eslicarbazepine acetate Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
4303 236395-14-5

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • eslicarbazepine acetate
  • zebinix
  • exelief
  • aptiom
  • BIA 2-093
  • Sep-0002093
Eslicarbazepine acetate is extensively converted to eslicarbazepine, which is considered to be responsible for therapeutic effects in humans. The precise mechanism(s) by which eslicarbazepine exerts anticonvulsant activity is unknown but is thought to involve inhibition of voltage-gated sodium channels.
  • Molecular weight: 296.33
  • Formula: C17H16N2O3
  • CLOGP: 1.50
  • LIPINSKI: 0
  • HAC: 5
  • HDO: 1
  • TPSA: 72.63
  • ALOGS: -3.43
  • ROTB: 2
  • Status: ONP
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
0.80 g O

ADMET properties:

None

Approvals:

DateAgencyCompanyOrphan
Nov. 8, 2013 FDA SUNOVION PHARMS 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
Seizure 171.22 47.42 69 796 122985 46562212
Hyponatraemia 117.35 47.42 50 815 101282 46583915
Generalised tonic-clonic seizure 65.74 47.42 23 842 27099 46658098

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
Seizure 187.65 48.57 68 459 98407 29853544
Focal dyscognitive seizures 56.96 48.57 11 516 1302 29950649
Simple partial seizures 50.71 48.57 8 519 290 29951661

Pharmacologic Action:

SourceCodeDescription
ATC N03AF04 NERVOUS SYSTEM
ANTIEPILEPTICS
ANTIEPILEPTICS
Carboxamide derivatives
MeSH PA D000927 Anticonvulsants
MeSH PA D002317 Cardiovascular Agents
MeSH PA D002491 Central Nervous System Agents
MeSH PA D049990 Membrane Transport Modulators
MeSH PA D026941 Sodium Channel Blockers
MeSH PA D061567 Voltage-Gated Sodium Channel Blockers
FDA PE N0000008486 Decreased Central Nervous System Disorganized Electrical Activity
FDA MoA N0000185506 Cytochrome P450 3A4 Inducers
FDA MoA N0000182140 Cytochrome P450 2C19 Inhibitors

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Partial seizure indication 29753000

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 13.73 acidic

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
Sodium channel alpha subunit Ion channel BLOCKER CHEMBL CHEMBL

External reference:

IDSource
4033118 VUID
N0000190128 NUI
D09215 KEGG_DRUG
104746-04-5 SECONDARY_CAS_RN
4033116 VANDF
4033118 VANDF
C3693080 UMLSCUI
C2725260 UMLSCUI
CHEMBL87992 ChEMBL_ID
DB09119 DRUGBANK_ID
CHEMBL315985 ChEMBL_ID
179344 PUBCHEM_CID
C416835 MESH_SUPPLEMENTAL_RECORD_UI
C571001 MESH_SUPPLEMENTAL_RECORD_UI
8403 INN_ID
BEA68ZVB2K UNII
S5VXA428R4 UNII
9881504 PUBCHEM_CID
7350 IUPHAR_LIGAND_ID
DB14575 DRUGBANK_ID
1482501 RXNORM
207443 MMSL
29871 MMSL
d07507 MMSL
013276 NDDF
013277 NDDF
697998007 SNOMEDCT_US
700015007 SNOMEDCT_US
715615002 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Aptiom HUMAN PRESCRIPTION DRUG LABEL 1 63402-202 TABLET 200 mg ORAL NDA 32 sections
Aptiom HUMAN PRESCRIPTION DRUG LABEL 1 63402-204 TABLET 400 mg ORAL NDA 32 sections
Aptiom HUMAN PRESCRIPTION DRUG LABEL 1 63402-206 TABLET 600 mg ORAL NDA 32 sections
Aptiom HUMAN PRESCRIPTION DRUG LABEL 1 63402-208 TABLET 800 mg ORAL NDA 32 sections