Prakt. Lékáren. 2019; 15(1e) | DOI: 10.36290/lek.2019.023

Brexpiprazole

Miloslav Kopeček
Národní ústav duševního zdraví Klecany a Klinika psychiatrie 3. LF UK Praha

Brexpiprazole is a second generation antipsychotic that works as a partial agonist at serotonin 5-HT1A and dopamine D2 receptors and an antagonist
at serotonin 5-HT2A. Brexpiprazole showed efficacy for the treatment of schizophrenia in the range of 2 to 4 mg/d and as an adjunct to
antidepressant therapy in major depressive disorder when dosed at 2 to 3 mg/d. It has European Medicines Agency approval for monotherapy
treatment of adult schizophrenia but has not approval for adjunctive treatment to antidepressants for MDD as in USA. The most common adverse effects include akathisia and weight gain. Advantages of brexpiprazole include once -daily dosing, good tolerability, and lack of effect
on QTc interval and sexual function.

Keywords: antipsychotic, brexpiprazole, depressive disorder, partial dopamine agonist, schizophrenia

Published: March 15, 2019  Show citation

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Kopeček M. Brexpiprazole. Praktické lékárenství. 2019;15(E-verze 1/19):. doi: 10.36290/lek.2019.023.
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References

  1. Češková E. Postavení aripiprazolu v klinické praxi. Čes a slov Psychiatrie 2011; 107: 110-114.
  2. Mohr P, Kopeček M, Brunovský M, et al. Kariprazin in Klinická psychofarmakologie. Maxdorf, 2017, pp.161-164.
  3. Ceskova E, Silhan P. Novel treatment options in depression and psychosis. Neuropsychiatr Dis Treat 2018; 14: 741-747. Go to original source... Go to PubMed...
  4. 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; 69: 1211-1220. Go to original source... Go to PubMed...
  5. Maeda K, Sugino H, Akazawa H, et al. Brexpiprazole I: in vitro and in vivo characterization of a novel serotonin-dopamine activity modulator. J Pharmacol Exp Ther 2014; 350: 589-604. Go to original source... Go to PubMed...
  6. Mohr P, Kopeček M, Brunovský M, et al. Brexpiprazol, in Klinická psychofarmakologie. Maxdorf, 2017, pp.135-138.
  7. Stahl SM. Mechanism of action of brexpiprazole: comparison with aripiprazole. CNS Spectr 2016; 21:1-6. Go to original source...
  8. Citrome L, Ota A, Nagamizu K, et al. The effect of brexpiprazole (OPC-34712) and aripiprazole in adult patients with acute schizophrenia: results from a randomized, exploratory study. Int Clin Psychopharmacol 2016; 31: 192-201. Go to original source... Go to PubMed...
  9. Citrome L. Activating and Sedating Adverse Effects of Second-Generation Antipsychotics in the Treatment of Schizophrenia and Major Depressive Disorder. Absolute Risk Increase and Number Needed to Harm. J Clin Psychopharmacol 2017; 37: 138-147. Go to original source... Go to PubMed...
  10. Stoner SC. Management of serious cardiac adverse effects of antipsychotic medications. Ment Health Clin 2017; 7: 246-254. Go to original source... Go to PubMed...
  11. Polcwiartek C, Sneider B, Graff C, et al. The cardiac safety of aripiprazole treatment in patients at high risk for torsade: a systematic review with a meta-analytic approach. Psychopharmacology (Berl) 2015; 232: 3297-3308. Go to original source...
  12. Chattopadhyay A, Frey S,Green G. Bifeprunox versus placebo for schizophrenia. Cochrane Database Syst Rev 2016; 10: CD012029. Go to original source...
  13. Maeda K, Lerdrup L, Sugino H, et al. Brexpiprazole II: antipsychotic-like and procognitive effects of a novel serotonin-dopamine activity modulator. J Pharmacol Exp Ther 2014; 350: 605-614. Go to original source... Go to PubMed...
  14. Rexulti (brexpiprazole) [product information]. Tokyo, Japan: Otsuka Pharmaceutical Co, Ltd 2015.
  15. I. OPDC: PET Trial to Assess the Receptor Occupancy of Brexpiprazole in Adult Subjects With Schizophrenia. [cited 2018 Nov 11]. Available from: http://clinicaltrials.gov/show/NCT01854944
  16. Correll CU, Skuban A, Ouyang J, et al. Efficacy and Safety of Brexpiprazole for the Treatment of Acute Schizophrenia: A 6-Week Randomized, Double-Blind, Placebo-Controlled Trial. Am J Psychiatry 2015; 172: 870-880. Go to original source... Go to PubMed...
  17. Kane JM, Skuban A, Ouyang J, et al. A multicenter, randomized, double-blind, controlled phase 3 trial of fixed-dose brexpiprazole for the treatment of adults with acute schizophrenia. Schizophr Res 2015; 164: 127-135. Go to original source... Go to PubMed...
