Otsuka America Pharmaceutical, Inc. (OAPI) and Lundbec announced that the US Food and Drug Administration (FDA) has expanded the label of Abilify Maintena (aripiprazole) for extended-release injectable suspension to include a new injection site, the deltoid muscle of the arm. Healthcare providers will now have the option for either a gluteal or deltoid injection site for administering Abilify Maintena to patients with schizophrenia.

Abilify Maintena is the first and only once-monthly injection of a dopamine D2 partial agonist (the first injection is accompanied by 14 days of oral antipsychotic therapy) approved for the treatment of adults with schizophrenia. It was originally indicated for only gluteal injection when approved by the FDA in February 2013. The approval of the deltoid injection site was based on two studies that evaluated the safety and tolerability and pharmacokinetics of Abilify Maintena administered in the deltoid muscle compared to the gluteal muscle in adult patients with schizophrenia.

“Having more choices and flexibility in the administration of Abilify Maintena for the treatment of schizophrenia may help strengthen the patient-physician alliance for the long-term management of the disease,” said study investigator David Walling, Ph.D., chief executive officer and principal investigator, CNS Network.

“It is important to offer an administration option for the deltoid muscle, in addition to the gluteal muscle, because some patients and physicians prefer the deltoid muscle site for injection.”

This new deltoid administration offering for Abilify Maintena is scheduled to be commercially available in the fall of 2015.

The pharmacokinetics, safety and tolerability of Abilify Maintena administered in the deltoid muscle compared to the gluteal muscle was evaluated in two, open-label studies in stable patients aged 18-64 years with a current diagnosis of schizophrenia. One study was a randomized, single-dose, parallel-arm, relative bioavailability study comparing the pharmacokinetic parameters of Abilify Maintena 400 mg after injection in the deltoid muscle of 17 patients, with the injection in the gluteal muscle of 18 patients. The second study was a multiple-dose, parallel-arm study designed to evaluate the safety and tolerability of Abilify Maintena 400 mg injections in the deltoid muscle, and to derive pharmacokinetic parameters following five monthly injections. In this study, 141 patients were randomized to the study and 138 received at least one dose of Abilify Maintena 400 mg injection either in the deltoid (N=71) or gluteal (N=67) muscle; subsequent doses were administered to all patients in the deltoid muscle. Of the patients who received at least one dose of Abilify Maintena, 97.1 per cent of subjects had no dose adjustment; only four patients had a dose reduction to 300 mg.

In an open-label study comparing bioavailability of Abilify Maintena administered in the deltoid or gluteal muscle, injection site pain was observed in both groups at approximately equal rates. Furthermore, in the second study, multiple injections of Abilify Maintena 400 mg in the deltoid muscle resulted in comparable maximal- and minimal-plasma concentrations and comparable exposures of aripiprazole compared with injections in the gluteal muscle, as measured in earlier studies.

These data were presented earlier this year at the American Society of Clinical Psychopharmacology (ASCP) annual meeting in Miami, Florida.

Abilify Maintena (aripiprazole) is available in the US for the treatment of schizophrenia. Efficacy and safety for Abilify Maintena is supported by a short-term (12 weeks), randomized, double-blind, placebo-controlled trial in acutely relapsed adults, as well as a longer term (52 weeks) placebo-controlled, double-blind, randomized-withdrawal study for the maintenance treatment of schizophrenia.1

Abilify Maintena, an atypical antipsychotic, is an intramuscular depot formulation of aripiprazole. It is a sterile lyophilized powder that, when reconstituted with sterile water for injection, forms an injectable suspension that can be administered monthly. After an initial injection of Abilify Maintena along with an overlapping 14-day dosing of oral antipsychotic treatment, subsequent injections of Abilify Maintena provide uninterrupted medication coverage for 30 days at a time. It provides a treatment option to address two of the most important considerations in the management of schizophrenia — improving symptoms in patients with an acute relapse of their disease and reducing the risk of relapse or the re-emergence of worsening of symptoms. Depot formulations of antipsychotic agents provide patients with concentrations of active drug that remain at a therapeutic range for an extended period of time.

Schizophrenia is a disease characterized by a distortion in the process of thinking and of emotional responsiveness. It most commonly manifests as hallucinations, paranoid or bizarre delusions, or disorganized speech and thinking, and is accompanied by significant social or occupational dysfunction. Onset of symptoms typically occurs in young adulthood and the condition is chronic, often requiring life-long treatment to mitigate symptoms. It has been estimated that schizophrenia affects approximately 1 per cent of the adult population in the US, and approximately 21 million people worldwide. In the US, there are approximately 2.4 million adults with schizophrenia, prevalent equally in both genders. While there is no cure for the disease, symptoms and risk of relapse – the re-emergence or worsening of psychotic symptoms10 – can be managed in most patients with appropriate antipsychotic treatment.

Otsuka America Pharmaceutical, Inc. is an innovative, fast-growing healthcare company that commercialises Otsuka-discovered and in-licensed products in the US, with a strong focus on neuroscience, oncology, cardio-renal, and medical devices.

Lundbeck US is an affiliate of H. Lundbeck A/S in Denmark, and focused solely on accelerating therapies for brain disorders.