choline fenofibrate indications/contra

Stem definitionDrug idCAS RN
clofibrate derivatives 4505 42017-89-0

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • choline fenofibrate
  • fenofibric acid
  • procetofenic acid
metabolite of lipantyl; structure; salt of cholesterylamine & 2-(4-(p-chlorobenzoyl)phenoxy)2-methylpropionic acid
  • Molecular weight: 318.75
  • Formula: C17H15ClO4
  • CLOGP: 4.07
  • LIPINSKI: 0
  • HAC: 4
  • HDO: 1
  • TPSA: 63.60
  • ALOGS: -4.80
  • ROTB: 5

Drug dosage:

DoseUnitRoute
0.14 g O

Approvals:

DateAgencyCompanyOrphan
Dec. 15, 2008 FDA ABBVIE

FDA Adverse Event Reporting System

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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
Blood triglycerides increased 371.63 48.04 77 1099 4473 3380210
Blood creatinine increased 331.07 48.04 95 1081 21723 3362960
Myalgia 303.24 48.04 97 1079 31978 3352705
High density lipoprotein decreased 265.06 48.04 46 1130 1004 3383679
Hepatic enzyme increased 186.60 48.04 55 1121 13570 3371113
Rash 139.06 48.04 69 1107 70752 3313931
Low density lipoprotein increased 125.83 48.04 27 1149 1817 3382866
Rhabdomyolysis 117.26 48.04 40 1136 15689 3368994
Blood creatine phosphokinase increased 116.53 48.04 38 1138 12975 3371708
Pancreatitis 86.04 48.04 31 1145 14214 3370469
Liver function test abnormal 85.19 48.04 30 1146 12871 3371812
Nausea 74.96 48.04 58 1118 129587 3255096
Muscle spasms 60.78 48.04 29 1147 26874 3357809
Glomerular filtration rate decreased 57.18 48.04 15 1161 2376 3382307
Abdominal pain 53.76 48.04 32 1144 46193 3338490
Pruritus 50.79 48.04 31 1145 46802 3337881
Creatinine renal clearance increased 49.50 48.04 9 1167 254 3384429

Pharmacologic Action:

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SourceCodeDescription
ATC C10AB11 CARDIOVASCULAR SYSTEM
LIPID MODIFYING AGENTS
LIPID MODIFYING AGENTS, PLAIN
Fibrates
MeSH PA D000924 Anticholesteremic Agents
MeSH PA D000963 Antimetabolites
MeSH PA D000960 Hypolipidemic Agents
MeSH PA D057847 Lipid Regulating Agents
FDA EPC N0000175596 Peroxisome Proliferator Receptor alpha Agonist

Drug Use (View source of the data)

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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
Hypothyroidism contraindication 40930008 DOID:1459
Acute nephropathy contraindication 58574008
Hepatic failure contraindication 59927004
Diabetes mellitus contraindication 73211009 DOID:9351
Leukopenia contraindication 84828003 DOID:615
Chronic renal failure syndrome contraindication 90688005 DOID:784
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

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Dissociation levelDissociation constantType (acidic/basic)
pKa1 3.71 acidic

Orange Book patent data (new drug applications)

