Identification

Name
Fenofibrate
Accession Number
DB01039
Description

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
Thumb
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

Associated Conditions
Contraindications & Blackbox Warnings
Learn about our commercial Contraindications & Blackbox Warnings data.
Learn More
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

TargetActionsOrganism
APeroxisome proliferator-activated receptor alpha
agonist
Humans
UMatrix metalloproteinase-25
inhibitor
Humans
UNuclear receptor subfamily 1 group I member 2
partial agonist
Humans
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
Learn about our commercial Adverse Effects data.
Learn More
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

Affected organisms
  • Humans and other mammals
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.
DrugInteraction
AbacavirFenofibrate may decrease the excretion rate of Abacavir which could result in a higher serum level.
AbametapirThe serum concentration of Fenofibrate can be increased when it is combined with Abametapir.
AbataceptThe metabolism of Fenofibrate can be increased when combined with Abatacept.
AbemaciclibThe metabolism of Abemaciclib can be decreased when combined with Fenofibrate.
AcalabrutinibThe metabolism of Fenofibrate can be decreased when combined with Acalabrutinib.
AcarboseAcarbose may decrease the excretion rate of Fenofibrate which could result in a higher serum level.
AceclofenacAceclofenac may decrease the excretion rate of Fenofibrate which could result in a higher serum level.
AcemetacinAcemetacin may decrease the excretion rate of Fenofibrate which could result in a higher serum level.
AcenocoumarolThe metabolism of Acenocoumarol can be decreased when combined with Fenofibrate.
AcetaminophenThe metabolism of Fenofibrate can be increased when combined with Acetaminophen.
Additional Data Available
  • Extended Description
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    Extended description of the mechanism of action and particular properties of each drug interaction.

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  • Severity
    Severity
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    A severity rating for each drug interaction, from minor to major.

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  • Evidence Level
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  • Action
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Food Interactions
  • Take with food. Bioavailability is increased 2- to 3-fold when taken with food.

Products

Purchasing individual compounds or compound libraries for your research?
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Active Moieties
NameKindUNIICASInChI Key
Fenofibric acidprodrugBGF9MN2HU142017-89-0MQOBSOSZFYZQOK-UHFFFAOYSA-N
Product Images
International/Other Brands
Fenogal (SMB Laboratories) / Lipanthyl (Abbott) / Lipantil / Lipidil (lbirn)
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
AntaraCapsule130 mg/1OralOscient Pharmaceuticals Corporation2008-01-30Not applicableUS flag
AntaraCapsule130 mg/1OralPhysicians Total Care, Inc.2005-12-272011-06-30US flag
AntaraCapsule130 mg/1OralLupin Pharmaceuticals, Inc.2009-09-25Not applicableUS flag
AntaraCapsule90 mg/1OralLupin Pharmaceuticals, Inc.2013-11-01Not applicableUS flag
AntaraCapsule43 mg/1OralOscient Pharmaceuticals Corporation2008-01-30Not applicableUS flag
AntaraCapsule30 mg/1OralLupin Pharmaceuticals, Inc.2013-11-01Not applicableUS flag
AntaraCapsule43 mg/1OralLupin Pharmaceuticals, Inc.2009-09-25Not applicableUS flag
Feno-micro-200CapsuleOralPro Doc Limitee1999-08-272020-05-04Canada flag
FenofibrateCapsule50 mg/1OralH2-Pharma, LLC2014-05-052016-05-02US flag
FenofibrateCapsule100 mgOralAa Pharma Inc1996-10-02Not applicableCanada flag
Additional Data Available
  • Application Number
    Application Number
    Available for Purchase

    A unique ID assigned by the FDA when a product is submitted for approval by the labeller.

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  • Product Code
    Product Code
    Available for Purchase

    A governmentally-recognized ID which uniquely identifies the product within its regulatory market.

