Evaluating the efficacy and safety of the currently available once-every-two months long-acting injectable formulations of aripiprazole for the treatment of schizophrenia or as a maintenance monotherapy for bipolar I disorder in adults

ABSTRACT

Introduction

An aripiprazole long-acting injectable (LAI) antipsychotic is now available for gluteal administration every 2 months via two different formulations: aripiprazole lauroxil (AL) and aripiprazole monohydrate (Ari 2MRTU). These longer dosing regimens of aripiprazole LAI offer new potential benefits for patients.

Areas covered

The authors review the evidence supporting the efficacy and safety of aripiprazole LAIs given every 2 months for the treatment of schizophrenia or bipolar disorder (BD) in adults. The article culminates with the authors’ expert perspectives on the subject.

Expert opinion

AL 1064 mg every 2 months has established efficacy for the treatment of schizophrenia based on pharmacokinetic bridging studies and prospective data for treatment of an acute exacerbation of schizophrenia. In an open-label trial, Ari 2MRTU showed efficacy for the treatment of schizophrenia and BD type I based on pharmacokinetic parameters (comparable to aripiprazole once-monthly 400 mg); it also showed efficacy regarding the secondary endpoints. Multiple doses of AL 1064 mg or Ari 2MRTU 960 mg are generally well tolerated, in line with the safety profile of oral aripiprazole, with the exception of the injection-site reactions. While AL may require a 1-day initiation regimen, Ari 2MRTU 960 covers all the recommended doses of oral aripiprazole (10–20 mg).

KEYWORDS:

• Long-acting injectable
• aripiprazole
• antipsychotic
• schizophrenia
• bipolar disorder

Article highlights

• Aripiprazole long-acting injectables (LAIs) given every 2 months are available in two formulations: aripiprazole lauroxil (AL) 1064 mg and aripiprazole monohydrate (Ari 2MRTU) 960 mg.

• AL 1064 mg, a prodrug of aripiprazole, was approved by the Food and Drug Administration (FDA) for the treatment of patients with schizophrenia in June 2017, and Ari 2MRTU 960 mg was approved by the FDA for the treatment of schizophrenia and for the maintenance treatment of BD type I in adults in April 2023.

• AL and Ari 2MRTU are generally well tolerated, in line with the safety profile of oral aripiprazole, with the exception of injection-site reactions.

• AL 1064 may only require a 1-day initiation regimen without oral supplementation of aripiprazole, but it only corresponds to a 15 mg daily dose of oral aripiprazole.

• Ari 2MRTU 960 covers all the recommended doses of oral aripiprazole (10–20 mg) but requires oral supplementation for 14 consecutive days in patients receiving oral aripiprazole or any other oral antipsychotic.

Declaration of interest

L Samalin has received personal fees and/or non-financial support from Janssen-Cilag, Lundbeck, Otsuka, Rovi and Sanofi. PM Llorca has received personal fees and/or non-financial support from Eisai, Ethypharm, Janssen Pharmaceuticals, Lundbeck, Merck Sharp and Dohme, Neuraxpharm, Novartis, Otsuka, Roche, Rovi and Sanofi. The authors have no other relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript apart from those disclosed.

Reviewer disclosures

Peer reviewers on this manuscript have no relevant financial or other relationships to disclose.

Additional information

Funding

This paper was not funded.