BGG492 (selurampanel), an AMPA/kainate receptor antagonist drug for epilepsy

摘要

Introduction: AMPA-type glutamate receptor (AMPAR) antagonism is under development as a novel mechanism of action for antiepileptic drugs. Selurampanel (BGG492) is an experimental competitive AMPA antagonist currently in clinical trials. Areas covered: This article provides a review of the roles of glutamate receptors, especially of the AMPA type, in normal and epileptic synaptic transmission. It also provides a discussion of the mechanisms of action of AMPAR antagonist compounds. The article includes a summary of the preclinical and clinical data on the efficacy and safety of BGG492 and provides a discussion of the future role of these compounds in clinical therapy. Expert opinion: Since many persons with epilepsy remain inadequately treated, compounds exploiting new mechanisms for seizure control are welcome. Based on available clinical trial data as adjunctive therapy, the AMPAR antagonists will likely be highly useful in a small subset of persons and moderately helpful in a larger subset, similar to other new drugs for epilepsy developed since 1993. It remains impossible to predict which patients will respond to which class of drugs.