Cenobamate

Cenobamate, sold under the brand name Xcopri, is for the treatment of partial-onset seizures in adults.[1]

Cenobamate
Clinical data
Trade namesXcopri
Other namesYKP3089
Routes of
administration		By mouth
Legal status
Legal status
Identifiers
CAS Number
PubChem CID
DrugBank
ChemSpider
UNII
ChEMBL
Chemical and physical data
FormulaC10H10ClN5O2
Molar mass267.67 g·mol−1
3D model (JSmol)

It was approved for medical use in the United States in 2019.[1]

Pharmacology

Pharmacodynamics

Cenobamate is a voltage-gated sodium channel (VGSC) blocker.[2] It is a selective blocker of the inactivated state of VGSCs, preferentially inhibiting persistent sodium current.[2] It has been proposed that cenobamate additionally enhances presynaptic release of γ-aminobutyric acid (GABA), thereby increasing inhibitory GABAergic neurotransmission.[2]

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.[1]

The U.S. Food and Drug Administration (FDA) approved cenobamate in November 2019, and granted the application for Xcopri to SK Life Science Inc.[1][3]

References
  1. "FDA approves new treatment for adults with partial-onset seizures". U.S. Food and Drug Administration. 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.
  2. 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.
  3. "Cenobamate FDA Approval Status". Drugs.com. 13 November 2019. Retrieved 22 November 2019.
  • "Cenobamate". Drug Information Portal. U.S. National Library of Medicine (NLM).


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