Cenobamate


Cenobamate, sold under the brand name Xcopri, is for the treatment of partial-onset seizures in adults.
It was approved for medical use in the United States in November 2019 and placed in Schedule V in March 2020.

Pharmacology

Pharmacodynamics

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

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 daily reduced the percent of seizures per 28 days compared with the placebo group. The recommended maintenance dose, following a titration 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.
The U.S. Food and Drug Administration approved cenobamate in November 2019, and granted the application for Xcopri to SK Life Science Inc.