Bexicaserin: A Comprehensive Report on its Pharmacology, Clinical Development, and Therapeutic Potential

1. Introduction to Bexicaserin

1.1. Overview and Chemical Identity

Bexicaserin is an investigational oral pharmaceutical agent primarily under development for the treatment of seizures associated with developmental and epileptic encephalopathies (DEEs), a group of severe, often drug-resistant, epilepsy syndromes.[1] The compound has a history of investigation under different developmental code names, reflecting its evolving therapeutic focus. Initially explored for obesity under the code ATHX-105 by Athersys, Inc. [4], it was later designated LP352 and AN352 during its development for neurological disorders by Longboard Pharmaceuticals.[1] This progression from a metabolic disorder indication to a specialized area of rare neurological diseases illustrates a common path in pharmaceutical development, where emerging data or strategic re-evaluation can lead to a refocusing of a compound's potential.

Chemically, bexicaserin is (3R)-N-(2,2-difluoroethyl)-3-methyl-1,10-diazatricyclo[6.4.1.0^4,13]trideca-4,6,8(13)-triene-5-carboxamide.[7] Its Chemical Abstracts Service (CAS) Number is 2035818-24-5, and it is registered in DrugBank under the accession number DB18885.[1] The molecular formula of bexicaserin is C₁₅H₁₉F₂N₃O, corresponding to a molar mass of 295.334 g·mol⁻¹.[1] The primary route of administration for bexicaserin in clinical studies is oral.[1]

1.2. Drug Class