Brexpiprazole (brand name Rexulti) is a second-generation (“atypical”) antipsychotic first introduced in the US in 2015.
As of March 2020, it is available only as a brand name preparation (no generic), Rexulti®, that is manufactured by Otsuka Pharmaceutical Company Ltd and co-marketed with H. Lundbeck A/S.
On this page, we present basic information about this medication. Other articles on this website with more advanced information and tips related to this medication are linked to under Related Pages below.
1. The treatment of schizophrenia
2. Adjunctive therapy to antidepressants for the treatment of major depressive disorder (MDD).
1. Partial agonist at the 5-HT1A, D2, and D3 receptors
2. Antagonist at 5-HT2A, 5-HT2B, 5-HT7, alpha-1 (subtypes A, B, and D), and alpha-2C receptors.
1. For adjunctive treatment of major depressive disorder
Recommended starting dosage– 0.5 mg or 1 mg once daily Titrate up to the target dosage of 2 mg once daily
Maximum recommended daily dosage–3 mg.
2. For the treatment of schizophrenia
Recommended starting dosage is 1 mg/day for four days
Then, 2 mg/day for three days Then 4 mg/day.
The recommended target dose is 2 mg to 4 mg once daily.
Potential side effects
Please see THIS PAGE for a handout listing both the common and less common side effects of this medication along with the percentages of patients who report them.
Dose adjustments are recommended for patients who are:
1. Poor metabolizers on the CYP450 2D6 isoenzyme, or
2. Taking strong inducers/ inhibitors of CYP2D6 and/or CYP3A4.
Dosage forms and strengths
Rexulti® is available as tablets in the following dosage strengths: 0.25 mg, 0.5 mg, 1 mg, 2 mg, 3 mg, and 4 mg
Important! Please refer to the full Prescribing Information (see link below) before prescribing this medication.
Citrome L. Brexpiprazole for schizophrenia and as adjunct for major depressive disorder: a systematic review of the efficacy and safety profile for this newly approved antipsychotic – what is the number needed to treat, number needed to harm and likelihood to be helped or harmed? Int J Clin Pract. 2015 Sep;69(9):978-97. PubMed PMID: 26250067.
Citrome L. The ABC’s of dopamine receptor partial agonists – aripiprazole, brexpiprazole and cariprazine: the 15-min challenge to sort these agents out. Int J Clin Pract. 2015 Nov;69(11):1211-20. PubMed PMID: 26477545.
Goff DC. Brexpiprazole: A New Antipsychotic Following in the Footsteps of Aripiprazole. Am J Psychiatry. 2015 Sep 1;172(9):820-1. PubMed PMID: 26324298.
Randomized, placebo-controlled clinical trials in schizophrenia
Correll CU, Skuban A, Ouyang J, Hobart M, Pfister S, McQuade RD, Nyilas M, Carson WH, Sanchez R, Eriksson H. Efficacy and Safety of Brexpiprazole for the Treatment of Acute Schizophrenia: A 6-Week Randomized, Double-Blind, Placebo-Controlled Trial. Am J Psychiatry. 2015 Sep 1;172(9):870-80. PubMed PMID: 25882325.
Kane JM, Skuban A, Ouyang J, Hobart M, Pfister S, McQuade RD, Nyilas M, Carson WH, Sanchez R, Eriksson H. A multicenter, randomized, double-blind, controlled phase 3 trial of fixed-dose brexpiprazole for the treatment of adults with acute schizophrenia. Schizophr Res. 2015 May;164(1-3):127-35. PubMed PMID: 25682550.
Randomized, placebo-controlled clinical trials of adjunctive use in major depressive disorder
Thase ME, Youakim JM, Skuban A, Hobart M, Zhang P, McQuade RD, Nyilas M, Carson WH, Sanchez R, Eriksson H. Adjunctive brexpiprazole 1 and 3 mg for patients with major depressive disorder following inadequate response to antidepressants: a phase 3, randomized, double-blind study. J Clin Psychiatry. 2015 Sep;76(9):1232-40. PubMed PMID: 26301771.
Thase ME, Youakim JM, Skuban A, Hobart M, Augustine C, Zhang P, McQuade RD, Carson WH, Nyilas M, Sanchez R, Eriksson H. Efficacy and safety of adjunctive brexpiprazole 2 mg in major depressive disorder: a phase 3, randomized, placebo-controlled study in patients with inadequate response to antidepressants. J Clin Psychiatry. 2015 Sep;76(9):1224-31. PubMed PMID: 26301701.
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