Brexpiprazole is a Small Molecule owned by Otsuka Pharmaceutical, and is involved in 60 clinical trials, of which 51 were completed, 8 are ongoing, and 1 is planned.

Brexpiprazole is a serotonin-dopamine activity modulator (SDAM) that acts as a partial agonist at 5-HT1A and dopamine D2 receptors at similar potency, and an antagonist at 5-HT2A and noradrenaline alpha1B/2C receptors. Dopamine partial agonist distinguishing characteristic is their mechanism of action. These drugs are partial agonists at dopamine D2/D3 receptors and can act as dopaminergic stabilizers, performing as dopamine antagonists in conditions of dopamine hyperactivity and exhibiting dopamine agonist properties in states of hypoactivity.

The revenue for Brexpiprazole is expected to reach a total of $18.7bn through 2038. This change impacts the valuation of this asset and is an important factor to understand the current value of the drug in a clinical process. GlobalData uses proprietary data and analytics to provide a complete picture of this assessment in their Brexpiprazole NPV Report.

Brexpiprazole is originated and owned by Otsuka Pharmaceutical. Otsuka Holdings and H. Lundbeck are the other companies associated in development or marketing of Brexpiprazole.

Brexpiprazole Overview

Brexpiprazole (Rexulti, Rxulti) is a quinolinone derivative, acts as anti-psychotic agent. It is formulated as tablets, and film coated tablets for oral route of administration. Rexulti is indicated for treatment of schizophrenia, as a maintenance treatment of schizophrenia in adults and as an adjunctive treatment of major depressive disorder (MDD). Rexulti is indicated for the treatment of adult and pediatric patients of age with 13 years and older.

It is under development for the treatment of post-traumatic stress disorder, irritability associated with pervasive developmental disorder, agitation associated with dementia of the Alzheimer's type, and schizophrenia. It was also under development for the treatment of attention deficit hyperactivity disorder, borderline personality disorder and bipolar disorder.

Otsuka Holdings Overview

Otsuka Holdings (Otsuka) is a holding company, which operates various businesses such as pharmaceuticals, nutraceuticals, consumer products and other businesses through its subsidiaries. It focuses on the research and development, manufacture, and sale of medicines for the treatment of cancer, cardiovascular diseases, central nervous system disorders, ophthalmic diseases, gastrointestinal and respiratory diseases, infectious diseases, dermatological conditions and allergies. The company’s product portfolio includes pharmaceutical products, cosmetics, functional foods and beverages, alcoholic beverages, fine chemicals, electronic equipment, functional chemicals, medical devices and OTC products. It markets its products in North America, Europe, and Asia. Otsuka is headquartered in Chiyoda-ku, Tokyo, Japan.

The company reported revenues of (Yen) JPY1,498,276 million for the fiscal year ended December 2021 (FY2021), an increase of 5.3% over FY2020. In FY2021, the company’s operating margin was 10.3%, compared to an operating margin of 13.8% in FY2020. In FY2021, the company recorded a net margin of 8.4%, compared to a net margin of 10.4% in FY2020. The company reported revenues of JPY451,811 million for the third quarter ended September 2022, an increase of 4.1% over the previous quarter.

Quick View – Brexpiprazole

Report Segments
  • Innovator (NME)
Drug Name
  • Brexpiprazole
Administration Pathway
  • Intramuscular
  • Oral
  • Subcutaneous
Therapeutic Areas
  • Central Nervous System
Key Companies
  • Sponsor Company: Otsuka Pharmaceutical
  • Originator: Otsuka Pharmaceutical
Highest Development Stage
  • Marketed


GlobalData, the leading provider of industry intelligence, provided the underlying data, research, and analysis used to produce this article.

To create this model, GlobalData takes into account factors including patent law, known and projected regulatory approval processes, cash flows, drug margins and company expenses. Combining these data points with GlobalData’s world class analysis creates high value models that companies can use to help in evaluation processes for each drug or company.

The rNPV method integrates the probability of a drug reaching a clinical stage into the cash flow at that time, which provides a more accurate valuation, as it considers the probability that the drug never makes it through the clinical pathway to commercialization. GlobalData’s rNPV model uses proprietary likelihood of approval (LoA) and phase transition success rate (PTSR) data for the indication in the highest development stage, which can be found on GlobalData’s Pharmaceutical Intelligence Center.