November 21, 2022 - Luye Pharma Group announced today that a pivotal study conducted in the U.S. for the company's in-house developed innovative formulation, Paliperidone Palmitate Extended-release Injectable Suspension (LY03010), has achieved the endpoints based on completed data analysis. According to the pre-IND meeting with the U.S. Food and Drug Administration (FDA), the company will submit the New Drug Application (NDA) for LY03010 to the FDA through the 505(b)(2) pathway.
LY03010 is an extended-release injectable suspension for single monthly dosage by intramuscular injection, indicated for the treatment of schizophrenia and schizoaffective disorders. As a long-acting injection, LY03010 can improve the common medication compliance issues associated with oral antipsychotic drugs and patients with schizophrenia. Compared to another similar drug on the market, INVEGA SUSTENNA®, LY03010 optimizes the initial dosing regimen, increasing patient compliance and potentially bringing greater convenience to patients. In the pre-IND meeting, the FDA confirmed that demonstration of steady state bioequivalence after multiple doses would be acceptable to support the 505(b)(2) NDA submission for LY03010.
The pivotal study is a randomized, multiple-dose, open-label, parallel-group study to evaluate the pharmacokinetic profiles of LY03010 and the relative steady state bioavailability of LY03010 versus INVEGA SUSTENNA® in patients with schizophrenia or schizoaffective disorder. 281 patients were randomized with a 1:1 ratio into the LY03010 and INVEGA SUSTENNA® groups.
The study demonstrated the steady state bioequivalence of LY03010 using the optimized initial dosing regimen compared with INVEGA SUSTENNA® using its original initial dosing regimen. The results also show that after the initial injection of LY03010, desirable exposure levels were achieved within 1 week, which was comparable to INVEGA SUSTENNA®. LY03010 was well tolerated, with no unexpected treatment-emergent adverse events compared to INVEGA SUSTENNA®. This study suggests that LY03010 could be more convenient to administer and improve patient compliance by optimizing the initial dosing regimen, while ensuring efficacy and safety.
Schizophrenia is a severe mental disorder, characterized by profound disruptions in thinking and affects the language, perception, and self-cognition of patients. According to the World Health Organization, schizophrenia affects more than 24 million people worldwide. According to Johns Hopkins data, approximately 3 million Americans are affected by schizophrenia. The incidence of schizophrenia is growing every year, bringing with it a heavy burden to patients’ families and wider society due to the poor compliance, low treatment rate, high recurrence rate, high hospitalization rate and high disability rate typical of the disease.
The long-acting injection comes in a new dosage form and was developed in recent years for the treatment of schizophrenia. Compared with the standard oral dosage form, a lower frequency of administration is required, in addition to the long-acting injection’s ability to maintain a stable and effective drug concentration in the blood for extended periods of time, improving patient compliance and the long-term effectiveness of treatment.
Driven by the huge demand from patients and the high clinical value of long-acting injections, publicly available information shows that Paliperidone Palmitate long-acting injection generated global sales of US$4.022 billion in 2021 and US$3.132 billion between January and September 2022.
Yang Rongbing, President of Luye Pharma Group, said: “The purpose of developing innovative formulations is to address unmet clinical needs, which includes covering aspects such as drug efficacy, compliance issues 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 by bringing differentiated and clinically meaningful innovation to the market. We are rapidly advancing with the development of LY03010 and hope to provide a new treatment option to patients as quickly as we can.”
The Central Nervous System (CNS) therapeutic area, including schizophrenia, is a therapeutic area of strategic focus for Luye Pharma. The company has launched several products targeting this field, including Toludesvenlafaxine Hydrochloride Extended-release Tablets (Ruoxinlin®), Risperidone Microspheres for Injection (Rykindo®), Quetiapine Fumarate Tablets (Seroquel®), Quetiapine Fumarate Extended-release Tablets, Rivastigmine Once-a-day Transdermal Patch, Rivastigmine Twice-weekly Transdermal Patch, and others, with coverage in over 80 countries and regions around the world, including large pharmaceutical markets in China, the U.S., Europe and Japan, as well as fast growing emerging markets. In addition to the above, new investigational drugs such as Rotigotine Extended-release Microspheres for Injection LY03003 and VMAT2 inhibitor LY03015 are under development, both in China and overseas markets. LY03010 is expected to further enrich the company’s product pipeline in the CNS field, strengthen resources and bolster existing advantages, accelerating the company’s growth of coverage and development in this therapeutic field.