Biohaven Reports First-in-Human Dosing of Oral PKM2 Modulator, BHV-8100, Targeting Metabolic Restoration and Immunomodulation

BHV-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 exposures Penetrates 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 controls Exhibits robust beneficial effects across a spectrum of preclinical models of Alzheimer's, and multiple sclerosis: restores metabolic deficits, reduces inflammation and neurodegeneration, and enhances remyelination PKM2 modulation offers a potential new paradigm for treating large, underserved, and high-value indications in neurology, ophthalmology, and immunology  NEW HAVEN, Conn., June 1, 2026 /PRNewswire/ -- Biohaven Ltd.