fenofibrate Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
clofibrate derivatives, peroxisome proliferator activated receptor-alpha(PPAR-alpha) agonists 1152 49562-28-9

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • fenofibrate
  • clorofibrate
  • fenobrate
  • lipofene
  • procetofen
  • procetofene
An antilipemic agent which reduces both CHOLESTEROL and TRIGLYCERIDES in the blood.
  • Molecular weight: 360.83
  • Formula: C20H21ClO4
  • CLOGP: 5.23
  • LIPINSKI: 1
  • HAC: 4
  • HDO: 0
  • TPSA: 52.60
  • ALOGS: -5.71
  • ROTB: 7

  • Status: OFP

  • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
0.20 g O

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 2 Benet LZ, Broccatelli F, Oprea TI
S (Water solubility) 0.00 mg/mL Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine) 0.10 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 5.74 ┬ÁM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD

Approvals:

DateAgencyCompanyOrphan
Dec. 31, 1993 FDA ABBVIE

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Rhabdomyolysis 272.81 49.20 65 890 6639 2350491
Acute kidney injury 247.41 49.20 82 873 28040 2329090
Myalgia 176.83 49.20 61 894 23272 2333858
Drug interaction 138.17 49.20 54 901 29109 2328021
Drug hypersensitivity 132.59 49.20 60 895 46583 2310547
Hepatic function abnormal 114.28 49.20 32 923 6060 2351070
Blood creatine phosphokinase increased 110.26 49.20 30 925 5106 2352024
Cholestasis 105.00 49.20 27 928 3694 2353436
Hepatitis 99.57 49.20 29 926 6308 2350822
Myopathy 89.24 49.20 20 935 1523 2355607
Pancreatitis acute 84.94 49.20 23 932 3830 2353300
Jaundice 76.81 49.20 23 932 5485 2351645
Hepatocellular injury 70.05 49.20 20 935 4035 2353095
Completed suicide 68.82 49.20 30 925 21004 2336126
Pyrexia 67.35 49.20 40 915 53668 2303462
Photosensitivity reaction 65.43 49.20 17 938 2410 2354720
Renal impairment 63.14 49.20 23 932 10069 2347061
Alkalosis hypochloraemic 61.93 49.20 8 947 15 2357115
Myoglobin blood increased 60.51 49.20 11 944 287 2356843
Somnolence 59.40 49.20 28 927 23457 2333673
Agranulocytosis 59.35 49.20 17 938 3465 2353665
International normalised ratio increased 58.38 49.20 20 935 7316 2349814
High density lipoprotein decreased 58.35 49.20 11 944 352 2356778
Aspartate aminotransferase increased 58.15 49.20 23 932 12589 2344541
Renal failure 57.54 49.20 25 930 17324 2339806
Lichen nitidus 57.24 49.20 7 948 6 2357124
Rash 56.07 49.20 37 918 59521 2297609
Alanine aminotransferase increased 55.77 49.20 23 932 14009 2343121
Lichenoid keratosis 52.25 49.20 10 945 347 2356783
Hyponatraemia 50.10 49.20 21 934 13304 2343826
Haematoma muscle 49.56 49.20 7 948 32 2357098

FDA Adverse Event Reporting System (Male)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Rhabdomyolysis 253.37 35.81 76 904 11014 1734787
High density lipoprotein decreased 239.08 35.81 43 937 615 1745186
Blood creatine phosphokinase increased 211.93 35.81 63 917 8793 1737008
Drug interaction 201.92 35.81 81 899 27877 1717924
Pancreatitis acute 156.11 35.81 42 938 4045 1741756
Myalgia 128.59 35.81 50 930 15608 1730193
Acute kidney injury 112.94 35.81 58 922 34886 1710915
Liver disorder 108.34 35.81 34 946 5602 1740199
Completed suicide 92.45 35.81 40 940 16272 1729529
Myopathy 85.17 35.81 22 958 1791 1744010
Renal failure 84.60 35.81 40 940 19977 1725824
Alanine aminotransferase increased 82.47 35.81 34 946 12244 1733557
Renal impairment 82.38 35.81 34 946 12280 1733521
Aspartate aminotransferase increased 79.81 35.81 32 948 10724 1735077
Hepatic function abnormal 77.56 35.81 28 952 7046 1738755
Drug-induced liver injury 76.87 35.81 23 957 3214 1742587
Blood triglycerides increased 72.82 35.81 21 959 2579 1743222
Ependymoma 69.89 35.81 10 970 26 1745775
Liver function test abnormal 67.78 35.81 24 956 5702 1740099
Hepatitis 63.35 35.81 22 958 4933 1740868
Chondrocalcinosis 51.49 35.81 8 972 42 1745759
Photosensitivity reaction 48.37 35.81 14 966 1736 1744065
Jaundice 48.23 35.81 19 961 6043 1739758
Gamma-glutamyltransferase increased 47.77 35.81 18 962 5080 1740721
Drug hypersensitivity 45.32 35.81 24 956 15111 1730690
Agranulocytosis 42.30 35.81 15 965 3561 1742240
Blood creatinine increased 41.41 35.81 22 958 13924 1731877
Myositis 40.66 35.81 12 968 1591 1744210
Pyrexia 38.34 35.81 33 947 46367 1699434
Lung disorder 37.07 35.81 15 965 5104 1740697

