Brexpiprazole is an atypical antipsychotic used mainly for the treatment of schizophrenia and as an adjunct in major depressive disorder (MDD). It acts as a serotonin–dopamine activity modulator, with partial agonist effects on dopamine D2 and serotonin 5-HT1A receptors and antagonist activity at serotonin 5-HT2A receptors, which together contribute to its antipsychotic and antidepressant actions. Brexpiprazole was developed as a next-generation alternative to aripiprazole, designed to maintain efficacy while improving tolerability and reducing side effects such as akathisia. It was first approved by the U.S. FDA on 10 July 2015 (marketed as Rexulti) for schizophrenia and as an add-on treatment for MDD in adults. Later, on 11 May 2023, it received FDA approval for the treatment of agitation associated with dementia due to Alzheimer’s disease, becoming the first approved therapy for this condition. Overall, brexpiprazole is recognized as a well-tolerated and effective option in modern psychiatric treatment.