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Otsuka product development storiesCNS area Product story

As long as there are unmet patient needs,
our work continues

The difficulty in pinpointing the causes of diseases of the central nervous system presents a challenge to new drug development.
Despite these obstacles, Otsuka Pharmaceutical discovered and developed ABILIFY, ABILIFY MAINTENA and most recently REXULTI, an antipsychotic drug with a unique pharmacological profile.

A challenge born from failure

Diseases of the central nervous system include schizophrenia, depression, bipolar disorder, and Alzheimer’s disease. The underlying causes of these diseases have yet to be precisely elucidated, making the research and development of treatments extremely challenging. Cures for these disorders remain elusive, while expectations from patients and their families for new, better drugs remain high.
The creation of ground-breaking medicines often involves many failures - but viewed from a new angle, these can sometimes be seen as spurs to try different research approaches. Such was the case when scientists researching non-drowsy antihistamines found that mice fell asleep during tests of drug candidates. Although not suitable as antihistamines, they speculated that the candidates might have an effect on the central nervous system (CNS). Ultimately research pursued a different path that culminated in the discovery of the antipsychotic ABILIFY. Taking untraveled paths has characterized Otsuka’s CNS-related research during the past 40 years.

In 2002, we released the anti-psychotic drug "ABILIFY" in the United States, our first original medication. Many antipsychotic drugs that were sold at that time had antagonist effects that inhibited the dopamine D2 receptor. However, ABILIFY works by suppressing dopamine neurotransmission when dopamine secretion is excessive, and activating it when there is deficient dopamine secretion, meaning that it has the world's first dopamine system stabilizer (DSS) mechanism.
CNS diseases and their treatments are often accompanied by adherence issues: patients may lack an understanding of their condition, dislike the side effects of their medication and stop taking it, or forget to take it. This often leads to relapses. For better patient outcomes and improved adherence, desirable antipsychotic medications are effective but also have minimal side effects. Due to its unique characteristics, ABILIFY has gained wide recognition and usage from doctors and patients worldwide, and is now used in approximately 60 countries and regions.

Towards further contributions

Addressing adherence issues from another direction, Otsuka Pharmaceutical also developed the antipsychotic ABILIFY MAINTENA, a once-monthly injectable suspension. Development of ABILIFY MAINTENA began before ABILIFY had even gained approval, and production requires sterile production facilities and additional cutting-edge technologies. Lacking these in-house, Otsuka acquired the necessary technology and expertise from scratch. Launched in the U.S. in 2013, and Japan in 2015, the drug is now used in 35 countries.*1
The research plan for future antipsychotic drugs began in 1999. The team, consisting of members from various fields including synthesis, pharmacology and safety, brought together their experience and knowledge cultivated during the development of antipsychotics, and dedicated themselves to working towards a solution.
In 2015, the new antipsychotic REXULTI was approved by the U.S. FDA as adjunctive treatment for adults with major depressive disorder and as a treatment for adults with schizophrenia.*2 This drug is believed to exert a partial agonistic effect on the dopamine receptor D2 and serotonin receptor 5-HT1A and an antagonistic effect on serotonin receptor 5-HT2A (Serotonin Dopamine Activity Modulator: SDAM). We are also pursuing a Phase III clinical trial for the treatment of agitation in Alzheimer’s-type dementia.

Seeking untapped new solutions

Looking to help patients with psychiatric diseases and their caregivers or doctor to measure whether the patient is taking their medication, Otsuka and U.S. -based Proteus Digital Health, Inc. are developing a digital medical system that combines Otsuka’s ABILIFY with the Proteus Ingestible Sensor embedded in a single pill to digitally record ingestion.
Additionally, in 2016, the company founded a joint venture, Otsuka Digital Health Co., Ltd. in partnership with IBM Japan. Otsuka Digital Health is engaged in the development and sale of MENTAT, specialized software that automatically integrates and analyzes patient medical records. The databases enable hospital medical staff to gain more meaningful insights from electronic medical records and therefore enable them to provide a higher quality of medical care to patients.

  1. 1As of December 2016
  2. 2Not yet approved in Japan (as of December 2016)

Global collaboration in Central Nervous System therapies

In addition to creating new products on our own, we collaborate with other companies to share our strengths and ideas in order to discover, develop and deliver high-value, breakthrough products.


Avanir Pharmaceuticals
Engaged in R&D and commercialization of pharmaceutical treatments for CNS diseases such as PBA.
Astex Pharmaceuticals
Focused on R&D for the treatment of cancers and CNS diseases, using proprietary, fragment-based drug discovery technology (FBDD) for candidate leads.


H. Lundbeck
Dedicated to R&D and marketing of treatments for brain diseases such as depression and anxiety disorders. Collaborates with Otsuka on ABILIFY MAINTENA, REXULTI and multiple drug candidates.
Pursues R&D and marketing of pharmaceutical and biotech products, with a focus on neurology and immunology. Otsuka holds exclusive rights in Japan for development and marketing of UCB’s Neupro patch. UCB Japan and Otsuka also co-promote E Keppra in Japan.

CNS area

In addition to our antipsychotic drugs REXULTI*, ABILIFY MAINTENA and ABILIFY, we have marketing rights to the antiepileptic E Keppra, and Neupro patch, a transdermal dopamine agonist used to treat restless legs syndrome and Parkinson’s disease. In the U.S. we also market NUEDEXTA*, the first approved treatment for pseudobulbar affect (PBA, involuntary, sudden, and frequent episodes of laughing and/or crying).

  • Sold in the U.S.