Pharmacologic Action:

SourceCodeDescription
ATC C10AB05 CARDIOVASCULAR SYSTEM
LIPID MODIFYING AGENTS
LIPID MODIFYING AGENTS, PLAIN
Fibrates
ATC C10BA03 CARDIOVASCULAR SYSTEM
LIPID MODIFYING AGENTS
LIPID MODIFYING AGENTS, COMBINATIONS
HMG CoA reductase inhibitors in combination with other lipid modifying agents
ATC C10BA04 CARDIOVASCULAR SYSTEM
LIPID MODIFYING AGENTS
LIPID MODIFYING AGENTS, COMBINATIONS
HMG CoA reductase inhibitors in combination with other lipid modifying agents
ATC C10BA09 CARDIOVASCULAR SYSTEM
LIPID MODIFYING AGENTS
LIPID MODIFYING AGENTS, COMBINATIONS
HMG CoA reductase inhibitors in combination with other lipid modifying agents
FDA EPC N0000175596 Peroxisome Proliferator Receptor alpha Agonist
FDA MoA N0000175375 Peroxisome Proliferator-activated Receptor alpha Agonists
FDA CS M0199111 PPAR alpha
MeSH PA D000963 Antimetabolites
MeSH PA D000960 Hypolipidemic Agents
MeSH PA D057847 Lipid Regulating Agents
CHEBI has role CHEBI:35679 antilipemic drug

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Hypercholesterolemia indication 13644009
Hyperlipidemia indication 55822004 DOID:1168
Hypoalphalipoproteinemia indication 190785000
Familial hypercholesterolemia - heterozygous indication 238079002
Mixed hyperlipidemia indication 267434003
Hypertriglyceridemia indication 302870006
Agranulocytosis contraindication 17182001 DOID:12987
Myositis contraindication 26889001 DOID:633
Primary biliary cirrhosis contraindication 31712002 DOID:12236
Disorder of gallbladder contraindication 39621005 DOID:0060262
Acute nephropathy contraindication 58574008
Hepatic failure contraindication 59927004
Leukopenia contraindication 84828003 DOID:615
Disorder of muscle contraindication 129565002 DOID:423
Liver function tests abnormal contraindication 166603001
Acute pancreatitis contraindication 197456007 DOID:2913
Impaired renal function disorder contraindication 197663003
Disease of liver contraindication 235856003 DOID:409
Rhabdomyolysis contraindication 240131006
Calculus in biliary tract contraindication 266474003
Anemia contraindication 271737000 DOID:2355
Thrombocytopenic disorder contraindication 302215000 DOID:1588
Thromboembolic disorder contraindication 371039008
Breastfeeding (mother) contraindication 413712001

