• SKIP TO CONTENT
  • SKIP NAVIGATION
  • Patient Resources
    • Clinical Trial Listings
    • What are Clinical Trials?
    • Become a Clinical Trial Volunteer
    • Useful Resources
    • FDA Approved Drugs
  • Professional Resources
    • Research Center Profiles
    • Market Research
    • Benchmark Reports
    • FDA Approved Drugs
    • Training Guides
    • Books
    • eLearning
    • Events
    • Newsletters
    • White Papers
    • SOPs
  • White Papers
  • Clinical Trial Listings
  • Advertise
  • Sign In
  • Create Account
  • Sign Out
  • My Account
Home » Directories » FDA Approved Drugs » Rexulti (brexpiprazole)

AND
  • A
  • B
  • C
  • D
  • E
  • F
  • G
  • H
  • I
  • J
  • K
  • L
  • M
  • N
  • O
  • P
  • Q
  • R
  • S
  • T
  • U
  • V
  • W
  • X
  • Y
  • Z

Rexulti (brexpiprazole)

  • Profile

Profile

Contact Information

Contact: Otsuka Pharmaceuticals
Website: https://www.rexulti.com/

Currently Enrolling Trials

    Show More

    Rexulti (brexpiprazole) - 3 indications

    Scroll down for additional information for each indication:
    • for the treatment of depression and schizophrenia in adults; approved July 2015 
    • for the treatment of agitation associated with dementia due to Alzheimer’s disease; approved May of 2023

    General Information

    Rexulti (brexpiprazole) is an atypical antipsychotic.

    Rexulti is specifically indicated:

    • for use as an adjunctive therapy to antidepressants for the treatment of major depressive disorder (MDD) in adults
    • for the treatment of schizophrenia in adults and pediatric patients ages 13 years and older
    • for the treatment of agitation associated with dementia due to Alzheimer’s disease

    Rexulti is supplied as a tablet for oral administration. Scroll down for specific dosing and administration recommendations for each indication: 

    Mechanism of Action

    Rexulti (brexpiprazole) is an atypical antipsychotic. The mechanism of action of brexpiprazole in the treatment of major depressive disorder or schizophrenia is unknown. However, the efficacy of brexpiprazole may be mediated through a combination of partial agonist activity at serotonin 5-HT1A and dopamine D2 receptors, and antagonist activity at serotonin 5-HT2A receptors. 

    Side Effects

    Adverse effects associated with the use of Rexulti may include, but are not limited to, the following:

    • akathisia
    • weight gain

    Rexulti comes with a black box warning of increased mortality in elderly patients with dementia-related psychosis; and a potential risk in the increase of the risk of suicidal thoughts and behaviors in patients aged 24 years and younger.

  • Indication 1 - as an adjunctive therapy to antidepressants for the treatment of major depressive disorder (MDD) in adults

  • approved July 2015

  • Dosing/Administration
  • The recommended starting dose is 0.5 mg or 1 mg once daily, taken orally with or without food. Titrate to 1 mg once daily, then up to the target dosage of 2 mg once daily. Dosage increases should occur at weekly intervals based on the patient’s clinical response and tolerability. The maximum recommended daily dosage is 3 mg. Periodically reassess to determine the continued need and appropriate dosage for treatment.

  • Clinical Trial Results
  • The efficacy of Rexulti in the adjunctive treatment of major depressive disorder (MDD) was evaluated in two 6-week, double-blind, placebo-controlled, fixed-dose trials of adults meeting DSM-IV-TR criteria for MDD, with or without symptoms of anxiety, who had an inadequate response to prior antidepressant therapy (1 to 3 courses) in the current episode and who had also demonstrated an inadequate response throughout the 8 weeks of prospective antidepressant treatment. In Study 228 (Study 1) subjects were randomized to Rexulti 2 mg once a day or placebo. In Study 227 (Study 2) subjects were randomized to Rexulti 1 or 3 mg once a day or placebo. For subjects randomized to Rexulti, all subjects initiated treatment at 0.5 mg once daily during Week 1. At Week 2, the Rexulti dosage was increased to 1 mg in all treatment groups, and either maintained at 1 mg or increased to 2 mg or 3 mg once daily, based on treatment assignment, from Week 3 onwards. The dosages were then maintained for the 4 remaining weeks. The primary endpoint was change from baseline to Week 6 in the Montgomery-Asberg Depression Rating Scale (MADRS), a 10-item clinician-related scale used to assess the degree of depressive symptomatology, with 0 representing no symptoms, and 60 representing worst symptoms. At randomization, the mean MADRS total score was 27. In both studies adjunctive brexpiprazole showed greater improvement than adjunctive placebo in MADRS total score at Week 6 in the efficacy population per final protocol in Study 1 (2mg+ADT [N=175]: -3.21), and in Study 2 (1mg+ADT [N=211]: -1.30, 3mg+ADT [N=213]: -1.95). Similar results were observed for the efficacy population in both studies. The completion rate was high (>90%) and comparable across brexpiprazole and placebo groups.

