Biohaven (BHVN) said Monday it has initiated first-in-human dosing of BHV-8100, an experimental oral, brain-penetrant PKM2 modulator being developed for neurological, retinal and inflammatory diseases.

The Phase 1 study is evaluating the drug's safety, tolerability and pharmacokinetics in healthy volunteers, according to the company.

Biohaven said early data showed BHV-8100 achieved projected therapeutic exposure levels, supported once-daily dosing and was generally well tolerated, with most adverse events reported as mild and spontaneously resolving.

The company also highlighted preclinical findings from human brain studies showing BHV-8100 increased cerebral glucose utilization and lactate production by up to three times, suggesting improved brain energy metabolism.

The effects were particularly pronounced in brains from patients with Alzheimer's disease, it said.