Explore a selection of our essential drug information below, or:
Identification
- Summary
Fenofibrate is a peroxisome proliferator receptor alpha activator used to lower LDL-C, total-C, triglycerides, and Apo B, while increasing HDL-C in hypercholesterolemia, dyslipidemia, and hypertriglyceridemia.
- Brand Names
- Antara, Cholib, Fenoglide, Lipidil Supra, Lipofen, Tricor, Triglide
- Generic Name
- Fenofibrate
- DrugBank Accession Number
- DB01039
- Background
Fenofibrate is a fibric acid derivative like clofibrate and gemfibrozil.4 Fenofibrate is used to treat primary hypercholesterolemia, mixed dyslipidemia, severe hypertriglyceridemia.11,12
Fenofibrate was granted FDA approval on 31 December 1993.10
- Type
- Small Molecule
- Groups
- Approved
- Structure
Structure for Fenofibrate (DB01039)
- Weight
- Average: 360.831
Monoisotopic: 360.112836867 - Chemical Formula
- C20H21ClO4
- Synonyms
- 2-(4-(4-Chlorobenzoyl)phenoxy)-2-methylpropanoic acid 1-methylethyl ester
- Fenofibrate
- Fenofibrato
- Fenofibratum
- Finofibrate
- FNF
- Isopropyl (4'-(p-chlorobenzoyl)-2-phenoxy-2-methyl)propionate
- Isopropyl 2-(4-(4-chlorobenzoyl)phenoxy)-2-methylpropionate
- Procetofen
Pharmacology
- Indication
Fenofibrate is indicated as adjunctive therapy to diet to reduce elevated LDL-C, Total-C, Triglycerides, and Apo B, and to increase HDL-C adults with primary hypercholesterolemia or mixed dyslipidemia.11,12 Fenofibrate is also indicated to treat adults with severe hypertriglyceridemia.11,12
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Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Treatment of Mixed dyslipidemia •••••••••••• ••••• Treatment of Mixed dyslipidemia •••••••••••• ••••• Used in combination to manage Mixed dyslipidemia Regimen in combination with: Simvastatin (DB00641) ••• ••••• Treatment of Primary hypercholesterolemia •••••••••••• ••••• Treatment of Severe hypertriglyceridemia •••••••••••• ••••• - Contraindications & Blackbox Warnings
Prevent Adverse Drug Events TodayTap into our Clinical API for life-saving information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.Avoid life-threatening adverse drug events with our Clinical API- Pharmacodynamics
Fenofibrate is a fibrate that activates peroxisome proliferator activated receptor alpha (PPARα) to alter lipid metabolism and treat primary hypercholesterolemia, mixed dyslipidemia, and severe hypertriglyceridemia.8,11,12 Fenofibrate requires once daily dosing and has a half life of 19-27 hours so its duration of action is long.3,11,12 Fenofibrate capsules are given at a dose of 50-150mg daily so the therapeutic index is wide.12 Patients should be counselled about the risk of rhabdomyolysis, myopathy, and cholelithiasis when taking fibrates.11,12
- Mechanism of action
Fenofibrate activates peroxisome proliferator activated receptor alpha (PPARα), increasing lipolysis, activating lipoprotein lipase, and reducing apoprotein C-III.8,11,12 PPARα is a nuclear receptor and its activation alters lipid, glucose, and amino acid homeostasis.8 Activation of PPARα activates transcription of gene transcription and translation that generates peroxisomes filled with hydrogen peroxide, reactive oxygen species, and hydroxyl radicals that also participate in lipolysis.9 This mechanism of increased lipid metabolism is also associated with increased oxidative stress on the liver.9 In rare cases this stress can lead to cirrhosis and chronic active hepatitis.8,11,12
Target Actions Organism APeroxisome proliferator-activated receptor alpha agonistHumans UNuclear receptor subfamily 1 group I member 2 partial agonistHumans UMatrix metalloproteinase-25 inhibitorHumans - Absorption
A single 300mg oral dose of fenofibrate reaches a Cmax of 6-9.5mg/L with a Tmax of 4-6h in healthy, fasting volunteers.4
- Volume of distribution
The volume of distribution of fenofibrate is 0.89L/kg,4 and can be as high as 60L.3
- Protein binding
Fenofibrate is 99% protein bound in serum,11,12 primarily to albumin.2
- Metabolism
Fenofibrate is completely hydrolyzed by liver carboxylesterase 1 to fenofibric acid.6,11,12 Fenofibric acid is either glucuronidated or has its carbonyl group reduced to a benzhydrol that is then glucuronidated.11,12 Glucuronidation of fenofibrate metabolites is mediated by UGT1A9.5 Reduction of the carbonyl group is primarily mediated by CBR1 and minorly by AKR1C1, AKR1C2, AKR1C3, and AKR1B1.7
Hover over products below to view reaction partners
- Route of elimination
5-25% of a dose of fenofibrate is eliminated in the feces, while 60-88% is eliminated in the urine.2,11,12 70-75% of the dose recovered in the urine is in the form of fenofibryl glucuronide and 16% as fenofibric acid.2
- Half-life
Fenofibric acid, the active metabolite of fenofibrate, has a half life of 23 hours.11,12 Fenofibrate has a half life of 19-27 hours in healthy subjects and up to 143 hours in patients with renal failure.3
- Clearance
The oral clearance of fenofibrate is 1.1L/h in young adults and 1.2L/h in the elderly.11,12
- Adverse Effects
Improve decision support & research outcomesWith structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates. View sample adverse effects data in our new Data Library!Improve decision support & research outcomes with our structured adverse effects data.- Toxicity
The oral LD50 in rats is >2g/kg and in mice is 1600mg/kg.13 The oral TDLO in rats is 9mg/kg.13
Treat patients with supportive care including monitoring of vital signs and observing clinical status.11,12 Recent overdose may be treated with inducing vomiting or gastric lavage.11,12 Due to fenofibrate's extensive protein binding, hemodialysis is not expected to be useful.2,11,12
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs
- Not Available
Interactions
- Drug Interactions
- This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Drug Interaction Integrate drug-drug
interactions in your softwareAbacavir Fenofibrate may decrease the excretion rate of Abacavir which could result in a higher serum level. Abametapir The serum concentration of Fenofibrate can be increased when it is combined with Abametapir. Abatacept The metabolism of Fenofibrate can be increased when combined with Abatacept. Abemaciclib The metabolism of Abemaciclib can be decreased when combined with Fenofibrate. Abrocitinib The metabolism of Abrocitinib can be decreased when combined with Fenofibrate. - Food Interactions
- Take with food. Bioavailability is increased 2- to 3-fold when taken with food.
