Cenobamate

Cenobamate, sold under the brand name Xcopri among others, is a medication used 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 (VGSC) 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 (GABA), 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 (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.
Society and culture.
Legal status.
The U.S. Food and Drug Administration (FDA) approved cenobamate in November 2019, and granted the application for Xcopri to SK Life Science Inc.
On 28 January 2021, the Committee for Medicinal Products for Human Use (CHMP) of the European Medicines Agency (EMA) adopted a positive opinion, recommending the granting of a marketing authorization for the medicinal product Ontozry, intended for adults with epilepsy whose disease is not adequately controlled despite a history of treatment with at least two anti-epileptic medicinal products. The applicant for this medicinal product is Arvelle Therapeutics Netherlands B.V.