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

Stem definitionDrug idCAS RN
tranquillizers, propanediol and pentanediol derivatives 5355 913088-80-9

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • ontozry
  • cenobamate
  • YKP3089
  • xcopri
The precise mechanism by which cenobamate exerts its therapeutic effects in patients with partial-onset seizures is unknown. Cenobamate has been demonstrated to reduce repetitive neuronal firing by inhibiting voltage-gated sodium currents. It is also a positive allosteric modulator of the gamma-aminobutyric acid (GABAA) ion channel.
  • Molecular weight: 267.67
  • Formula: C10H10ClN5O2
  • CLOGP: 1.25
  • LIPINSKI: 0
  • HAC: 7
  • HDO: 1
  • TPSA: 95.92
  • ALOGS: -2.46
  • ROTB: 5

  • Status: ONP

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

Drug dosage:

DoseUnitRoute
0.20 g O

ADMET properties:

None

Approvals:

DateAgencyCompanyOrphan
March 26, 2021 EMA ARVELLE THERAPEUTICS NETHERLANDS B.V.
Nov. 21, 2019 FDA SK LIFE SCIENCE INC

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

FDA Adverse Event Reporting System (Geriatric)

None

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC N03AX25 NERVOUS SYSTEM
ANTIEPILEPTICS
ANTIEPILEPTICS
Other antiepileptics
MeSH PA D000927 Anticonvulsants
MeSH PA D002491 Central Nervous System Agents

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

DiseaseRelationSNOMED_IDDOID
Partial seizure indication 29753000
Epilepsy having focal-onset seizures indication 84757009 DOID:1826
Genetic short QT syndrome contraindication 698273002




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 13.88 acidic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
100MG XCOPRI SK LIFE N212839 March 10, 2020 RX TABLET ORAL March 10, 2025 NEW CHEMICAL ENTITY
12.5MG XCOPRI SK LIFE N212839 March 10, 2020 RX TABLET ORAL March 10, 2025 NEW CHEMICAL ENTITY
150MG XCOPRI SK LIFE N212839 March 10, 2020 RX TABLET ORAL March 10, 2025 NEW CHEMICAL ENTITY
200MG XCOPRI SK LIFE N212839 March 10, 2020 RX TABLET ORAL March 10, 2025 NEW CHEMICAL ENTITY
25MG XCOPRI SK LIFE N212839 March 10, 2020 RX TABLET ORAL March 10, 2025 NEW CHEMICAL ENTITY
50MG XCOPRI SK LIFE N212839 March 10, 2020 RX TABLET ORAL March 10, 2025 NEW CHEMICAL ENTITY

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Gamma-aminobutyric acid receptor subunit alpha-4 Ion channel ALLOSTERIC MODULATOR EC50 4.38 IUPHAR
Gamma-aminobutyric acid receptor subunit alpha-6 Ion channel ALLOSTERIC MODULATOR EC50 4.24 IUPHAR

External reference:

IDSource
P85X70RZWS UNII
C4550368 UMLSCUI
CHEMBL3989949 ChEMBL_ID
11962412 PUBCHEM_CID
DB06119 DRUGBANK_ID
D11150 KEGG_DRUG
10773 IUPHAR_LIGAND_ID
2265690 RXNORM
332202 MMSL
38242 MMSL
d09522 MMSL
830240007 SNOMEDCT_US
830244003 SNOMEDCT_US
4039272 VANDF
018214 NDDF
C000654784 MESH_SUPPLEMENTAL_RECORD_UI
10116 INN_ID

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Xcopri HUMAN PRESCRIPTION DRUG LABEL 1 71699-050 TABLET, FILM COATED 50 mg ORAL NDA 32 sections
Xcopri HUMAN PRESCRIPTION DRUG LABEL 1 71699-100 TABLET, FILM COATED 100 mg ORAL NDA 32 sections
Xcopri HUMAN PRESCRIPTION DRUG LABEL 1 71699-150 TABLET, FILM COATED 150 mg ORAL NDA 32 sections
Xcopri HUMAN PRESCRIPTION DRUG LABEL 1 71699-200 TABLET, FILM COATED 200 mg ORAL NDA 32 sections