Scroll

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

Stem definition	Drug id	CAS RN
clofibrate derivatives, peroxisome proliferator activated receptor-alpha(PPAR-alpha) agonists	362	41859-67-0

Description:

Molecule	Description
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

Molecule

Description

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:

Dose	Unit	Route
0.60	g	O

ADMET properties:

Property	Value	Reference
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:

Date	Agency	Company	Orphan
Jan. 1, 1978	YEAR INTRODUCED

FDA Adverse Event Reporting System (Female)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients 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 term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients 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 term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients 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:

Source	Code	Description
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|

Disease	Relation	SNOMED_ID	DOID
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 level	Dissociation constant	Type (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:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Peroxisome proliferator-activated receptor alpha	Nuclear hormone receptor	Q07869	PPARA_HUMAN	AGONIST	EC50	4.30	IUPHAR	IUPHAR
3-hydroxy-3-methylglutaryl-coenzyme A reductase	Enzyme	P04035	HMDH_HUMAN	INHIBITOR			SCIENTIFIC LITERATURE	SCIENTIFIC LITERATURE
Lipoprotein lipase	Enzyme	P06858	LIPL_HUMAN				WOMBAT-PK
Fatty acid-binding protein, intestinal	Cytosolic other	P12104	FABPI_HUMAN		Ki	4.48	CHEMBL
Peroxisome proliferator-activated receptor delta	Nuclear hormone receptor	Q03181	PPARD_HUMAN		EC50	4.45	CHEMBL
Peroxisome proliferator-activated receptor gamma	Nuclear hormone receptor	P37231	PPARG_HUMAN		EC50	4.18	WOMBAT-PK
Fatty acid-binding protein, liver	Unclassified		FABPL_RAT		Ki	4.35	CHEMBL

External reference:

ID	Source
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