  18. Ishigooka J, Iwashita S,Tadori Y. Efficacy and safety of brexpiprazole for the treatment of acute schizophrenia in Japan: A 6-week, randomized, double-blind, placebo-controlled study. Psychiatry Clin Neurosci 2018; 72: 692-700. Go to original source... Go to PubMed...
  19. Kishi T, Oya K, Matsui Y, et al. Comparison of the efficacy and safety of 4 and 2 mg/day brexpiprazole for acute schizophrenia: a meta-analysis of double-blind, randomized placebo-controlled trials. Neuropsychiatr Dis Treat 2018; 14: 2519-2530. Go to original source... Go to PubMed...
  20. Fleischhacker WW, Hobart M, Ouyang J, et al. Efficacy and Safety of Brexpiprazole (OPC-34712) as Maintenance Treatment in Adults with Schizophrenia: a Randomized, Double-Blind, Placebo-Controlled Study. Int J Neuropsychopharmacol 2017; 20: 11-21. Go to original source...
  21. Thase ME, Youakim JM, Skuban A, et al. 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; 76: 1224-1231. Go to original source... Go to PubMed...
  22. Thase ME, Youakim JM, Skuban A, et al. 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; 76: 1232-1240. Go to original source... Go to PubMed...
  23. Hobart M, Skuban A, Zhang P, et al. A Randomized, Placebo-Controlled Study of the Efficacy and Safety of Fixed-Dose Brexpiprazole 2 mg/d as Adjunctive Treatment of Adults With Major Depressive Disorder. J Clin Psychiatry 2018; 79. Go to original source... Go to PubMed...
  24. Bauer M, Hefting N, Lindsten A, et al: A randomised, placebo-controlled 24-week study evaluating adjunctive brexpiprazole in patients with major depressive disorder. Acta Neuropsychiatr 2018; 1-9. Go to original source... Go to PubMed...
  25. Lepola U, Hefting N, Zhang D, et al. Adjunctive brexpiprazole for elderly patients with major depressive disorder: An open-label, long-term safety and tolerability study. Int J Geriatr Psychiatry 2018; 33: 1403-1410. Go to original source... Go to PubMed...
  26. Otsuka Pharmaceutical Development & Commercialization I. A study of two fixed-doses of brexpiprazole in the treatment of subjects with agitation associated with dementia of the Alzheimer's type [Internet] Bethesda (MD): National Library of Medicine (US); 2000 [cited 2018 Nov 11]. Available from: http://clinicaltrials.gov/show/NCT01862640
  27. Rexulti, brexpiprazole (summary of product characteristics). the European Medicines Agency http://www.ema.europa.eu. 2018.
  28. Ivkovic J, Lindsten A, George V, et a. Effect of Brexpiprazole on Prolactin: An Analysis of Short- and Long-Term Studies in Schizophrenia. J Clin Psychopharmacol 2019; 39: 13-19. Go to original source... Go to PubMed...
  29. Forbes A, Hobart M, Ouyang J, et al. A Long-Term, Open-Label Study to Evaluate the Safety and Tolerability of Brexpiprazole as Maintenance Treatment in Adults with Schizophrenia. Int J Neuropsychopharmacol 2018; 21: 433-441. Go to original source... Go to PubMed...
  30. Newcomer JW, Eriksson H, Zhang P, et al. Changes in metabolic parameters and body weight in brexpiprazole-treated patients with acute schizophrenia: pooled analyses of phase 3 clinical studies. Curr Med Res Opin 2018; 34: 2197-2205. Go to original source... Go to PubMed...
  31. Otsuka America Pharmaceutical I. Data on file (REX-024). Safety Profile for REXULTI(R) (brexpiprazole) as Adjunctive Treatment in MDD, 2018. [cited 2019 Jan 14]. Available from: https://www.rexultihcp.com/mdd/safety
  32. Markovic M, Gallipani A, Patel KH, et al. Brexpiprazole. Ann Pharmacother 2017; 51: 315-322. Go to original source... Go to PubMed...
  33. Diefenderfer LA,Iuppa C: Brexpiprazole. A review of a new treatment option for schizophrenia and major depressive disorder. Ment Health Clin 2017; 7: 207-212. Go to original source... Go to PubMed...
  34. Moore TJ, Glenmullen J,Mattison DR. Reports of pathological gambling, hypersexuality, and compulsive shopping associated with dopamine receptor agonist drugs. JAMA Intern Med 2014; 174: 1930-1933. Go to original source... Go to PubMed...
  35. Hiemke C, Bergemann N, Clement HW, et al. Consensus Guidelines for Therapeutic Drug Monitoring in Neuropsychopharmacology: Update 2017. Pharmacopsychiatry 2018; 51: 9-62. Go to original source... Go to PubMed...
  36. 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; 69: 978-997. Go to original source... Go to PubMed...
  37. Frankel JS,Schwartz TL. Brexpiprazole and cariprazine: distinguishing two new atypical antipsychotics from the original dopamine stabilizer aripiprazole. Ther Adv Psychopharmacol 2017; 7: 29-41. Go to original source... Go to PubMed...




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