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Bexicaserin is an investigational oral small molecule that acts as a highly selective serotonin 5-HT2C receptor agonist (sometimes described as a "superagonist"). It is being developed primarily for the treatment of seizures associated with developmental and epileptic encephalopathies (DEEs), including Dravet syndrome and Lennox-Gastaut syndrome. Bexicaserin works by selectively activating the 5-HT2C receptor in the brain and spinal cord, which modulates GABAergic neurotransmission to suppress central hyperexcitability—a key factor in seizure activity. Unlike some other serotonergic agents, bexicaserin has negligible activity at 5-HT2A and 5-HT2B receptors, reducing risks such as cardiac valvulopathy. Clinical trials have shown significant reductions in motor seizure frequency among DEE patients treated with bexicaserin compared to placebo. The drug was originally developed by Longboard Pharmaceuticals; development is now led by Lundbeck following acquisition[4][5][6][7][8][9].
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