"目录号: HY-14164A
Zileuton sodium 是一种有效的，选择性的5-lipoxygenase抑制剂，具有抗炎的作用。
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U-73122-Zileuton-ML355-Enazadrem-LY 178002-Malotilate-RWJ 63556-S-2474-CMI-392-CMI977-PGS-IN-1-RS4317-S-(+)-Marmesin-U66858-
生物活性
Description
Zileuton sodium is a potent and selective inhibitor of5-lipoxygenase, exhibiting inflammatory activities.
In Vitro
In anti-CD3-treated cells, IL-2 decreases in zileuton-treated and untreated cells with increasing incubation time. Zileuton likely reduces IL-2 levels by inhibiting 5-lipoxygenase, hence leukotriene B4 production, an IL-2 inducer[2].
In Vivo
In zileuton (5 mg/kg, p.o.) treated I/R rat, the effect of zileuton to decrease NF-κB expression does not change significantly in the presence of COX inhibitors, and the group reveals significantly lower level of NF-κB staining. Zileuton (5 mg/kg, p.o.) treatment given to I/R rats decreases apoptotic index significantly. Zileuton has no significant effect on increased serum TNF-α levels in I/R group[1]. Zileuton (1200 mg/kg) inhibits the polyp formation in APCΔ468colon and small intestine. Zileuton treatment inhibits the proliferation rates of non epithelial cells in polyps, and increases the apoptosis rates in polyps in rat. There is significant increase in the number of apoptotic cells in the Zileuton-treated cells both in small intestine and in the colon. The reduced proliferation rate may significantly contribute to the reduction of polyposis in both the small intestine and colon of Zileuton-fed APCΔ468mice[3].
Clinical Trial
Children's Hospital Medical Center, Cincinnati
Sickle Cell Disease
September 2010
Phase 1
University of Massachusetts, Worcester
Chronic Myelogenous Leukemia
January 2010
Phase 1
University of Massachusetts, Worcester-Bristol-Myers Squibb
Chronic Myelogenous Leukemia
January 2014
Phase 1
Gelb, Arthur F., M.D.
Asthma
September 2005
Phase 4
Critical Therapeutics
Asthma
July 2007
Phase 4
National Cancer Institute (NCI)
Pulmonary Nodules-Tobacco Use Disorder
January 13, 2016
Phase 2
University of Michigan-National Institutes of Health (NIH)
Idiopathic Pulmonary Fibrosis
January 2001
Phase 2
Critical Therapeutics
Asthma
September 2007
Phase 2
University of Minnesota - Clinical and Translational Science Institute-National Heart, Lung, and Blood Institute (NHLBI)
Pulmonary Disease, Chronic Obstructive
March 2007
Phase 3
Barbara Ann Karmanos Cancer Institute-National Cancer Institute (NCI)
Head and Neck Cancer-Lung Cancer
June 2003
Phase 2
National Cancer Institute (NCI)
Tobacco Use Disorder
May 2010
Phase 1-Phase 2
Critical Therapeutics
Acne Vulgaris
November 2004
Phase 2
Critical Therapeutics
Asthma
January 2006
Phase 1-Phase 2
Cornerstone Therapeutics Inc.
Asthma
March 2013
Phase 4
Alliance for Clinical Trials in Oncology-National Cancer Institute (NCI)
Lung Cancer
December 2003
Phase 2
Washington University School of Medicine-Doris Duke Charitable Foundation
Lung Inflammation
July 2011
Early Phase 1
National Human Genome Research Institute (NHGRI)-National Institutes of Health Clinical Center (CC)
Hermansky-Pudlak Syndrome (HPS)-Pulmonary Fibrosis-Oculocutaneous Albinism-Platelet Storage Pool Deficiency-Metabolic Disease
April 2007
Phase 1-Phase 2
Pfizer
Asthma
July 2008
Phase 2
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