Brexpiprazole-Pharmacologic Properties and Use in Schizophrenia and Mood Disorders

In 2002, the first III generation antipsychotic drug was registered-aripiprazole. Its partial dopaminergic agonism underlies its unique mechanism of action and the potentially beneficial influence on the positive, negative, or cognitive symptoms. Due to its relatively high intrinsic activity, the drug could often cause agitation, anxiety, or akathisia. For this reason, efforts were made to develop a drug which would retain the positive favorable actions of aripiprazole but present a more advantageous clinical profile. This turned out to be brexpiprazole, which was registered in 2015. Its pharmacodynamic and pharmacokinetic profile (similarly to the other most recent antipsychotics, i.e., lurasidone or cariprazine) shows promise of increasing the effectiveness of schizophrenia treatment in the dimensions in which the previous antipsychotics were not sufficiently effective, including negative, depressive, or cognitive symptoms. Like other new antipsychotics, it can also be useful in the treatment of mood disorders, for instance drug-resistant depression. Previous reviews focused on the use of brexpiprazole in specific diagnostic groups. The aim of this article is to provide the readers with an overview of data on the mechanism of action, clinical effectiveness in all studied diagnostic groups, as well as potential drug-food interactions, and the safety of brexpiprazole.

Automated summary

The first III generation antipsychotic drug, aripiprazole, was registered in 2002. It has a unique mechanism of action and potentially beneficial influence on symptoms of schizophrenia. However, it can cause agitation, anxiety, or akathisia. Brexpiprazole, registered in 2015, was developed to retain the positive actions of aripiprazole while presenting a better clinical profile. It shows promise in treating symptoms that previous antipsychotics were not sufficiently effective in, including negative, depressive, or cognitive symptoms.