Products
Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.- Active Moieties
Name Kind UNII CAS InChI Key Fenofibric acid prodrug BGF9MN2HU1 42017-89-0 MQOBSOSZFYZQOK-UHFFFAOYSA-N - Product Images
- International/Other Brands
- Fenogal (SMB Laboratories) / Lipanthyl (Abbott) / Lipantil / Lipidil (lbirn)
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Antara Capsule 130 mg/1 Oral Physicians Total Care, Inc. 2005-12-27 2011-06-30 US 
Antara Capsule 90 mg/1 Oral Lupin Pharmaceuticals, Inc. 2013-11-01 Not applicable US Antara Capsule 43 mg/1 Oral Oscient Pharmaceuticals Corporation 2008-01-30 Not applicable US Antara Capsule 130 mg/1 Oral Lupin Pharmaceuticals, Inc. 2009-09-25 Not applicable US Antara Capsule 30 mg/1 Oral Lupin Pharmaceuticals, Inc. 2013-11-01 Not applicable US - Generic Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Aa-feno-micro Capsule 67 mg Oral Aa Pharma Inc 2001-02-21 Not applicable Canada 
Aa-feno-micro Capsule 200 mg Oral Aa Pharma Inc 1999-03-29 Not applicable Canada Aa-feno-super Tablet 160 mg Oral Aa Pharma Inc 2006-04-21 Not applicable Canada Aa-feno-super Tablet 200 mg Oral Aa Pharma Inc Not applicable Not applicable Canada Aa-feno-super Tablet 100 mg Oral Aa Pharma Inc 2006-04-21 Not applicable Canada - Mixture Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image ACIDO FENOFIBRICO / ROSUVASTATINA 135 MG/10 MG Fenofibrate (135 mg) + Rosuvastatin calcium (10 mg) Capsule, coated Oral TECNOQUIMICAS S.A. 2019-03-19 Not applicable Colombia 
CHOLIB Fenofibrate (145 MG) + Simvastatin (40 MG) Tablet, film coated Oral Viatris Healthcare Limited 2014-07-08 Not applicable Italy 
CHOLIB Fenofibrate (145 MG) + Simvastatin (20 MG) Tablet, film coated Oral Viatris Healthcare Limited 2014-07-08 Not applicable Italy Cholib Fenofibrate (145 mg) + Simvastatin (40 mg) Tablet, film coated Oral Viatris Healthcare Limited 2016-09-08 Not applicable EU 
Cholib Fenofibrate (145 mg) + Simvastatin (20 mg) Tablet, film coated Oral Viatris Healthcare Limited 2016-09-08 Not applicable EU - Unapproved/Other Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image SECALIP SR 250 MG KAPSUL, 30 ADET Fenofibrate (250 mg) Capsule Oral ABBOTT LABORATUARLARI İTHALAT İHRACAT VE TİC. LTD. ŞTİ. 2018-02-20 Not applicable Turkey 
Categories
- ATC Codes
- C10BA03 — Pravastatin and fenofibrate
- C10BA — Combinations of various lipid modifying agents
- C10B — LIPID MODIFYING AGENTS, COMBINATIONS
- C10 — LIPID MODIFYING AGENTS
- C — CARDIOVASCULAR SYSTEM
- C10BA — Combinations of various lipid modifying agents
- C10B — LIPID MODIFYING AGENTS, COMBINATIONS
- C10 — LIPID MODIFYING AGENTS
- C — CARDIOVASCULAR SYSTEM
- C10AB — Fibrates
- C10A — LIPID MODIFYING AGENTS, PLAIN
- C10 — LIPID MODIFYING AGENTS
- C — CARDIOVASCULAR SYSTEM
- C10BA — Combinations of various lipid modifying agents
- C10B — LIPID MODIFYING AGENTS, COMBINATIONS
- C10 — LIPID MODIFYING AGENTS
- C — CARDIOVASCULAR SYSTEM
- Drug Categories
- Acids, Acyclic
- Agents Causing Muscle Toxicity
- Benzene Derivatives
- Benzophenones
- BSEP/ABCB11 Substrates
- Butyrates
- Cytochrome P-450 CYP2A6 Inhibitors
- Cytochrome P-450 CYP2A6 Inhibitors (weak)
- Cytochrome P-450 CYP2C19 Inhibitors
- Cytochrome P-450 CYP2C19 Inhibitors (weak)
- Cytochrome P-450 CYP2C8 Inhibitors
- Cytochrome P-450 CYP2C8 Inhibitors (weak)
- Cytochrome P-450 CYP2C9 Inhibitors
- Cytochrome P-450 CYP2C9 Inhibitors (strength unknown)
- Cytochrome P-450 CYP3A Substrates
- Cytochrome P-450 CYP3A4 Substrates
- Cytochrome P-450 CYP3A4 Substrates (strength unknown)
- Cytochrome P-450 Enzyme Inhibitors
- Cytochrome P-450 Substrates
- Drugs that are Mainly Renally Excreted
- Ethers
- Fatty Acids
- Fatty Acids, Volatile
- Fibric Acid Derivatives
- Fibric Acids
- Hypolipidemic Agents
- Hypolipidemic Agents Indicated for Hyperlipidemia
- Isobutyrates
- Ketones
- Lipid Modifying Agents
- Lipid Modifying Agents, Plain
- Lipid Regulating Agents
- Lipids
- Non-statin Hypolipidemic Agents Indicated for Hyperlipidemia
- Noxae
- P-glycoprotein inhibitors
- Peroxisome Proliferator Receptor alpha Agonist
- Peroxisome Proliferator-activated Receptor alpha Agonists
- Phenols
- Phenyl Ethers
- Toxic Actions
- UGT1A9 Substrates
- Chemical TaxonomyProvided by Classyfire
- Description
- This compound belongs to the class of organic compounds known as benzophenones. These are organic compounds containing a ketone attached to two phenyl groups.
- Kingdom
- Organic compounds
- Super Class
- Benzenoids
- Class
- Benzene and substituted derivatives
- Sub Class
- Benzophenones
- Direct Parent
- Benzophenones
- Alternative Parents
- Diphenylmethanes / Aryl-phenylketones / Phenoxyacetic acid derivatives / Phenoxy compounds / Phenol ethers / Benzoyl derivatives / Chlorobenzenes / Alkyl aryl ethers / Aryl chlorides / Carboxylic acid esters show 4 more
- Substituents
- Alkyl aryl ether / Aromatic homomonocyclic compound / Aryl chloride / Aryl halide / Aryl ketone / Aryl-phenylketone / Benzophenone / Benzoyl / Carbonyl group / Carboxylic acid derivative show 16 more
- Molecular Framework
- Aromatic homomonocyclic compounds
- External Descriptors
- aromatic ether, carboxylic ester, monochlorobenzenes, chlorobenzophenone (CHEBI:5001)
- Affected organisms
- Humans and other mammals
Chemical Identifiers
- UNII
- U202363UOS
- CAS number
- 49562-28-9
- InChI Key
- YMTINGFKWWXKFG-UHFFFAOYSA-N
- InChI
- InChI=1S/C20H21ClO4/c1-13(2)24-19(23)20(3,4)25-17-11-7-15(8-12-17)18(22)14-5-9-16(21)10-6-14/h5-13H,1-4H3
- IUPAC Name
- propan-2-yl 2-[4-(4-chlorobenzoyl)phenoxy]-2-methylpropanoate
- SMILES
- CC(C)OC(=O)C(C)(C)OC1=CC=C(C=C1)C(=O)C1=CC=C(Cl)C=C1
References
- Synthesis Reference
Jean-Francois Boyer, "Medicine based on fenofibrate, and a method of preparing it." U.S. Patent US4800079, issued January, 1988.