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Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
Aa-feno-microCapsuleOralAa Pharma Inc2001-02-21Not applicableCanada flag
Aa-feno-microCapsuleOralAa Pharma Inc1999-03-29Not applicableCanada flag
Apo-feno-superTabletOralApotex CorporationNot applicableNot applicableCanada flag
Apo-feno-superTabletOralApotex Corporation2006-04-21Not applicableCanada flag
Apo-feno-superTabletOralApotex Corporation2006-04-21Not applicableCanada flag
Ava-fenofibrate MicroCapsuleOralAvanstra Inc2011-08-222014-08-21Canada flag
Dom-fenofibrate MicroCapsuleOralDominion Pharmacal1999-12-162018-10-10Canada flag
Dom-fenofibrate SupraTabletOralDominion PharmacalNot applicableNot applicableCanada flag
Dom-fenofibrate SupraTabletOralDominion PharmacalNot applicableNot applicableCanada flag
FenofibrateTablet54 mg/1OralA-S Medication Solutions2018-07-20Not applicableUS flag
Additional Data Available
  • Application Number
    Application Number
    Available for Purchase

    A unique ID assigned by the FDA when a product is submitted for approval by the labeller.

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  • Product Code
    Product Code
    Available for Purchase

    A governmentally-recognized ID which uniquely identifies the product within its regulatory market.

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Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing EndRegionImage
CholibFenofibrate (145 mg) + Simvastatin (40 mg)Tablet, film coatedOralMylan Products Limited2013-08-26Not applicableEU flag
CholibFenofibrate (145 mg) + Simvastatin (40 mg)Tablet, film coatedOralMylan Products Limited2013-08-26Not applicableEU flag
CholibFenofibrate (145 mg) + Simvastatin (20 mg)Tablet, film coatedOralMylan Products Limited2013-08-26Not applicableEU flag
CholibFenofibrate (145 mg) + Simvastatin (20 mg)Tablet, film coatedOralMylan Products Limited2013-08-26Not applicableEU flag
CholibFenofibrate (145 mg) + Simvastatin (40 mg)Tablet, film coatedOralMylan Products Limited2013-08-26Not applicableEU flag
CholibFenofibrate (145 mg) + Simvastatin (20 mg)Tablet, film coatedOralMylan Products Limited2013-08-26Not applicableEU flag

Categories

ATC Codes
C10BA03 — Pravastatin and fenofibrateC10AB05 — FenofibrateC10BA09 — Rosuvastatin and fenofibrateC10BA04 — Simvastatin and fenofibrate
Drug Categories
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)

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
  1. 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. [PubMed:27594083]
  2. Chapman MJ: Pharmacology of fenofibrate. Am J Med. 1987 Nov 27;83(5B):21-5. doi: 10.1016/0002-9343(87)90867-9. [PubMed:3318449]
  3. 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. [PubMed:9515185]
  4. 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. [PubMed:2226216]
  5. 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. [PubMed:12582161]
  6. 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. [PubMed:23386599]
  7. 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. [PubMed:27599626]
  8. 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. [PubMed:19251819]
  9. Qi C, Zhu Y, Reddy JK: Peroxisome proliferator-activated receptors, coactivators, and downstream targets. Cell Biochem Biophys. 2000;32 Spring:187-204. [PubMed:11330046]
  10. FDA Approved Drug Products: Lipidil Fenofibrate Oral Capsules (Discontinued) [Link]
  11. FDA Approved Drug Products: Fenofibrate Oral Tablets [Link]
  12. FDA Approved Drug Products: Fenofibrate Oral Capsules [Link]
  13. Cayman Chemicals: Fenofibrate MSDS [Link]
Human Metabolome Database
HMDB0015173
KEGG Drug
D00565
KEGG Compound
C07586
PubChem Compound
3339
PubChem Substance
46507371
ChemSpider
3222
BindingDB
50085042
RxNav
8703
ChEBI
5001
ChEMBL
CHEMBL672
ZINC
ZINC000000584092
Therapeutic Targets Database
DAP000270
PharmGKB
PA449594
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
PDRhealth
PDRhealth Drug Page
Wikipedia
Fenofibrate
AHFS Codes
  • 24:06.06 — Fribic Acid Derivatives
FDA label
Download (283 KB)
MSDS
Download (19.3 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4CompletedBasic ScienceDiabetes / Diabetic Retinopathy (DR)1
4CompletedPreventionCholesterol, HDL1
4CompletedPreventionDyslipidemia / Type 2 Diabetes Mellitus1
4CompletedTreatmentAcute Coronary Syndromes (ACS) / High Cholesterol1
4CompletedTreatmentAtherogenic Dyslipidemia / Obesity Associated Disorder1
4CompletedTreatmentBMI >30 kg/m2 / Cardiovascular Heart Disease / Hypertriglyceridemias / Lipid Disorders1
4CompletedTreatmentCardiovascular Heart Disease / Dyslipidemia / Hypertriglyceridemias1
4CompletedTreatmentCoronary Heart Disease (CHD) / Hyperlipidemias1
4CompletedTreatmentDyslipidemia2
4CompletedTreatmentFenofibrate/Simvastatin Comparison1

