"目录号: HY-14664
Fluvastatin (Leschol)能抑制HMG-CoA还原酶活性，IC50为8 nM。
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生物活性
Description
Fluvastatin (Leschol) inhibits HMG-CoA reductase activity with IC50 of 8 nM.IC50 value: 8 nMTarget: HMG-CoA reductaseFluvastatin is a competitive inhibitor of hydroxymethylglutaryl-coenzyme A reductase (HMGCR), the enzyme that catalyzes the conversion of HMG-CoA to mevalonic acid, the rate-limiting step in cholesterol biosynthesis. Human hepatocellular carcinoma cell (HCC) studies indicate that Fluvastatin induces G2/M phase arrest. In the presence of Fluvastatin, HCC cells show a decrease of Bcl-2 and procaspase-9 expression, and an increase in Bax, cleaved caspase-3, and cytochrome c. Fluvastatin is antilipemic and is used to reduce plasma cholesterol levels and prevent cardiovascular disease.
Clinical Trial
Novartis
Metabolic Syndrome
September 2006
Phase 4
Novartis Pharmaceuticals-Novartis
Lipid Metabolism Disorders
January 2012
Phase 4
Hospital for Special Surgery, New York-University of Texas
Antiphospholipid Syndrome
May 2008
Phase 2
Irene Burger-University of Basel-University of Zurich
Adipose Tissue, Brown-Insulin Resistance-Clinical Trial
May 31, 2017
Phase 4
Corcept Therapeutics
Healthy Subjects
September 2008
Phase 1
Medical University of Graz
Hypercholesterolemia
September 2005
Phase 4
Novartis Pharmaceuticals-Novartis
Graft Vasculopathy
September 2001
Phase 4
University of Bologna
Heart Transplantation-Hypercholesterolemia
November 2004
Phase 4
Bader, Ted, M.D.-VA Office of Research and Development
Chronic Hepatitis C
June 2007
Phase 2
Beijing Anzhen Hospital-Novartis
Coronary Heart Disease-Atherosclerosis
July 2012
Phase 4
University of Chicago
Hepatitis C-Hepatitis C Virus
February 2010
Phase 2
Novartis
Metabolic Syndrome
October 2004
Phase 4
Bader, Ted, M.D.-VA Office of Research and Development
Hepatitis C
September 2006
Novartis
Dyslipidemia
August 2004
Phase 4
AORTICA Group
Aortic Valve Stenosis
October 2006
Phase 4
University of Schleswig-Holstein
Renal Transplantation
April 2003
Phase 2-Phase 3
Novartis
Mixed Dyslipidemia-Hypercholesterolemia
June 2005
Phase 3
Novartis-Ministry of Health, Czech Republic
Coronary Disease-Myocardial Infarction
November 2003
Phase 4
Novartis
Dyslipidemia
May 2005
Phase 4
Novartis
Hypertension-Dyslipidemia
July 2004
Phase 4
Novartis
Heterozygous Familial Hypercholesterolemia-Mixed Dyslipidemia
October 2001
Phase 3
University of California, San Francisco-National Cancer Institute (NCI)
Breast Cancer
July 2006
Phase 2
University Hospital Inselspital, Berne
Drug-Interactions
Phase 4
Novartis Pharmaceuticals-Novartis
Osteoporosis
June 2007
Phase 4
University Hospital, Saarland-Novartis
Impotence
October 2006
Phase 3
Novartis
Dyslipidemia
August 2003
Phase 3
University of Schleswig-Holstein
Renal Transplantation
April 2005
Phase 4
Novartis
Dyslipidemia
August 2006
Phase 4
Yokohama City University Medical Center
Coronary Disease-Hypercholesterolemia
October 2007
Phase 4
University Health Network, Toronto
Prostate Cancer
February 2014
Phase 2
University of Schleswig-Holstein
Renal Transplantation
May 2004
Phase 4
Centre Oscar Lambret-Reliable Cancer Therapies
Glioma
June 2014
Phase 1
Novartis
Hypertension, Dyslypidaemia
July 2005
Phase 4
Mario Negri Institute for Pharmacological Research
Chronic Nephropathy-Proteinuria-Hypertension
March 2003
Phase 3
University of Leipzig-Novartis
Aortic Valve Stenosis
January 2003
Phase 2
Martin-Luther-Universität Halle-Wittenberg-Novartis
Aging-Inflammation
October 2009
Phase 2
Kitasato University-Tokai University-Yokohama City University Medical Center-St. Marianna University School of Medicine
Type 2 Diabetes Mellitus-Hypertension
October 2006
Phase 4
Mario Negri Institute for Pharmacological Research
Alport Syndrome
January 2004
Phase 2
The Canadian College of Naturopathic Medicine-Canada Post Corporation-Canadian Union of Postal Workers
Cardiovascular Disease
April 2008
Phase 3
Canadian Network for Observational Drug Effect Studies, CNODES-Drug Safety and Effectiveness Network, Canada-Canadian Institutes of Health Research (CIHR)
Hypercholesterolemia
January 2011
Canadian Network for Observational Drug Effect Studies, CNODES-Drug Safety and Effectiveness Network, Canada-Canadian Institutes of Health Research (CIHR)
Diabetes Mellitus, Type 2-Cardiovascular Disease
July 2012
Merck Sharp & Dohme Corp.
Hypercholesterolemia
January 1, 2005
Phase 3
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