US4800079- General References
- Wei X, Li P, Liu M, Du Y, Wang M, Zhang J, Wang J, Liu H, Liu X: Absolute oral bioavailability of fenofibric acid and choline fenofibrate in rats determined by ultra-performance liquid chromatography tandem mass spectrometry. Biomed Chromatogr. 2017 Apr;31(4). doi: 10.1002/bmc.3832. Epub 2016 Oct 10. [Article]
- Chapman MJ: Pharmacology of fenofibrate. Am J Med. 1987 Nov 27;83(5B):21-5. doi: 10.1016/0002-9343(87)90867-9. [Article]
- Miller DB, Spence JD: Clinical pharmacokinetics of fibric acid derivatives (fibrates). Clin Pharmacokinet. 1998 Feb;34(2):155-62. doi: 10.2165/00003088-199834020-00003. [Article]
- Balfour JA, McTavish D, Heel RC: Fenofibrate. A review of its pharmacodynamic and pharmacokinetic properties and therapeutic use in dyslipidaemia. Drugs. 1990 Aug;40(2):260-90. doi: 10.2165/00003495-199040020-00007. [Article]
- Barbier O, Villeneuve L, Bocher V, Fontaine C, Torra IP, Duhem C, Kosykh V, Fruchart JC, Guillemette C, Staels B: The UDP-glucuronosyltransferase 1A9 enzyme is a peroxisome proliferator-activated receptor alpha and gamma target gene. J Biol Chem. 2003 Apr 18;278(16):13975-83. Epub 2003 Feb 11. [Article]
- Laizure SC, Herring V, Hu Z, Witbrodt K, Parker RB: The role of human carboxylesterases in drug metabolism: have we overlooked their importance? Pharmacotherapy. 2013 Feb;33(2):210-22. doi: 10.1002/phar.1194. [Article]
- Malatkova P, Kanavi M, Nobilis M, Wsol V: In vitro metabolism of fenofibric acid by carbonyl reducing enzymes. Chem Biol Interact. 2016 Oct 25;258:153-8. doi: 10.1016/j.cbi.2016.09.001. Epub 2016 Sep 4. [Article]
- Liu A, Patterson AD, Yang Z, Zhang X, Liu W, Qiu F, Sun H, Krausz KW, Idle JR, Gonzalez FJ, Dai R: Fenofibrate metabolism in the cynomolgus monkey using ultraperformance liquid chromatography-quadrupole time-of-flight mass spectrometry-based metabolomics. Drug Metab Dispos. 2009 Jun;37(6):1157-63. doi: 10.1124/dmd.108.025817. Epub 2009 Feb 27. [Article]
- Qi C, Zhu Y, Reddy JK: Peroxisome proliferator-activated receptors, coactivators, and downstream targets. Cell Biochem Biophys. 2000;32 Spring:187-204. [Article]
- FDA Approved Drug Products: Lipidil Fenofibrate Oral Capsules (Discontinued) [Link]
- FDA Approved Drug Products: Fenofibrate Oral Tablets [Link]
- FDA Approved Drug Products: Fenofibrate Oral Capsules [Link]
- Cayman Chemicals: Fenofibrate MSDS [Link]
- External Links
- Human Metabolome Database
- HMDB0015173
- KEGG Drug
- D00565
- KEGG Compound
- C07586
- PubChem Compound
- 3339
- PubChem Substance
- 46507371
- ChemSpider
- 3222
- BindingDB
- 50085042
- 8703
- ChEBI
- 5001
- ChEMBL
- CHEMBL672
- ZINC
- ZINC000000584092
- Therapeutic Targets Database
- DAP000270
- PharmGKB
- PA449594
- PDBe Ligand
- J3O
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- PDRhealth
- PDRhealth Drug Page
- Wikipedia
- Fenofibrate
- PDB Entries
- 8k8j
- FDA label
- Download (283 KB)
- MSDS
- Download (19.3 KB)
Clinical Trials
- Clinical Trials
Clinical Trial & Rare Diseases Add-on Data Package
Explore 4,000+ rare diseases, orphan drugs & condition pairs, clinical trial why stopped data, & more. Preview package Phase Status Purpose Conditions Count Start Date Why Stopped 100+ additional columns Unlock 175K+ rows when you subscribe.View sample dataNot Available Available Not Available Cardiovascular Disease (CVD) / Diabetes 1 somestatus stop reason just information to hide Not Available Available Not Available Hyperlipidemias 1 somestatus stop reason just information to hide Not Available Completed Not Available Coronavirus Disease 2019 (COVID‑19) 1 somestatus stop reason just information to hide Not Available Completed Not Available Dyslipidemia 2 somestatus stop reason just information to hide Not Available Completed Not Available Dyslipidemia / Vascular Diseases 1 somestatus stop reason just information to hide
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Abbott Laboratories Ltd.
- Amerisource Health Services Corp.
- A-S Medication Solutions LLC
- Atlantic Biologicals Corporation
- Cardinal Health
- Catalent Pharma Solutions
- Dispensing Solutions
- Ethypharm
- Fournier Pharma Inc.
- Galephar Pharmaceutical Research Inc.
- Gate Pharmaceuticals
- Global Pharmaceuticals
- Impax Laboratories Inc.
- Karalex Pharmaceuticals
- Kowa Pharmaceuticals America Inc.
- Laboratories Fournier Sca
- Lake Erie Medical and Surgical Supply
- Lupin Pharmaceuticals Inc.
- Mikart Inc.
- Murfreesboro Pharmaceutical Nursing Supply
- Mutual Pharmaceutical Co.
- Mylan
- Novopharm Ltd.
- Oscient Pharmaceuticals
- PD-Rx Pharmaceuticals Inc.
- Pharmacy Service Center
- Physicians Total Care Inc.
- Promex Medical Inc.
- Ranbaxy Laboratories
- Reliant Pharmaceuticals
- Resource Optimization and Innovation LLC
- Sciele Pharma Inc.
- Shionogi Pharma Inc.
- Skyepharma Production Sas
- Southwood Pharmaceuticals
- Teva Pharmaceutical Industries Ltd.
- United Research Laboratories Inc.
