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Rykindo® Launched! First Innovative Microsphere Formulation Independently Developed in China

2021 / 03 / 29 Publisher:Luye Life Sciences Group

Luye Pharma Group held a launch conference on March 27, 2021 to officially announce the launch of a new drug Rykindo® (Risperidone Microspheres for Injection (II)) in China.

Rykindo® is an extended release microspheres injection developed by Luye Pharma on its world-leading microsphere technology platform and represents an innovative new therapy for the treatment of schizophrenia. It is the first innovative microsphere formulation independently developed and owned by a Chinese company, including all related intellectual property, and is currently undergoing global registration. It is also China’s first independently developed second-generation long-acting injectable antipsychotic. The launch of Rykindo® brings new hope for societal reintegration to around ten million schizophrenia patients in China.


High Recurrence Due to Low Medication Adherence: A Major Obstacle to Treatment

Schizophrenia is a chronic, persistent disease with recurrent episodes. A high recurrence rate due to treatment discontinuation or reduced use of medication by patients is a major obstacle to effective treatment. Data shows that 60% of patients who have experienced a first episode have poor adherence to medication and a relapse rate of over 80% within 5 years. Multiple relapses lead to prolonged disease duration, increase the difficulty of treatment, and significantly increase the cost of treatment.

“The focus of schizophrenia treatment has shifted from controlling symptoms to improving cognition, facilitating rehabilitation, and ultimately the reintegration of patients into society. In this process, improving patient medication adherence to prevent relapse is the key to effective treatment,” said Prof. Cai Jun, a chief physician at Shanghai Mental Health Center Affiliated with Shanghai Jiao Tong University School of Medicine. “Long-acting injectable antipsychotics significantly improve patient adherence compared to oral formulations and are an important treatment strategy for relapse prevention.”

The 2020 Expert Consensus on Long-acting Injectables in the Treatment of Schizophrenia has included second-generation long-acting injectables as a first-line treatment for schizophrenia patients at the acute and maintenance phases2. Globally, a consensus is building which indicates long-acting agents will be one of the main therapeutics for the future treatment of schizophrenia. Prof. Cai said, “Due to the high recurrence rate of schizophrenia, we are advocating the early use of long-acting injectables no matter what stage of the disease patients are at. As the first of China’s second-generation long-acting injectables, Rykindo® could be considered as an upgraded version of a commercially available long-acting injection, and suitable for the whole treatment course for schizophrenia, providing a new treatment option for patients.”


Innovative Microsphere Formulation Improves Safety and Adherence to Schizophrenia Treatment

Rykindo® is administered bi-weekly by intramuscular injection and can significantly improve the medication adherence issues which are common among schizophrenia patients treated with oral antipsychotic drugs.

Patients are less likely to skip or forget drug administration with Rykindo®, which requires a much lower frequency of administration compared to oral formulations. Unlike with oral formulations, patients treated with Rykindo® can maintain steady plasma drug levels and a smaller peak-trough gap, which helps lower the risk of dose-dependent adverse effects and improves medication safety.

“Most patients with schizophrenia have difficulty adhering to daily oral drugs. Some of them stop taking their drugs because they cannot tolerate the adverse effects of the medicines, which is another reason for poor medication adherence. Rykindo®’s dosing regimen and the steady, persistent plasma drug levels could improve the long term medication adherence of patients,” said Prof. Mei Qiyi, a chief physician at Suzhou Guangji Hospital.

Furthermore, compared to the other marketed drug, there is no need for administration of the oral formulation following the first injection of Rykindo® and steady plasma drug levels can be reached much faster with Rykindo® than with the comparison product.

“Rykindo® has a fast onset of action after injection, allowing for rapid control of psychotic symptoms. Meanwhile, its rapid clearance after discontinuation makes it easier for physicians to quickly adjust treatment plans according to patient conditions," added Prof. Mei Qiyi, “I am glad to see formulation innovation in the field of schizophrenia treatment in China, which provides patients with new drugs with more clinical benefits. I believe that with the launch of Rykindo®, more patients now have a chance for a better prognosis and to reintegrate into society.”


