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bepridil 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| vasodilators | 342 | 64706-54-3 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
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.
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 |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| kinase-safety-class | ACVR2A,ACVR2B,AKT1,AKT2,AKT3,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK4,CDK5,CDK9,DDR1,DYRK1B,EIF2AK3,EPHB4,ERBB2,FLT3,GRK2,ITK,JAK2,JAK3,MAP3K7,MAPK10,MAPK12,MAPK7,MAPKAPK2,MET,NTRK2,PDK2,PDK4,PDPK1,PIK3CB,PIM2,PRKDC,SIK2,SIK3,STK33,TEK,TGFBR1,TTK | 42 | |||
| kinase-selectivity-class | AXL,GRK2 | 2 | |||
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 |
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 | 98.46 | 38.10 | 34 | 366 | 78428 | 42542507 |
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 | 90.15 | 38.02 | 33 | 626 | 139301 | 110449339 |
| Cardiac tamponade | 50.36 | 38.02 | 12 | 647 | 11295 | 110577345 |
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:35554 | cardiovascular drug |
| CHEBI has role | CHEBI:35620 | vasodilator agent |
| CHEBI has role | CHEBI:35674 | antihypertensive agent |
| CHEBI has role | CHEBI:38070 | anti-arrhythmia drug |
| CHEBI has role | CHEBI:38215 | calcium channel blocker |
| MeSH PA | D000077264 | Calcium-Regulating Hormones and Agents |
| MeSH PA | D000889 | Anti-Arrhythmia Agents |
| MeSH PA | D000959 | Antihypertensive Agents |
| MeSH PA | D002121 | Calcium Channel Blockers |
| MeSH PA | D002317 | Cardiovascular Agents |
| MeSH PA | D014665 | Vasodilator Agents |
| MeSH PA | D049990 | Membrane Transport Modulators |
Related Drugs by ATC class:
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 | BLOCKER | Ki | 5.15 | WOMBAT-PK | CHEMBL | |||
| Voltage-dependent L-type calcium channel subunit alpha-1C | Ion channel | BLOCKER | SCIENTIFIC LITERATURE | SCIENTIFIC LITERATURE | |||||
| Voltage-dependent L-type calcium channel subunit alpha-1D | Ion channel | BLOCKER | SCIENTIFIC LITERATURE | SCIENTIFIC LITERATURE | |||||
| Potassium channel subfamily K member 2 | Ion channel | IC50 | 5.39 | CHEMBL | |||||
| Potassium voltage-gated channel subfamily KQT member 4 | Ion channel | BLOCKER | IC50 | 5 | IUPHAR | ||||
| Sodium channel protein type 5 subunit alpha | Ion channel | WOMBAT-PK | |||||||
| Potassium/sodium hyperpolarization-activated cyclic nucleotide-gated channel 4 | Ion channel | IC50 | 5.31 | WOMBAT-PK | |||||
| Sodium channel alpha subunits; brain (Types I, II, III) | Ion channel | IC50 | 6.08 | CHEMBL | |||||
| Potassium channel subfamily T member 1 | Ion channel | IC50 | 4.79 | CHEMBL | |||||
| Potassium voltage-gated channel subfamily H member 2 | Ion channel | IC50 | 6.26 | WOMBAT-PK | |||||
| Voltage-dependent P/Q-type calcium channel subunit alpha-1A | Ion channel | BLOCKER | Ki | 6.60 | WOMBAT-PK | ||||
| Lethal factor | Enzyme | IC50 | 5.32 | CHEMBL | |||||
| Voltage-dependent L-type calcium channel subunit alpha-1C | Ion channel | IC50 | 4.66 | CHEMBL | |||||
| Potassium channel subfamily T member 1 | Ion channel | GATING INHIBITOR | IC50 | 6 | IUPHAR |
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 |
| 4019549 | VANDF |
| 4019631 | VANDF |
| 003562 | NDDF |
| 004519 | NDDF |
| 108530004 | SNOMEDCT_US |
| 108531000 | SNOMEDCT_US |
| 372503006 | SNOMEDCT_US |
Pharmaceutical products:
None