Pharmacokinetic evaluation of Aripiprazole Monohydrate as a once every 2-months long-acting injectable for schizophrenia.

Long-acting injectable (LAI) antipsychotics are often considered preferable to their oral counterparts for the long-term maintenance treatment of schizophrenia. One goal of LAI drug development is to extend the dose interval between injection visits. Aripiprazole Monohydrate (AM, Abilify Maintena®) was approved in 2013 as a monthly formulation, but a 2-month interval formulation (Ari2M, Abilify Asimtufii®) was approved by the FDA in 2023 for the treatment of schizophrenia in adults and maintenance monotherapy of Bipolar I disorder in adults, and by the EMA as Abilify Maintena® 960 mg in 2024 with the indication of maintenance treatment of schizophrenia in adult patients stabilized with oral aripiprazole. This review covers the development and pharmacokinetics of the 2-month formulation and provides data on the safety and pharmacokinetic modeling which informed its regulatory approval. Ari2M 960 mg Q2M can be safely substituted for AOM 400 mg Q1M and Ari2M 720 mg Q2M for AOM 300 mg Q1M as per clinician and patient preference. The new formulation employs a ready-to-use prefilled syringe, must be administered in the gluteal muscle, and can be given within ±2 weeks of the scheduled injection date. Reinitiation is only necessary if ≥14 weeks have passed since the prior injection.