Brexpiprazole: A Review in Schizophrenia

• Published in: Drugs (New York, N.Y.) N.Y.), 2019-02, Vol.79 (2), p.189-200
• Main Author: Frampton, James E.
• Format: Article
• Language: English
• Subjects: Adis Drug Evaluation; Adults; Antipsychotic Agents - administration & dosage; Antipsychotic Agents - adverse effects; Antipsychotic Agents - therapeutic use; Antipsychotics; Aripiprazole; Aripiprazole - therapeutic use; Dopamine; Dopamine Agonists - therapeutic use; Dopamine D2 receptors; Dose-Response Relationship, Drug; Drug Approval; Drug dosages; Extrapyramidal system; Humans; Internal Medicine; Japan; Medicine; Medicine & Public Health; Mental disorders; Metabolism; Noradrenaline; Norepinephrine; Patients; Pharmacology/Toxicology; Pharmacotherapy; Psychosis; Psychotropic drugs; Quinolones - administration & dosage; Quinolones - adverse effects; Quinolones - therapeutic use; Receptors; Schizophrenia; Schizophrenia - drug therapy; Serotonin; Serotonin Receptor Agonists - therapeutic use; Serotonin S1 receptors; Serotonin S2 receptors; Signs and symptoms; Social interactions; Statistical analysis; Studies; Thiophenes - administration & dosage; Thiophenes - adverse effects; Thiophenes - therapeutic use; United States; Weight
• ISSN: 0012-6667; 1179-1950
• DOI: 10.1007/s40265-019-1052-5

Brexpiprazole (Rxulti ® , Rexulti ® ) is an oral atypical antipsychotic agent approved for the treatment of schizophrenia in the EU (in adult patients) and the USA, as well as in some other countries, including Japan. Like aripiprazole, it is a partial agonist at dopamine D 2 and serotonin 5-HT 1A receptors and an antagonist at serotonin 5-HT 2A receptors. However, brexpiprazole displays less intrinsic activity at D 2 receptors and, coupled with actions at 5HT 1A , 5HT 2A and noradrenaline α 1B receptors that are at least as potent as its action at D 2 receptors, is predicted to demonstrate a lower propensity for activating adverse events and extrapyramidal symptoms than aripiprazole. Brexpiprazole 2–4 mg/day produced statistically significant and clinically meaningful improvements in overall symptomatology and psychosocial functioning compared with placebo in adults with acute exacerbation of schizophrenia. As maintenance treatment, brexpiprazole 1–4 mg/day significantly delayed the time to relapse compared with placebo in patients who were already stabilized on the drug and was associated with stabilization or continued improvement in patients’ symptoms and functioning. Brexpiprazole was generally well tolerated, exhibiting an adverse event profile characterized by a relatively low incidence of activating and sedating adverse effects, small changes in QT interval and metabolic parameters that were not clinically significant, and moderate weight gain. Clinical evidence to date suggests it usefully extends the range of therapeutic options for schizophrenia.