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
FormRouteStrength
CapsuleOral130 mg/1
CapsuleOral30 mg/1
CapsuleOral43 mg/1
CapsuleOral90 mg/1
TabletOral
Tablet, film coatedOral
CapsuleOral200 MG
Capsule, extended releaseOral
TabletOral160 mg
Capsule, extended releaseOral250 MG
CapsuleOral134 mg/1
CapsuleOral200 mg/1
CapsuleOral67 mg/1
TabletOral145 mg/301
TabletOral160 mg/301
TabletOral54 mg/1
Tablet, coatedOral145 mg/1
Tablet, coatedOral160 mg/1
Tablet, coatedOral48 mg/1
Tablet, coatedOral54 mg/1
Tablet, film coatedOral145 mg/1
Tablet, film coatedOral160 mg/1
Tablet, film coatedOral48 mg/1
TabletOral145 MG
Capsule, gelatin coated200 mg
TabletOral120 mg/1
TabletOral40 mg/1
CapsuleOral
Capsule, coatedOral200 mg
CapsuleOral160 MG
Tablet, coatedOral145 MG
Tablet, coatedOral160 MG
Tablet, film coatedOral160 mg
CapsuleOral267 mg
Tablet, film coatedOral145 mg
Tablet, film coatedOral
CapsuleOral100 mg/1
CapsuleOral150 mg/1
CapsuleOral50 mg/1
Capsule, coated pellets250 mg
CapsuleOral100 MG
CapsuleOral250 MG
Tablet, film coatedOral54 mg/1
Capsule, coatedOral160 mg
CapsuleOral40 MG
Pellet250 mg
Capsule, coatedOral135 mg
CapsuleOral300 MG
TabletOral145 mg/1
TabletOral160 mg/1
TabletOral48 mg/1
TabletOral50 mg/1
Prices
Unit descriptionCostUnit
Triglide 160 mg tablet6.39USD tablet
Fenoglide 120 mg tablet5.17USD tablet
Antara 130 mg capsule5.13USD capsule
Tricor 145 mg tablet4.69USD tablet
Lipofen 150 mg capsule3.55USD capsule
Lofibra 200 mg capsule3.25USD capsule
Lofibra 160 mg tablet3.11USD tablet
Fenofibrate Micronized 200 mg capsule2.77USD capsule
Fenofibrate 160 mg2.47USD tablet
Fenofibrate 160 mg tablet2.38USD tablet
Lofibra 134 mg capsule2.03USD capsule
Antara 43 mg capsule1.8USD capsule
Fenofibrate Micronized 134 mg capsule1.79USD capsule
Fenoglide 40 mg tablet1.72USD tablet
Tricor 48 mg tablet1.63USD tablet
Triglide 50 mg tablet1.49USD tablet
Lipidil Supra 160 mg Tablet1.4USD tablet
Lofibra 67 mg capsule1.26USD capsule
Lipidil Micro 200 mg Capsule1.23USD capsule
Lipidil Supra 100 mg Tablet1.22USD tablet
Apo-Feno-Micro 200 mg Capsule1.14USD capsule
Fenofibrate Micro 200 mg Capsule1.14USD capsule
Mylan-Fenofibrate Micro 200 mg Capsule1.14USD capsule
Novo-Fenofibrate Micronized 200 mg Capsule1.14USD capsule
Pms-Fenofibrate Micro 200 mg Capsule1.14USD capsule
Ratio-Fenofibrate Mc 200 mg Capsule1.14USD capsule
Fenofibrate Micronized 67 mg capsule1.0USD capsule
Lofibra 54 mg tablet0.99USD tablet
Fenofibrate 54 mg tablet0.81USD tablet
Apo-Feno-Super 160 mg Tablet0.79USD tablet
Novo-Fenofibrate-S 160 mg Tablet0.79USD tablet
Sandoz Fenofibrate S 160 mg Tablet0.79USD tablet
Apo-Feno-Super 100 mg Tablet0.68USD tablet
Novo-Fenofibrate-S 100 mg Tablet0.68USD tablet
Sandoz Fenofibrate S 100 mg Tablet0.68USD tablet
Apo-Fenofibrate 100 mg Capsule0.64USD capsule
Apo-Feno-Micro 67 mg Capsule0.45USD capsule
Novo-Fenofibrate Micronized 67 mg Capsule0.45USD capsule
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)Region
US5145684No1992-09-082011-01-25US flag
CA2487054No2008-03-182023-05-23Canada flag
CA2219475No2002-07-092017-12-11Canada flag
US8124125No2012-02-282024-10-01US flag
US8481078No2013-07-092024-10-01US flag
US7658944No2010-02-092024-12-09US flag
US9173847No2015-11-032024-10-01US flag
US6277405No2001-08-212018-01-09US flag
US7037529No2006-05-022018-01-09US flag
US6074670No2000-06-132018-01-09US flag
US7041319No2006-05-092018-01-09US flag
US6652881No2003-11-252018-01-09US flag
US6589552No2003-07-082018-01-09US flag
US6696084No2004-02-242021-09-11US flag
US6375986No2002-04-232020-09-21US flag
US7320802No2008-01-222023-02-21US flag
US7276249No2007-10-022023-02-21US flag
US8026281No2011-09-272025-04-22US flag
US9314447No2016-04-192033-05-31US flag
US7863331No2011-01-042020-08-08US flag
US7101574No2006-09-052020-08-20US flag
Additional Data Available
  • Filed On
    Filed On
    Available for Purchase

