Luye Pharma Launches China's First Independently Developed Innovative Microsphere Formulation Releego® (Risperidone Microspheres for Injection [II]) to Address Unmet Clinical Needs in Schizophrenia Treatment
On March 27, Luye Pharma Group announced the official market launch of its independently developed novel antipsychotic drug, Risperidone Microspheres for Injection (II) (brand name: Ruoxintuo).
Rixintuo is developed based on Luye Pharma’s globally leading microsphere technology platform. It is China’s first independently developed, innovatively formulated microsphere preparation with independent intellectual property rights that has undergone global registration. It is also the first domestically developed long-acting injectable formulation of a second-generation antipsychotic drug in China. Rixintuo is indicated for the treatment of prominent positive and negative symptoms associated with acute and chronic schizophrenia and other psychotic disorders, and it can alleviate affective symptoms related to schizophrenia.
Professor Cai Jun, Chief Physician at the Shanghai Mental Health Center, Shanghai Jiao Tong University School of Medicine, stated, “Rixintuo represents a further improvement and upgrade over existing long-acting injectables on the market, making it suitable for full-course treatment of schizophrenia and providing patients with a new therapeutic option.”
Schizophrenia is a chronic, protracted disease characterized by recurrent episodes. Disease relapse resulting from treatment discontinuation or unauthorized dose reduction by patients constitutes a major challenge in the current management of schizophrenia. Data indicate that 60% of patients experiencing their first episode exhibit poor medication adherence, with a five-year relapse rate exceeding 80%. Recurrent episodes lead to disease prolongation, increase the complexity of treatment, and substantially escalate healthcare costs.
As an innovative microsphere formulation, Rixintuo significantly improves the poor medication adherence commonly observed with oral antipsychotics in patients with schizophrenia by modifying the drug release mechanism. It also eliminates the need for supplemental oral medication following the initial injection, a requirement associated with another commercially available long-acting injectable, thereby delivering superior clinical benefits to patients.
“Most patients with schizophrenia struggle to adhere to daily oral medication regimens. Some discontinue treatment due to intolerance of adverse drug reactions, which contributes to poor medication adherence. The administration route of Ruixintuo, along with its stable and sustained plasma drug concentrations, better ensures long-term effective treatment for patients,” pointed out Professor Mei Qiyi, Chief Physician at Suzhou Guangji Hospital. “Ruixintuo takes effect rapidly after injection, allowing for quick control of psychotic symptoms, and is rapidly cleared from the body after discontinuation, facilitating timely adjustments to the treatment plan by physicians based on the patient’s condition.”
In the field of pharmaceutical R&D, microsphere formulations represented by Risperidone Microspheres (Ruixintuo), liposomes, and transdermal patches are all classified as novel, high-end drug delivery systems. Unlike many pharmaceutical companies that focus heavily on developing drugs for popular targets, Luye Pharma has adopted a unique product development strategy—addressing clinical pain points by improving and innovating upon already marketed formulations. This approach yields innovative drug products with clear clinical advantages, such as enhanced efficacy, reduced side effects, and improved patient compliance, thereby delivering tangible benefits to patients.
Industry insiders have stated that due to high technical barriers and significant development challenges, few domestic enterprises are engaged in the research and development of high-end formulations. However, establishing a firm foothold in this field can build sustainable competitive advantages for companies. According to statistical data, generic versions of high-end formulations are difficult to develop. Taking microspheres, which represent the highest level of technical difficulty, as an example, several blockbuster products have emerged globally over the past decade, yet most remain exclusive offerings, underscoring their strong market competitiveness.
At the national level, multiple policies in recent years have continuously encouraged and promoted the clinical development and industrialization of improved new drugs, represented by advanced drug delivery systems. The "Guidelines for the Development Plan of the Pharmaceutical Industry," jointly issued by the Ministry of Industry and Information Technology and other ministries, specifically highlights key breakthroughs in advanced formulations such as microspheres and their industrialization technologies. The 14th Five-Year Plan also emphasizes achieving breakthroughs in high-end drug design, manufacturing processes, and novel excipients.
In developed countries in Europe and the United States, improved new drugs, including advanced formulations, are also an important component of innovative drugs. In the U.S. FDA’s registration classification system, innovative formulations are categorized under 505(b)(2). Over the past decade, 505(b)(2) applications have accounted for 63.7% of the New Drug Applications (NDAs) for innovative drugs approved by the U.S. FDA. Taking products from multinational pharmaceutical companies as examples, several of AstraZeneca’s inhalation formulations and Takeda’s leuprolide acetate microspheres for injection are both instances of dosage form innovation.
“The purpose of formulation innovation is to address unmet clinical needs, encompassing aspects such as efficacy, compliance, and side effects. We focus on patient experience and needs, striving to alleviate the disease burden and improve clinical benefits for patients by providing differentiated, clinically valuable innovative products,” said Yang Rongbing, President of Luye Pharma Group.
A survey of China’s pharmaceutical industry reveals that companies dedicated to innovation in advanced drug formulations are few and far between. Taking microspheres, a novel drug delivery technology, as an example, key technologies were historically controlled by developed countries in Europe and the United States. This has resulted in weak industrial translation capabilities for drug delivery technologies in China. In particular, the inability of pilot-scale technical equipment to meet requirements in the industrialization phase constitutes a major challenge for domestic manufacturers of long-acting microsphere formulations. Industrialization capability is precisely the core competitive advantage of independent corporate innovation. Therefore, establishing high-level technical platforms is crucial to overcoming the challenges associated with the industrialization of novel formulations such as microspheres. As one clinical expert candidly stated, “The barriers to researching, developing, and manufacturing specialized formulations are high. Companies must meet several critical conditions, including having both a robust technical platform and production lines. The regulatory approval process alone excludes many enterprises.”
Through more than a decade of accumulation, Luye Pharma has broken the monopoly of overseas technologies and established a platform encompassing core key technologies, including high drug-loading, low burst-release microsphere preparation technology, in vitro–in vivo correlation (IVIVC) evaluation for long-acting sustained-release formulations, and industrial-scale microsphere manufacturing technologies and equipment. This has enabled the company to develop international competitiveness in this field. In particular, the industrial research capabilities of its microsphere technology platform are at an internationally leading level, with all pilot-scale technical equipment and manufacturing processes independently developed.
The market launch of Rixintuo marks a breakthrough from zero to one for Luye Pharma’s microsphere technology platform, which has been under development for many years. Professor Cai Jun, Chief Physician at the Shanghai Mental Health Center affiliated with Shanghai Jiao Tong University School of Medicine, stated that in terms of dosage form innovation, the core technologies behind all previously available long-acting injectables for schizophrenia—whether based on microsphere or crystal structures—were controlled by foreign entities. Currently, only microsphere technology has achieved an independent intellectual property breakthrough in China. “Innovation is most challenging during the phase of going from zero to one; only after achieving this initial breakthrough can further development follow.”
Yao Jian, Vice President of the Sales and Marketing Department at Luye Pharma (China), stated, “Luye Pharma has broken through technical barriers and established a globally leading microsphere technology platform, achieving comprehensive breakthroughs in the research and development and industrial translation of microsphere technology. In the future, we will launch more microsphere products based on this platform.”
Starting with Rixin Tuo, Luye Pharma will leverage this mature technology platform to accelerate the development and commercialization of additional microsphere products, including rotigotine microspheres for injection (LY03003) for the treatment of Parkinson’s disease, goserelin acetate sustained-release microspheres for injection (LY01005) for the treatment of hormone-dependent conditions such as prostate cancer and breast cancer, and LY03009 for the treatment of Parkinson’s disease and restless legs syndrome.