Brexpiprazole for the treatment of schizophrenia

ABSTRACT

Brexpiprazole (OPC-34712) is a novel serotonin-dopamine activity modulator, which has recently been approved by the U.S Food and Drug Administration for the treatment of schizophrenia. The aim of this paper is to systematically synthesize all data of the efficacy, safety and tolerability of Brexpiprazole in treating schizophrenia. The terms ‘Brexpiprazole’, ‘OPC-34712’ and ‘schizophrenia’ were searched. A total of 12 clinical trials with 7 available data records were found. The pooled effect size of Brexpiprazole 1 mg, 2 mg and 4 mg were all superior to placebo in terms of the change from baseline in positive and negative syndrome scale (PANSS) total score at week 6 (weighted mean difference = −3.74, p = 0.044; weighted mean difference = −5.76, p < 0.01 and weighted mean difference = −7.03, p < 0.01, respectively) when compared to that of the placebo in treating acute schizophrenia. Brexpiprazole displays a good safety and tolerability profile. The incidence of akathisia, headache, insomnia, sedation, agitation, diarrhea, weight gained, nausea, and dyspepsia are comparable to placebo.

KEYWORDS:

• Partial dopamine agonist
• schizophrenia
• D2 receptor partial agonist
• Brexpiprazole
• OPC-34712

Financial & competing interests disclosure

The author has no relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript. This includes employment, consultancies, honoraria, stock ownership or options, expert testimony, grants or patents received or pending, or royalties.

Key issues

• Brexpiprazole is a novel serotonin-dopamine activity modulator (SDAM), a partial agonist at 5-HT_1A and dopamine D₂ receptors.

• Brexpiprazole equates to a superior successor of Aripiprazole (Abilify), with slightly different activities at the serotonin and dopamine receptors, and this could imply an improved clinical profile with fewer side effects such as restlessness and akathisia.

• In terms of efficacy, Brexpiprazole 4 mg showed statistically significant improvement over placebo in both the primary end point (PANSS total score) and secondary end point.

• Brexpiprazole 4 mg was the optimal effective dose for treating patients with acute episode of schizophrenia.

• Brexpiprazole displayed a good safety and tolerability profile. The incidence of akathisia, headache, insomnia, sedation, agitation, diarrhea, weight gained, nausea, and dyspepsia were comparable to placebo.

• Overall, there were no significant changes in lipid profiles or glycemic parameters in long term use of Brexpiprazole as maintenance treatment of schizophrenia