Aripiprazole 2-Month Ready-to-Use: A Novel Long-Acting Injectable Antipsychotic Formulation for Administration Once Every 2 Months

This work was sponsored by Otsuka Pharmaceutical Development & Commercialization Inc. (Princeton, NJ, USA) and H. Lundbeck A/S (Valby, Denmark). Aripiprazole 2-month ready-to-use (Ari 2MRTU) is a novel long-acting injectable (LAI) formulation of aripiprazole monohydrate for gluteal intramuscular administration once every 2 months. In the US, Ari 2MRTU is approved for the treatment of schizophrenia and maintenance monotherapy treatment of bipolar I disorder (BP-I). Ari 2MRTU has been shown to be generally well tolerated, with minimal injection-site reactions observed in adults with schizophrenia or BP-I. Ari 2MRTU is presented as a prolonged-release suspension in a single-use, ready-to-use, pre-filled syringe. Each syringe contains 960mg of aripiprazole monohydrate (total volume 3.2mL) for administration once every 2 months. In case of tolerability issues, a 720mg dose of Ari 2MRTU (total volume 2.4mL) is available. The suspension is a white to off-white color, with a neutral pH; Ari 2MRTU should be stored at controlled room temperature. For patients who have never taken aripiprazole, tolerability to aripiprazole must be established before treatment initiation. Overlapping treatment with oral aripiprazole is required during treatment initiation unless patients have been stabilized on aripiprazole once-monthly. The recommended maintenance dose of Ari 2MRTU is 96 mg. A maintenance dose of 720 mg is recommended in patients who are poor metabolizers of CYP2D6 or who are taking strong inhibitors of CYP2D6 or CYP3A4. Following an initial dose, Ari 2MRTU should be administered once every 2 months (56 days after the previous injection). In conclusion, Ari 2MRTU is a novel LAI formulation of aripiprazole monohydrate presented in a ready-to-use syringe. The 2-month dosing interval may reduce treatment burden for patients and clinicians.