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Fenofibrate

Fenofibrate

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商品描述
Fenofibrate,HY-17356,MCE:
Description

Fenofibrate is a PPARα agonist with an EC50 of 30 μM.

IC50 & Target

CYP2C19

0.2 μM (IC50)

CYP2B6

0.7 μM (IC50)

CYP2C9

9.7 μM (IC50)

CYP2C8

4.8 μM (IC50)

CYP3A4

142.1 μM (IC50)

PPARα

30 μM (IC50)

In Vitro

Fenofibrate is a relatively potent inhibitor of CYP2B6 (IC50=0.7±0.2 μM) and CYP2C19 (IC50=0.2±0.1 μM). Fenofibrate is also a moderate inhibitor of CYP2C8 (IC50=4.8±1.7 μM) and CYP2C9 (IC50=9.7 μM). Fenofibrate binds to and inhibits cytochrome P450 epoxygenase (CYP)2C with higher affinity than to PPARα. Fenofibrate is a well-known PPARα agonist, but an in vitro assessment of 209 frequently prescribed drugs and related xenobiotics suggests that Fenofibrate is also a potent inhibitor of cytochrome P450 epoxygenase (CYP)2C. The affinity of Fenofibrate to CYP2C is >10 times higher (EC50=2.39±0.4 μM) than to PPARα (EC50=30 μM). Fenofibrate at a low dose inhibits CYP2C8 activity without PPARα activation.

In Vivo

Daily intake of Fenofibrate at this low dose (10 μg/g/day) inhibits retinal and choroidal neovascularization induced by CYP2C8 overexpression by 29% (P=0.021) and 36% (P=1.2×10−9) respectively[2].

