-induced pancreatic growth. | 2007 Feb |
|
| Endogenous cholecystokinin reduces food intake and increases Fos-like immunoreactivity in the dorsal vagal complex but not in the myenteric plexus by CCK1 receptor in the adult rat. | 2007 Mar |
|
| Matrix metalloproteinase gene delivery for liver fibrosis. | 2008 Feb |
|
| CCK-induced pancreatic growth is not limited by mitogenic capacity in mice. | 2008 May |
|
| Activation of submucosal but not myenteric plexus of the gastrointestinal tract accompanies reduction of food intake by camostat. | 2008 Oct 9 |
|
| Active site conformational changes of prostasin provide a new mechanism of protease regulation by divalent cations. | 2009 May |
|
| Camostat attenuates airway epithelial sodium channel function in vivo through the inhibition of a channel-activating protease. | 2009 May |
|
| ONO 3403, a synthetic serine protease inhibitor, inhibits lipopolysaccharide-induced tumor necrosis factor-{alpha} and nitric oxide production and protects mice from lethal endotoxic shock. | 2011 Feb |
|
| Reduced sodium transport with nasal administration of the prostasin inhibitor camostat in subjects with cystic fibrosis. | 2013 Jul |
Sample Use Guides
1. Remission of acute symptoms of chronic pancreatitis. The usual dosage for oral use is 600 mg of camostat mesilate daily in three divided doses. The dosage may be adjusted according to the patient’s symptoms. 2. Postoperative reflux esophagitis. The usual dosage for oral use is 300 mg of camostat mesilate daily in three divided doses after each meal.
Route of Administration:
Oral
| Substance Class |
Chemical
Created
by
admin
on
Edited
Tue Oct 22 05:42:43 UTC 2019
by
admin
on
Tue Oct 22 05:42:43 UTC 2019
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| Record UNII |
0FD207WKDU
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| Record Status |
Validated (UNII)
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| Record Version |
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Official Name | English | ||
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Common Name | English | ||
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Common Name | English | ||
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| Classification Tree | Code System | Code | ||
|---|---|---|---|---|
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WHO-VATC |
QB02AB04
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WHO-ATC |
B02AB04
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NCI_THESAURUS |
C783
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admin on Tue Oct 22 05:42:43 UTC 2019 , Edited by admin on Tue Oct 22 05:42:43 UTC 2019
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FDA ORPHAN DRUG |
338211
Created by
admin on Tue Oct 22 05:42:43 UTC 2019 , Edited by admin on Tue Oct 22 05:42:43 UTC 2019
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C73213
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5068
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6432
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SALT/SOLVATE -> PARENT |
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ACTIVE MOIETY |
