"目录号: HY-14268
Febuxostat(TEI 6720;TMX 67 )是选择性黄嘌呤氧化酶（XO）抑制剂，Ki为0.6 nM。
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Allopurinol-Topiroxostat-Baicalein-Benzbromarone-Febuxostat D9-Phytic acid-
生物活性
Description
Febuxostat(TEI 6720;TMX 67 ) is selective xanthine oxidase inhibitor with Ki of 0.6 nM.IC50 value: 0.6 nM (Ki) [1]Target: xanthine oxidasein vitro: Febuxostat displays potent mixed-type inhibition of the activity of purified bovine milk xanthine oxidase, with Ki and Ki' values of 0.6 nM and 3.1 nM respectively, indicating inhibition of both the oxidized and reduced forms of xanthine oxidase [1]. in vivo: Febuxostat (5–6 mg/kg/day) combined with fructose significantly lowers blood pressure, UA, triglycerides, and insulin in rats compared with fructose alone. Febuxostat (5–6 mg/kg/day) combined with fructose also reduces glomerular pressure, renal vasoconstriction, and afferent arteriolar area in rats compared with fructose alone [2]. Febuxostat prevents hyperuricemia in 5/6 nephrectomy (5/6 Nx)+oxonic acid (OA)+Febuxostat(Fx) rats and ameliorates proteinuria, preserves renal function and prevents glomerular hypertension in both 5/6 nephrectomy (5/6 Nx)+vehicle (V)+Febuxostat(Fx) and 5/6 nephrectomy (5/6 Nx)+oxonic acid (OA)+Febuxostat(Fx) groups [3]. Febuxostat (5 mg/kg/d by gavage for 8 days) treatment after transverse aortic constriction (TAC) attenuates the TAC-induced left ventricular (LV) hypertrophy and dysfunction. Febuxostat blunts the TAC-induced increases in nitrotyrosine (indicating reduced myocardial oxidative stress), p-Erk(Thr202/Tyr204), and p-mTOR(Ser2488), with no effect on total Erk or total mTOR [4].
Clinical Trial
University of Mississippi Medical Center
Blood Pressure-Gout
January 2010
Takeda
Coronary Artery Disease
May 2013
Phase 4
University of Utah-Takeda
Chronic Kidney Disease-Diabetes
May 2011
Takeda
Joint Damage
March 2010
Phase 2
Takeda
Renal Impairment
April 2010
Phase 2
Nuon Therapeutics, Inc.
Gout-Hyperuricemia
September 2009
Phase 2
Takeda
Hypertension
February 2012
Phase 2
Takeda
Angina
July 2012
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Ardea Biosciences, Inc.
Healthy
June 2013
Phase 1
Takeda
Gout
February 2015
Phase 1
Freed Study Group-Teijin Pharma
Hyperuricemia
November 2013
Yokohama City University Medical Center
Coronary Artery Disease
October 2014
Phase 4
Menarini Group
Tumor Lysis Syndrome
October 2012
Phase 3
University of California, San Diego
Prehypertension-Gout-Pulse Wave Velocity-Hypertension-24 Hour Blood Pressure
October 2011
Phase 4
VA Office of Research and Development
Gout-Chronic Kidney Diseases
March 6, 2017
Phase 4
Takeda
Healthy Volunteers
August 2015
Phase 1
Jiangsu HengRui Medicine Co., Ltd.
Gout
February 17, 2017
Phase 1
Takeda
Gout
July 2002
Phase 3
Landspitali University Hospital-Mayo Clinic-National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK)
Adenine Phosphoribosyltransferase Deficiency
May 2013
Phase 4
Shanghai 10th People's Hospital
Chronic Kidney Disease-Hyperuricemia-Abnormal Renal Function
January 2015
Getz Pharma
Hyperuricemia
November 2013
Phase 4
Takeda-Teijin America, Inc.
Cardiovascular Disease
April 2010
Phase 3
Takeda
Gout
February 2003
Phase 3
Shanghai 10th People's Hospital
Chronic Kidney Disease-Hyperuricemia-Abnormal Renal Function
October 2016
Takeda
Gout
July 2003
Phase 3
Takeda
Hyperuricosuria-Kidney Stones
February 2010
Phase 2
AstraZeneca
Hyperuricemia-Albuminuria-Type 2 Diabetes
May 18, 2017
Phase 2
Xijing Hospital-Qingdao Shengbang Pharmaceutical Co., Ltd.
Gout
July 2011
Phase 3
Takeda
Gout
February 2007
Phase 3
Astellas Pharma Taiwan, Inc.-Astellas Pharma Inc
Gout
March 2011
Phase 3
Takeda
Healthy Volunteers
March 2015
Phase 1
Benha University-New Jeddah Clinic Hospital
Hyperuricemia-Hemodialysis Complication
January 1, 2017
Paul N. Hopkins-University of Utah
Hypertension
March 2011
Phase 4
Ain Shams University
Endothelial Dysfunction-Endstage Renal Disease
August 2016
Phase 2-Phase 3
Ardea Biosciences, Inc.
Gout
October 2014
Phase 2
CymaBay Therapeutics, Inc.
Hyperuricemia-Gout
August 2011
Phase 2
SK Chemicals Co.,Ltd.
Gout
August 2006
Phase 3
Takeda
Gout
April 2014
Phase 3
Takeda
Gout-Moderate Renal Impairment
May 2014
Phase 2
University Health Network, Toronto-Canadian Institutes of Health Research (CIHR)-Toronto General Hospital-University of Toronto
Type 1 Diabetes Mellitus
December 2012
Phase 4
CymaBay Therapeutics, Inc.
Gout-Hyperuricemia
August 2014
Phase 2
Sun Yat-sen University
Hyperuricemia
July 2017
Phase 4
Menarini International Operations Luxembourg SA
Gout
July 2015
Phase 4
Takeda
Gout
March 2001
Phase 2
Takeda
Gout
January 2001
Phase 2
Ardea Biosciences, Inc.
Tophaceous Gout
January 2012
Phase 3
AstraZeneca-Ardea Biosciences, Inc.
Gout and Asymptomatic Hyperuricemia
December 2014
Phase 1-Phase 2
University of Texas Southwestern Medical Center
Gout
May 2012
Phase 4
University of South Florida-Takeda Pharmaceuticals North America, Inc.
Gout
May 2010
Phase 4
Tongji Hospital
Primary Gout
January 2013
Phase 4
TWi Biotechnology, Inc.
Gout Flares
January 2013
Phase 2
TWi Biotechnology, Inc.
Gout
December 2014
