Brexpiprazole (brand name Rexulti) is a second-generation (“atypical”) antipsychotic first introduced in the US in 2015. Rexulti® is manufactured by Otsuka Pharmaceutical Company Ltd and co-marketed with H. Lundbeck A/S.
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.
Recommended target dose is 2 mg to 4 mg once daily.
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
Please refer to Prescribing Information (see link below) for complete discussion of dosage, administration, warnings and precautions, contraindications, etc.
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.
Copyright 2016, Rajnish Mago, MD. All rights reserved. May not be reproduced in any form without express written permission.
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