Catalog No.S7218 Synonyms: Avelestat
Molecular Weight(MW): 545.53
Alvelestat (AZD9668) is an oral, highly selective inhibitor of neutrophil elastase (NE) with IC50 and Ki of 12 nM and 9.4 nM, at least 600-fold more selective over other serine proteases. Phase 2.
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Choose Selective Serine Protease Inhibitors
|Description||Alvelestat (AZD9668) is an oral, highly selective inhibitor of neutrophil elastase (NE) with IC50 and Ki of 12 nM and 9.4 nM, at least 600-fold more selective over other serine proteases. Phase 2.|
AZD9668 inhibits plasma NE activity in zymosan-stimulated whole blood, and also inhibits NE activity on the surface of stimulated polymorphonuclear cells and in the supernatant of primed, stimulated cells. 
|In vivo||In mice and rats, AZD9668 (p.o.) prevents human NE-induced lung injury. In a mouse model of smoke-induced airway inflammation, AZD9668 significantly reduces the number of BAL neutrophils and BAL IL-1β. In a guinea pig chronic smoke model, AZD9668 prevents airspace enlargement and small airway wall remodeling in guinea pigs in response to chronic tobacco smoke exposure. |
|In vitro||DMSO||100 mg/mL (183.3 mM)|
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Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT02669251||Recruiting||Drug: MPH966||Chronic Graft vs Host Disease|Chronic Graft-Versus-Host-Disease|Bronchiolitis Obliterans Syndrome||National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC)||April 28 2016||Phase 1|Phase 2|
|NCT01214122||Withdrawn||Drug: AZD9668|Drug: Warfarin||Pharmacokinetics|Pharmacodynamics||AstraZeneca||November 2010||Phase 1|
|NCT01161355||Completed||Drug: AZD9668||Healthy||AstraZeneca||June 2010||Phase 1|
|NCT01147549||Completed||Drug: [C14]AZD9668||Healthy||AstraZeneca||June 2010||Phase 1|
|NCT01035411||Completed||Drug: AZD9668||Chronic Obstructive Pulmonary Disease||AstraZeneca||November 2009||Phase 1|
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