CVN766

CVN766 is a highly selective, orally active small-molecule antagonist of the orexin 1 receptor (Ox1R), developed by Cerevance for the treatment of psychiatric and CNS-controlled metabolic disorders. Orexin is a neuropeptide involved in regulating mood, motivation, reward pathways, and stress responses; dysregulation of orexin signaling has been implicated in psychiatric conditions such as schizophrenia, addictions (including food), and anxiety. Unlike previous compounds that also antagonize the orexin 2 receptor (Ox2R) and cause unwanted somnolence or sleep effects, CVN766 demonstrates over 1,000-fold selectivity for Ox1R versus Ox2R. This high selectivity may mitigate off-target risks like somnolence observed with less selective agents. Preclinical studies show that CVN766 has high brain permeability and prolonged receptor occupancy with a favorable pharmacokinetic and safety profile suitable for clinical evaluation across various psychiatric indications. It has demonstrated efficacy in preclinical models relevant to cognition deficits, negative symptoms of schizophrenia, dependency-type behaviors (binge eating, alcohol/nicotine dependence), and anxiety[1][2][5][7].