Biohaven begins first human trial of brain-penetrant drug BHV-8100
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Biohaven Reports First-in-Human Dosing of Oral PKM2 Modulator, BHV-8100, Targeting Metabolic Restoration and Immunomodulation
June 1, 2026 7:30 AM EDTBHV-8100 is an orally administered, brain-penetrant PKM2 modulator; a novel therapeutic class addressing the bioenergetic and immunometabolic basis of systemic and central nervous system disorders First-in-human study initiated with dose escalation ongoing; preliminary data in healthy participants demonstrates favorable pharmacokinetics supporting convenient, once-daily dosing and well a tolerated profile at projected therapeutic exposuresPenetrates blood-brain barrier and reverses metabolic dysfunction with 3-fold improvement in glucose utilization in human, whole brain model (Bexorg BrainEx platform, physiologically reactivated brains from human donors); preferential metabolic rescue in Alzheimer's disease donor brains vs... More