- Dosage Forms
Form Route Strength Capsule Oral 160.00 mg Capsule Oral 67 mg Tablet Oral 100 mg Tablet Oral 160 mg Tablet Oral 200 mg Capsule Oral 130 mg/1 Capsule Oral 30 mg/1 Capsule Oral 43 mg/1 Capsule Oral 90 mg/1 Tablet Oral Tablet, film coated Oral Tablet, film coated Oral 145.0 mg Tablet Oral 145.000 mg Capsule Oral 160.000 mg Capsule, extended release Oral 200 MG Capsule, coated Oral 200 mg Capsule, extended release Oral 250 MG Capsule Oral 134 mg/1 Capsule Oral 200 mg/1 Capsule Oral 67 mg/1 Tablet Oral 145 mg/301 Tablet Oral 54 mg/1 Tablet, coated Oral 145 mg/1 Tablet, coated Oral 160 mg/1 Tablet, coated Oral 48 mg/1 Tablet, coated Oral 54 mg/1 Tablet, film coated Oral 145 mg/1 Tablet, film coated Oral 160 mg/1 Tablet, film coated Oral 48 mg/1 Capsule, coated Oral 100 mg Capsule, gelatin coated 200 mg Tablet Oral 120 mg/1 Tablet Oral 40 mg/1 Capsule Oral 200.000 mg Tablet Oral 160.000 mg Capsule Oral 267 mg Tablet, film coated Oral 145 mg Capsule Oral 100 mg / cap Tablet Oral 48 mg Capsule Oral 67 mg / cap Capsule Oral 100 mg/1 Capsule Oral 150 mg/1 Capsule Oral 50 mg/1 Capsule, coated pellets 250 mg Capsule Oral 250 MG Tablet, film coated Oral 54 mg/1 Tablet, film coated Oral Capsule Oral Capsule Oral 160 mg Tablet Oral 145.0 mg Tablet Oral 48.0 mg Pellet 250 mg Tablet, coated Oral Capsule, coated Oral Tablet, coated Oral 145 mg Tablet Oral 145 mg/1 Tablet Oral 160 mg/1 Tablet Oral 48 mg/1 Tablet Oral 50 mg/1 Tablet Oral 160.00 mg Tablet Oral Capsule Oral Capsule Oral 200 mg Capsule Oral 100 mg Tablet, coated Oral 160 mg Tablet, film coated Oral 160 mg Capsule Oral 160 mg Tablet Oral 145 mg Capsule Oral 300 mg - Prices
Unit description Cost Unit Triglide 160 mg tablet 6.39USD tablet Fenoglide 120 mg tablet 5.17USD tablet Antara 130 mg capsule 5.13USD capsule Tricor 145 mg tablet 4.69USD tablet Lipofen 150 mg capsule 3.55USD capsule Lofibra 200 mg capsule 3.25USD capsule Lofibra 160 mg tablet 3.11USD tablet Fenofibrate Micronized 200 mg capsule 2.77USD capsule Fenofibrate 160 mg 2.47USD tablet Fenofibrate 160 mg tablet 2.38USD tablet Lofibra 134 mg capsule 2.03USD capsule Antara 43 mg capsule 1.8USD capsule Fenofibrate Micronized 134 mg capsule 1.79USD capsule Fenoglide 40 mg tablet 1.72USD tablet Tricor 48 mg tablet 1.63USD tablet Triglide 50 mg tablet 1.49USD tablet Lipidil Supra 160 mg Tablet 1.4USD tablet Lofibra 67 mg capsule 1.26USD capsule Lipidil Micro 200 mg Capsule 1.23USD capsule Lipidil Supra 100 mg Tablet 1.22USD tablet Apo-Feno-Micro 200 mg Capsule 1.14USD capsule Fenofibrate Micro 200 mg Capsule 1.14USD capsule Mylan-Fenofibrate Micro 200 mg Capsule 1.14USD capsule Novo-Fenofibrate Micronized 200 mg Capsule 1.14USD capsule Pms-Fenofibrate Micro 200 mg Capsule 1.14USD capsule Ratio-Fenofibrate Mc 200 mg Capsule 1.14USD capsule Fenofibrate Micronized 67 mg capsule 1.0USD capsule Lofibra 54 mg tablet 0.99USD tablet Fenofibrate 54 mg tablet 0.81USD tablet Apo-Feno-Super 160 mg Tablet 0.79USD tablet Novo-Fenofibrate-S 160 mg Tablet 0.79USD tablet Sandoz Fenofibrate S 160 mg Tablet 0.79USD tablet Apo-Feno-Super 100 mg Tablet 0.68USD tablet Novo-Fenofibrate-S 100 mg Tablet 0.68USD tablet Sandoz Fenofibrate S 100 mg Tablet 0.68USD tablet Apo-Fenofibrate 100 mg Capsule 0.64USD capsule Apo-Feno-Micro 67 mg Capsule 0.45USD capsule Novo-Fenofibrate Micronized 67 mg Capsule 0.45USD capsule DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region US5145684 No 1992-09-08 2011-01-25 US CA2487054 No 2008-03-18 2023-05-23 Canada CA2219475 No 2002-07-09 2017-12-11 Canada US8124125 No 2012-02-28 2024-10-01 US US8481078 No 2013-07-09 2024-10-01 US US7658944 No 2010-02-09 2024-12-09 US US9173847 No 2015-11-03 2024-10-01 US US6277405 No 2001-08-21 2018-01-09 US US7037529 No 2006-05-02 2018-01-09 US US6074670 No 2000-06-13 2018-01-09 US US7041319 No 2006-05-09 2018-01-09 US US6652881 No 2003-11-25 2018-01-09 US US6589552 No 2003-07-08 2018-01-09 US US6696084 No 2004-02-24 2021-09-11 US US6375986 No 2002-04-23 2020-09-21 US US7320802 No 2008-01-22 2023-02-21 US US7276249 No 2007-10-02 2023-02-21 US US8026281 No 2011-09-27 2025-04-22 US US9314447 No 2016-04-19 2033-05-31 US US7863331 No 2011-01-04 2020-08-08 US US7101574 No 2006-09-05 2020-08-20 US
Properties
- State
- Solid
- Experimental Properties
Property Value Source melting point (°C) 79-82 FDA Label logP 5.2 Wei et al, 2017 - Predicted Properties
Property Value Source Water Solubility 0.000707 mg/mL ALOGPS logP 4.86 ALOGPS logP 5.28 Chemaxon logS -5.7 ALOGPS pKa (Strongest Basic) -4.9 Chemaxon Physiological Charge 0 Chemaxon Hydrogen Acceptor Count 3 Chemaxon Hydrogen Donor Count 0 Chemaxon Polar Surface Area 52.6 Å2 Chemaxon Rotatable Bond Count 7 Chemaxon Refractivity 97.13 m3·mol-1 Chemaxon Polarizability 38.15 Å3 Chemaxon Number of Rings 2 Chemaxon Bioavailability 1 Chemaxon Rule of Five No Chemaxon Ghose Filter Yes Chemaxon Veber's Rule No Chemaxon MDDR-like Rule No Chemaxon - Predicted ADMET Features
Property Value Probability Human Intestinal Absorption + 0.987 Blood Brain Barrier + 0.9334 Caco-2 permeable + 0.648 P-glycoprotein substrate Non-substrate 0.5571 P-glycoprotein inhibitor I Non-inhibitor 0.5995 P-glycoprotein inhibitor II Non-inhibitor 0.7632 Renal organic cation transporter Non-inhibitor 0.9042 CYP450 2C9 substrate Non-substrate 0.7897 CYP450 2D6 substrate Non-substrate 0.9147 CYP450 3A4 substrate Substrate 0.6735 CYP450 1A2 substrate Inhibitor 0.7599 CYP450 2C9 inhibitor Non-inhibitor 0.9071 CYP450 2D6 inhibitor Non-inhibitor 0.9231 CYP450 2C19 inhibitor Inhibitor 0.7619 CYP450 3A4 inhibitor Non-inhibitor 0.831 CYP450 inhibitory promiscuity Low CYP Inhibitory Promiscuity 0.7088 Ames test Non AMES toxic 0.9133 Carcinogenicity Non-carcinogens 0.6373 Biodegradation Not ready biodegradable 0.9918 Rat acute toxicity 2.2250 LD50, mol/kg Not applicable hERG inhibition (predictor I) Weak inhibitor 0.9887 hERG inhibition (predictor II) Non-inhibitor 0.9083
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
- Chromatographic Properties
Collision Cross Sections (CCS)
Adduct CCS Value (Å2) Source type Source [M-H]- 197.8946018 predictedDarkChem Lite v0.1.0 [M-H]- 197.6429018 predictedDarkChem Lite v0.1.0 [M-H]- 196.58305 predictedDeepCCS 1.0 (2019) [M+H]+ 198.4822018 predictedDarkChem Lite v0.1.0 [M+H]+ 197.7325018 predictedDarkChem Lite v0.1.0 [M+H]+ 199.30074 predictedDeepCCS 1.0 (2019) [M+Na]+ 197.7688018 predictedDarkChem Lite v0.1.0 [M+Na]+ 198.1241018 predictedDarkChem Lite v0.1.0 [M+Na]+ 207.45436 predictedDeepCCS 1.0 (2019)
Targets
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- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Agonist
- General Function
