BHVN•BHVN•Biohaven initiated first-in-human dosing of BHV-8100, an oral brain-penetrant PKM2 modulator, with dose escalation underway and healthy volunteers showing favorable pharmacokinetics supporting once-daily administration and good tolerability. Ex vivo human BrainEx data reveal a 3-fold increase in whole-brain glucose utilization and preferential metabolic rescue in Alzheimer’s donor brains.
Biohaven has launched the first-in-human dose escalation study of BHV-8100, marking its transition into clinical development. Healthy volunteers are currently enrolled and receiving ascending oral doses to assess initial safety and pharmacokinetic parameters.
Preliminary results demonstrate favorable pharmacokinetics consistent with once-daily dosing and a well-tolerated safety profile at projected therapeutic exposure levels. No serious adverse events have been reported and dose escalation continues under protocol.
Using the BrainEx ex vivo human brain platform, administration of BHV-8100 produced a 3-fold increase in whole-brain glucose utilization. The compound showed preferential metabolic rescue in Alzheimer’s disease donor brains compared with controls, confirming blood-brain barrier penetration and target engagement.
Preclinical studies of BHV-8100 across Alzheimer’s, multiple sclerosis, retinal degeneration and immunologic models demonstrated restoration of metabolic deficits, reduction of neuroinflammation and enhanced neuroprotection. These data support development in high-value neurological, ophthalmological and immunological indications.
