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

Stem definition	Drug id	CAS RN
tranquillizers, propanediol and pentanediol derivatives	5355	913088-80-9

Description:

Molecule	Description
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

Molecule

Description

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:

Dose	Unit	Route
0.20	g	O

ADMET properties:

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Property	Value	Reference
S (Water solubility)	1.70 mg/mL	Bocci G, Oprea TI, Benet LZ
BDDCS (Biopharmaceutical Drug Disposition Classification System)	1	Bocci G, Oprea TI, Benet LZ

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Approvals:

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Date	Agency	Company	Orphan
March 26, 2021	EMA	ARVELLE THERAPEUTICS NETHERLANDS B.V.
Nov. 21, 2019	FDA	SK LIFE SCIENCE INC

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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:

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Source	Code	Description
ATC	N03AX25	NERVOUS SYSTEM ANTIEPILEPTICS ANTIEPILEPTICS Other antiepileptics
FDA MoA	N0000181004	Sodium Channel Antagonists
FDA MoA	N0000182139	Cytochrome P450 2B6 Inhibitors
FDA MoA	N0000182140	Cytochrome P450 2C19 Inhibitors
FDA MoA	N0000185506	Cytochrome P450 3A4 Inducers
FDA MoA	N0000187063	Cytochrome P450 2C8 Inducers
FDA MoA	N0000187064	Cytochrome P450 2B6 Inducers
FDA MoA	N0000190114	Cytochrome P450 3A Inhibitors
FDA MoA	N0000193997	GABA A Receptor Positive Modulators
MeSH PA	D000927	Anticonvulsants

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

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

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🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	13.88	acidic

Orange Book patent data (new drug applications)

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Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Patent number	Patent expiration date	Patent use
100MG	XCOPRI	SK LIFE	N212839	March 10, 2020	RX	TABLET	ORAL	11654133	June 16, 2039	CO-ADMINISTRATION OF CENOBAMATE WITH PHENOBARBITAL AND/OR PHENYTOIN FOR THE TREATMENT OF PARTIAL ONSET SEIZURES
12.5MG	XCOPRI	SK LIFE	N212839	March 10, 2020	RX	TABLET	ORAL	11654133	June 16, 2039	CO-ADMINISTRATION OF CENOBAMATE WITH PHENOBARBITAL AND/OR PHENYTOIN FOR THE TREATMENT OF PARTIAL ONSET SEIZURES
150MG	XCOPRI	SK LIFE	N212839	March 10, 2020	RX	TABLET	ORAL	11654133	June 16, 2039	CO-ADMINISTRATION OF CENOBAMATE WITH PHENOBARBITAL AND/OR PHENYTOIN FOR THE TREATMENT OF PARTIAL ONSET SEIZURES
200MG	XCOPRI	SK LIFE	N212839	March 10, 2020	RX	TABLET	ORAL	11654133	June 16, 2039	CO-ADMINISTRATION OF CENOBAMATE WITH PHENOBARBITAL AND/OR PHENYTOIN FOR THE TREATMENT OF PARTIAL ONSET SEIZURES
25MG	XCOPRI	SK LIFE	N212839	March 10, 2020	RX	TABLET	ORAL	11654133	June 16, 2039	CO-ADMINISTRATION OF CENOBAMATE WITH PHENOBARBITAL AND/OR PHENYTOIN FOR THE TREATMENT OF PARTIAL ONSET SEIZURES
50MG	XCOPRI	SK LIFE	N212839	March 10, 2020	RX	TABLET	ORAL	11654133	June 16, 2039	CO-ADMINISTRATION OF CENOBAMATE WITH PHENOBARBITAL AND/OR PHENYTOIN FOR THE TREATMENT OF PARTIAL ONSET SEIZURES

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Orange Book exclusivity data (new drug applications)

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Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Exclusivity date	Description
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

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Bioactivity Summary:

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Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Mechanism action	Bioact source	MoA source
Gamma-aminobutyric acid receptor subunit alpha-4	Ion channel	P48169	GBRA4_HUMAN	ALLOSTERIC MODULATOR	EC50	4.38		IUPHAR
Gamma-aminobutyric acid receptor subunit alpha-6	Ion channel	Q16445	GBRA6_HUMAN	ALLOSTERIC MODULATOR	EC50	4.24		IUPHAR

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External reference:

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ID	Source
018214	NDDF
10116	INN_ID
10773	IUPHAR_LIGAND_ID
11962412	PUBCHEM_CID
2265690	RXNORM
332202	MMSL
38242	MMSL
4039272	VANDF
830240007	SNOMEDCT_US
830244003	SNOMEDCT_US

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Xcopri	HUMAN PRESCRIPTION DRUG LABEL	1	71699-050	TABLET, FILM COATED	50 mg	ORAL	NDA	33 sections
Xcopri	HUMAN PRESCRIPTION DRUG LABEL	1	71699-050	TABLET, FILM COATED	50 mg	ORAL	NDA	33 sections
Xcopri	HUMAN PRESCRIPTION DRUG LABEL	1	71699-050	TABLET, FILM COATED	50 mg	ORAL	NDA	33 sections
Xcopri	HUMAN PRESCRIPTION DRUG LABEL	1	71699-100	TABLET, FILM COATED	100 mg	ORAL	NDA	33 sections
Xcopri	HUMAN PRESCRIPTION DRUG LABEL	1	71699-100	TABLET, FILM COATED	100 mg	ORAL	NDA	33 sections
Xcopri	HUMAN PRESCRIPTION DRUG LABEL	1	71699-100	TABLET, FILM COATED	100 mg	ORAL	NDA	33 sections
Xcopri	HUMAN PRESCRIPTION DRUG LABEL	1	71699-150	TABLET, FILM COATED	150 mg	ORAL	NDA	33 sections
Xcopri	HUMAN PRESCRIPTION DRUG LABEL	1	71699-150	TABLET, FILM COATED	150 mg	ORAL	NDA	33 sections
Xcopri	HUMAN PRESCRIPTION DRUG LABEL	1	71699-150	TABLET, FILM COATED	150 mg	ORAL	NDA	33 sections
Xcopri	HUMAN PRESCRIPTION DRUG LABEL	1	71699-200	TABLET, FILM COATED	200 mg	ORAL	NDA	33 sections

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