Drug intelligence / Profile preview

ethosuximide + topiramate

Development stage
Preclinical
Lead developer
Ortho-McNeil Pharmaceuticals
Modality
Small Molecules
Administration
Oral
01

Overview

This is a combination of two antiepileptic drugs (AEDs): ethosuximide and topiramate. Ethosuximide primarily acts by blocking T-type voltage-gated calcium channels in thalamic neurons, which suppresses the paroxysmal three cycle per second spike and wave activity associated with absence seizures. It is primarily used for the treatment of petit mal epilepsy (absence seizures). Topiramate is a broad-spectrum anticonvulsant with multiple mechanisms of action, including blocking voltage-sensitive sodium channels, enhancing GABA activity, antagonizing glutamate receptors, and inhibiting carbonic anhydrase. It is used to treat various types of seizures and for migraine prevention. The combination has shown potential synergistic effects in experimental models, particularly against pentylenetetrazol-induced seizures in mice.

02

Targets

iGluR (Ionotropic receptor 76b (Ir76b))NaV (Voltage-gated sodium channels)CA (Carbonic anhydrase)GABRR (GABA-A receptor subunit rho)CaV3 (Caveolin-3)

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