cenobamate
Trade name: Xcopri
Approved
Nov 21, 2019
Cenobamate (also known as YKP3089) is a small molecule sodium channel blocker in development for the treatment of partial-onset seizures in adult patients. In mice and rats, Cenobamate displayed an anticonvulsant activity in the maximal electroshock test and prevented seizures induced by chemical convulsants such as pentylenetetrazol and picrotoxin. In addition, Cenobamate was reported to be effective in two models of focal seizure, the hippocampal kindled rat and the mouse 6 Hz psychomotor seizure models. Two completed adequate and well-controlled clinical studies demonstrated a significant reduction in focal seizures with Cenobamate in patients with epilepsy, and a long-term open-label phase 3 safety clinical trial is currently ongoing. Cenobamate is considered a new generation antiepileptic therapy and clinical trials have shown that it may be more effective and safer than existing drugs. If licensed, Cenobamate will offer a new adjunctive treatment option for patients with partial focal epilepsy. — NCATS
Clinical trial activity
21 trials · 6 clinical orgs · 3 marketing orgs
Earliest trial started Aug 1, 2007 (NCT00616148)
Timeline
2010s
2020s
- Jun 2, 2025
ZENARA — Marketing Organization
- Apr 28, 2026
Aurobindo Pharma — Marketing Organization
Indications
Approved for
Mechanism of action
- GABA-A receptorAGONIST
GABA-A receptor agonist
- Sodium channel alpha subunitINHIBITOR
Sodium channel alpha subunit inhibitor
The precise mechanism in seizures is unknown. Reduces neuronal firing associated with sodium currents and increases the activity of the GABA-A channels. It appears to inhibit the non-inactivated, persistent (repetitive) component of sodium currents that may be associated with epilepsy.
- Sodium channel protein type 1 subunit alpha (SCN1A) ↗
- Sodium channel protein type 5 subunit alpha (SCN5A) ↗
- Sodium channel protein type 4 subunit alpha (SCN4A) ↗
- Sodium channel protein type 7 subunit alpha (SCN7A) ↗
- Sodium channel protein type 2 subunit alpha (SCN2A) ↗
- Sodium channel protein type 9 subunit alpha (SCN9A) ↗
- Sodium channel protein type 3 subunit alpha (SCN3A) ↗
- Sodium channel protein type 11 subunit alpha (SCN11A) ↗
- Sodium channel protein type 8 subunit alpha (SCN8A) ↗
- Sodium channel protein type 10 subunit alpha (SCN10A) ↗
- Sodium channel protein type I alpha subunit
- Sodium channel protein type V alpha subunit
- Sodium channel protein type IV alpha subunit
- Sodium channel protein type VII alpha subunit
- Sodium channel protein type IX alpha subunit
- Sodium channel protein type II alpha subunit
- Sodium channel protein type III alpha subunit
- Sodium channel protein type XI alpha subunit
- Sodium channel protein type VIII alpha subunit
- Sodium channel protein type X alpha subunit
- Sodium channel alpha subunits; brain (Types I, II, III)
- GABA-A receptor; anion channelPOSITIVE ALLOSTERIC MODULATOR
GABA-A receptor; anion channel positive allosteric modulator
The precise mechanism in seizures is unknown.
- Gamma-aminobutyric acid receptor subunit alpha-1 (GABRA1) ↗
- Gamma-aminobutyric acid receptor subunit beta-2 (GABRB2) ↗
- Gamma-aminobutyric acid receptor subunit gamma-2 (GABRG2) ↗
- Gamma-aminobutyric acid receptor subunit beta-3 (GABRB3) ↗
- Gamma-aminobutyric acid receptor subunit alpha-4 (GABRA4) ↗
- Gamma-aminobutyric acid receptor subunit gamma-3 (GABRG3) ↗
- Gamma-aminobutyric acid receptor subunit theta (GABRQ) ↗
- Gamma-aminobutyric acid receptor subunit alpha-3 (GABRA3) ↗
- Gamma-aminobutyric acid receptor subunit pi (GABRP) ↗
- Gamma-aminobutyric acid receptor subunit delta (GABRD) ↗
- Gamma-aminobutyric acid receptor subunit gamma-1 (GABRG1) ↗
- Gamma-aminobutyric acid receptor subunit beta-1 (GABRB1) ↗
- Gamma-aminobutyric acid receptor subunit epsilon (GABRE) ↗
- Gamma-aminobutyric acid receptor subunit alpha-2 (GABRA2) ↗
- Gamma-aminobutyric acid receptor subunit alpha-5 (GABRA5) ↗
- Gamma-aminobutyric acid receptor subunit alpha-6 (GABRA6) ↗
- GABA receptor alpha-1 subunit
- GABA receptor beta-2 subunit
- GABA receptor alpha-4 subunit
- GABA receptor delta subunit
- GABA receptor alpha-5 subunit
- GABA receptor alpha-6 subunit
- GABA receptor beta-3 subunit
- GABA receptor alpha-3 subunit
- GABA receptor alpha-2 subunit
