BI 3821001

BI 3821001 is a small molecule antagonist of the G protein-coupled receptor 151 (GPR151) currently under development by Boehringer Ingelheim. GPR151 is an orphan G protein-coupled receptor that is highly and selectively expressed in the habenula, a brain region that acts as a critical relay between the forebrain and the midbrain, regulating the activity of dopaminergic and serotonergic neurons. Dysregulation of the habenula is associated with various psychiatric conditions, including schizophrenia. By antagonizing GPR151, BI 3821001 aims to modulate these neurotransmitter pathways to treat cognitive impairment associated with schizophrenia (CIAS). The drug is being evaluated in Phase I clinical trials to determine its safety, tolerability, and pharmacokinetic profile in healthy volunteers.