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

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 77.09 26.28 18 1459 3150 50600497
Vascular stent stenosis 68.37 26.28 12 1465 498 50603149
Coronary artery thrombosis 65.53 26.28 13 1464 1054 50602593
Carotid arteriosclerosis 60.66 26.28 12 1465 959 50602688
Arterial stenosis 60.51 26.28 11 1466 558 50603089
Helicobacter gastritis 55.70 26.28 12 1465 1458 50602189
Cor pulmonale acute 45.81 26.28 8 1469 322 50603325
Hepatic cyst 42.38 26.28 12 1465 4481 50599166
Cardiorenal syndrome 41.32 26.28 8 1469 571 50603076
Coronary artery stenosis 38.40 26.28 11 1466 4278 50599369
Acute coronary syndrome 33.69 26.28 12 1465 9362 50594285
Coronary artery occlusion 32.34 26.28 11 1466 7492 50596155
Glycosylated haemoglobin decreased 30.36 26.28 6 1471 476 50603171
Hallucinations, mixed 30.02 26.28 9 1468 4094 50599553
Thalamus haemorrhage 28.95 26.28 6 1471 604 50603043
Obstruction gastric 26.97 26.28 6 1471 843 50602804

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 40.08 24.43 22 1680 24363 29548462
Hypertriglyceridaemia 38.77 24.43 15 1687 7460 29565365
Hepatic function abnormal 32.76 24.43 23 1679 39236 29533589
Periorbital haemorrhage 28.28 24.43 5 1697 107 29572718
Diabetes mellitus 25.71 24.43 20 1682 39811 29533014
Blood creatine phosphokinase increased 25.35 24.43 20 1682 40624 29532201

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 53.80 23.20 17 3310 5196 64490209
Vascular stent stenosis 50.25 23.20 12 3315 1297 64494108
Hypertriglyceridaemia 47.99 23.20 19 3308 11186 64484219
Coronary artery thrombosis 45.36 23.20 13 3314 2856 64492549
Carotid arteriosclerosis 44.74 23.20 12 3315 2067 64493338
Arterial stenosis 44.49 23.20 11 3316 1374 64494031
Helicobacter gastritis 44.07 23.20 12 3315 2188 64493217
Hepatic function abnormal 43.97 23.20 32 3295 64281 64431124
Acute kidney injury 42.79 23.20 80 3247 449160 64046245
Pancreatitis acute 40.38 23.20 26 3301 42829 64452576
Cor pulmonale acute 36.19 23.20 8 3319 614 64494791
Rhabdomyolysis 35.95 23.20 33 3294 91693 64403712
Hepatic cyst 33.81 23.20 12 3315 5228 64490177
Cardiorenal syndrome 30.64 23.20 8 3319 1242 64494163
Hyperuricaemia 29.25 23.20 13 3314 10178 64485227
Blood creatine phosphokinase increased 28.83 23.20 24 3303 58534 64436871
Renal impairment 26.98 23.20 34 3293 134983 64360422
Acute coronary syndrome 26.71 23.20 15 3312 19295 64476110
Periorbital haemorrhage 25.62 23.20 5 3322 208 64495197
Glycosylated haemoglobin decreased 25.48 23.20 6 3321 610 64494795
Coronary artery stenosis 24.95 23.20 12 3315 11236 64484169
Cerebral infarction 24.85 23.20 19 3308 41025 64454380
Interstitial lung disease 23.43 23.20 27 3300 97705 64397700

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
003937 NDDF
319937007 SNOMEDCT_US
396025003 SNOMEDCT_US

Pharmaceutical products:

None