    The date on which a patent was filed with the relevant government.

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Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)79-82FDA Label
logP5.2Wei et al, 2017
Predicted Properties
PropertyValueSource
Water Solubility0.000707 mg/mLALOGPS
logP4.86ALOGPS
logP5.28ChemAxon
logS-5.7ALOGPS
pKa (Strongest Basic)-4.9ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count3ChemAxon
Hydrogen Donor Count0ChemAxon
Polar Surface Area52.6 Å2ChemAxon
Rotatable Bond Count7ChemAxon
Refractivity97.13 m3·mol-1ChemAxon
Polarizability38.15 Å3ChemAxon
Number of Rings2ChemAxon
Bioavailability1ChemAxon
Rule of FiveNoChemAxon
Ghose FilterYesChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET Features
PropertyValueProbability
Human Intestinal Absorption+0.987
Blood Brain Barrier+0.9334
Caco-2 permeable+0.648
P-glycoprotein substrateNon-substrate0.5571
P-glycoprotein inhibitor INon-inhibitor0.5995
P-glycoprotein inhibitor IINon-inhibitor0.7632
Renal organic cation transporterNon-inhibitor0.9042
CYP450 2C9 substrateNon-substrate0.7897
CYP450 2D6 substrateNon-substrate0.9147
CYP450 3A4 substrateSubstrate0.6735
CYP450 1A2 substrateInhibitor0.7599
CYP450 2C9 inhibitorNon-inhibitor0.9071
CYP450 2D6 inhibitorNon-inhibitor0.9231
CYP450 2C19 inhibitorInhibitor0.7619
CYP450 3A4 inhibitorNon-inhibitor0.831
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.7088
Ames testNon AMES toxic0.9133
CarcinogenicityNon-carcinogens0.6373
BiodegradationNot ready biodegradable0.9918
Rat acute toxicity2.2250 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9887
hERG inhibition (predictor II)Non-inhibitor0.9083
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSNot Available
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available
LC-MS/MS Spectrum - LC-ESI-qTof , PositiveLC-MS/MSNot Available
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-001i-0090000000-f4e7816cd30c8701cce3
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-03di-0029000000-60bbd2de375b9b56ec55
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-001i-0190000000-6e83f7c906eaeb363caf
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-0019-0930000000-fccf28abf1a426a6949b
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-000i-0900000000-07739caadc1c26a7baaa
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-000i-0900000000-5045a0039b18e3d7dd9a
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-000i-1900000000-25a145c2138d34aa4b52
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-03di-0029000000-a98245ce05ccb6a6707e
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-001i-0190000000-4e9b3e71fc7960db389e
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-0019-0930000000-9d3908b5ee8b5f59218d
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-000i-0900000000-1090af5e239a872654d9
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-000i-0900000000-5dcab26837d06f9756f8
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-000i-1900000000-2663fed5f3ba78d3c7a5
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-001i-0090000000-4933bea6ce44715c6172
MS/MS Spectrum - , positiveLC-MS/MSsplash10-01qi-0595000000-d3c4c1cce3b5e1fbb33f
MS/MS Spectrum - , positiveLC-MS/MSsplash10-01qi-1594000000-9756f301ee5d44577654
MS/MS Spectrum - , positiveLC-MS/MSsplash10-000i-3920000000-91103d7fd9d1063bae9a
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-0019-0941000000-27e0cd2c4e952b499a9a

