Brexpiprazole

Schizophrenia and major depressive disorder are high-incidence psychiatric disorders that have long been plagued by the pain points of insufficient clinical treatment response rate and poor tolerance to adverse reactions, while the launch of brexpiprazole provides a better treatment option for such patients. As a third-generation atypical antipsychotic, it is a dopamine D2 receptor partial agonist, and also has partial agonistic activity on 5-hydroxytryptamine 1A receptor and antagonistic effect on 5-hydroxytryptamine 2A receptor. It can precisely regulate the level of neurotransmitters, improve both the positive and negative symptoms of schizophrenia, and serve as an adjuvant treatment for major depressive disorder, reducing the risk of common adverse reactions of traditional antipsychotics such as extrapyramidal reactions and elevated prolactin. It is suitable for adult patients with schizophrenia and adult patients with major depressive disorder who have poor response to antidepressants.

The global brexpiprazole market size exceeded US$3 billion in 2021. In recent years, with the increase in the diagnosis rate of psychiatric disorders and the expansion of indication scope, the market size still maintains an average annual growth rate of around 7%. At present, the global market is dominated by the original research product, and the domestic market is still in the stage of exclusive possession by the original research product. A number of pharmaceutical companies have laid out the research and development of generic drugs. With the expiration of core patents, it is expected that domestic generic drugs will be approved for launch one after another in the next 3 to 5 years, and the market accessibility will be greatly improved.

The original brexpiprazole was jointly developed by Japan's Otsuka Pharmaceutical and Denmark's Lundbeck Pharmaceutical, with the original brand name Rexulti®. Its core compound patent in the United States will expire in 2033, and the compound patent in China will expire in 2029. The main dosage form of the original research product is oral tablet, with specifications including 0.25mg, 0.5mg, 1mg, 2mg, 3mg and 4mg. The original research tablet has been included in the Catalogue of Marketed Drugs in China as the reference preparation, and is also listed as the FDA reference preparation. At present, there is no brexpiprazole API approved for marketing in China. A number of enterprises have submitted API DMF registration applications which are under the review stage. The original preparation was approved for marketing by the China NMPA in 2021. (Data as of July 2024, please refer to the official website of CDE for the latest information)

CATO provides a full set of brexpiprazole impurity reference standards, covering all key impurities in the synthesis route and degradation process. All products meet the requirements of relevant regulations of the Chinese Pharmacopoeia and FDA. Most products are in regular stock. Spot orders placed before 16:00 can be delivered on the same day, which can fully meet the full-process needs of pharmaceutical companies in generic drug research and development, quality research and declaration.