Febuxostat是选择性黄嘌呤氧化酶(XO)抑制剂,Ki为0.6 nM。
Febuxostat is a selective xanthine oxidase inhibitor with Ki of 0.6 nM.
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] Takano Y, et al. Life Sci, 2005, 76(16), 1835-1847.
[2] Johji Nomura et. Al. PLoS ONE, 8(9), e75527 (2013)
分子式 C16H16N2O3S |
分子量 316.37 |
CAS号 144060-53-7 |
储存方式 ﹣20 ℃冷藏长期储存。冰袋运输 |
溶剂(常温) |
DMSO 60 mg/mL |
Water <1 mg/mL |
Ethanol <1 mg/mL |
体内溶解度
NCT Number | Conditions | Interventions | Sponsor/Collaborators | Phases | Start Date | Last Updated |
NCT01701622 | Blood Pressure|Gout | Drug: febuxostat | University of Mississippi Medical Center | 2010-01-01 | 2013-02-08 | |
NCT01763996 | Coronary Artery Disease | Drug: Febuxostat|Drug: Febuxostat placebo | Takeda | Phase 4 | 2013-05-01 | 2016-03-10 |
NCT01350388 | Chronic Kidney Disease|Diabetes | Drug: Febuxostat|Drug: Placebo | University of Utah|Takeda | 2011-05-01 | 2016-08-09 | |
NCT01078389 | Joint Damage | Drug: Febuxostat|Drug: Placebo for Febuxostat | Takeda | Phase 2 | 2010-03-01 | 2014-09-03 |
NCT01082640 | Renal Impairment | Drug: Febuxostat|Drug: Placebo | Takeda | Phase 2 | 2010-04-01 | 2013-09-23 |
NCT00995618 | Gout|Hyperuricemia | Drug: Tranilast|Drug: Febuxostat|Drug: Combination - Tranilast and Febuxostat | Nuon Therapeutics, Inc. | Phase 2 | 2009-09-01 | 2011-01-05 |
NCT01496469 | Hypertension | Drug: Febuxostat|Drug: Placebo | Takeda | Phase 2 | 2012-02-01 | 2015-07-31 |
NCT01549977 | Angina | Drug: Febuxostat|Drug: Placebo | Takeda | Phase 2 | 2012-07-01 | 2013-10-30 |
NCT01883167 | Healthy | Drug: RDEA3170 10 mg|Drug: Febuxostat 40 mg|Drug: placebo | Ardea Biosciences, Inc. | Phase 1 | 2013-06-01 | 2014-01-08 |
NCT02374164 | Gout | Drug: Febuxostat XR | Takeda | Phase 1 | 2015-02-01 | 2016-03-25 |
NCT01984749 | Hyperuricemia | Drug: Febuxostat | Freed Study Group|Teijin Pharma | 2013-11-01 | 2016-08-25 | |
NCT02279342 | Coronary Artery Disease | Drug: Febuxostat | Yokohama City University Medical Center | Phase 4 | 2014-10-01 | 2014-10-30 |
NCT01724528 | Tumor Lysis Syndrome | Drug: Febuxostat|Drug: Allopurinol | Menarini Group | Phase 3 | 2012-10-01 | 2014-10-27 |
NCT01472692 | Prehypertension|Gout|Pulse Wave Velocity|Hypertension|24 Hour Blood Pressure | Drug: Febuxostat | University of California, San Diego | Phase 4 | 2011-10-01 | 2014-03-31 |
NCT02579096 | Gout|Chronic Kidney Diseases | Drug: Allopurinol|Drug: Febuxostat|Drug: Placebo, vehicle control (Febuxostat-shaped)|Drug: Placebo, vehicle control (Allopurinol-shaped) | VA Office of Research and Development | Phase 4 | 2017-03-06 | 2017-03-24 |
NCT02504320 | Healthy Volunteers | Drug: Febuxostat XR 80 mg Capsule F1|Drug: Febuxostat XR 80 mg Capsule F2|Drug: Febuxostat XR 80 mg Capsule F3|Drug: Febuxostat XR 80 mg Capsule F4 | Takeda | Phase 1 | 2015-08-01 | 2016-11-25 |
NCT00102440 | Gout | Drug: Febuxostat|Drug: Febuxostat|Drug: Allopurinol | Takeda | Phase 3 | 2002-07-01 | 2012-01-31 |
NCT02752633 | Adenine Phosphoribosyltransferase Deficiency | Drug: Allopurinol|Drug: Febuxostat | Landspitali University Hospital|Mayo Clinic|National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK) | Phase 4 | 2013-05-01 | 2016-04-22 |
NCT02600780 | Hyperuricemia | Drug: Febuxostat|Drug: Allopurinol | Getz Pharma | Phase 4 | 2013-11-01 | 2015-11-06 |
NCT02338323 | Chronic Kidney Disease|Hyperuricemia|Abnormal Renal Function | Drug: Febuxostat|Drug: Benzbromarone | Shanghai 10th People's Hospital | 2015-01-01 | 2016-05-05 | |
NCT01101035 | Cardiovascular Disease | Drug: Febuxostat|Drug: Allopurinol | Takeda|Teijin America, Inc. | Phase 3 | 2010-04-01 | 2016-08-17 |
NCT00174915 | Gout | Drug: Febuxostat|Drug: Febuxostat|Drug: Febuxostat|Drug: Allopurinol|Drug: Placebo | Takeda | Phase 3 | 2003-02-01 | 2012-01-31 |
NCT02944214 | Chronic Kidney Disease|Hyperuricemia|Abnormal Renal Function | Drug: Febuxostat|Drug: Benzbromarone | Shanghai 10th People's Hospital | 2016-10-01 | 2016-10-24 | |
NCT00175019 | Gout | Drug: Febuxostat|Drug: Febuxostat|Drug: Allopurinol | Takeda | Phase 3 | 2003-07-01 | 2010-07-22 |
NCT01077284 | Hyperuricosuria|Kidney Stones | Drug: Febuxostat|Drug: Allopurinol|Drug: Placebo | Takeda | Phase 2 | 2010-02-01 | 2013-01-14 |
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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