Targets

Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Agonist
General Function
Zinc ion binding
Specific 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 oleyleth...
Gene Name
PPARA
Uniprot ID
Q07869
Uniprot Name
Peroxisome proliferator-activated receptor alpha
Molecular Weight
52224.595 Da
References
  1. 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. [PubMed:10494028]
  2. 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. [PubMed:10799317]
  3. 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. [PubMed:11018525]
  4. 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. [PubMed:11342537]
  5. 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. [PubMed:11474486]
  6. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]
  7. 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. [PubMed:10828060]
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
  1. 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. [PubMed:17353509]
  2. 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. [PubMed:17606858]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Partial agonist
General Function
Zinc ion binding
Specific 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 an...
Gene Name
NR1I2
Uniprot ID
O75469
Uniprot Name
Nuclear receptor subfamily 1 group I member 2
Molecular Weight
49761.245 Da
References
  1. 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. [PubMed:20024649]

Enzymes

Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Substrate
General Function
Retinoic acid binding
Specific Function
UDPGT is of major importance in the conjugation and subsequent elimination of potentially toxic xenobiotics and endogenous compounds. This isoform has specificity for phenols. Isoform 2 lacks trans...
Gene Name
UGT1A9
Uniprot ID
O60656
Uniprot Name
UDP-glucuronosyltransferase 1-9
Molecular Weight
59940.495 Da
References
  1. 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. [PubMed:15304429]
  2. 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. [PubMed:12582161]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Triglyceride lipase activity
Specific Function
Involved in the detoxification of xenobiotics and in the activation of ester and amide prodrugs. Hydrolyzes aromatic and aliphatic esters, but has no catalytic activity toward amides or a fatty acy...
Gene Name
CES1
Uniprot ID
P23141
Uniprot Name
Liver carboxylesterase 1
Molecular Weight
62520.62 Da
References
  1. 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. [PubMed:23386599]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Prostaglandin-e2 9-reductase activity
Specific 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. ...
Gene Name
CBR1
Uniprot ID
P16152
Uniprot Name
Carbonyl reductase [NADPH] 1
Molecular Weight
30374.73 Da
References
  1. 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. [PubMed:27599626]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Steroid hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP2C8
Uniprot ID
P10632
Uniprot Name
Cytochrome P450 2C8
Molecular Weight
55824.275 Da
References
  1. 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. [PubMed:15601807]
  2. 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. [PubMed:26721703]
  3. 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. [PubMed:27720395]
  4. FDA Approved Drug Products: Fenofibrate Oral Tablets [Link]
  5. FDA Approved Drug Products: Fenofibrate Oral Capsules [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Steroid hydroxylase activity
Specific Function
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 im...
Gene Name
CYP2C19
Uniprot ID
P33261
Uniprot Name
Cytochrome P450 2C19
Molecular Weight
55930.545 Da
References
  1. FDA Approved Drug Products: Fenofibrate Oral Tablets [Link]
  2. FDA Approved Drug Products: Fenofibrate Oral Capsules [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Steroid hydroxylase activity
