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ES-481 is a novel small molecule drug in clinical development as an oral therapy for neurological disorders. It acts as a potent and selective antagonist of transmembrane AMPA receptor regulatory protein (TARP)-γ8-dependent AMPA receptors. This mechanism targets excitatory neurotransmission implicated in seizure activity and tremor. ES-481 has demonstrated anti-seizure efficacy in patients with drug-resistant epilepsy (DRE) and is also being investigated for essential tremor. In Phase 2 trials, it showed significant reduction in seizure frequency compared to placebo and was generally well tolerated up to the highest tested dose of 75 mg twice daily[1][4][6]. The drug is being developed by ES Therapeutics.
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