Building a World-Leading Microsphere Technology Platform to Serve Unmet Patient Needs

“The purpose of formulation innovation is to address unmet clinical needs, covering aspects including efficacy, compliance and side effects, among others. With a focus on patient experience and needs, we are committed to working tirelessly to reduce the burden of disease and improve clinical benefits for patients by bringing differentiated and clinically meaningful innovations,” said Mr. Yang Rongbing, President of Luye Pharma Group.

Microsphere formulations represent one type of novel high-end formulation with release rates and release periods that can be designed according to clinical needs. Drugs in microspheres can release continuously and consistently for a week to several months, improving efficacy and reducing side effects. Microspheres are a complex formulation with high technical barriers, and are difficult to develop and manufacture. The technology lies mostly in the hands of a few overseas companies.

The launch of Rykindo® indicates an end to an overseas technology monopoly and positions Luye Pharma as one of the few Chinese companies to master the key processes involved in the manufacture of microspheres. After more than a decade of continuing efforts, Luye Pharma has established a platform with core competencies, allowing the company to gain an international edge in the field. Core technologies include production of microspheres with a high drug-loading capacity and a low burst release, evaluation of in vitro–in vivo release correlation for long-acting sustained release formulations, and commercial manufacturing technology and equipment for the production of microspheres. Of particular note, the platform is world-leading in terms of R&D capacity for commercial manufacturing of microspheres, and the pilot technical equipment and manufacturing processes were all independently developed.

After achieving breakthroughs in R&D and commercial manufacturing on the microsphere technology platform, the commercialization of Rykindo®, the first microspheres product developed on the platform, has been gaining momentum. Just 40 days after the marketing authorization was granted on January 12, 2021, Rykindo® is available in many provinces and cities across China. In addition, to bring the benefits of Rykindo® to more patients around the world, registration is being conducted simultaneously in various global markets, with the process entering the new drug application stage in the U.S. and pivotal clinical trials being carried out in Europe.

“The launch of Rykindo® is significant in that it attests to our long-standing commitment to providing innovative therapeutic solutions based on patient needs. It is also a “zero to one” breakthrough for our microsphere technology platform, giving momentum to the development and early launch of more innovative microsphere formulations on this platform to serve more patients,” said Mr. Yang Rongbing.

In addition to Rykindo®, Luye Pharma has a series of microsphere products in various stages of development, all on the innovative microsphere technology platform, enjoying competitive strengths and targeting major therapeutic areas, such as oncology and the central nervous system. Products include Rotigotine Extended Release Microspheres for Injection (LY03003) for Parkinson's disease, Goserelin Acetate Extended Release Microspheres for Injection (LY01005) for prostate cancer, breast cancer and other sex hormone dependent diseases, and LY03009 for Parkinson's disease and restless legs syndrome. Once launched, these new drugs will form a rich product portfolio with Rykindo®. The company will continue leveraging its technical strengths to bring more treatment options to patients.




About Rykindo®

Rykindo® (Risperidone Microspheres for Injection (II)) is an innovative microsphere formulation independently developed by Luye Pharma. Administered bi-weekly by intramuscular injection, Rykindo® is indicated for the treatment of acute and chronic schizophrenia and significant positive and negative symptoms of various other psychotic states, alleviating the affective symptoms associated with schizophrenia.

Due to its significant clinical advantages, Rykindo® was granted priority review by the Center for Drug Evaluation under the National Medical Products Administration (NMPA) in December 2019, and marketing authorization by NMPA on January 12, 2021. In addition to the approval in China, registration of Rykindo® is being conducted simultaneously in various global markets, with the process entering the new drug application stage in the U.S. and pivotal clinical trials being carried out in Europe.

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