Acid dissociation constants calculated using MoKa v3.0.0

None

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
130MG ANTARA (MICRONIZED) LUPIN ATLANTIS N021695 Nov. 30, 2004 RX CAPSULE ORAL 7863331 Aug. 8, 2020 TREATING HYPERCHOLESTEROLEMIAS WITH REDUCTION OF FOOD EFFECT
130MG ANTARA (MICRONIZED) LUPIN ATLANTIS N021695 Nov. 30, 2004 RX CAPSULE ORAL 7863331 Aug. 8, 2020 TREATING HYPERTRIGLYCERIDEMIAS WITH REDUCTION OF FOOD EFFECT
43MG ANTARA (MICRONIZED) LUPIN ATLANTIS N021695 Nov. 30, 2004 RX CAPSULE ORAL 7863331 Aug. 8, 2020 TREATING HYPERCHOLESTEROLEMIAS WITH REDUCTION OF FOOD EFFECT
43MG ANTARA (MICRONIZED) LUPIN ATLANTIS N021695 Nov. 30, 2004 RX CAPSULE ORAL 7863331 Aug. 8, 2020 TREATING HYPERTRIGLYCERIDEMIAS WITH REDUCTION OF FOOD EFFECT
145MG TRICOR ABBVIE N021656 Nov. 5, 2004 RX TABLET ORAL 6375986 Sept. 21, 2020 ADJUNCTIVE THERAPY TO DIET IN ADULTS TO REDUCE LDL-C, TOTAL-C, TRIGLYCERIDES AND APO B, AND INCREASE HDL-C IN PATIENTS WITH PRIMARY HYPERCHOLESTEROLEMIA OR MIXED DYSLIPIDEMIA (TYPES IIA, IIB) AND TO TREAT HYPERTRIGLYCERIDEMIA (TYPES IV, V)
48MG TRICOR ABBVIE N021656 Nov. 5, 2004 RX TABLET ORAL 6375986 Sept. 21, 2020 ADJUNCTIVE THERAPY TO DIET IN ADULTS TO REDUCE LDL-C, TOTAL-C, TRIGLYCERIDES AND APO B, AND INCREASE HDL-C IN PATIENTS WITH PRIMARY HYPERCHOLESTEROLEMIA OR MIXED DYSLIPIDEMIA (TYPES IIA, IIB) AND TO TREAT HYPERTRIGLYCERIDEMIA (TYPES IV, V)
160MG TRIGLIDE SKYEPHARMA AG N021350 May 7, 2005 RX TABLET ORAL 6696084 Sept. 11, 2021 A METHOD OF TREATING DYSLIPIDEMIA AND DYSLIPOPROTEINEMIA USING A DOSAGE FORM THAT CAN PROVIDE AN EFFECTIVE AMOUNT OF FENOFIBRATE TO A PATIENT IN A FASTED STATE WHICH IS AT LEAST 90% OF THE AUC AMOUNT PROVIDED BY THE DOSAGE FORM
50MG TRIGLIDE SKYEPHARMA AG N021350 May 7, 2005 DISCN TABLET ORAL 6696084 Sept. 11, 2021 A METHOD OF TREATING DYSLIPIDEMIA AND DYSLIPOPROTEINEMIA USING A DOSAGE FORM THAT CAN PROVIDE AN EFFECTIVE AMOUNT OF FENOFIBRATE TO A PATIENT IN A FASTED STATE WHICH IS AT LEAST 90% OF THE AUC AMOUNT PROVIDED BY THE DOSAGE FORM
145MG TRICOR ABBVIE N021656 Nov. 5, 2004 RX TABLET ORAL 7320802 Feb. 21, 2023 ADJUNCTIVE THERAPY TO DIET IN ADULTS TO REDUCE LDL-C, TRIGLYCERIDES AND APO B, AND INCREASE HDL-C IN PATIENTS WITH PRIMARY HYPERCHOLESTEROLEMIA OR MIXED DYSLIPIDEMIA (TYPES IIA, IIB) AND TO TREAT HYPERTRIGLYCERIDEMIA (TYPES IV, V)
48MG TRICOR ABBVIE N021656 Nov. 5, 2004 RX TABLET ORAL 7320802 Feb. 21, 2023 ADJUNCTIVE THERAPY TO DIET IN ADULTS TO REDUCE LDL-C, TRIGLYCERIDES AND APO B, AND INCREASE HDL-C IN PATIENTS WITH PRIMARY HYPERCHOLESTEROLEMIA OR MIXED DYSLIPIDEMIA (TYPES IIA, IIB) AND TO TREAT HYPERTRIGLYCERIDEMIA (TYPES IV, V)
120MG FENOGLIDE SALIX N022118 Aug. 10, 2007 RX TABLET ORAL 8124125 Oct. 1, 2024 FOR REDUCING TOTAL CHOLESTEROL (TOTAL-C), LDL-C, APO-LIPOPROTEIN B, OR TOTAL TRIGLYCERIDES, AND TREATING HYPERTRIGLYCERIDEMIA
120MG FENOGLIDE SALIX N022118 Aug. 10, 2007 RX TABLET ORAL 8481078 Oct. 1, 2024 USE OF FENOFIBRATE FOR REDUCING ELEVATED TOTAL CHOLESTEROL (TOTAL-C), LDL-C, APO-LIPOPROTEIN B, OR TOTAL TRIGLYCERIDES
40MG FENOGLIDE SALIX N022118 Aug. 10, 2007 RX TABLET ORAL 8124125 Oct. 1, 2024 FOR REDUCING TOTAL CHOLESTEROL (TOTAL-C), LDL-C, APO-LIPOPROTEIN B, OR TOTAL TRIGLYCERIDES, AND TREATING HYPERTRIGLYCERIDEMIA
40MG FENOGLIDE SALIX N022118 Aug. 10, 2007 RX TABLET ORAL 8481078 Oct. 1, 2024 USE OF FENOFIBRATE FOR REDUCING ELEVATED TOTAL CHOLESTEROL (TOTAL-C), LDL-C, APO-LIPOPROTEIN B, OR TOTAL TRIGLYCERIDES
30MG ANTARA (MICRONIZED) LUPIN ATLANTIS N021695 Oct. 18, 2013 RX CAPSULE ORAL 8026281 April 22, 2025 TREATING PRIMARY HYPERCHOLESTEROLEMIA AND MIXED DYSLIPIDEMIA
30MG ANTARA (MICRONIZED) LUPIN ATLANTIS N021695 Oct. 18, 2013 RX CAPSULE ORAL 8026281 April 22, 2025 TREATING SEVERE HYPERTRIGLYCERIDEMIA
90MG ANTARA (MICRONIZED) LUPIN ATLANTIS N021695 Oct. 18, 2013 RX CAPSULE ORAL 8026281 April 22, 2025 TREATING PRIMARY HYPERCHOLESTEROLEMIA AND MIXED DYSLIPIDEMIA
90MG ANTARA (MICRONIZED) LUPIN ATLANTIS N021695 Oct. 18, 2013 RX CAPSULE ORAL 8026281 April 22, 2025 TREATING SEVERE HYPERTRIGLYCERIDEMIA
90MG ANTARA (MICRONIZED) LUPIN ATLANTIS N021695 Oct. 18, 2013 RX CAPSULE ORAL 9314447 May 31, 2033 TREATING PRIMARY HYPERCHOLESTEROLEMIA AND MIXED DYSLIPIDEMIA
90MG ANTARA (MICRONIZED) LUPIN ATLANTIS N021695 Oct. 18, 2013 RX CAPSULE ORAL 9314447 May 31, 2033 TREATING SEVERE HYPERTRIGLYCERIDEMIA

