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 |
|---|---|
|
Synonyms:
|
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.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 0.20 | g | O |
ADMET properties:
| 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 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| 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:
| Source | Code | Description |
|---|---|---|
| ATC | N03AX25 | NERVOUS SYSTEM ANTIEPILEPTICS ANTIEPILEPTICS Other antiepileptics |
| MeSH PA | D000927 | Anticonvulsants |
| MeSH PA | D002491 | Central Nervous System Agents |
| 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 |
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| 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 level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 13.88 | acidic |
Orange Book patent data (new drug applications)
| 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 |
Orange Book exclusivity data (new drug applications)
| 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 |
Bioactivity Summary:
| 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 | ALLOSTERIC MODULATOR | EC50 | 4.38 | IUPHAR | ||||
| Gamma-aminobutyric acid receptor subunit alpha-6 | Ion channel | ALLOSTERIC MODULATOR | EC50 | 4.24 | IUPHAR |
External reference:
| ID | Source |
|---|---|
| P85X70RZWS | UNII |
| C4550368 | UMLSCUI |
| CHEMBL3989949 | ChEMBL_ID |
| 11962412 | PUBCHEM_CID |
| DB06119 | DRUGBANK_ID |
| D11150 | KEGG_DRUG |
| 10116 | INN_ID |
| 10773 | IUPHAR_LIGAND_ID |
| 018214 | NDDF |
| 830240007 | SNOMEDCT_US |
| 830244003 | SNOMEDCT_US |
| 4039272 | VANDF |
| 2265690 | RXNORM |
| 332202 | MMSL |
| 38242 | MMSL |
| d09522 | MMSL |
| C000654784 | MESH_SUPPLEMENTAL_RECORD_UI |
Pharmaceutical products:
| 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 |
| Xcopri | HUMAN PRESCRIPTION DRUG LABEL | 1 | 71699-200 | TABLET, FILM COATED | 200 mg | ORAL | NDA | 33 sections |
| Xcopri | HUMAN PRESCRIPTION DRUG LABEL | 1 | 71699-200 | TABLET, FILM COATED | 200 mg | ORAL | NDA | 33 sections |