Second-generation
antipsychotics have demonstrated efficacy for patients with
schizophrenia but are associated with wide-ranging side effects.
Brexpiprazole, a
serotonin-
dopamine activity modulator, has demonstrated efficacy in adult patients with
schizophrenia. This paper provides an overview of the safety and tolerability of
brexpiprazole in patients with
schizophrenia through examination of pooled safety data from one Phase 2 and two Phase 3 6-week, short-term studies, and two open-label, 52-week, long-term studies. In the short-term studies, there were no reports of treatment-emergent adverse events (TEAEs) with an incidence≥5% and twice that of placebo in patients treated with
brexpiprazole 2-4mg. In the long-term studies, TEAEs reported by ≥5% of patients were
schizophrenia (10.7%),
insomnia (8.0%), weight increase (7.7%),
headache (6.0%), and agitation (5.2%).
Akathisia rates were low in the short- (5.8%, pooled
brexpiprazole group) and long-term studies (4.6%). Sedation rates were low in the short- (2.3%, pooled
brexpiprazole group) and long-term studies (0.9%). Mean
body weight increase was 1.1kg in both short- and long-term studies. For all studies, changes from baseline to last visit in laboratory parameters, electrocardiogram values, and vital signs were small and not clinically relevant. Changes in
lipid profiles or other metabolic parameters were also small. Collectively, these studies suggest that
brexpiprazole was well tolerated, with a favorable safety profile that does not exhibit significant rates of important adverse events that can be seen with existing
antipsychotics (
akathisia, sedation,
weight gain, or QTc prolongation), and therefore may provide a useful treatment option for patients with
schizophrenia. ClinicalTrials.gov: NCT00905307; NCT01396421; NCT01393613; NCT01649557; NCT01397786.