Cenobamate

Cenobamate, sold under the brand name Xcopri, is for the treatment of partial-onset seizures in adults.[2][3]

Cenobamate

Clinical data
Trade names	Xcopri
Other names	YKP3089
AHFS/Drugs.com	xcopri
Routes of administration	By mouth
Legal status
Legal status	US: Schedule V [1]
Identifiers
IUPAC name [(1R)-1-(2-chlorophenyl)-2-(tetrazol-2-yl)ethyl] carbamate
CAS Number	913088-80-9
PubChem CID	11962412
PubChem SID	376219074
DrugBank	DB06119
ChemSpider	10136642
UNII	P85X70RZWS
KEGG	D11150
ChEMBL	ChEMBL3989949
Chemical and physical data
Formula	C10H10ClN5O2
Molar mass	267.67 g·mol^−1
3D model (JSmol)	Interactive image
SMILES C1=CC=C(C(=C1)C(CN2N=CN=N2)OC(=O)N)Cl
InChI InChI=1S/C10H10ClN5O2/c11-8-4-2-1-3-7(8)9(18-10(12)17)5-16-14-6-13-15-16/h1-4,6,9H,5H2,(H2,12,17)/t9-/m0/s1 Key:GFHAXPJGXSQLPT-VIFPVBQESA-N

It was approved for medical use in the United States in November 2019[2][3][4] and placed in Schedule V in March 2020.[5]

Pharmacology

Pharmacodynamics

Cenobamate is a voltage-gated sodium channel (VGSC) blocker.[6] It is a selective blocker of the inactivated state of VGSCs, preferentially inhibiting persistent sodium current.[6] It has been proposed that cenobamate additionally enhances presynaptic release of γ-aminobutyric acid (GABA), thereby increasing inhibitory GABAergic neurotransmission.[6]

History

The safety and efficacy of cenobamate to treat partial-onset seizures was established in two randomized, double-blind, placebo-controlled studies that enrolled 655 adults. In these studies, patients had partial-onset seizures with or without secondary generalization for an average of approximately 24 years and median seizure frequency of 8.5 seizures per 28 days during an 8-week baseline period. During the trials, doses of 100, 200, and 400 milligrams (mg) daily reduced the percent of seizures per 28 days compared with the placebo group. The recommended maintenance dose, following a titration (medication adjustment) period, is 200 mg daily; however, some patients may need an additional titration to 400 mg daily, the maximum recommended dose, based on their clinical response and tolerability.[2]

The U.S. Food and Drug Administration (FDA) approved cenobamate in November 2019, and granted the application for Xcopri to SK Life Science Inc.[2][3][4][7]

References

1. "Schedules of Controlled Substances: Placement of Cenobamate in Schedule V". Federal Register. 10 March 2020.
2. "FDA approves new treatment for adults with partial-onset seizures". U.S. Food and Drug Administration (FDA) (Press release). 21 November 2019. Archived from the original on 22 November 2019. Retrieved 21 November 2019. This article incorporates text from this source, which is in the public domain.
3. "Drug Trials Snapshots: Xcopri". U.S. Food and Drug Administration (FDA). 3 December 2019. Archived from the original on 19 December 2019. Retrieved 18 December 2019. This article incorporates text from this source, which is in the public domain.
4. "Drug Approval Package: Xcopri". U.S. Food and Drug Administration (FDA). 10 December 2019. Archived from the original on 19 December 2019. Retrieved 18 December 2019. This article incorporates text from this source, which is in the public domain.
5. "2020 - Placement of Cenobamate in Schedule V". DEA Diversion Control Division. 10 March 2020. Retrieved 11 March 2020.
6. Younus, Iyan; Reddy, Doodipala Samba (2017). "A resurging boom in new drugs for epilepsy and brain disorders". Expert Review of Clinical Pharmacology. 11 (1): 27–45. doi:10.1080/17512433.2018.1386553. ISSN 1751-2433.
7. "Cenobamate FDA Approval Status". Drugs.com. 13 November 2019. Retrieved 22 November 2019.

Further reading

• "Drug Approval Package: Xcopri". U.S. Food and Drug Administration (FDA).

External links

• "Cenobamate". Drug Information Portal. U.S. National Library of Medicine (NLM).