Background: Schizophrenia is a chronic and debilitating mental disorder that affects the
patient’s and their family's life. The disease remains a complicated disorder that is challenging to
treat, despite there being a large antipsychotic armamentarium. Brexpiprazole acts both as a partial
agonist at the serotonin 5-HT1A and dopamine D2 receptors and as an antagonist at the serotonin 5-
HT2A and noradrenaline alpha1B and alpha2C receptors, all with similar potency. This balanced receptor
profile may produce promising antipsychotic effects on positive, negative and cognitive symptoms
in schizophrenia with minimal adverse effects.
Methods: This review summarizes the pharmacodynamics and pharmacokinetic profile of brexpiprazole
and the clinical trial information pertaining to its effectiveness and safety and tolerability, discusses
its best clinical use, and compares its clinical profile to those of other widely used antipsychotic
Results: Brexpiprazole demonstrated significant clinical efficacy and had good safety and tolerability
in well-designed trials with patients with schizophrenia. This agent may be a useful treatment alternative.
Conclusion: However, it will be valuable to consider a long-term observational study that includes an
active comparator, especially other second-generation antipsychotics (SGAs), to further evaluate the
efficacy and safety of brexpiprazole in the treatment of schizophrenia.