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Peroxisome proliferator-activated receptor alpha Nuclear hormone receptor AGONIST IC50 6 CHEMBL CHEMBL
5-hydroxytryptamine receptor 2A GPCR Ki 6.22 DRUG MATRIX
5-hydroxytryptamine receptor 2C GPCR Ki 5.91 DRUG MATRIX
D(3) dopamine receptor GPCR Ki 4.33 DRUG MATRIX
Beta-3 adrenergic receptor GPCR Ki 4.03 DRUG MATRIX
Sodium-dependent dopamine transporter Transporter Ki 5.16 DRUG MATRIX
Sodium-dependent noradrenaline transporter Transporter Ki 4.67 DRUG MATRIX
Acetylcholinesterase Enzyme IC50 4.81 DRUG MATRIX
Peroxisome proliferator-activated receptor gamma Nuclear hormone receptor EC50 6.24 CHEMBL
Adenosine receptor A3 GPCR Ki 5.49 DRUG MATRIX
Cruzipain Enzyme IC50 4.21 CHEMBL
Fatty acid-binding protein, liver Unclassified Kd 7.74 CHEMBL

External reference:

IDSource
4021098 VUID
N0000148554 NUI
C0033228 UMLSCUI
D00565 KEGG_DRUG
108603001 SNOMEDCT_US
4021098 VANDF
12032 MMSL
44688 MMSL
8703 RXNORM
386879008 SNOMEDCT_US
d04286 MMSL
003789 NDDF
CHEMBL672 ChEMBL_ID
DB01039 DRUGBANK_ID
U202363UOS UNII
3996 INN_ID
CHEBI:5001 CHEBI
D011345 MESH_DESCRIPTOR_UI
3339 PUBCHEM_CID
7186 IUPHAR_LIGAND_ID
DB13873 DRUGBANK_ID

