bezafibrate 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
clofibrate derivatives, peroxisome proliferator activated receptor-alpha(PPAR-alpha) agonists 362 41859-67-0

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • bezafibrate
  • befizal
  • benzofibrate
  • difaterol
  • bezatol
  • bezalip
An antilipemic agent that lowers CHOLESTEROL and TRIGLYCERIDES. It decreases LOW DENSITY LIPOPROTEINS and increases HIGH DENSITY LIPOPROTEINS.
  • Molecular weight: 361.82
  • Formula: C19H20ClNO4
  • CLOGP: 3.70
  • LIPINSKI: 0
  • HAC: 5
  • HDO: 2
  • TPSA: 75.63
  • ALOGS: -5.37
  • ROTB: 7

Drug dosage:

DoseUnitRoute
0.60 g O

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 2 Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine) 40 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 23.69 µM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability) 99 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
S (Water solubility) 0.00 mg/mL Bocci G, Oprea TI, Benet LZ

Approvals:

DateAgencyCompanyOrphan
Jan. 1, 1978 YEAR INTRODUCED

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
Diverticular perforation 77.33 26.49 18 1616 3524 63483864
Vascular stent stenosis 68.90 26.49 12 1622 541 63486847
Coronary artery thrombosis 66.31 26.49 13 1621 1126 63486262
Arterial stenosis 61.33 26.49 11 1623 588 63486800
Carotid arteriosclerosis 60.60 26.49 12 1622 1094 63486294
Helicobacter gastritis 55.80 26.49 12 1622 1640 63485748
Cor pulmonale acute 45.18 26.49 8 1626 397 63486991
Hepatic cyst 42.24 26.49 12 1622 5142 63482246
Cardiorenal syndrome 39.02 26.49 8 1626 867 63486521
Coronary artery stenosis 38.67 26.49 11 1623 4733 63482655
Acute coronary syndrome 34.26 26.49 12 1622 10114 63477274
Coronary artery occlusion 32.75 26.49 11 1623 8180 63479208
Glycosylated haemoglobin decreased 30.15 26.49 6 1628 560 63486828
Hallucinations, mixed 29.69 26.49 9 1625 4820 63482568
Thalamus haemorrhage 28.80 26.49 6 1628 703 63486685

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
Pancreatitis acute 37.51 24.74 22 1952 28119 34926838
Hypertriglyceridaemia 37.25 24.74 15 1959 8433 34946524
Hepatic function abnormal 30.61 24.74 23 1951 44340 34910617
Periorbital haemorrhage 28.38 24.74 5 1969 107 34954850
Blood creatine phosphokinase increased 28.19 24.74 22 1952 44835 34910122
Brain stem ischaemia 25.95 24.74 5 1969 177 34954780
Renal impairment 25.57 24.74 29 1945 94484 34860473
Cerebral infarction 25.32 24.74 17 1957 27438 34927519
Diabetes mellitus 25.23 24.74 21 1953 46852 34908105

FDA Adverse Event Reporting System (Geriatric)

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
Diverticular perforation 57.37 22.20 18 3747 5875 79734748
Vascular stent stenosis 49.47 22.20 12 3753 1515 79739108
Hypertriglyceridaemia 47.25 22.20 19 3746 12721 79727902
Coronary artery thrombosis 45.47 22.20 13 3752 3093 79737530
Hepatic function abnormal 45.07 22.20 33 3732 73074 79667549
Arterial stenosis 45.06 22.20 11 3754 1425 79739198
Helicobacter gastritis 43.84 22.20 12 3753 2437 79738186
Carotid arteriosclerosis 42.88 22.20 12 3753 2644 79737979
Acute kidney injury 41.95 22.20 82 3683 519322 79221301
Pancreatitis acute 39.00 22.20 26 3739 49578 79691045
Cor pulmonale acute 36.00 22.20 8 3757 688 79739935
Rhabdomyolysis 35.12 22.20 33 3732 103098 79637525
Blood creatine phosphokinase increased 34.46 22.20 27 3738 66063 79674560
Hepatic cyst 33.08 22.20 12 3753 6077 79734546
Renal impairment 29.87 22.20 37 3728 157746 79582877
Cardiorenal syndrome 29.44 22.20 8 3757 1581 79739042
Interstitial lung disease 29.06 22.20 31 3734 112569 79628054
Hyperuricaemia 28.53 22.20 13 3752 11786 79728837
Cerebral infarction 26.74 22.20 20 3745 45656 79694967
Acute coronary syndrome 26.68 22.20 15 3750 21118 79719505
Glycosylated haemoglobin decreased 25.23 22.20 6 3759 696 79739927
Periorbital haemorrhage 24.86 22.20 5 3760 266 79740357
Coronary artery stenosis 24.77 22.20 12 3753 12472 79728151
Diabetes mellitus 24.62 22.20 24 3741 78366 79662257
Blood triglycerides increased 24.06 22.20 14 3751 21026 79719597
Erythema multiforme 23.57 22.20 13 3752 17638 79722985
Primary mediastinal large B-cell lymphoma stage IV 22.73 22.20 3 3762 9 79740614
Coronary artery occlusion 22.45 22.20 12 3753 15303 79725320

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC C10AB02 CARDIOVASCULAR SYSTEM
LIPID MODIFYING AGENTS
LIPID MODIFYING AGENTS, PLAIN
Fibrates
MeSH PA D000963 Antimetabolites
MeSH PA D000960 Hypolipidemic Agents
MeSH PA D057847 Lipid Regulating Agents
CHEBI has role CHEBI:35679 antilipemic drugs
CHEBI has role CHEBI:35703 Xenobiotic
CHEBI has role CHEBI:78298 environmental contaminants
CHEBI has role CHEBI:176497 geroprotectors

Drug Use | Suggest Off label Use Form| |View source of the data|

DiseaseRelationSNOMED_IDDOID
Hypercholesterolemia indication 13644009
Hyperlipidemia indication 55822004 DOID:1168
End stage renal disease contraindication 46177005 DOID:784




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 3.71 acidic
pKa2 12.78 acidic

Orange Book patent data (new drug applications)

None

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 EC50 4.30 IUPHAR IUPHAR
3-hydroxy-3-methylglutaryl-coenzyme A reductase Enzyme INHIBITOR SCIENTIFIC LITERATURE SCIENTIFIC LITERATURE
Lipoprotein lipase Enzyme WOMBAT-PK
Fatty acid-binding protein, intestinal Cytosolic other Ki 4.48 CHEMBL
Peroxisome proliferator-activated receptor delta Nuclear hormone receptor EC50 4.45 CHEMBL
Peroxisome proliferator-activated receptor gamma Nuclear hormone receptor EC50 4.18 WOMBAT-PK
Fatty acid-binding protein, liver Unclassified Ki 4.35 CHEMBL

External reference:

IDSource
N0000166742 NUI
D01366 KEGG_DRUG
1525 RXNORM
C0005330 UMLSCUI
CHEBI:47612 CHEBI
PEM PDB_CHEM_ID
CHEMBL264374 ChEMBL_ID
DB01393 DRUGBANK_ID
D001629 MESH_DESCRIPTOR_UI
39042 PUBCHEM_CID
2668 IUPHAR_LIGAND_ID
3968 INN_ID
Y9449Q51XH UNII
319937007 SNOMEDCT_US
396025003 SNOMEDCT_US
003937 NDDF

Pharmaceutical products:

None