bezafibrate indications/contra

Stem definitionDrug idCAS RN
clofibrate derivatives 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

Approvals:

DateAgencyCompanyOrphan
Jan. 1, 1978 YEAR INTRODUCED

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
Rhabdomyolysis 106.22 65.51 22 83 15707 3370047

Pharmacologic Action:

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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 drug

Drug Use (View source of the data)

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

Acid dissociation constants calculated using MoKa v3.0.0

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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:

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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
Peroxisome proliferator-activated receptor gamma Nuclear hormone receptor EC50 4.18 WOMBAT-PK
Peroxisome proliferator-activated receptor delta Nuclear hormone receptor EC50 4.45 CHEMBL
Fatty acid-binding protein, intestinal Cytosolic other Ki 4.48 CHEMBL
Lipoprotein lipase Enzyme WOMBAT-PK
Fatty acid-binding protein, liver Unclassified Ki 4.35 CHEMBL

External reference:

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

Pharmaceutical products:

None