bepotastine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |

Stem definitionDrug idCAS RN
antihistaminics 341 125602-71-3

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • bepotastine
  • bepotastine besilate
  • bepreve
  • bepotastine besylate
  • Molecular weight: 388.89
  • Formula: C21H25ClN2O3
  • CLOGP: 0.28
  • LIPINSKI: 0
  • HAC: 5
  • HDO: 1
  • TPSA: 62.66
  • ALOGS: -3.89
  • ROTB: 8

  • Status: OFP

  • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

None

ADMET properties:

PropertyValueReference
BA (Bioavailability) 85 %

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
kinase-safety-class ACVR2A,ACVR2B,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK5,CDK9,DYRK1B,EIF2AK3,EPHB4,ERBB2,GRK2,ITK,MAPK7,MAPKAPK2,NTRK2,PDK1,PDK2,PDK4,PIK3CB,PRKDC,SIK2,TEK,TGFBR1 26
kinase-selectivity-class AXL,EIF2AK3,GRK2,SIK2,STK33,TEK 6
pfas-class PFAS structural alert (1 = True, 0 = False) 0

Approvals:

DateAgencyCompanyOrphan
Sept. 8, 2009 FDA BAUSCH AND LOMB INC

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
Interstitial lung disease 26.92 25.35 15 1153 76390 90550889

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
Hepatic function abnormal 38.55 26.57 21 1073 51546 42568695
Interstitial lung disease 35.23 26.57 23 1071 78439 42541802
Nasal turbinate abnormality 27.59 26.57 4 1090 54 42620187

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
Interstitial lung disease 58.36 22.35 37 2403 139297 110447562
Hepatic function abnormal 56.58 22.35 31 2409 89264 110497595
Pemphigoid 35.08 22.35 14 2426 19693 110567166
Erythema multiforme 34.16 22.35 14 2426 21083 110565776
Neutrophil count decreased 33.71 22.35 25 2415 120916 110465943
Platelet count decreased 32.10 22.35 32 2408 230411 110356448
Drug eruption 29.53 22.35 17 2423 53642 110533217
Nasal turbinate abnormality 29.21 22.35 4 2436 41 110586818
Hypopituitarism 23.07 22.35 7 2433 4383 110582476

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
MeSH PA D018926 Anti-Allergic Agents
FDA EPC N0000175587 Histamine-1 Receptor Antagonist
CHEBI has role CHEBI:37955 H<small><sub>1</sub></small>-receptor antagonist
CHEBI has role CHEBI:50857 anti-allergic agent
CHEBI has role CHEBI:66981 ophthalmology drug
CHEBI has role CHEBI:50177 dermatologic drug

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

DiseaseRelationSNOMED_IDDOID
Allergic conjunctivitis indication 473460002 DOID:11204




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 3.54 acidic
pKa2 9.51 Basic
pKa3 4.25 Basic

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
Histamine H1 receptor GPCR ANTAGONIST DRUGBANK CHEMBL

External reference:

IDSource
4029223 VUID
N0000181653 NUI
D01654 KEGG_DRUG
658552 RXNORM
C2698371 UMLSCUI
CHEBI:71204 CHEBI
CHEMBL1201758 ChEMBL_ID
DB04890 DRUGBANK_ID
CHEMBL1201759 ChEMBL_ID
C108476 MESH_SUPPLEMENTAL_RECORD_UI
164522 PUBCHEM_CID
7466 IUPHAR_LIGAND_ID
C511534 MESH_SUPPLEMENTAL_RECORD_UI
7648 INN_ID
190786-44-8 SECONDARY_CAS_RN
HYD2U48IAS UNII
167734 MMSL
26713 MMSL
347164 MMSL
4029223 VANDF
4029224 VANDF
010865 NDDF
010866 NDDF
443616002 SNOMEDCT_US
707083009 SNOMEDCT_US
770926005 SNOMEDCT_US
HYD2U48IAS INXIGHT DRUGS

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Bepotastine Besilate HUMAN PRESCRIPTION DRUG LABEL 1 0378-7055 SOLUTION/ DROPS 15 mg OPHTHALMIC ANDA 24 sections
Bepotastine Besilate HUMAN PRESCRIPTION DRUG LABEL 1 0378-7055 SOLUTION/ DROPS 15 mg OPHTHALMIC ANDA 24 sections
Bepreve HUMAN PRESCRIPTION DRUG LABEL 1 24208-629 SOLUTION/ DROPS 15 mg OPHTHALMIC NDA 21 sections
Bepotastine Besilate HUMAN PRESCRIPTION DRUG LABEL 1 24208-630 SOLUTION/ DROPS 15 mg OPHTHALMIC NDA authorized generic 22 sections
Bepotastine Besilate Ophthalmic Solution 1.5% Human Prescription Drug Label 1 46708-598 SOLUTION/ DROPS 15 mg OPHTHALMIC ANDA 21 sections
BEPREVE HUMAN PRESCRIPTION DRUG LABEL 1 54868-6299 SOLUTION/ DROPS 15 mg OPHTHALMIC NDA 21 sections
Bepotastine Besilate Ophthalmic Solution 1.5% Human Prescription Drug Label 1 62332-598 SOLUTION/ DROPS 15 mg OPHTHALMIC ANDA 21 sections
Bepotastine Besilate HUMAN PRESCRIPTION DRUG LABEL 1 70069-711 SOLUTION 15 mg OPHTHALMIC ANDA 21 sections
Bepotastine Besilate HUMAN PRESCRIPTION DRUG LABEL 1 70069-712 SOLUTION 15 mg OPHTHALMIC ANDA 21 sections
Bepotastine Besilate HUMAN PRESCRIPTION DRUG LABEL 1 82260-630 SOLUTION/ DROPS 15 mg OPHTHALMIC NDA authorized generic 21 sections