- GABA-A receptor; GABA-A site (alpha1/beta2 interface)
- GABA-A receptor; alpha-3/beta-3/gamma-2
- GABA-A receptor; alpha-1/beta-3/gamma-2
- GABA-A receptor; alpha-5/beta-3/gamma-2
- GABA-A receptor; alpha-2/beta-3/gamma-2
- GABA-A receptor; alpha-1/beta-2/gamma-2
- GABA-A receptor; alpha-6/beta-3/gamma-2
- GABA-A receptor; benzodiazepine site
- GABA-A receptor; agonist GABA site
- GABA A receptor alpha-2/beta-2/gamma-2
- GABA A receptor alpha-3/beta-2/gamma-2
- GABA A receptor alpha-6/beta-2/gamma-2
- GABA A receptor alpha-1/beta-1/gamma-2
- GABA A receptor alpha-4/beta-3/gamma-2
- Gamma-aminobutyric acid receptor subunit alpha-4/beta3/delta
- Gamma-aminobutyric acid receptor subunit alpha-1/ beta-1
- Gamma-aminobutyric acid receptor subunit alpha-2/beta-2
- Gamma-aminobutyric acid receptor subunit alpha-3/ beta-2
- Gamma-aminobutyric acid receptor subunit alpha-3/ beta-3/gamma-3
- Gamma-aminobutyric acid receptor subunit alpha-3/beta-3
- Gamma-aminobutyric acid receptor subunit alpha-3/beta-3/theta
- Gamma-aminobutyric acid receptor subunit alpha-5/beta-2
- Gamma-aminobutyric acid receptor subunit alpha-5/beta-3/gamma-3
- Gamma-aminobutyric acid receptor subunit alpha-6/beta-3
- GABA-A receptor alpha-1/beta-3
- Gamma-aminobutyric acid receptor subunit alpha-1/beta-2/delta
- Gamma-aminobutyric acid receptor subunit alpha-4/beta-2/delta
- Gamma-aminobutyric acid receptor subunit beta-1/beta-2
- Gamma-aminobutyric acid receptor subunit alpha-5/beta-3
- Gamma-aminobutyric acid receptor subunit alpha-2/beta-3
- Gamma-aminobutyric acid receptor subunit alpha-1/alpha-2/beta-2/gamma-2
- Gamma-aminobutyric acid receptor subunit alpha-1/gamma-2
- Gamma-aminobutyric acid receptor subunit alpha-4/beta-2/gamma-2
- Gamma-aminobutyric acid receptor subunit alpha-4/beta-1/delta
- Gamma-aminobutyric acid receptor subunit alpha-5/beta-2/gamma-2
- GABA receptor beta-1 subunit
- Gamma-aminobutyric acid receptor subunit alpha-2/beta-1/gamma-2
Approval history
- approvedNov 21, 2019
Chemistry & pharmacology
SMILES
NC(=O)O[C@@H](CN1N=CN=N1)C2=CC=CC=C2Cl- Mol. weight
- 267.672 g/mol
- Lipinski Ro5
- Pass
- Rule of 3
- No
- Chirality
- Single Stereoisomer
- Inorganic
- No
- Polymer
- No
- Delivery
- Oral
- Availability
- Prescription Only
Oral
Yes
Parenteral
No
Topical
No
Sources
- WikipediaCenobamate ↗
- NCATSP85X70RZWS ↗
- ChEMBLCHEMBL3989949 ↗
Also known as
- ykp3089
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT06453213 | Phase 4 | Oct 14, 2024 | Arvelle |
| NCT06352723 | Early Phase 1 (Phase 1) | Apr 30, 2024 | Harvard University |
| NCT06590896 | Phase 2 | Nov 4, 2022 | Ono Pharmaceuticals |
| NCT05572255 | Phase 1 | Sep 27, 2022 | Arvelle |
| NCT06579573 | Phase 3 | Jul 12, 2022 | Ono Pharmaceuticals |
| NCT05067634 | Phase 3 | Jan 31, 2022 | Arvelle |
| NCT04791553 | Phase 1 | Jun 17, 2021 | Arvelle |
| NCT04903314 | Phase 1 | May 27, 2021 | Arvelle |
| NCT04557085 | Phase 3 | Feb 28, 2021 | Arvelle |
| NCT04690751 | Phase 1 | Dec 21, 2020 | Arvelle |
| NCT03961568 | Phase 3 | May 31, 2019 | Arvelle |
| NCT03686033 | Phase 2 | Nov 2, 2018 | Eisai |
| NCT03678753 | Phase 3 | Sep 30, 2018 | Arvelle |
| NCT03402178 | Phase 1 | Dec 21, 2017 | Eisai |
| NCT03509285 | Phase 1 | Mar 8, 2017 | Arvelle |
| NCT03234699 | Phase 1 | Feb 22, 2017 | Arvelle |
| NCT02535091 | Phase 3 | Jul 1, 2016 | Arvelle |
| NCT01866111 | Phase 2 | Jul 1, 2013 | Arvelle |
| NCT01397968 | Phase 2 | May 1, 2011 | Arvelle |
| NCT00616148 | Phase 2 | Aug 1, 2007 | Arvelle, New York University, The Epilepsy Study Consortium |
Organizations
Research & Development (6)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| Arvelle | For profit | 16 | 16 | 5 | 2007 |
| Eisai | For profit | 2 | 2 | 2 | 2017 |
| Ono Pharmaceuticals | For profit | 2 | 2 | 2 | 2022 |
| Harvard University | Academic/Hospital | 1 | 1 | 1 | 2024 |
| New York University | Academic/Hospital | 1 | 0 | 1 | 2007 |
| The Epilepsy Study Consortium | Academic/Hospital | 1 | 0 | 1 | 2007 |
Marketing (5)
| Organization | Org type | Relationship | Date |
|---|---|---|---|
| Arvelle | For profit | NDA | Nov 21, 2019 |
| Arvelle | For profit | MKTG | Nov 21, 2019 |
| Arvelle | For profit | SYN | Nov 21, 2019 |
| Aurobindo Pharma | For profit | MKTG | Apr 28, 2026 |
| ZENARA | For profit | MKTG | Jun 2, 2025 |