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Tricor HUMAN PRESCRIPTION DRUG LABEL 1 0074-3173 TABLET 48 mg ORAL NDA 17 sections
Tricor HUMAN PRESCRIPTION DRUG LABEL 1 0074-3189 TABLET 145 mg ORAL NDA 17 sections
Tricor HUMAN PRESCRIPTION DRUG LABEL 1 0074-6122 TABLET 48 mg ORAL NDA 17 sections
Tricor HUMAN PRESCRIPTION DRUG LABEL 1 0074-6123 TABLET 145 mg ORAL NDA 17 sections
Fenofibrate HUMAN PRESCRIPTION DRUG LABEL 1 0093-2060 TABLET 145 mg ORAL NDA authorized generic 18 sections
Fenofibrate HUMAN PRESCRIPTION DRUG LABEL 1 0093-2061 TABLET 48 mg ORAL NDA authorized generic 18 sections
Fenofibrate HUMAN PRESCRIPTION DRUG LABEL 1 0093-7755 TABLET 48 mg ORAL NDA authorized generic 18 sections
Fenofibrate HUMAN PRESCRIPTION DRUG LABEL 1 0093-7756 TABLET 145 mg ORAL NDA authorized generic 18 sections
Fenofibrate HUMAN PRESCRIPTION DRUG LABEL 1 0115-0511 CAPSULE 67 mg ORAL ANDA 13 sections
Fenofibrate HUMAN PRESCRIPTION DRUG LABEL 1 0115-0522 CAPSULE 134 mg ORAL ANDA 13 sections
Fenofibrate HUMAN PRESCRIPTION DRUG LABEL 1 0115-0533 CAPSULE 200 mg ORAL ANDA 13 sections
Fenofibrate HUMAN PRESCRIPTION DRUG LABEL 1 0115-1522 TABLET 40 mg ORAL NDA authorized generic 17 sections
Fenofibrate HUMAN PRESCRIPTION DRUG LABEL 1 0115-1523 TABLET 120 mg ORAL NDA authorized generic 17 sections
FENOFIBRATE HUMAN PRESCRIPTION DRUG LABEL 1 0115-5511 TABLET 54 mg ORAL ANDA 17 sections
FENOFIBRATE HUMAN PRESCRIPTION DRUG LABEL 1 0115-5522 TABLET 160 mg ORAL ANDA 17 sections
FENOFIBRATE HUMAN PRESCRIPTION DRUG LABEL 1 0179-0091 TABLET 160 mg ORAL ANDA 13 sections
FENOFIBRATE HUMAN PRESCRIPTION DRUG LABEL 1 0179-0103 TABLET 54 mg ORAL ANDA 13 sections
Fenofibrate HUMAN PRESCRIPTION DRUG LABEL 1 0378-3065 TABLET, FILM COATED 48 mg ORAL ANDA 16 sections
Fenofibrate HUMAN PRESCRIPTION DRUG LABEL 1 0378-3066 TABLET, FILM COATED 145 mg ORAL ANDA 16 sections
Fenofibrate HUMAN PRESCRIPTION DRUG LABEL 1 0378-4390 TABLET 40 mg ORAL ANDA 16 sections
Fenofibrate HUMAN PRESCRIPTION DRUG LABEL 1 0378-4391 TABLET 120 mg ORAL ANDA 16 sections
Fenofibrate HUMAN PRESCRIPTION DRUG LABEL 1 0378-6088 CAPSULE 43 mg ORAL ANDA 17 sections
Fenofibrate HUMAN PRESCRIPTION DRUG LABEL 1 0378-6089 CAPSULE 130 mg ORAL ANDA 17 sections
Fenofibrate HUMAN PRESCRIPTION DRUG LABEL 1 0378-7100 TABLET, FILM COATED 54 mg ORAL ANDA 17 sections
Fenofibrate HUMAN PRESCRIPTION DRUG LABEL 1 0378-7101 TABLET, FILM COATED 160 mg ORAL ANDA 17 sections
Fenofibrate HUMAN PRESCRIPTION DRUG LABEL 1 0378-8628 CAPSULE 67 mg ORAL ANDA 12 sections
Fenofibrate HUMAN PRESCRIPTION DRUG LABEL 1 0378-8629 CAPSULE 134 mg ORAL ANDA 12 sections
Fenofibrate HUMAN PRESCRIPTION DRUG LABEL 1 0378-8630 CAPSULE 200 mg ORAL ANDA 12 sections
Fenofibrate HUMAN PRESCRIPTION DRUG LABEL 1 0615-7548 CAPSULE 200 mg ORAL ANDA 13 sections
Fenofibrate HUMAN PRESCRIPTION DRUG LABEL 1 0615-8165 TABLET 160 mg ORAL ANDA 16 sections