NYMC Faculty Publications

Brexpiprazole: A New Dopamine D₂Receptor Partial Agonist for the Treatment of Schizophrenia and Major Depressive Disorder

Author Type(s)

Faculty

DOI

10.1358/dot.2015.51.7.2358605

Journal Title

Drugs of Today

First Page

397

Last Page

414

Document Type

Article

Publication Date

7-1-2015

Department

Psychiatry and Behavioral Sciences

Keywords

Major Depressive Disorder, Dopamine Agonists, Humans, Quinolones, Receptors, Dopamine D2, Schizophrenia, Thiophenes

Disciplines

Medicine and Health Sciences

Abstract

Brexpiprazole is a dopamine D₂receptor partial agonist. Compared with aripiprazole, it is more potent at 5-HT1A receptors and displays less intrinsic activity at D₂receptors. Brexpiprazole also has potent antagonistic activity at 5-HT2A as well as alpha-adrenergic receptors. In addition to results from phase II trials, data are available from two pivotal phase III, randomized, placebo-controlled trials of brexpiprazole for the acute treatment of schizophrenia and two pivotal phase III, randomized, placebo-controlled trials of adjunctive brexpiprazole for the acute treatment of major depressive disorder in patients with inadequate response to antidepressant medication treatment. Overall tolerability is promising, with rates of discontinuation due to adverse events lower or slightly higher than that observed for placebo. Although overall akathisia was more commonly observed with brexpiprazole than with placebo, the absolute risk increase attributable to brexpiprazole appears small. Short-term weight gain appears modest; however, outliers with an increase of ≥ 7% of body weight were evident in open-label long-term safety studies.

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