  • Indication 2 - for the treatment of schizophrenia in adults and pediatric patients ages 13 years and older

  • approved July 2015

  • Dosing/Administration
  • Adults:
  • The recommended starting dose is is 1 mg once daily on Days 1 to 4, taken orally with or without food. The recommended target dosage is 2 mg to 4 mg once daily. Titrate to 2 mg once daily on Day 5 through Day 7, then to 4 mg on Day 8 based on the patient’s clinical response and tolerability. The maximum recommended daily dosage is 4 mg. Periodically reassess to determine the continued need and appropriate dosage for treatment. 
  • Pediatrics 13 to 17 years of age:
  • The recommended starting dose is 0.5 mg/day. The recommended maintenance dose is 2 to 4 mg/day and the maximum dose is 4 mg/day.

  • Clinical Trial Results
    The efficacy of Rexulti in the treatment of adults with schizophrenia was demonstrated in two 6-week, randomized, double-blind, placebo-controlled, fixed-dose clinical trials in subjects who met DSM-IV-TR criteria for schizophrenia. In both studies, Study 231 (Study 3) and Study 230 (Study 4), subjects were randomized to Rexulti 2 or 4 mg once per day or placebo. Subjects in the Rexulti groups initiated treatment at 1 mg once daily on Days 1 to 4. The Rexulti dosage was increased to 2 mg on Days 5 to 7. The dosage was then either maintained at 2 mg once daily or increased to 4 mg once daily, depending on treatment assignment, for the 5 remaining weeks. The primary efficacy endpoint of both trials was the change from baseline to Week 6 in the Positive and Negative Syndrome Scale (PANSS) total score. In one study, brexpiprazole 4mg and 2mg demonstrated greater improvement than placebo in the primary endpoint of change from baseline to Week 6 in Positive and Negative Syndrome Scale (PANSS) Total Score (4mg: -19.65 and 2mg: -20.73 vs. placebo -12.01; 0.25mg was similar to placebo -14.90). In the other study, brexpiprazole 4mg showed improvement over placebo in the primary endpoint of PANSS Total Score from baseline to Week 6 (-20.0 vs. -13.5), while the 2mg (-16.6) and 1mg (-16.9) doses showed numeric improvement versus placebo (-13.5). 

  • Indication 3 - for the treatment of agitation associated with dementia due to Alzheimer’s disease

  • approved May 2023

  • Dosing/Administration
  • The recommended starting dose is 0.5 mg taken once daily on Days 1 to 7. Increase the dosage on Days 8 through 14 to 1 mg once daily, and on Day 15 to 2 mg once daily. The recommended target dose is 2 mg once daily. The dosage can be increased to the maximum recommended daily dosage of 3 mg once daily after at least 14 days, based on clinical response and tolerability.

  • Clinical Trial Results
  • FDA approval was based on two Phase 3, 12-week, randomized, double-blind, placebo-controlled fixed-dose studies that evaluated the frequency of agitation symptoms in patients with dementia due to Alzheimer’s disease based on the Cohen-Mansfield Agitation Inventory (CMAI) total score. The primary endpoint was a change in agitation symptom frequency (CMAI total score) from baseline at Week 12 in both studies. Brexpiprazole patients with agitation associated with dementia due to Alzheimer’s disease achieved a 31% greater reduction from baseline in frequency of agitation symptoms vs. placebo.
  • Approval Date: 2015-07-01
    Company Name: Otsuka
    Back to Listings

    Upcoming Events

    • 14Apr

      MAGI 2024: The Clinical Research Conference

    Featured Products

    • Surviving an FDA GCP Inspection

      Surviving an FDA GCP Inspection: Resources for Investigators, Sponsors, CROs and IRBs

    • Best Practices for Clinical Trial Site Management

      Best Practices for Clinical Trial Site Management

    Featured Stories

    • Jonathan Seltzer

      Thought Leadership: Remote Patient Monitoring Gives New View of Safety in Cardiac Clinical Trials

    • Quality_Compass-360x240.png

      Ask the Experts: Applying Quality by Design to Protocols

    • Obesity Treatment Patient

      Clinical Trials Need Greater Representation of Obese Patients, Experts Say

    • Modernize-360x240.png

      FDA IT Modernization Plan Prioritizes Data-Sharing, AI, Collaboration and More

    Standard Operating Procedures for Risk-Based Monitoring of Clinical Trials

    The information you need to adapt your monitoring plan to changing times.

    Learn More Here
    • About Us
    • Contact Us
    • Privacy Policy
    • Do Not Sell or Share My Data

    Footer Logo

    300 N. Washington St., Suite 200, Falls Church, VA 22046, USA

    Phone 703.538.7600 – Toll free 888.838.5578

    Copyright © 2023. All Rights Reserved. Design, CMS, Hosting & Web Development :: ePublishing