- Ligand-activated transcription factor. Key regulator of lipid metabolism. Activated by the endogenous ligand 1-palmitoyl-2-oleoyl-sn-glycerol-3-phosphocholine (16:0/18:1-GPC). Activated by oleylethanolamide, a naturally occurring lipid that regulates satiety. Receptor for peroxisome proliferators such as hypolipidemic drugs and fatty acids. Regulates the peroxisomal beta-oxidation pathway of fatty acids. Functions as a transcription activator for the ACOX1 and P450 genes. Transactivation activity requires heterodimerization with RXRA and is antagonized by NR2C2. May be required for the propagation of clock information to metabolic pathways regulated by PER2
- Specific Function
- Dna binding
- Gene Name
- PPARA
- Uniprot ID
- Q07869
- Uniprot Name
- Peroxisome proliferator-activated receptor alpha
- Molecular Weight
- 52224.595 Da
References
- Clavey V, Copin C, Mariotte MC, Bauge E, Chinetti G, Fruchart J, Fruchart JC, Dallongeville J, Staels B: Cell culture conditions determine apolipoprotein CIII secretion and regulation by fibrates in human hepatoma HepG2 cells. Cell Physiol Biochem. 1999;9(3):139-49. [Article]
- Chaput E, Saladin R, Silvestre M, Edgar AD: Fenofibrate and rosiglitazone lower serum triglycerides with opposing effects on body weight. Biochem Biophys Res Commun. 2000 May 10;271(2):445-50. [Article]
- Casas F, Pineau T, Rochard P, Rodier A, Daury L, Dauca M, Cabello G, Wrutniak-Cabello C: New molecular aspects of regulation of mitochondrial activity by fenofibrate and fasting. FEBS Lett. 2000 Sep 29;482(1-2):71-4. [Article]
- Bouly M, Masson D, Gross B, Jiang XC, Fievet C, Castro G, Tall AR, Fruchart JC, Staels B, Lagrost L, Luc G: Induction of the phospholipid transfer protein gene accounts for the high density lipoprotein enlargement in mice treated with fenofibrate. J Biol Chem. 2001 Jul 13;276(28):25841-7. Epub 2001 May 7. [Article]
- Dana SL, Hoener PA, Bilakovics JM, Crombie DL, Ogilvie KM, Kauffman RF, Mukherjee R, Paterniti JR Jr: Peroxisome proliferator-activated receptor subtype-specific regulation of hepatic and peripheral gene expression in the Zucker diabetic fatty rat. Metabolism. 2001 Aug;50(8):963-71. [Article]
- Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
- Guerre-Millo M, Gervois P, Raspe E, Madsen L, Poulain P, Derudas B, Herbert JM, Winegar DA, Willson TM, Fruchart JC, Berge RK, Staels B: Peroxisome proliferator-activated receptor alpha activators improve insulin sensitivity and reduce adiposity. J Biol Chem. 2000 Jun 2;275(22):16638-42. [Article]
- Zhou Y, Zhang Y, Zhao D, Yu X, Shen X, Zhou Y, Wang S, Qiu Y, Chen Y, Zhu F: TTD: Therapeutic Target Database describing target druggability information. Nucleic Acids Res. 2024 Jan 5;52(D1):D1465-D1477. doi: 10.1093/nar/gkad751. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Partial agonist
- General Function
- Nuclear receptor that binds and is activated by variety of endogenous and xenobiotic compounds. Transcription factor that activates the transcription of multiple genes involved in the metabolism and secretion of potentially harmful xenobiotics, drugs and endogenous compounds. Activated by the antibiotic rifampicin and various plant metabolites, such as hyperforin, guggulipid, colupulone, and isoflavones. Response to specific ligands is species-specific. Activated by naturally occurring steroids, such as pregnenolone and progesterone. Binds to a response element in the promoters of the CYP3A4 and ABCB1/MDR1 genes
- Specific Function
- Dna-binding transcription activator activity, rna polymerase ii-specific
- Gene Name
- NR1I2
- Uniprot ID
- O75469
- Uniprot Name
- Nuclear receptor subfamily 1 group I member 2
- Molecular Weight
- 49761.245 Da
References
- Creusot N, Kinani S, Balaguer P, Tapie N, LeMenach K, Maillot-Marechal E, Porcher JM, Budzinski H, Ait-Aissa S: Evaluation of an hPXR reporter gene assay for the detection of aquatic emerging pollutants: screening of chemicals and application to water samples. Anal Bioanal Chem. 2010 Jan;396(2):569-83. doi: 10.1007/s00216-009-3310-y. Epub 2009 Nov 29. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- May activate progelatinase A
- Specific Function
- Metalloendopeptidase activity
- Gene Name
- MMP25
- Uniprot ID
- Q9NPA2
- Uniprot Name
- Matrix metalloproteinase-25
- Molecular Weight
- 62553.445 Da
References
- Duhaney TA, Cui L, Rude MK, Lebrasseur NK, Ngoy S, De Silva DS, Siwik DA, Liao R, Sam F: Peroxisome proliferator-activated receptor alpha-independent actions of fenofibrate exacerbates left ventricular dilation and fibrosis in chronic pressure overload. Hypertension. 2007 May;49(5):1084-94. Epub 2007 Mar 12. [Article]
- Lebrasseur NK, Duhaney TA, De Silva DS, Cui L, Ip PC, Joseph L, Sam F: Effects of fenofibrate on cardiac remodeling in aldosterone-induced hypertension. Hypertension. 2007 Sep;50(3):489-96. Epub 2007 Jul 2. [Article]
Enzymes
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Substrate
- General Function
- UDP-glucuronosyltransferase (UGT) that catalyzes phase II biotransformation reactions in which lipophilic substrates are conjugated with glucuronic acid to increase the metabolite's water solubility, thereby facilitating excretion into either the urine or bile (PubMed:12181437, PubMed:15470161, PubMed:15472229, PubMed:18004212, PubMed:18052087, PubMed:18674515, PubMed:19545173). Essential for the elimination and detoxification of drugs, xenobiotics and endogenous compounds (PubMed:12181437, PubMed:18004212). Catalyzes the glucuronidation of endogenous estrogen hormones such as estradiol and estrone (PubMed:15472229). Also catalyzes the glucuronidation of the isoflavones genistein, daidzein, glycitein, formononetin, biochanin A and prunetin, which are phytoestrogens with anticancer and cardiovascular properties (PubMed:18052087, PubMed:19545173). Involved in the glucuronidation of the AGTR1 angiotensin receptor antagonist caderastan, a drug which can inhibit the effect of angiotensin II (PubMed:18674515). Involved in the biotransformation of 7-ethyl-10-hydroxycamptothecin (SN-38), the pharmacologically active metabolite of the anticancer drug irinotecan (PubMed:12181437, PubMed:20610558). Also metabolizes mycophenolate, an immunosuppressive agent (PubMed:15470161, PubMed:18004212)
- Specific Function
- Enzyme binding
- Gene Name
- UGT1A9
- Uniprot ID
- O60656
- Uniprot Name
- UDP-glucuronosyltransferase 1A9
- Molecular Weight
- 59940.495 Da
References
- Williams JA, Hyland R, Jones BC, Smith DA, Hurst S, Goosen TC, Peterkin V, Koup JR, Ball SE: Drug-drug interactions for UDP-glucuronosyltransferase substrates: a pharmacokinetic explanation for typically observed low exposure (AUCi/AUC) ratios. Drug Metab Dispos. 2004 Nov;32(11):1201-8. doi: 10.1124/dmd.104.000794. Epub 2004 Aug 10. [Article]
