BACKGROUND: Schizophrenia is a chronic and debilitating mental
disorder that affects the patient’s and their family’s life. The disease
remains a complicated disorder that is challenging to treat, despite there
being a large antipsychotic armamentarium. Brexpiprazole acts both as a
partial agonist at the serotonin 5-HT1A and dopamine D2 receptors and as an
antagonist at the serotonin 5-HT2A and noradrenaline alpha1B and alpha2C
receptors, all with similar potency. This balanced receptor profile may
produce promising antipsychotic effects on positive, negative and cognitive
symptoms in schizophrenia with minimal adverse effects.
METHODS: This review summarizes the pharmacodynamics and pharmacokinetic
profile of brexpiprazole and the clinical trial information pertaining to
its effectiveness and safety and tolerability, discusses its best clinical
use, and compares its clinical profile to those of other widely used
RESULTS: Brexpiprazole demonstrated significant clinical efficacy and had
good safety and tolerability in well-designed trials with patients with
schizophrenia. This agent may be a useful treatment alternative.
CONCLUSION: However, it will be valuable to consider a long-term
observational study that includes an active comparator, especially other
second-generation antipsychotics (SGAs), to further evaluate the efficacy
and safety of brexpiprazole in the treatment of schizophrenia.
Keywords: Brexpirazole, metabolism, schizophrenia, pharmacological
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