Brexpiprazole: First Global Approval

Brexpiprazole (Rexulti (R)) is an atypical antipsychotic that has been developed by Otsuka Pharmaceutical Co. Ltd and H. Lundbeck A/S as an oral treatment for several psychiatric disorders. Brexpiprazole is a novel serotonin-dopamine activity modulator that acts as a partial agonist of serotonin 1A (5-HT1A) and dopamine D-2 receptors, as well as a potent antagonist of 5-HT2A receptors and noradrenergic alpha(1B) and alpha(2C) receptors. In July 2015, brexpiprazole received its first approval in the USA for use as an adjunctive treatment of major depressive disorder (MDD) and the treatment of schizophrenia. In several countries, brexpiprazole is in development for MDDs, schizophrenia, post-traumatic stress disorder and agitation in patients with dementia of the Alzheimer's type. This article summarizes the milestones in the development of brexpiprazole leading to its first global approval in MDD and schizophrenia.