Background:
Cenobamate, a sodium channel blocker, enhances GABAergic transmission and has the potential to be a versatile CNS drug.
Cenobamate (YKP3089) protects against MES induced seizures in mice with an ED50 of 9.8 mg/kg i.p., and in rats with an ED50 of 1.9 mg/kg p.o. In the sc Met seizures model, Cenobamate given ip inhibited the clonic seizures in mice and rats, with ED50 values of 28.5 and 13.6 mg/kg, respectively. Cenobamate is also effective against seizure induced by picrotoxin with an ED50 of 34.5 mg/kg in mice. Cenobamate is effective in reducing significantly the expression of stage 5 seizures in the hippocampal kindled rat (ED50=16.4 mg/kg). Cenobamate is effective in the mouse 6 Hz psychomotor seizure model at 22, 32 and 44 mA, with ED50 values of 11.0, 17.9 and 16.5 mg/kg, respectively. Cenobamate also protects against lithiumpilocarpine-induced intractable seizures in rats (ip) (ED50=7.0 mg/kg)[2].
[1]. Zaccara G, et al. Do traditional anti-seizure drugs have a future? A review of potential anti-seizure drugs in clinical development. Pharmacol Res. 2016 Feb;104:38-48. [2]. Bialer M, et al. Progress report on new antiepileptic drugs: a summary of the Ninth Eilat Conference (EILAT IX). Epilepsy Res. 2009 Jan;83(1):1-43.
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