Clinical Trial
NCT Number Sponsor Condition Start Date Phase
NCT02306889 Ranbaxy Laboratories Limited|Ranbaxy Inc. Healthy January 2010 Not Applicable
NCT00092573 Merck Sharp & Dohme Corp. Hypercholesterolemia|Hypertriglyceridemia April 2003 Phase 3
NCT01109758 Solvay Pharmaceuticals Healthy March 2008 Phase 1
NCT00483210 University of Arkansas|National Institutes of Health (NIH) Tissue Lipid Metabolism Not Applicable
NCT00362934 Solvay Pharmaceuticals Hyperlipidemia October 2006 Phase 3
NCT00459745 Shionogi|Integrium|Shionogi Inc. Combined Hyperlipidemia April 2007 Phase 3
NCT00543647 Solvay Pharmaceuticals Healthy Volunteers August 2002 Phase 1
NCT00076518 National Institute of Allergy and Infectious Diseases (NIAID) HIV Infections|Hypertriglyceridemia Phase 2
NCT01462877 Abbott|Rundo International Pharmaceutical Research & Development Co.,Ltd. Dyslipidemias|Cardiovascular Diseases|Hypertriglyceridemia October 2011 Phase 4
NCT00613613 University of Minnesota - Clinical and Translational Science Institute|Laval University Dyslipidemia January 2008 Phase 4
NCT01141296 University of Miami|Mayo Clinic Primary Biliary Cirrhosis April 2011 Phase 2
NCT01101204 Medical University of Silesia Diabetes|Dyslipidemia|Inflammation|Cytokines July 2012 Not Applicable
NCT01142323 University of Miami|University of Florida Primary Sclerosing Cholangitis October 2010 Phase 1|Phase 2
NCT02890992 Sanofi|Regeneron Pharmaceuticals Hypercholesterolaemia September 15, 2016 Phase 2
NCT00362765 Solvay Pharmaceuticals Type 2 Diabetes|Dyslipidemia October 2006 Phase 2|Phase 3
NCT00361868 Solvay Pharmaceuticals Dyslipidemia|Glucose Metabolism Disorder June 2006 Phase 3
NCT02262143 IlDong Pharmaceutical Co Ltd Mixed Dyslipidemias November 2014 Phase 3
NCT00362323 Solvay Pharmaceuticals Dyslipidemia+Glucose Metabolism Disorder October 2006 Phase 3
NCT02823366 Xijing Hospital of Digestive Diseases Primary Biliary Cirrhosis January 2016 Phase 3
NCT00965315 National Taiwan University Hospital Diabetes|CVD
NCT00542178 National Heart, Lung, and Blood Institute (NHLBI)|National Eye Institute (NEI) Diabetic Retinopathy October 2003 Phase 3
NCT01767610 Hanlim Pharm. Co., Ltd. Healthy Male Volunteers January 2013 Phase 1
NCT01289639 VA Office of Research and Development Fatty Liver October 2005 Not Applicable
NCT00732485 The University of Texas Medical Branch, Galveston|Shriners Hospitals for Children Burn August 2008 Phase 2|Phase 3
NCT00000620 National Heart, Lung, and Blood Institute (NHLBI)|National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK)|National Institute on Aging (NIA)|National Eye Institute (NEI)|Centers for Disease Control and Prevention Atherosclerosis|Cardiovascular Diseases|Hypercholesterolemia|Hypertension|Diabetes Mellitus, Type 2|Diabetes Mellitus|Coronary Disease September 1999 Phase 3
NCT00349128 Solvay Pharmaceuticals Dyslipidemia+Glucose Metabolism Disorder January 2004 Phase 2|Phase 3
NCT02886299 Cairo University Fenofibrate+Simvastatin Comparison October 2013 Phase 4
NCT00552747 National Heart Institute, Mexico Coronary Heart Disease|Hyperlipidemia October 2007 Phase 4
NCT02354976 AstraZeneca Non-alcoholic Fatty Liver Disease (NAFLD|Hypertriglyceridemia September 1, 2015 Phase 2
NCT03510715 Sanofi|Regeneron Pharmaceuticals Hypercholesterolemia September 3, 2018 Phase 3
NCT00357500 Dana-Farber Cancer Institute|National Cancer Institute (NCI)|Boston Children´s Hospital Central Nervous System Tumor, Pediatric|Leukemia|Lymphoma|Neuroblastoma|Sarcoma|Unspecified Childhood Solid Tumor, Protocol Specific January 2005 Phase 2
NCT01878227 Zhejiang University Hyperlipoproteinemia July 2010 Phase 3
NCT01927315 University of Padova|Azienda Ospedaliera di Padova Diabetes|Diabetic Retinopathy August 2013 Phase 4
NCT00359281 Aegerion Pharmaceuticals, Inc. Healthy March 2006 Phase 2
NCT00006412 National Institute of Allergy and Infectious Diseases (NIAID) HIV Infections|Lipodystrophy Phase 3
NCT02965911 Beijing 302 Hospital Primary Biliary Cirrhosis January 2016 Phase 1|Phase 2
NCT00376285 Pfizer Obesity November 2006 Phase 1
NCT00092560 Merck Sharp & Dohme Corp. Hypercholesterolemia|Hypertriglyceridemia December 2002 Phase 3
NCT01723735 Sanofi|Regeneron Pharmaceuticals Hypercholesterolemia November 2012 Phase 1
NCT02984982 Sanofi|Regeneron Pharmaceuticals Hypercholesterolemia|Acute Coronary Syndrome November 15, 2016 Phase 4
NCT01594983 Novartis Pharmaceuticals|Novartis Non Familial Chylocmicronemia Syndrome (Non-FCS) June 2012 Phase 2
NCT00775359 Ranbaxy Laboratories Limited|Ranbaxy Inc. Healthy August 2002 Not Applicable
NCT00726856 Merck Sharp & Dohme Corp. Dyslipidemia May 2007
