YKP-3089

Absorption

Cenobamate is 88% orally bioavailable with a Tmax of 1-4 hours. A high fat meal does not significantly impact the pharmacokinetics of cenobamate.

Toxicity

There is limited information regarding the signs, symptoms, and treatment of a cenobamate overdose. Symptomatic and supportive treatment is recommended and there is limited data on the utility of dialysis to remove cenobamate from blood.

The Uses of YKP-3089

Cenobamate can be used to treat focal-onset seizures in adults.

Indications

Cenobamate is indicated for the treatment of partial onset seizures in adults.

Background

Cenobamate, or YKP-3089, is an antiepileptic drug developed by SK Pharmaceuticals and used to treat partial onset seizures. The exact mechanism of action has not been described in the literature, though it positively modulates GABAA and inhibits voltage gated sodium channels.
Cenobamate was granted FDA approval on 21 November 2019.

Pharmacokinetics

The mechanism of cenobamate is unknown, however it modulates GABAA and inhibit voltage gated sodium channels. Cenobamate is given once daily and so it has a long duration of action. The therapeutic window is wide as doses of 750mg can be well tolerated. Patients should be counselled regarding the risk of DRESS syndrome, QT interval shortening, suicidal behavior, and neurological adverse effects.

Metabolism

Data regarding the metabolism of cenobamate is lacking, however it is mostly glucuronidated by UGT2B7 and UGT2B4 or oxidized by a number of cytochromes.