Zileuton是一种口服有效的5-脂氧合酶抑制剂,因而可抑制白三烯(LTB 4,LTC 4,LTD 4和LTE 4)的形成。
Zileuton is an orally active inhibitor of 5-lipoxygenase, and thus inhibits leukotrienes (LTB4, LTC4, LTD4, and LTE4) formation, used to decrease the symptoms of asthma.
动物 A (mg/kg) = 动物 B (mg/kg)×动物 B的Km系数/动物 A的Km系数 | |
例如,已知某工具药用于小鼠的剂量为88 mg/kg , 则用于大鼠的剂量换算方法:将88 mg/kg 乘以小鼠的Km系数(3),再除以大鼠的Km系数(6),得到该药物用于大鼠的等效剂量44 mg/kg。
[1] Rossi A1, et al. Br J Pharmacol, 2010, 161(3), 555-570.
[2] McMillan et al (1992) Pre-clinical pharmacology of ICI D2138, a potent orally-active non-redox inhibitor of 5-lipoxygenase. Br.J.Pharmacol. 107 1042.
[3] Malo et al (1994) The 5-lipoxygenase inhibitory activity of zileuton in in vitro and in vivo models of antigen-induced airway anaphylaxis. Pulm.Pharmacol. 7 73.
[4] Lu et al (2003) Mechanism-based inhibition of human liver microsomal cytochrome P450 1A2 by zileuton, a 5-lipoxygenase inhibitor. Drug Metab.Dispos. 31 1352.
分子式 C11H12N2O2S |
分子量 236.29 |
CAS号 111406-87-2 |
储存方式 ﹣20 ℃冷藏长期储存。冰袋运输 |
溶剂(常温) |
DMSO 47 mg/mL |
Water <1 mg/mL |
Ethanol 47 mg/mL |
体内溶解度
NCT Number | Conditions | Interventions | Sponsor/Collaborators | Phases | Start Date | Last Updated |
NCT01136941 | Sickle Cell Disease | Drug: Zileuton | Children's Hospital Medical Center, Cincinnati | Phase 1 | 2010-09-01 | 2014-06-17 |
NCT01130688 | Chronic Myelogenous Leukemia | Drug: Zileuton | University of Massachusetts, Worcester | Phase 1 | 2010-01-01 | 2015-05-26 |
NCT02047149 | Chronic Myelogenous Leukemia | Drug: Zileuton (Zyflo庐) Dasatinib (Sprycel庐)|Drug: Dosing with Zileuton/Dasatinib in CML|Drug: Daily dosing of Zileuton/Dasatinib|Drug: Daily dosing with Zileuton/Dasatinib for CML | University of Massachusetts, Worcester|Bristol-Myers Squibb | Phase 1 | 2014-01-01 | 2016-09-29 |
NCT00575861 | Asthma | Drug: zileuton | Gelb, Arthur F., M.D. | Phase 4 | 2005-09-01 | 2007-12-18 |
NCT00486343 | Asthma | Drug: Zileuton CR|Drug: Placebo | Critical Therapeutics | Phase 4 | 2007-07-01 | 2008-04-01 |
NCT02348203 | Pulmonary Nodules|Tobacco Use Disorder | Drug: Aspirin|Other: Laboratory Biomarker Analysis|Other: Placebo|Other: Placebo|Drug: Zileuton | National Cancer Institute (NCI) | Phase 2 | 2016-01-01 | 2017-01-31 |
NCT00262405 | Idiopathic Pulmonary Fibrosis | Drug: zileuton|Drug: azathioprine/prednisone | University of Michigan|National Institutes of Health (NIH) | Phase 2 | 2001-01-01 | 2015-12-02 |
NCT00534625 | Asthma | Drug: zileuton|Drug: placebo|Drug: zileuton | Critical Therapeutics | Phase 2 | 2007-09-01 | 2008-03-19 |
NCT00493974 | Pulmonary Disease, Chronic Obstructive | Drug: Zileuton|Drug: Placebo | University of Minnesota - Clinical and Translational Science Institute|National Heart, Lung, and Blood Institute (NHLBI) | Phase 3 | 2007-03-01 | 2016-08-24 |
NCT00056004 | Head and Neck Cancer|Lung Cancer | Drug: zileuton | Barbara Ann Karmanos Cancer Institute|National Cancer Institute (NCI) | Phase 2 | 2003-06-01 | 2013-04-25 |
NCT01021215 | Tobacco Use Disorder | Drug: Zileuton|Drug: Celecoxib|Other: laboratory biomarker analysis | National Cancer Institute (NCI) | Phase 1|Phase 2 | 2010-05-01 | 2015-04-01 |
NCT00098358 | Acne Vulgaris | Drug: Zileuton | Critical Therapeutics | Phase 2 | 2004-11-01 | 2007-02-05 |
NCT00299065 | Asthma | Drug: Zileuton injection | Critical Therapeutics | Phase 1|Phase 2 | 2006-01-01 | 2007-09-24 |
NCT01805687 | Asthma | Drug: Zileuton extended release | Cornerstone Therapeutics Inc. | Phase 4 | 2013-03-01 | 2014-08-22 |
NCT00070486 | Lung Cancer | Drug: carboplatin|Drug: celecoxib|Drug: gemcitabine hydrochloride|Drug: zileuton | Alliance for Clinical Trials in Oncology|National Cancer Institute (NCI) | Phase 2 | 2003-12-01 | 2016-06-28 |
NCT01174056 | Lung Inflammation | Drug: Zileuton|Drug: Pioglitazone placebo|Drug: Zileuton placebo|Drug: Pioglitazone | Washington University School of Medicine|Doris Duke Charitable Foundation | Early Phase 1 | 2011-07-01 | 2014-04-22 |
NCT00467831 | Hermansky-Pudlak Syndrome (HPS)|Pulmonary Fibrosis|Oculocutaneous Albinism|Platelet Storage Pool Deficiency|Metabolic Disease | Drug: Losartan|Drug: Zileuton|Drug: N-Acetylcysteine|Drug: Pravastatin|Drug: Erythromycin | National Human Genome Research Institute (NHGRI)|National Institutes of Health Clinical Center (CC) | Phase 1|Phase 2 | 2007-04-01 | 2013-06-03 |
NCT00723021 | Asthma | Drug: PF-04191834|Drug: PF-04191834|Drug: PF-04191834|Drug: zileuton|Drug: Placebo | Pfizer | Phase 2 | 2008-07-01 | 2012-12-27 |
NCT01125748 | Allergic Asthma | Drug: Omalizumab|Drug: Placebo|Drug: Asthma therapies | Genentech, Inc. | Phase 4 | 2010-05-01 | 2014-10-08 |
NCT00595114 | Asthma|Pulmonary Disease, Chronic Obstructive | Brigham and Women's Hospital|National Heart, Lung, and Blood Institute (NHLBI) | Early Phase 1 | 2007-12-01 | 2016-09-04 |
注:以上所有数据均来自公开文献,并不保证对所有实验均有效,数据仅供参考。
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