Lacosamide

DB06218ApprovedInvestigationalSmall moleculeAnti-epileptic Agent Anticonvulsants Miscellaneous Anticonvulsants

Lacosamide is an antiepileptic drug used to treat partial-onset seizures and primary generalized tonic-clonic seizures. As a chiral functionalized amino acid, it works by blocking slowly inactivating components of voltage-gated sodium currents.

Mechanism: Caused by neuronal hyperexcitability, seizures in epilepsy involve sustained firing of sodium-dependent action potentials. The slow inactivation process, intrinsic to voltage-gated sodium channel functioning, has been implicated in the paroxysmal depolarizing shifts associated with epileptic activity. The exact mechanism of action of lacosamide is not fully known; however, in vitro electrophysiological studies have shown that lacosamide selectively enhances the slow inactivation of voltage-gated sodium channels, shifting the slow inactivation curve to more hyperpolarized potentials and augmenting the maximal fraction of channels in the slow inactivated state. This results in the stabilization of hyperexcitable neuronal membranes and inhibition of repetitive neuronal firing. Lacosamide does not affect the fast component of voltage-gated sodium currents, unlike traditional sodium channel blockers.
Curator reviewed · 5 references
Primary indication: In the US and Europe, lacosamide is indicated for the treatment of partial-onset seizures in children and adults.Curator reviewed · 9 structured indications
Formula / weight: C₁₃H₁₈N₂O₃ · 250.2936 g/mol (avg)
First approval: Canada, 2010 · United States, 2008 · European Union, 2008
Also known as: (+)-(2R)-2-(ACETYLAMINO)-N-BENZYL-3-METHOXYPROPANAMIDE · (2R)-2-(Acetylamino)-3-methoxy-N-(phenylmethyl)propanamide · (R)-2-acetamido-N-benzyl-3- methoxypropionamide · (R)-LACOSAMIDE 1 · Erlosamide
Code names: ADD-243037 · SPM-927
Brand names: Lacosamide Accord
Lacosamide Adroiq
Lacosamide UCB
Motpoly
Vimpat