Brexpiprazole: A Novel Third-generation Antipsychotic Drug

Abstract

Brexpiprazole, a third-generation antipsychotic drug, was approved for the treatment of schizophrenia and as adjunctive treatment of major depressive disorder in 2015 by the US Food and Drug Administration. The drug is structurally and pharmacologically similar to aripiprazole. Its mechanism of action is serotonin-dopamine activity modulator. It has higher affinity to 5-HT_1A, α_1B, D₂, 5-HT_2A and α_2C, but lower intrinsic activity at dopamine D₂ receptor than aripiprazole. It was also found that brexpiprazole had low antimuscarinic activity. However, the efficacy of brexpiprazole is non-inferior compared with aripiprazole for improving positive and negative symptoms of schizophrenia. Some studies reported that brexpiprazole was better than aripiprazole at reducing impulsi–vity and showing some benefits of social function. In terms of safety, cardiometabolic effects, including weight gain, hypertriglyceridemia and hyperglycemia, are common adverse effects. Nevertheless, the incidence of extrapyramidal symptoms (EPS) and hyperprolactinemia are re–latively low. Compared to aripiprazole, patients treated with brexpiprazole were well tolerated as akathisia was lower. Hence, brexpiprazole is considered to be an alternative drug for trea–ting positive, negative, and cognitive symptoms in patients with acute and chronic schizophrenia, as well as for patients who are intolerant to adverse effects such as EPS, hyperprolactinemia from other antipsychotics.