NCT01320345 University of Sydney|Abbott|University of Melbourne|St Vincent´s Hospital Melbourne|Melbourne Health|Royal Prince Alfred Hospital, Sydney, Australia Type 1 Diabetes Mellitus|Retinopathy|Diabetic Nephropathy September 2011 Phase 3
NCT02455336 VA Office of Research and Development Spinal Cord Injury|Dyslipidemia May 18, 2015 Phase 2|Phase 3
NCT00816829 Solvay Pharmaceuticals Dyslipidemia|Sleep Apnea Syndrome|Overweight|Obesity September 2005 Phase 2
NCT00673309 The University of Texas Medical Branch, Galveston|National Institutes of Health (NIH) Burns July 2002 Phase 2|Phase 3
NCT01752842 Washington University School of Medicine|National Institutes of Health (NIH)|National Heart, Lung, and Blood Institute (NHLBI)|Leducq Foundation Type II Diabetes Mellitus|Diabetes Complications March 2013 Not Applicable
NCT00169559 GlaxoSmithKline Dyslipidaemias November 2003 Phase 2
NCT02015988 Koval´ O., MD|Dnipropetrovsk State Medical Academy Acute Coronary Syndrome|Diabetes Mellitus, Type 2|Hypertriglyceridemia January 2014 Phase 4
NCT00349284 Solvay Pharmaceuticals Hyperlipidemia Combined January 2005 Phase 3
NCT00819910 Ahmad Slim|GlaxoSmithKline|Brooke Army Medical Center Hypertriglyceridemia in Type 4 Hyperlipidemia|Non Diabetic Subjects With Normoglycemia September 2008 Phase 4
NCT02781584 Gilead Sciences Nonalcoholic Steatohepatitis (NASH) July 13, 2016 Phase 2
NCT00252499 US Department of Veterans Affairs|VA Office of Research and Development Fatty Liver|Insulin Resistance October 2005 Not Applicable
NCT00400231 University of Pennsylvania|Abbott Metabolic Syndrome x August 2005 Phase 2
NCT00145431 Pfizer Hyperlipoproteinemia Type III March 2005 Phase 3
NCT02066207 Chong Kun Dang Pharmaceutical Dyslipidemia (Fredrickson Type ?a)|Dyslipidemia (Fredrickson Type ?b) March 18, 2014 Phase 1
NCT01048502 University of Pennsylvania|National Heart, Lung, and Blood Institute (NHLBI)|GlaxoSmithKline Cardiovascular Disease January 2010 Not Applicable
NCT00304993 Foundation Research, Florida|GlaxoSmithKline|Kos Pharmaceuticals|Abbott Metabolic Syndrome X|Insulin Resistance January 2001 Phase 4
NCT00754039 Daiichi Sankyo, Inc. Hypercholesterolemia|Hyperlipidemia, Familial Combined February 2003 Phase 4
NCT02153879 Institut Investigacio Sanitaria Pere Virgili|Spanish Biomedical Research Centre in Diabetes and Associated Metabolic Disorders Type 2 Diabetes Mellitus|Dyslipidemia February 2009 Phase 4
NCT00884819 Lawson Health Research Institute Polycystic Ovary Syndrome December 2008 Not Applicable
NCT00923676 University of Campania Luigi Vanvitelli Sexual Dysfunction|Hyperlipidemia April 2008 Phase 4
NCT00261352 AstraZeneca Type 2 Diabetes March 2005 Phase 3
NCT03510884 Sanofi|Regeneron Pharmaceuticals Hypercholesterolaemia May 31, 2018 Phase 3
NCT03011450 Kowa Research Institute, Inc. Severe Hypertriglyceridemia November 26, 2016 Phase 3
NCT00644592 University of Florida|American College of Clinical Pharmacy Healthy March 2008 Not Applicable
NCT00928694 Merck Sharp & Dohme Corp. Dyslipidemia February 2003 Phase 1
NCT00361751 National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK)|Shriners Hospitals for Children Burns|Insulin Resistance May 2003 Phase 2
NCT00960687 Mutual Pharmaceutical Company, Inc. Healthy October 2007 Phase 1
NCT00422396 University of Michigan|Abbott Hypertriglyceridemia With the Metabolic Syndrome January 2001 Not Applicable
NCT00470262 VA Office of Research and Development Metabolic Syndrome X|Prediabetic State January 2007 Not Applicable
NCT00872599 Vanderbilt University|National Institutes of Health (NIH) Hypertension September 2009 Phase 4
NCT00683176 Abbott Products|Abbott Diabetic Macular Edema September 2008 Phase 2
NCT00961116 Mutual Pharmaceutical Company, Inc. Healthy October 2007 Phase 1
NCT03439345 University of Oxford|National Institute for Health Research, United Kingdom|University of Glasgow|University of Aberdeen|University of Dundee|University of Edinburgh|NHS Scotland Diabetic Retinopathy Screening Collaborative Diabetic Retinopathy July 23, 2018 Phase 4
NCT00775827 Ranbaxy Laboratories Limited|Ranbaxy Inc. Healthy November 2002 Not Applicable
NCT00559962 Aegerion Pharmaceuticals, Inc. Hyperlipidemia October 2007 Phase 2
NCT00348725 Solvay Pharmaceuticals Dyslipidemia+Glucose Metabolism Disorder April 2005 Phase 3
NCT01148004 National Institutes of Health Clinical Center (CC) HIV|Fenofibrate|Protease Inhibitors|Hypertriglyceridemia|Glucuronosyltransferase May 13, 2010 Phase 1
NCT03615534 Lewai Sharki Abdulaziz, MSc PhD|Al-Kindy College of Medicine Atherogenic Dyslipidemia|Obesity Associated Disorder October 1, 2014 Phase 4