- Barbier O, Villeneuve L, Bocher V, Fontaine C, Torra IP, Duhem C, Kosykh V, Fruchart JC, Guillemette C, Staels B: The UDP-glucuronosyltransferase 1A9 enzyme is a peroxisome proliferator-activated receptor alpha and gamma target gene. J Biol Chem. 2003 Apr 18;278(16):13975-83. Epub 2003 Feb 11. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Involved in the detoxification of xenobiotics and in the activation of ester and amide prodrugs (PubMed:18762277, PubMed:7980644, PubMed:9169443, PubMed:9490062). Hydrolyzes aromatic and aliphatic esters, but has no catalytic activity toward amides or a fatty acyl-CoA ester (PubMed:18762277, PubMed:7980644, PubMed:9169443, PubMed:9490062). Hydrolyzes the methyl ester group of cocaine to form benzoylecgonine (PubMed:7980644). Catalyzes the transesterification of cocaine to form cocaethylene (PubMed:7980644). Displays fatty acid ethyl ester synthase activity, catalyzing the ethyl esterification of oleic acid to ethyloleate (PubMed:7980644). Converts monoacylglycerides to free fatty acids and glycerol. Hydrolyzes of 2-arachidonoylglycerol and prostaglandins (PubMed:21049984). Hydrolyzes cellular cholesteryl esters to free cholesterols and promotes reverse cholesterol transport (RCT) by facilitating both the initial and final steps in the process (PubMed:11015575, PubMed:16024911, PubMed:16971496, PubMed:18762277). First of all, allows free cholesterol efflux from macrophages to extracellular cholesterol acceptors and secondly, releases free cholesterol from lipoprotein-delivered cholesteryl esters in the liver for bile acid synthesis or direct secretion into the bile (PubMed:16971496, PubMed:18599737, PubMed:18762277)
- Specific Function
- Carboxylesterase activity
- Gene Name
- CES1
- Uniprot ID
- P23141
- Uniprot Name
- Liver carboxylesterase 1
- Molecular Weight
- 62520.62 Da
References
- Laizure SC, Herring V, Hu Z, Witbrodt K, Parker RB: The role of human carboxylesterases in drug metabolism: have we overlooked their importance? Pharmacotherapy. 2013 Feb;33(2):210-22. doi: 10.1002/phar.1194. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- NADPH-dependent reductase with broad substrate specificity. Catalyzes the reduction of a wide variety of carbonyl compounds including quinones, prostaglandins, menadione, plus various xenobiotics. Catalyzes the reduction of the antitumor anthracyclines doxorubicin and daunorubicin to the cardiotoxic compounds doxorubicinol and daunorubicinol (PubMed:15799708, PubMed:17344335, PubMed:17912391, PubMed:18449627, PubMed:18826943, PubMed:1921984, PubMed:7005231). Can convert prostaglandin E to prostaglandin F2-alpha (By similarity). Can bind glutathione, which explains its higher affinity for glutathione-conjugated substrates. Catalyzes the reduction of S-nitrosoglutathione (PubMed:17344335, PubMed:18826943). In addition, participates in the glucocorticoid metabolism by catalyzing the NADPH-dependent cortisol/corticosterone into 20beta-dihydrocortisol (20b-DHF) or 20beta-corticosterone (20b-DHB), which are weak agonists of NR3C1 and NR3C2 in adipose tissue (PubMed:28878267)
- Specific Function
- 15-hydroxyprostaglandin dehydrogenase (nadp+) activity
- Gene Name
- CBR1
- Uniprot ID
- P16152
- Uniprot Name
- Carbonyl reductase [NADPH] 1
- Molecular Weight
- 30374.73 Da
References
- Malatkova P, Kanavi M, Nobilis M, Wsol V: In vitro metabolism of fenofibric acid by carbonyl reducing enzymes. Chem Biol Interact. 2016 Oct 25;258:153-8. doi: 10.1016/j.cbi.2016.09.001. Epub 2016 Sep 4. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- A cytochrome P450 monooxygenase involved in the metabolism of various endogenous substrates, including fatty acids, steroid hormones and vitamins (PubMed:11093772, PubMed:14559847, PubMed:15766564, PubMed:19965576, PubMed:7574697). Mechanistically, uses molecular oxygen inserting one oxygen atom into a substrate, and reducing the second into a water molecule, with two electrons provided by NADPH via cytochrome P450 reductase (NADPH--hemoprotein reductase) (PubMed:11093772, PubMed:14559847, PubMed:15766564, PubMed:19965576, PubMed:7574697). Primarily catalyzes the epoxidation of double bonds of polyunsaturated fatty acids (PUFA) with a preference for the last double bond (PubMed:15766564, PubMed:19965576, PubMed:7574697). Catalyzes the hydroxylation of carbon-hydrogen bonds. Metabolizes all trans-retinoic acid toward its 4-hydroxylated form (PubMed:11093772). Displays 16-alpha hydroxylase activity toward estrogen steroid hormones, 17beta-estradiol (E2) and estrone (E1) (PubMed:14559847). Plays a role in the oxidative metabolism of xenobiotics. It is the principal enzyme responsible for the metabolism of the anti-cancer drug paclitaxel (taxol) (PubMed:26427316)
- Specific Function
- Arachidonic acid epoxygenase activity
- Gene Name
- CYP2C8
- Uniprot ID
- P10632
- Uniprot Name
- Cytochrome P450 2C8
- Molecular Weight
- 55824.275 Da
References
- Walsky RL, Gaman EA, Obach RS: Examination of 209 drugs for inhibition of cytochrome P450 2C8. J Clin Pharmacol. 2005 Jan;45(1):68-78. [Article]
- Backman JT, Filppula AM, Niemi M, Neuvonen PJ: Role of Cytochrome P450 2C8 in Drug Metabolism and Interactions. Pharmacol Rev. 2016 Jan;68(1):168-241. doi: 10.1124/pr.115.011411. [Article]
- Gong Y, Shao Z, Fu Z, Edin ML, Sun Y, Liegl RG, Wang Z, Liu CH, Burnim SB, Meng SS, Lih FB, SanGiovanni JP, Zeldin DC, Hellstrom A, Smith LEH: Fenofibrate Inhibits Cytochrome P450 Epoxygenase 2C Activity to Suppress Pathological Ocular Angiogenesis. EBioMedicine. 2016 Nov;13:201-211. doi: 10.1016/j.ebiom.2016.09.025. Epub 2016 Sep 30. [Article]
- FDA Approved Drug Products: Fenofibrate Oral Tablets [Link]
- FDA Approved Drug Products: Fenofibrate Oral Capsules [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- A cytochrome P450 monooxygenase involved in the metabolism of polyunsaturated fatty acids (PUFA) (PubMed:18577768, PubMed:19965576, PubMed:20972997). Mechanistically, uses molecular oxygen inserting one oxygen atom into a substrate, and reducing the second into a water molecule, with two electrons provided by NADPH via cytochrome P450 reductase (NADPH--hemoprotein reductase) (PubMed:18577768, PubMed:19965576, PubMed:20972997). Catalyzes the hydroxylation of carbon-hydrogen bonds. Hydroxylates PUFA specifically at the omega-1 position (PubMed:18577768). Catalyzes the epoxidation of double bonds of PUFA (PubMed:19965576, PubMed:20972997). Also metabolizes plant monoterpenes such as limonene. Oxygenates (R)- and (S)-limonene to produce carveol and perillyl alcohol (PubMed:11950794). Responsible for the metabolism of a number of therapeutic agents such as the anticonvulsant drug S-mephenytoin, omeprazole, proguanil, certain barbiturates, diazepam, propranolol, citalopram and imipramine. Hydroxylates fenbendazole at the 4' position (PubMed:23959307)
- Specific Function
- (r)-limonene 6-monooxygenase activity
- Gene Name
- CYP2C19
- Uniprot ID
- P33261
- Uniprot Name
- Cytochrome P450 2C19
- Molecular Weight
- 55944.565 Da
References
