Details
| Stereochemistry | ACHIRAL |
| Molecular Formula | C20H21N2O7S.Na.4H2O |
| Molecular Weight | 528.506 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
O.O.O.O.[Na+].CC(C)(C)C(=O)OC1=CC=C(C=C1)S(=O)(=O)NC2=C(C=CC=C2)C(=O)NCC([O-])=O
InChI
InChIKey=PLHREJBSQUSUCW-UHFFFAOYSA-M
InChI=1S/C20H22N2O7S.Na.4H2O/c1-20(2,3)19(26)29-13-8-10-14(11-9-13)30(27,28)22-16-7-5-4-6-15(16)18(25)21-12-17(23)24;;;;;/h4-11,22H,12H2,1-3H3,(H,21,25)(H,23,24);;4*1H2/q;+1;;;;/p-1
Sivelestat is a neutrophil elastase inhibitor approved in Japan and the Republic of Korea for acute lung injury, including acute respiratory distress syndrome in patients with systemic inflammatory response syndrome. Sivelestat is marketed as Elaspol in Japan. Sivelestat competitively inhibited human neutrophil elastase (IC50 = 0.044 uM, Ki = 0.2 uM). It also inhibited leukocyte elastase obtained from rabbit, rat, hamster and mouse.
Originator
Approval Year
PubMed
| Title | Date | PubMed |
|---|---|---|
| Relationship between neutrophil elastase and acute lung injury in humans. | 2004 |
|
| Neutrophil elastase inhibition in acute lung injury: results of the STRIVE study. | 2004 Aug |
|
| [Respiratory and cadiovascular management of septic ALI-ARDS and shock]. | 2004 Dec |
|
| Sivelestat, a specific neutrophil elastase inhibitor, prevented phorbol myristate acetate-induced acute lung injury in conscious rabbits. | 2005 |
|
| Protective effects of a selective neutrophil elastase inhibitor (sivelestat) on lipopolysaccharide-induced acute dysfunction of the pulmonary microcirculation. | 2005 Aug |
|
| Sivelestat, a neutrophil elastase inhibitor, attenuates neutrophil priming after hepatoenteric ischemia in rabbits. | 2005 Feb |
|
| Effects of sivelestat, a new elastase inhibitor, on IL-8 and MCP-1 production from stimulated human alveolar epithelial type II cells. | 2006 |
|
| Pretreatment of sivelestat sodium hydrate improves the lung microcirculation and alveolar damage in lipopolysaccharide-induced acute lung inflammation in hamsters. | 2006 Jul |
|
| A neutrophil elastase inhibitor, sivelestat, improves leukocyte deformability in patients with acute lung injury. | 2006 May |
|
| Sivelestat, a specific neutrophil elastase inhibitor, suppresses the growth of gastric carcinoma cells by preventing the release of transforming growth factor-alpha. | 2006 Oct |
|
| Neutrophil elastase inhibitor improves postoperative clinical courses after thoracic esophagectomy. | 2007 |
|
| Effects of sivelestat sodium hydrate on the reduction of radiation pneumonitis. | 2007 Dec |
|
| A neutrophil elastase inhibitor, sivelestat, ameliorates lung injury after hemorrhagic shock in rats. | 2007 Feb |
|
| Neutrophil elastase induces cell proliferation and migration by the release of TGF-alpha, PDGF and VEGF in esophageal cell lines. | 2007 Jan |
|
| [Outcome of patients with acute exacerbation of idiopathic interstitial fibrosis (IPF) treated with sivelestat and the prognostic value of serum KL-6 and surfactant protein D]. | 2007 Jun |
|
| Neutrophil elastase inhibitor prevents endotoxin-induced liver injury following experimental partial hepatectomy. | 2007 May |
|
| Addition of a neutrophil elastase inhibitor to the organ flushing solution decreases lung reperfusion injury in rat lung transplantation. | 2007 Nov |
|
| Effects of neutrophil elastase inhibitor on progression of acute lung injury following esophagectomy. | 2007 Oct |
|
| Neutrophil elastase inhibitor (sivelestat) attenuates subsequent ventilator-induced lung injury in mice. | 2007 Sep 24 |
|
| Neutrophil Proteases Activate Eosinophil Function in vitro. | 2008 |
|
| Continuous infusion of sivelestat sodium hydrate prevents lipopolysaccharide-induced intestinal paralysis and hypotension in conscious guinea-pigs. | 2008 Jul |
|
| Sivelestat and its role in tissue reperfusion injury. | 2008 Jun |
|
| Usefulness of a selective neutrophil elastase inhibitor (sivelestat) in septic ARDS patients after gastrointestinal surgery. | 2008 May-Jun |
|
| Sivelestat attenuates postoperative pulmonary dysfunction after total arch replacement under deep hypothermia. | 2008 Oct |
|
| Protective effect of sivelestat sodium (Eraspol) on postoperative lung dysfunction in patients with type A acute aortic dissection: a pilot study. | 2008 Oct |
|
| Sivelestat treatment for acute respiratory distress syndrome in an infant. | 2009 |
|
| Prevention of leukocyte activation by the neutrophil elastase inhibitor, sivelestat, in the hepatic microcirculation after ischemia-reperfusion. | 2009 Aug |
|
| Efficacy of neutrophil elastase inhibitor on type A acute aortic dissection. | 2010 Apr |
|
| Postischemic infusion of sivelestat sodium hydrate, a selective neutrophil elastase inhibitor, protects against myocardial stunning in swine. | 2010 Aug |
|
| Sivelestat (selective neutrophil elastase inhibitor) improves the mortality rate of sepsis associated with both acute respiratory distress syndrome and disseminated intravascular coagulation patients. | 2010 Jan |
|
| Neutrophil elastase inhibitor prevents ischemic brain damage via reduction of vasogenic edema. | 2010 Jul |
|
| Neutrophil elastase inhibitor improves survival of rats with clinically relevant sepsis. | 2010 May |
|
| Effect of a selective neutrophil elastase inhibitor on early recovery from body water imbalance after transthoracic esophagectomy. | 2010 Sep |
Patents
Sample Use Guides
0.2 mg/kg/hr continuous i.v. infusion - up to 14 days
Route of Administration:
Intravenous
Addition of 10 or 100 ug/ml sivelestat significantly (P < 0.05) inhibited the production of TNF-α from granulocytes induced by 10 ng/ml LPS. Granulocytic production of IL-8 induced by 1 ng/ml LPS was significantly (P < 0.05) inhibited by treatment with 1 ug/ml sivelestat, and upregulation of IL-8 by 10 ng/ml LPS was also significantly (P < 0.05) suppressed by 1 and 10 ug/ml sivelestat.
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NCI_THESAURUS |
C783
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m9966
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DTXSID0046727
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ACTIVE MOIETY
SUBSTANCE RECORD
