All FDA-approved EMA-approved PMDA-approved
Target Card Uniprot Example: P23975

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

Stem definition	Drug id	CAS RN
vasodilators	342	64706-54-3

Description:

Molecule

Description

Molfile Inchi Smiles Synonyms: bepridil hydrochloride hydrate bepridil hydrochloride bepridil dl-Bepridil (+/-)-Bepridil bepricol Org 5730 bepridil monohydrochloride monohydrate bepridil monohydrochloride cordium bepridil HCl

A long-acting calcium-blocking agent with significant anti-anginal activity. The drug produces significant coronary vasodilation and modest peripheral effects. It has antihypertensive and selective anti-arrhythmia activities and acts as a calmodulin antagonist. Molecular weight: 366.55 Formula: C24H34N2O CLOGP: 6.20 LIPINSKI: 1 HAC: 3 HDO: 0 TPSA: 15.71 ALOGS: -4.75 ROTB: 10 Status: OFM Legend: OFP - off patent OFM - off market ONP - on patent

Drug dosage:

Dose	Unit	Route
0.30	g	O

ADMET properties:

Property	Value	Reference
BDDCS (Biopharmaceutical Drug Disposition Classification System)	1	Benet LZ, Broccatelli F, Oprea TI
S (Water solubility)	5 mg/mL	Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine)	0.50 %	Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose)	18.20 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability)	61 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution)	10.10 L/kg	Lombardo F, Berellini G, Obach RS
CL (Clearance)	8.70 mL/min/kg	Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma)	0.00 %	Lombardo F, Berellini G, Obach RS
t_half (Half-life)	14.90 hours	Lombardo F, Berellini G, Obach RS

Approvals:

Date	Agency	Company	Orphan
Dec. 28, 1990	FDA

FDA Adverse Event Reporting System (Female)

None

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
Interstitial lung disease	97.12	43.85	31	255	65251	34891394

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
Interstitial lung disease	79.07	39.81	29	492	112571	79631296
Cardiac tamponade	51.66	39.81	12	509	9264	79734603

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	C08EA02	CARDIOVASCULAR SYSTEM CALCIUM CHANNEL BLOCKERS NON-SELECTIVE CALCIUM CHANNEL BLOCKERS Phenylalkylamine derivatives
CHEBI has role	CHEBI:35620	vasodilator agents
CHEBI has role	CHEBI:35674	antihypertensive drugs
CHEBI has role	CHEBI:38070	antiarrhythmic agent
CHEBI has role	CHEBI:38215	calcium channel blockers
MeSH PA	D000889	Anti-Arrhythmia Agents
MeSH PA	D000959	Antihypertensive Agents
MeSH PA	D002121	Calcium Channel Blockers
MeSH PA	D000077264	Calcium-Regulating Hormones and Agents
MeSH PA	D002317	Cardiovascular Agents
MeSH PA	D049990	Membrane Transport Modulators
MeSH PA	D014665	Vasodilator Agents

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

Disease	Relation	SNOMED_ID	DOID
Angina pectoris	indication	194828000

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	7.79	Basic
pKa2	3.96	Basic

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])	Mechanism action	Bioact source	MoA source
Voltage-dependent T-type calcium channel subunit alpha-1H	Ion channel	O95180	CAC1H_HUMAN	BLOCKER	Ki	5.15		WOMBAT-PK	CHEMBL
Voltage-dependent L-type calcium channel subunit alpha-1C	Ion channel	Q13936	CAC1C_HUMAN	BLOCKER				SCIENTIFIC LITERATURE	SCIENTIFIC LITERATURE
Voltage-dependent L-type calcium channel subunit alpha-1D	Ion channel	Q01668	CAC1D_HUMAN	BLOCKER				SCIENTIFIC LITERATURE	SCIENTIFIC LITERATURE
Voltage-dependent P/Q-type calcium channel subunit alpha-1A	Ion channel	O00555	CAC1A_HUMAN	BLOCKER	Ki	6.60		WOMBAT-PK
Potassium/sodium hyperpolarization-activated cyclic nucleotide-gated channel 4	Ion channel	Q9Y3Q4	HCN4_HUMAN		IC50	5.31		WOMBAT-PK
Sodium channel alpha subunits; brain (Types I, II, III)	Ion channel	P35498 Q99250 Q9NY46	SCN1A_HUMAN SCN2A_HUMAN SCN3A_HUMAN		IC50	6.08		CHEMBL
Potassium voltage-gated channel subfamily KQT member 4	Ion channel	P56696	KCNQ4_HUMAN	BLOCKER	IC50	5		IUPHAR
Sodium channel protein type 5 subunit alpha	Ion channel	Q14524	SCN5A_HUMAN					WOMBAT-PK
Potassium voltage-gated channel subfamily H member 2	Ion channel	Q12809	KCNH2_HUMAN		IC50	6.26		WOMBAT-PK
Lethal factor	Enzyme		LEF_BACAN		IC50	5.32		CHEMBL
Potassium channel subfamily T member 1	Ion channel		KCNT1_RAT	GATING INHIBITOR	IC50	6		IUPHAR
Voltage-dependent L-type calcium channel subunit alpha-1C	Ion channel		CAC1C_RABIT		IC50	4.66		CHEMBL

External reference:

ID	Source
4019549	VUID
N0000147653	NUI
D00631	KEGG_DRUG
74764-40-2	SECONDARY_CAS_RN
1436	RXNORM
C0005116	UMLSCUI
CHEBI:3061	CHEBI
BEP	PDB_CHEM_ID
CHEMBL1008	ChEMBL_ID
CHEMBL1200382	ChEMBL_ID
DB01244	DRUGBANK_ID
D015764	MESH_DESCRIPTOR_UI
2351	PUBCHEM_CID
2337	IUPHAR_LIGAND_ID
3465	INN_ID
755BO701MA	UNII
4267	MMSL
d00688	MMSL
108530004	SNOMEDCT_US
108531000	SNOMEDCT_US
372503006	SNOMEDCT_US
4019549	VANDF
4019631	VANDF
003562	NDDF
004519	NDDF

Pharmaceutical products:

None