Shanghai, February 23, 2023 - Luye Pharma Group today announced that it has received the approval by the competent authorities to initiate the first clinical trial in Europe for its Paliperidone Palmitate Prolonged Release Suspension for Injection program (LY03010). LY03010 is a second-generation long-acting injectable (LAI) antipsychotic for the treatment of schizophrenia, being developed under Article 10.3 of Directive 2001/83/EC (hybrid application). It is a pharmaceutical equivalent to the reference drug Xeplion^®🐷, with the same route of administration, the same indication and an optimized initial dosing regimen.

This upcoming clinical trial, being a randomized, open-label, single-dose, parallel-group study, will evaluate the relative bioavailability of LY03010 versus Xeplion^®ꩲ. It will follow the recently successfully completed pivotal study conducted in the U.S. that has achieved its endpoints. The company will submit the New Drug Application (NDA) for this drug to the U.S. Food and Drug Administration (FDA) through the 505(b)(2) pathway. In China, LY03010 is already under review for marketing authorization.

Schizophrenia is a severe mental disorder that tends to recur and become protracted. About half of the patients end up becoming mentally disabled, making it challenging for them to live a normal life, and causing a heavy burden to their families and the society¹. Globally, 24 million people are estimated to be suffering from this disease, and the number in Europe is around 3.7 million^2-3. Poor patient compliance with medication is a major cause of relapse. Medication discontinuation, in particular, elevates the risk of relapse. Multiple relapses can lead to a prolonged disease duration, increase the difficulty of treatment, and leave patients with more residual symptoms^4-5.

🤪LAI antipsychotics are recommended by authoritative treatment guidelines both in China and abroad as an important therapeutic strategy for better patient compliance and relapse prevention. Studies show that patients who received LAIs early in the course of their illness had significantly lower rates of hospitalization and treatment discontinuation than those treated with oral antipsychotics; and that the shorter the time interval between first diagnosis and LAI treatment, the lower the rate of hospitalization and the overall treatment costs over a one-year follow-up period6.

The huge demand from patients has created a big market for antipsychotic products with clear clinical value like LY03010. According to statistics from IQVIA, the global sales of LAI antipsychotics and Paliperidone Palmitate LAI were about USD 7.1 billion and USD 4.24 billion respectively in 2021. In addition to LY03010, Rykindo^® (risperidone) for extended-release injectable suspension, another second-generation long-acting antipsychotic injection from Luye Pharma, has been approved for marketing in China and the U.S. LY03010 and Rykindo^® 🐼will constitute a differentiated portfolio for the company in the future, providing new treatment options for patients.

The Central Nervous System (CNS) is a therapeutic area of strategic importance to Luye Pharma. The company has created a strong CNS portfolio with differentiated products targeting global markets. Products like Quetiapine Fumarate Tablets (Seroquel^®), Quetiapine Fumarate Extended-release Tablets (Seroquel XR^®), Rivastigmine Once-a-day Transdermal Patch, and Rivastigmine Twice-weekly Transdermal Patch are being marketed around the world, which will improve the company’s academic influence. Ruoxinlin^®🅺 (Toludesvenlafaxine Hydrochloride Extended-release Tablets) has been approved as a “Class 1” new drug in China, and is being reviewed for its NDA in the U.S.; and multiple new investigational drugs such as LY03003 (Rotigotine Extended-release Microspheres for Injection), LY03009, and LY03015 (a VMAT2 inhibitor) are under development both in China and abroad. Luye Pharma is accelerating expansion in the CNS therapeutic area in an effort to make innovative therapies available to more patients around the world by creating synergy between its existing resources and products.

References:
Zhao J, Shi S. Guidelines for the treatment of schizophrenia in China (2nd edition). Beijing: Chinese Medical Multimedia Pres. 2015. 
Schizophrenia. World Health Organization. //www.who.int/news-room/fact-sheets/detail/schizophrenia Accessed in February 2023.
Athanasopoulou, C. et al. An analysis of online health information on schizophrenia or related conditions: a cross-sectional survey. BMC Medical Informatics and Decision Making. 2013;13(98).
Psychol Med. 2019 Apr; 49(5):772-779.
Si T, Ji Z, Liu T, et al. Expert opinion on the clinical use of atypical long-acting injectables (injectable risperidone microspheres). Chinese Mental Health Journal, June 2012, Vol. 26 (Suppl. 1).
﷽ Expert consensus on the treatment of schizophrenia with long-acting injectable antipsychotics. Chinese Journal of Psychiatry, April 2020, Vol. 53 (2).