iclepertin + bosentan

iclepertin + bosentan refers to the co-administration of iclepertin (BI 425809), a selective glycine transporter-1 (GlyT1) inhibitor, and bosentan, a dual endothelin receptor antagonist. This combination has been primarily utilized in Phase 1 clinical pharmacology studies to evaluate drug-drug interactions. Iclepertin is being developed by Boehringer Ingelheim for cognitive impairment associated with schizophrenia (CIAS) and potentially other CNS disorders, acting to enhance NMDA receptor signaling by increasing synaptic glycine concentrations. Bosentan, a potent inducer of CYP3A4 and CYP2C9 enzymes, is used in these studies to determine the extent to which its induction affects the metabolic clearance and systemic exposure of iclepertin, which is a substrate for these metabolic pathways.

Other names

BI 425809 + bosentan