China's First Innovative Microsphere Drug Reziphon® (Risperidone Microspheres for Injection [II]) Receives NMPA Approval, Showcasing Luye Pharma’s Global Leadership in Advanced Drug Delivery Technology
Shanghai, January 14, 2021 – Luye Pharma Group announced that its independently developed innovative formulation, Risperidone Microspheres for Injection (II) (Ruixintuo®) has received marketing approval from the National Medical Products Administration of China for the treatment of acute and chronic schizophrenia, as well as other various psychotic states with prominent positive and negative symptoms. It can alleviate emotional symptoms associated with schizophrenia. Ruixintuo®It is an injectable sustained-release microsphere formulation, a new drug developed by Luye Pharma based on its globally leading novel long-acting formulation technology platform. It is the first independently developed innovative microsphere formulation in China with independent intellectual property rights for which global registration has been initiated.
Rixintuo®It is a Class 2 new drug (improved new drug), administered via intramuscular injection once every two weeks, offering significant clinical advantages. The long-acting sustained-release injection is suitable for long-term maintenance therapy in patients who respond effectively to oral medication. During the transition from oral to injectable formulation, it is essential to maintain stable therapeutic plasma concentrations to minimize potential fluctuations in the patient's condition caused by the switch. Ruixintuo®Stable blood drug concentrations in vivo can avoid the risk of missed doses or overdose associated with oral administration, significantly improving medication adherence, which is commonly poor among schizophrenia patients taking oral antipsychotics.
with Ruixintuo®In comparison, another commercially available drug has a drug release lag period of approximately 3 weeks after the initial injection; patients need to continuously take oral risperidone formulations during this 3-week lag period to maintain stable clinical therapeutic blood concentrations. However, Ruixintuo®By optimizing the drug release mechanism, the initial lag phase of drug release can be shortened, allowing therapeutic plasma concentrations to be achieved immediately after injection. This eliminates the need for supplemental oral medication following the initial injection, while maintaining stable clinical plasma concentrations, thereby enhancing the convenience of clinical treatment. For patients experiencing acute episodes and exhibiting poor adherence and compliance, Ruixintuo®Can rapidly control disease symptoms. In addition, the use of Ruixintuo®After discontinuation, the drug’s residence time in the body is significantly shorter than that of another commercially available agent, facilitating timely dose adjustments by physicians—a feature not offered by currently marketed long-acting antipsychotics. The clinical advantages of Ruixintuo® have led to greater acceptance among patients and clinicians.
Owing to its significant therapeutic advantages, Ruixintuo®In December 2019, it was included in the priority review program by the Center for Drug Evaluation of the National Medical Products Administration, enabling patients with schizophrenia in China to benefit early from this new treatment regimen.
The research and development of novel high-end formulations is regarded by many industry experts as an inevitable path and a frontier for the innovative development of China’s pharmaceutical industry, a determination driven by the clinical advantages of high-end formulations, their pharmacoeconomic value, and national drug safety strategies.
First, high-end complex formulations, such as liposomes and microspheres, often demonstrate significant clinical advantages, including improved efficacy and safety, thereby addressing unmet clinical needs. Second, injectable microsphere formulations are classified as complex drug products; their research, development, and manufacturing present substantial challenges and high technical barriers, with this technology predominantly controlled by a few foreign enterprises.
Luye Pharma Breaks Through Technical Barriers, Builds a Globally Leading Novel Formulation Technology Platform, and Successfully Develops Rixintuo®, thanks to its forward-looking strategic layout in this field, it once again demonstrates Luye Pharma’s outstanding capabilities and accumulated advantages in R&D strategy, innovation systems, design and development of process equipment and systems, commercial-scale manufacturing, quality management of clinical trials, and global patent protection. Ruixintuo®The achievement of this regulatory approval milestone is of significant importance for breaking technological monopolies and safeguarding medication safety for patients in China.