Specific 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. Const...
Gene Name
CYP2A6
Uniprot ID
P11509
Uniprot Name
Cytochrome P450 2A6
Molecular Weight
56501.005 Da
References
  1. FDA Approved Drug Products: Fenofibrate Oral Tablets [Link]
  2. FDA Approved Drug Products: Fenofibrate Oral Capsules [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Trans-1,2-dihydrobenzene-1,2-diol dehydrogenase activity
Specific Function
Converts progesterone to its inactive form, 20-alpha-dihydroxyprogesterone (20-alpha-OHP). In the liver and intestine, may have a role in the transport of bile. May have a role in monitoring the in...
Gene Name
AKR1C1
Uniprot ID
Q04828
Uniprot Name
Aldo-keto reductase family 1 member C1
Molecular Weight
36788.02 Da
References
  1. 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. [PubMed:27599626]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Trans-1,2-dihydrobenzene-1,2-diol dehydrogenase activity
Specific Function
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...
Gene Name
AKR1C2
Uniprot ID
P52895
Uniprot Name
Aldo-keto reductase family 1 member C2
Molecular Weight
36734.97 Da
References
  1. 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. [PubMed:27599626]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Trans-1,2-dihydrobenzene-1,2-diol dehydrogenase activity
Specific Function
Catalyzes the conversion of aldehydes and ketones to alcohols. Catalyzes the reduction of prostaglandin (PG) D2, PGH2 and phenanthrenequinone (PQ) and the oxidation of 9-alpha,11-beta-PGF2 to PGD2....
Gene Name
AKR1C3
Uniprot ID
P42330
Uniprot Name
Aldo-keto reductase family 1 member C3
Molecular Weight
36852.89 Da
References
  1. 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. [PubMed:27599626]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Glyceraldehyde oxidoreductase activity
Specific Function
Catalyzes the NADPH-dependent reduction of a wide variety of carbonyl-containing compounds to their corresponding alcohols with a broad range of catalytic efficiencies.
Gene Name
AKR1B1
Uniprot ID
P15121
Uniprot Name
Aldose reductase
Molecular Weight
35853.125 Da
References
  1. 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. [PubMed:27599626]
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
Steroid hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP2C9
Uniprot ID
P11712
Uniprot Name
Cytochrome P450 2C9
Molecular Weight
55627.365 Da
References
  1. 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. [PubMed:27026863]
  2. Kim KY, Mancano MA: Fenofibrate potentiates warfarin effects. Ann Pharmacother. 2003 Feb;37(2):212-5. doi: 10.1177/106002800303700210. [PubMed:12549950]
  3. 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. [PubMed:14682608]

Carriers

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Binder
General Function
Toxic substance binding
Specific Function
Serum albumin, the main protein of plasma, has a good binding capacity for water, Ca(2+), Na(+), K(+), fatty acids, hormones, bilirubin and drugs. Its main function is the regulation of the colloid...
Gene Name
ALB
Uniprot ID
P02768
Uniprot Name
Serum albumin
Molecular Weight
69365.94 Da
References
  1. Chapman MJ: Pharmacology of fenofibrate. Am J Med. 1987 Nov 27;83(5B):21-5. doi: 10.1016/0002-9343(87)90867-9. [PubMed:3318449]

Transporters

Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Substrate
General Function
Transporter activity
Specific Function
Involved in the ATP-dependent secretion of bile salts into the canaliculus of hepatocytes.
Gene Name
ABCB11
Uniprot ID
O95342
Uniprot Name
Bile salt export pump
Molecular Weight
146405.83 Da
References
  1. 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. [PubMed:24014644]

Drug created on June 13, 2005 07:24 / Updated on November 23, 2020 09:08

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