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Exhibits a high coumarin 7-hydroxylase activity. Can act in the hydroxylation of the anti-cancer drugs cyclophosphamide and ifosphamide. Competent in the metabolic activation of aflatoxin B1. Constitutes the major nicotine C-oxidase. Acts as a 1,4-cineole 2-exo-monooxygenase. Possesses low phenacetin O-deethylation activity
- Specific Function
- Arachidonic acid epoxygenase activity
- Gene Name
- CYP2A6
- Uniprot ID
- P11509
- Uniprot Name
- Cytochrome P450 2A6
- Molecular Weight
- 56517.005 Da
References
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Cytosolic aldo-keto reductase that catalyzes the NADH and NADPH-dependent reduction of ketosteroids to hydroxysteroids (PubMed:19218247). Most probably acts as a reductase in vivo since the oxidase activity measured in vitro is inhibited by physiological concentrations of NADPH (PubMed:14672942). Displays a broad positional specificity acting on positions 3, 17 and 20 of steroids and regulates the metabolism of hormones like estrogens and androgens (PubMed:10998348). May also reduce conjugated steroids such as 5alpha-dihydrotestosterone sulfate (PubMed:19218247). Displays affinity for bile acids (PubMed:8486699)
- Specific Function
- 17-alpha,20-alpha-dihydroxypregn-4-en-3-one dehydrogenase activity
- Gene Name
- AKR1C1
- Uniprot ID
- Q04828
- Uniprot Name
- Aldo-keto reductase family 1 member C1
- Molecular Weight
- 36788.02 Da
References
- Malatkova P, Kanavi M, Nobilis M, Wsol V: In vitro metabolism of fenofibric acid by carbonyl reducing enzymes. Chem Biol Interact. 2016 Oct 25;258:153-8. doi: 10.1016/j.cbi.2016.09.001. Epub 2016 Sep 4. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Cytosolic aldo-keto reductase that catalyzes the NADH and NADPH-dependent reduction of ketosteroids to hydroxysteroids (PubMed:19218247). Most probably acts as a reductase in vivo since the oxidase activity measured in vitro is inhibited by physiological concentrations of NADPH (PubMed:14672942). Displays a broad positional specificity acting on positions 3, 17 and 20 of steroids and regulates the metabolism of hormones like estrogens and androgens (PubMed:10998348). Works in concert with the 5-alpha/5-beta-steroid reductases to convert steroid hormones into the 3-alpha/5-alpha and 3-alpha/5-beta-tetrahydrosteroids. Catalyzes the inactivation of the most potent androgen 5-alpha-dihydrotestosterone (5-alpha-DHT) to 5-alpha-androstane-3-alpha,17-beta-diol (3-alpha-diol) (PubMed:15929998, PubMed:17034817, PubMed:17442338, PubMed:8573067). Also specifically able to produce 17beta-hydroxy-5alpha-androstan-3-one/5alphaDHT (PubMed:10998348). May also reduce conjugated steroids such as 5alpha-dihydrotestosterone sulfate (PubMed:19218247). Displays affinity for bile acids (PubMed:8486699)
- Specific Function
- Aldose reductase (nadph) activity
- Gene Name
- AKR1C2
- Uniprot ID
- P52895
- Uniprot Name
- Aldo-keto reductase family 1 member C2
- Molecular Weight
- 36734.97 Da
References
- Malatkova P, Kanavi M, Nobilis M, Wsol V: In vitro metabolism of fenofibric acid by carbonyl reducing enzymes. Chem Biol Interact. 2016 Oct 25;258:153-8. doi: 10.1016/j.cbi.2016.09.001. Epub 2016 Sep 4. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Cytosolic aldo-keto reductase that catalyzes the NADH and NADPH-dependent reduction of ketosteroids to hydroxysteroids. Acts as a NAD(P)(H)-dependent 3-, 17- and 20-ketosteroid reductase on the steroid nucleus and side chain and regulates the metabolism of androgens, estrogens and progesterone (PubMed:10622721, PubMed:11165022, PubMed:7650035, PubMed:9415401, PubMed:9927279). Displays the ability to catalyze both oxidation and reduction in vitro, but most probably acts as a reductase in vivo since the oxidase activity measured in vitro is inhibited by physiological concentration of NADPH (PubMed:11165022, PubMed:14672942). Acts preferentially as a 17-ketosteroid reductase and has the highest catalytic efficiency of the AKR1C enzyme for the reduction of delta4-androstenedione to form testosterone (PubMed:20036328). Reduces prostaglandin (PG) D2 to 11beta-prostaglandin F2, progesterone to 20alpha-hydroxyprogesterone and estrone to 17beta-estradiol (PubMed:10622721, PubMed:10998348, PubMed:11165022, PubMed:15047184, PubMed:19010934, PubMed:20036328). Catalyzes the transformation of the potent androgen dihydrotestosterone (DHT) into the less active form, 5-alpha-androstan-3-alpha,17-beta-diol (3-alpha-diol) (PubMed:10557352, PubMed:10998348, PubMed:11165022, PubMed:14672942, PubMed:7650035, PubMed:9415401). Also displays retinaldehyde reductase activity toward 9-cis-retinal (PubMed:21851338)
- Specific Function
- 15-hydroxyprostaglandin-d dehydrogenase (nadp+) activity
- Gene Name
- AKR1C3
- Uniprot ID
- P42330
- Uniprot Name
- Aldo-keto reductase family 1 member C3
- Molecular Weight
- 36852.89 Da
References
- Malatkova P, Kanavi M, Nobilis M, Wsol V: In vitro metabolism of fenofibric acid by carbonyl reducing enzymes. Chem Biol Interact. 2016 Oct 25;258:153-8. doi: 10.1016/j.cbi.2016.09.001. Epub 2016 Sep 4. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Catalyzes the NADPH-dependent reduction of a wide variety of carbonyl-containing compounds to their corresponding alcohols. Displays enzymatic activity towards endogenous metabolites such as aromatic and aliphatic aldehydes, ketones, monosacharides, bile acids and xenobiotics substrates. Key enzyme in the polyol pathway, catalyzes reduction of glucose to sorbitol during hyperglycemia (PubMed:1936586). Reduces steroids and their derivatives and prostaglandins. Displays low enzymatic activity toward all-trans-retinal, 9-cis-retinal, and 13-cis-retinal (PubMed:12732097, PubMed:19010934, PubMed:8343525). Catalyzes the reduction of diverse phospholipid aldehydes such as 1-palmitoyl-2-(5-oxovaleroyl)-sn -glycero-3-phosphoethanolamin (POVPC) and related phospholipid aldehydes that are generated from the oxydation of phosphotidylcholine and phosphatdyleethanolamides (PubMed:17381426). Plays a role in detoxifying dietary and lipid-derived unsaturated carbonyls, such as crotonaldehyde, 4-hydroxynonenal, trans-2-hexenal, trans-2,4-hexadienal and their glutathione-conjugates carbonyls (GS-carbonyls) (PubMed:21329684)
- Specific Function
- Aldose reductase (nadph) activity
- Gene Name
- AKR1B1
- Uniprot ID
- P15121
- Uniprot Name
- Aldo-keto reductase family 1 member B1
- Molecular Weight
- 35853.125 Da
References
- Malatkova P, Kanavi M, Nobilis M, Wsol V: In vitro metabolism of fenofibric acid by carbonyl reducing enzymes. Chem Biol Interact. 2016 Oct 25;258:153-8. doi: 10.1016/j.cbi.2016.09.001. Epub 2016 Sep 4. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- Curator comments
- There are conflicting data in the literature regarding the severity of inhibition. Some studies suggest mild inhibition and some suggest moderate inhibition.