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Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
105MG FIBRICOR ARALEZ PHARMS INC N022418 Aug. 14, 2009 RX TABLET ORAL 7569612 Aug. 20, 2027 ADJUNCTIVE THERAPY TO DIET IN PATIENTS WITH HYPERLIPIDEMIAS
105MG FIBRICOR ARALEZ PHARMS INC N022418 Aug. 14, 2009 RX TABLET ORAL 7741373 Aug. 20, 2027 ADJUNCTIVE THERAPY TO DIET TO PATIENTS WITH HYPERTRIGLYCERIDEMIA
105MG FIBRICOR ARALEZ PHARMS INC N022418 Aug. 14, 2009 RX TABLET ORAL 7741374 Aug. 20, 2027 ADJUNCTIVE THERAPY TO DIET IN PATIENTS WITH ELEVATED CHOLESTEROL AND/OR LIPID LEVELS
105MG FIBRICOR ARALEZ PHARMS INC N022418 Aug. 14, 2009 RX TABLET ORAL 7741374 Aug. 20, 2027 ADJUNCTIVE THERAPY TO DIET IN PATIENTS WITH MIXED DYSLIPIDEMIA
105MG FIBRICOR ARALEZ PHARMS INC N022418 Aug. 14, 2009 RX TABLET ORAL 7915247 Aug. 20, 2027 ADJUNCTIVE THERAPY TO DIET IN PATIENTS WITH HYPERLIPIDEMIAS
105MG FIBRICOR ARALEZ PHARMS INC N022418 Aug. 14, 2009 RX TABLET ORAL 7915247 Aug. 20, 2027 ADJUNCTIVE THERAPY TO DIET IN PATIENTS WITH MIXED DYSLIPIDEMIA
105MG FIBRICOR ARALEZ PHARMS INC N022418 Aug. 14, 2009 RX TABLET ORAL 7915247 Aug. 20, 2027 ADJUNCTIVE THERAPY TO DIET TO PATIENTS WITH HYPERTRIGLYCERIDEMIA
35MG FIBRICOR ARALEZ PHARMS INC N022418 Aug. 14, 2009 RX TABLET ORAL 7569612 Aug. 20, 2027 ADJUNCTIVE THERAPY TO DIET IN PATIENTS WITH HYPERLIPIDEMIAS
35MG FIBRICOR ARALEZ PHARMS INC N022418 Aug. 14, 2009 RX TABLET ORAL 7741373 Aug. 20, 2027 ADJUNCTIVE THERAPY TO DIET TO PATIENTS WITH HYPERTRIGLYCERIDEMIA
35MG FIBRICOR ARALEZ PHARMS INC N022418 Aug. 14, 2009 RX TABLET ORAL 7741374 Aug. 20, 2027 ADJUNCTIVE THERAPY TO DIET IN PATIENTS WITH ELEVATED CHOLESTEROL AND/OR LIPID LEVELS
35MG FIBRICOR ARALEZ PHARMS INC N022418 Aug. 14, 2009 RX TABLET ORAL 7741374 Aug. 20, 2027 ADJUNCTIVE THERAPY TO DIET IN PATIENTS WITH MIXED DYSLIPIDEMIA
35MG FIBRICOR ARALEZ PHARMS INC N022418 Aug. 14, 2009 RX TABLET ORAL 7915247 Aug. 20, 2027 ADJUNCTIVE THERAPY TO DIET IN PATIENTS WITH HYPERLIPIDEMIAS
35MG FIBRICOR ARALEZ PHARMS INC N022418 Aug. 14, 2009 RX TABLET ORAL 7915247 Aug. 20, 2027 ADJUNCTIVE THERAPY TO DIET IN PATIENTS WITH MIXED DYSLIPIDEMIA
35MG FIBRICOR ARALEZ PHARMS INC N022418 Aug. 14, 2009 RX TABLET ORAL 7915247 Aug. 20, 2027 ADJUNCTIVE THERAPY TO DIET TO PATIENTS WITH HYPERTRIGLYCERIDEMIA

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

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TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Peroxisome proliferator-activated receptor alpha Nuclear hormone receptor AGONIST Ki 4.46 CHEMBL CHEMBL
Fatty acid-binding protein, intestinal Cytosolic other Ki 6 CHEMBL
Fatty acid-binding protein, liver Unclassified Kd 7.03 CHEMBL

External reference:

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IDSource
D08890 KEGG_DRUG
C2586675 UMLSCUI
4BMH7IZT98 UNII
8868 INN_ID
856676-23-8 SECONDARY_CAS_RN
CHEMBL981 ChEMBL_ID
CHEMBL1201745 ChEMBL_ID
C014892 MESH_SUPPLEMENTAL_RECORD_UI
C006012 MESH_SUPPLEMENTAL_RECORD_UI
1433887 RXNORM
012921 NDDF
DB13873 DRUGBANK_ID
11350701 PUBCHEM_CID

Pharmaceutical products:

