Brexpiprazole – Psychopharmacology | Mechanism of Action | Clinical Application

Posted on:June 17, 2022
Last Updated: November 25, 2023
Time to read: 11–13 minutes

Brexpiprazole (Rexulti) is a partial dopamine (D2) agonist.

Brexpiprazole [7-{4-[4-(1-benzothiophene-4-yl) piperazin-1-yl]butoxy}quinolin-2(1H)-one] is a novel atypical antipsychotic that is structurally similar to the atypical antipsychotic, aripiprazole. [Maeda et al., 2014]. 

Brexpiprazole acts as a partial agonist at Dopamine D2 and Serotonin 5-HT1A receptors and is classified as a serotonin-dopamine activity modulator (SDAM). [Kikuchi et al., 2021]

Partial dopamine agonists as a group have been categorised as third-generation antipsychotics.  [Mailman et al., 2010]

The US FDA approved Brexpiprazole in July 2015 for the treatment of schizophrenia as well as adjunctive therapy to antidepressant medications for the treatment of major depressive disorder. [Rexulti (package insert)]

In Australia, it is approved only for the treatment of schizophrenia.

The current therapeutic model is to offer a broad-based strategy that treats positive (hallucination, delusion, and thought disorders) and negative (social withdrawal, lack of energy, emotion, and motivation) symptoms as well as improves cognitive deficits. [Lieberman et al., 2007]