NCT03001817 Kowa Research Institute, Inc. Severe Hypertriglyceridemia November 28, 2016 Phase 3
NCT01426438 AIDS Clinical Trials Group|National Institute of Allergy and Infectious Diseases (NIAID) HIV-1 Infection November 2011 Phase 2
NCT00703690 Merck Sharp & Dohme Corp. Metabolic X Syndrome Dyslipidemia January 2002 Phase 2
NCT00262964 Washington University School of Medicine|National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK) Non-alcoholic Fatty Liver Disease October 2004 Not Applicable
NCT00703755 Solvay Pharmaceuticals Patients With Metabolic Syndrome March 2003 Phase 2
NCT00491400 Boston University Diabetes Mellitus|Metabolic Syndrome September 2005 Not Applicable
NCT02306902 Ranbaxy Laboratories Limited|Ranbaxy Inc. Healthy October 2009 Not Applicable
NCT00246376 Baylor College of Medicine|National Heart, Lung, and Blood Institute (NHLBI)|Legacy Community Health Center Cardiovascular Diseases|Heart Diseases|HIV Infections|Hyperlipidemia|Hypertriglyceridemia|Insulin Resistance|Atherosclerosis January 2004 Not Applicable
NCT01674712 Abbott Dyslipidemia June 2012 Phase 3
NCT00139061 Pfizer Hyperlipidemia March 2005 Phase 3
NCT00490178 Solvay Pharmaceuticals Diabetes Mellitus, Type 2|Dyslipidemia March 2007 Phase 3
NCT00349635 Solvay Pharmaceuticals Obesity October 2004 Phase 2
NCT00627653 National Institute on Aging (NIA) Cardiovascular Diseases October 2005 Not Applicable
NCT03515213 University of California, Irvine Huntington Disease April 27, 2017 Phase 2
NCT01010516 University of Ioannina Dyslipidemia October 2009 Phase 4
NCT00504829 Veloxis Pharmaceuticals Dyslipidemia July 2007 Phase 2
NCT00843661 Ospedale di Circolo - Fondazione Macchi|Merck Sharp & Dohme Corp. HIV|Hyperlipidemia|HIV Infections March 2009 Phase 4
NCT01280604 Kaiser Permanente Hyperlipidemias October 2010 Not Applicable
NCT00575042 University of Florida|The PBCers Organization|Shionogi Inc. Primary Biliary Cirrhosis August 2007 Phase 2
NCT00745407 Gachon University Gil Medical Center Hypertriglyceridemia January 2005 Phase 4
NCT01023750 University of Alabama at Birmingham|Tufts University|University of Minnesota - Clinical and Translational Science Institute Hypertriglyceridemia|Insulin Resistance January 2010
NCT00309712 Intermountain Health Care, Inc.|Abbott|Merck Sharp & Dohme Corp. Type II Diabetes Mellitus|Mixed Dyslipidemia August 2002 Not Applicable
NCT00195793 Abbott Hyperlipidemia August 2004 Phase 3
NCT01965834 University of Miami Multiple Myeloma November 19, 2012 Phase 2
NCT01666041 Gachon University Gil Medical Center Hypertriglyceridemia January 2012 Phase 4
NCT00673881 Radiant Research Dyslipidemia March 2008 Phase 1|Phase 2
NCT00385658 Novartis Dyslipidemia August 2006 Phase 4
NCT01539616 Cadila Healthcare Limited Hypertriglyceridemia|Dyslipidemia November 2011 Phase 2
NCT00813527 Takeda Hyperlipidemias February 2006 Phase 2
NCT02232360 Gachon University Gil Medical Center|Daewoong Pharmaceutical Co. LTD. Coronary Artery Disease January 2014 Phase 3
NCT02452255 The University of Texas Medical Branch, Galveston|National Institute of General Medical Sciences (NIGMS)|Shriners Hospitals for Children Burn November 2015 Phase 2|Phase 3
NCT02642159 Sanofi|Regeneron Pharmaceuticals Dyslipidemia March 15, 2016 Phase 4
NCT02823353 Xijing Hospital of Digestive Diseases Primary Biliary Cirrhosis January 2016 Phase 3
NCT00632840 The University of Western Australia|National Heart Foundation, Australia Obesity|Lipid Disorders|Hypertriglyceridemia|Cardiovascular Disease June 2001 Phase 4
NCT00186537 Stanford University|Abbott Insulin Resistance|Hypertriglyceridemia September 2003 Not Applicable
NCT03557983 Second Affiliated Hospital of Soochow University Radiodermatitis June 13, 2018 Not Applicable
NCT01574131 The University of Texas Medical Branch, Galveston|Shriners Hospitals for Children Second or Third Degree Burns May 2012 Phase 4
NCT02314533 Beijing Chao Yang Hospital Microalbuminuria December 2014 Phase 4
NCT01956201 Chong Kun Dang Pharmaceutical Mixed Hyperlipidemia December 2013 Phase 3
NCT00809068 Keogh Institute for Medical Research HDL Cholesterol August 2005 Phase 4
Solvent & Solubility
In Vitro: 

DMSO : ≥ 47 mg/mL (130.26 mM)

* "≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
ConcentrationSolventMass 1 mg 5 mg 10 mg
1 mM 2.7714 mL 13.8569 mL 27.7139 mL
5 mM 0.5543 mL 2.7714 mL 5.5428 mL
10 mM 0.2771 mL 1.3857 mL 2.7714 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  corn oil

    Solubility: 33.33 mg/mL (92.37 mM); Clear solution; Need ultrasonic


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