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ProductCategoryIngredientsNDCFormQuantityRoute MarketingLabel
Trilipix HUMAN PRESCRIPTION DRUG LABEL 1 0074-3161 CAPSULE, DELAYED RELEASE 45 mg ORAL NDA 17 sections
Trilipix HUMAN PRESCRIPTION DRUG LABEL 1 0074-3162 CAPSULE, DELAYED RELEASE 135 mg ORAL NDA 17 sections
Trilipix HUMAN PRESCRIPTION DRUG LABEL 1 0074-9189 CAPSULE, DELAYED RELEASE 135 mg ORAL NDA 17 sections
Trilipix HUMAN PRESCRIPTION DRUG LABEL 1 0074-9642 CAPSULE, DELAYED RELEASE 45 mg ORAL NDA 17 sections
Fenofibric Acid HUMAN PRESCRIPTION DRUG LABEL 1 0115-1459 CAPSULE, DELAYED RELEASE 45 mg ORAL NDA 17 sections
Fenofibric Acid HUMAN PRESCRIPTION DRUG LABEL 1 0115-1460 CAPSULE, DELAYED RELEASE 135 mg ORAL NDA 17 sections
Fenofibric Acid HUMAN PRESCRIPTION DRUG LABEL 1 0115-1554 CAPSULE, DELAYED RELEASE 45 mg ORAL NDA 17 sections
Fenofibric Acid HUMAN PRESCRIPTION DRUG LABEL 1 0115-1555 CAPSULE, DELAYED RELEASE 135 mg ORAL NDA 17 sections
fenofibric acid HUMAN PRESCRIPTION DRUG LABEL 1 0228-2838 CAPSULE, DELAYED RELEASE 45 mg ORAL ANDA 18 sections
fenofibric acid HUMAN PRESCRIPTION DRUG LABEL 1 0228-2839 CAPSULE, DELAYED RELEASE 135 mg ORAL ANDA 18 sections
Fenofibric Acid HUMAN PRESCRIPTION DRUG LABEL 1 0378-2589 CAPSULE, DELAYED RELEASE PELLETS 45 mg ORAL ANDA 18 sections
Fenofibric Acid HUMAN PRESCRIPTION DRUG LABEL 1 0378-2590 CAPSULE, DELAYED RELEASE PELLETS 135 mg ORAL ANDA 18 sections
Fenofibric Acid HUMAN PRESCRIPTION DRUG LABEL 1 10370-209 CAPSULE, DELAYED RELEASE 45 mg ORAL ANDA 18 sections
Fenofibric Acid HUMAN PRESCRIPTION DRUG LABEL 1 10370-210 CAPSULE, DELAYED RELEASE 135 mg ORAL ANDA 18 sections
FIBRICOR HUMAN PRESCRIPTION DRUG LABEL 1 13310-101 TABLET 35 mg ORAL NDA 16 sections
FIBRICOR HUMAN PRESCRIPTION DRUG LABEL 1 13310-102 TABLET 105 mg ORAL NDA 16 sections
Fenofibric Acid HUMAN PRESCRIPTION DRUG LABEL 1 46708-244 CAPSULE, DELAYED RELEASE 45 mg ORAL ANDA 18 sections
Fenofibric Acid HUMAN PRESCRIPTION DRUG LABEL 1 46708-245 CAPSULE, DELAYED RELEASE 135 mg ORAL ANDA 18 sections
FIBRICOR HUMAN PRESCRIPTION DRUG LABEL 1 49708-101 TABLET 35 mg ORAL NDA 17 sections
FIBRICOR HUMAN PRESCRIPTION DRUG LABEL 1 49708-102 TABLET 105 mg ORAL NDA 17 sections
Fenofibric Acid HUMAN PRESCRIPTION DRUG LABEL 1 53489-677 TABLET 35 mg ORAL NDA authorized generic 17 sections
Fenofibric Acid HUMAN PRESCRIPTION DRUG LABEL 1 53489-678 TABLET 105 mg ORAL NDA authorized generic 17 sections
Trilipix HUMAN PRESCRIPTION DRUG LABEL 1 54868-5986 CAPSULE, DELAYED RELEASE 135 mg ORAL NDA 17 sections
Fenofibric Acid HUMAN PRESCRIPTION DRUG LABEL 1 60429-432 CAPSULE, DELAYED RELEASE 135 mg ORAL ANDA 18 sections
Fenofibric Acid HUMAN PRESCRIPTION DRUG LABEL 1 62332-244 CAPSULE, DELAYED RELEASE 45 mg ORAL ANDA 18 sections
Fenofibric Acid HUMAN PRESCRIPTION DRUG LABEL 1 62332-245 CAPSULE, DELAYED RELEASE 135 mg ORAL ANDA 18 sections
Fenofibric acid HUMAN PRESCRIPTION DRUG LABEL 1 68180-129 CAPSULE, DELAYED RELEASE 135 mg ORAL ANDA 18 sections
Fenofibric Acid HUMAN PRESCRIPTION DRUG LABEL 1 68382-077 CAPSULE, DELAYED RELEASE 45 mg ORAL NDA authorized generic 17 sections
Fenofibric Acid HUMAN PRESCRIPTION DRUG LABEL 1 68382-078 CAPSULE, DELAYED RELEASE 135 mg ORAL NDA authorized generic 17 sections
Fenofibric Acid HUMAN PRESCRIPTION DRUG LABEL 1 68382-232 CAPSULE, DELAYED RELEASE 45 mg ORAL NDA authorized generic 17 sections