In the "Guidelines for the Development Planning of the Pharmaceutical Industry" jointly issued in 2016 by the Ministry of Industry and Information Technology, the National Development and Reform Commission, the Ministry of Science and Technology, the Ministry of Commerce, the National Health and Family Planning Commission, and the former China Food and Drug Administration, it was explicitly stated that priority should be given to developing high-end formulations, including microspheres, and advancing industrialization technologies for such high-end formulations.
RuiXinTuo®The approval is regarded as a major milestone in the industry, signifying that Luye Pharma’s innovative microsphere technology platform, cultivated over many years, has successfully achieved industrialization and demonstrated global leadership. This represents not only a critical step in Luye Pharma’s globalization strategy but also a significant advancement for China in the field of innovative microsphere technologies, drawing widespread attention from all sectors.
Rixintuo®Following project initiation, the global launch strategy was finalized in 2011. FDA clinical trial applications commenced at the end of 2012, with Investigational New Drug (IND) approval obtained in early 2013. Authorization to submit a New Drug Application (NDA) was granted in 2015, and the production facility was completed in 2018. In 2019, the manufacturing base passed the U.S. FDA Pre-Approval Inspection (PAI) with zero deficiencies. The journey culminated in marketing approval from China’s National Medical Products Administration (NMPA), marking a decade of arduous effort. Behind this “ten-year endeavor to hone a single sword” lies Luye Pharma’s deeply ingrained spirit of “independent innovation and R&D,” as well as the silent dedication and commitment of every Luye researcher.
To enable more patients worldwide to benefit as soon as possible, Ruixintuo®Global registration and filing efforts are also proceeding in parallel. The product has entered the New Drug Application (NDA) stage in the United States, while pivotal clinical trials are underway in Europe. Patents for this product have been granted in China, the United States, Europe, Japan, South Korea, Russia, Canada, and Australia, with patent protection extending until 2032.
Schizophrenia is a chronic and severe mental disorder that affects more than 20 million people worldwide. The condition is highly disabling, and the risk of premature death among patients may be 2 to 3 times higher than that in the general population.Ⅰ. Schizophrenia is a key mental disorder targeted for prevention and control in China, with an estimated minimum of 10 million patients in the country.Ⅱ. The high relapse rate and fluctuating disease course caused by poor patient treatment adherence have become a major challenge in the management of schizophrenia.
Driven by substantial unmet patient needs, the current market size for schizophrenia in China has exceeded RMB 6 billion.Ⅲ, and its compound annual growth rate in recent years has been significantly higher than the market average. From a global treatment trend perspective, the share of long-acting injectables is also increasing year by year.
In addition to the approved Ruixintuo®Luye Pharma’s innovative microsphere technology platform leverages its core technological strengths to address patient needs, with in-depth layouts in major disease areas such as oncology and central nervous system disorders. The company has more than eight microsphere products at various stages of development, including a series of high-quality innovative products such as Rotigotine Microspheres for Injection (LY03003) for the treatment of Parkinson’s disease, Goserelin Acetate Sustained-Release Microspheres for Injection (LY01005) for sex hormone-dependent conditions like prostate cancer and breast cancer, and LY03009 for Parkinson’s disease and restless legs syndrome. These microsphere products feature dosing intervals ranging from one week to three months, offering significant clinical advantages, including enhanced efficacy and safety, ease of administration for healthcare providers, and improved patient adherence, thereby meeting the unmet clinical needs of a broader patient population. Future new drugs will form a rich product portfolio alongside the company’s marketed products, synergizing with existing resources and advantages to accelerate Luye Pharma’s global strategic layout in core therapeutic areas.
I. Schizophrenia, World Health Organization website: https://www.who.int/zh/news-room/fact-sheets/detail/schizophrenia
Ⅱ、Huang YQ, Wang Y, Wang H, et al. Lancet Psychiatry. Published Online February 18, 2019.
III. IQVIA Data