- General Function
- A cytochrome P450 monooxygenase involved in the metabolism of various endogenous substrates, including fatty acids and steroids (PubMed:12865317, PubMed:15766564, PubMed:19965576, PubMed:21576599, PubMed:7574697, PubMed:9435160, PubMed:9866708). Mechanistically, uses molecular oxygen inserting one oxygen atom into a substrate, and reducing the second into a water molecule, with two electrons provided by NADPH via cytochrome P450 reductase (NADPH--hemoprotein reductase) (PubMed:12865317, PubMed:15766564, PubMed:19965576, PubMed:21576599, PubMed:7574697, PubMed:9435160, PubMed:9866708). Catalyzes the epoxidation of double bonds of polyunsaturated fatty acids (PUFA) (PubMed:15766564, PubMed:19965576, PubMed:7574697, PubMed:9866708). Catalyzes the hydroxylation of carbon-hydrogen bonds. Metabolizes cholesterol toward 25-hydroxycholesterol, a physiological regulator of cellular cholesterol homeostasis (PubMed:21576599). Exhibits low catalytic activity for the formation of catechol estrogens from 17beta-estradiol (E2) and estrone (E1), namely 2-hydroxy E1 and E2 (PubMed:12865317). Catalyzes bisallylic hydroxylation and hydroxylation with double-bond migration of polyunsaturated fatty acids (PUFA) (PubMed:9435160, PubMed:9866708). Also metabolizes plant monoterpenes such as limonene. Oxygenates (R)- and (S)-limonene to produce carveol and perillyl alcohol (PubMed:11950794). Contributes to the wide pharmacokinetics variability of the metabolism of drugs such as S-warfarin, diclofenac, phenytoin, tolbutamide and losartan (PubMed:25994031)
- Specific Function
- (r)-limonene 6-monooxygenase activity
- Gene Name
- CYP2C9
- Uniprot ID
- P11712
- Uniprot Name
- Cytochrome P450 2C9
- Molecular Weight
- 55627.365 Da
References
- Prasad GS, Srisailam K, Sashidhar RB: Metabolic inhibition of meloxicam by specific CYP2C9 inhibitors in Cunninghamella blakesleeana NCIM 687: in silico and in vitro studies. Springerplus. 2016 Feb 24;5:166. doi: 10.1186/s40064-016-1794-4. eCollection 2016. [Article]
- Kim KY, Mancano MA: Fenofibrate potentiates warfarin effects. Ann Pharmacother. 2003 Feb;37(2):212-5. doi: 10.1177/106002800303700210. [Article]
- Fujino H, Yamada I, Shimada S, Hirano M, Tsunenari Y, Kojima J: Interaction between fibrates and statins--metabolic interactions with gemfibrozil. Drug Metabol Drug Interact. 2003;19(3):161-76. [Article]
Carriers
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Binder
- General Function
- Binds water, Ca(2+), Na(+), K(+), fatty acids, hormones, bilirubin and drugs (Probable). Its main function is the regulation of the colloidal osmotic pressure of blood (Probable). Major zinc transporter in plasma, typically binds about 80% of all plasma zinc (PubMed:19021548). Major calcium and magnesium transporter in plasma, binds approximately 45% of circulating calcium and magnesium in plasma (By similarity). Potentially has more than two calcium-binding sites and might additionally bind calcium in a non-specific manner (By similarity). The shared binding site between zinc and calcium at residue Asp-273 suggests a crosstalk between zinc and calcium transport in the blood (By similarity). The rank order of affinity is zinc > calcium > magnesium (By similarity). Binds to the bacterial siderophore enterobactin and inhibits enterobactin-mediated iron uptake of E.coli from ferric transferrin, and may thereby limit the utilization of iron and growth of enteric bacteria such as E.coli (PubMed:6234017). Does not prevent iron uptake by the bacterial siderophore aerobactin (PubMed:6234017)
- Specific Function
- Antioxidant activity
- Gene Name
- ALB
- Uniprot ID
- P02768
- Uniprot Name
- Albumin
- Molecular Weight
- 69365.94 Da
References
- Chapman MJ: Pharmacology of fenofibrate. Am J Med. 1987 Nov 27;83(5B):21-5. doi: 10.1016/0002-9343(87)90867-9. [Article]
Transporters
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Substrate
- General Function
- Catalyzes the transport of the major hydrophobic bile salts, such as taurine and glycine-conjugated cholic acid across the canalicular membrane of hepatocytes in an ATP-dependent manner, therefore participates in hepatic bile acid homeostasis and consequently to lipid homeostasis through regulation of biliary lipid secretion in a bile salts dependent manner (PubMed:15791618, PubMed:16332456, PubMed:18985798, PubMed:19228692, PubMed:20010382, PubMed:20398791, PubMed:22262466, PubMed:24711118, PubMed:29507376, PubMed:32203132). Transports taurine-conjugated bile salts more rapidly than glycine-conjugated bile salts (PubMed:16332456). Also transports non-bile acid compounds, such as pravastatin and fexofenadine in an ATP-dependent manner and may be involved in their biliary excretion (PubMed:15901796, PubMed:18245269)
- Specific Function
- Abc-type bile acid transporter activity
- Gene Name
- ABCB11
- Uniprot ID
- O95342
- Uniprot Name
- Bile salt export pump
- Molecular Weight
- 146405.83 Da
References
- Pedersen JM, Matsson P, Bergstrom CA, Hoogstraate J, Noren A, LeCluyse EL, Artursson P: Early identification of clinically relevant drug interactions with the human bile salt export pump (BSEP/ABCB11). Toxicol Sci. 2013 Dec;136(2):328-43. doi: 10.1093/toxsci/kft197. Epub 2013 Sep 6. [Article]
Drug created at June 13, 2005 13:24 / Updated at September 15, 2024 21:55