Shanghai, January 14, 2025 – Luye Pharma Group today announced that the U.S. Food and Drug Administration (FDA) has approved its Investigational New Drug (IND) application for LY03020, a dual TAAR1/5-HT2CR agonist intended to treat schizophrenia. Developed on the company’s New Chemical Entity/New Therapeutic Entity (NCE/NTE) platform, LY03020 is a next-generation antipsychotic and the world’s first agonist against both the trace amine-associated receptor 1 (TAAR1) and the 5-HT2C receptor (5-HT2CR). It is also undergoing clinical trials in China.
Schizophrenia is a severe mental disorder affecting 24 million people worldwide1, of which 3.7 million are in the U.S. 2About 30% of the treatment-resistant schizophrenia patients do not respond well to the first- and second-generation antipsychotics.3 The next-generation antipsychotics are highly anticipated to be able to address the unmet needs, as they can primarily activate the presynaptic membrane. This is a key difference in the mechanism of action (MoA) from existing antipsychotics that typically antagonize D2 and 5-HT2A receptors on the postsynaptic membrane. As a result, the next-generation antipsychotics are expected to help reduce adverse reactions such as extrapyramidal symptoms (EPS) and metabolic syndrome associated with existing antipsychotics while making significant improvements on the positive symptoms, negative symptoms and cognitive impairments common in schizophrenia.
LY03020 targets both TAAR1 and 5-HT2CR. TAAR1 is primarily expressed on the presynaptic membrane, and its activation reduces the release of monoamine neurotransmitters such as dopamine (DA) and serotonin (5-HT) into the synaptic cleft. 5-HT2CR is expressed on both pre- and post-synaptic membranes. The activation of presynaptic 5-HT2CR further lowers the release of neurotransmitters like 5-HT and enhances the inhibition of negative symptoms. The activation of postsynaptic 5-HT2CR helps to reduce metabolic syndrome such as weight gain and abnormal glucose/lipid levels.
Preclinical studies have demonstrated that LY03020 can make significant improvements on the positive and negative symptoms as well as cognitive impairments associated with schizophrenia, without noticeable risks for EPS or metabolic syndrome like weight gain and abnormal glucose/lipid levels.
Dr. Tian Jingwei, Executive Vice President of Luye Institute for Innovative Research, said: “There are huge unmet treatment needs in the Central Nervous System (CNS) therapeutic area, which includes schizophrenia, but new drug development aiming to address them has been relatively slow. We have built a differentiated CNS portfolio that is globally competitive. LY03020 is one of our investigational CNS drugs under development both in China and abroad. We are actively developing the next-generation medicines with novel mechanisms of action to stay ahead of the competition in this area and keep delivering what the patients need.”
Luye Pharma’s CNS portfolio includes Erzofri® (paliperidone palmitate) extended-release injectable suspension and Rykindo® (risperidone) for extended-release injectable suspension, both have been approved for marketing in the U.S.; and Ruoxinlin® (Toludesvenlafaxine Hydrochloride Extended-Release Tablets) and Jinyouping® (Rotigotine Microspheres for Injection), both have been launched in China. In addition, the company is conducting clinical trials for several other investigational drugs, such as LY03021, which targets NET, DAT and GABAAR, and LY03015, which targets VMAT2 and Sigma1.
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About Luye Pharma Group
Luye Pharma Group is an international pharmaceutical company dedicated to the R&D, manufacturing, and sale of innovative medications. The company has established R&D centers in China, the U.S. and Europe, with a robust pipeline of over 30 drug candidates in China and more than 10 drug candidates in other international markets. Luye Pharma maintains high-level international standards in novel drug delivery technologies including microspheres, liposomes, and transdermal drug delivery systems. The company has achieved multiple innovations in new chemical entities and antibodies, and is also actively making strategic developments in the fields of cell therapies and gene therapies.
Luye Pharma is developing a global supply chain of 8 manufacturing sites built up around the world, with GMP quality management and control systems established in line with international standards. With more than 30 products covering oncology, the central nervous system, cardiovascular, gastroenterology, metabolism and other therapeutic areas, business is conducted in over 80 countries and regions around the world, including the largest pharmaceutical markets - China, the U.S., Europe, and Japan, as well as in fast growing emerging markets.
References：
1. World Health Organization. Available at: https://www.who.int/zh/news-room/fact-sheets/detail/schizophrenia. Accessed on January 14, 2025
2. Treatment Advocacy Center. Available at: https://www.tac.org/research-weekly-more-people-with-schizophrenia-in-the-u-s-than-previously-reported/Accessed on January 14,2025
3. Disease Analysis: Schizophrenia. www.datamonitorhealthcare.com.
Shanghai, January 14, 2025 – Luye Pharma Group today announced that the U.S. Food and Drug Administration (FDA) has approved its Investigational New Drug (IND) application for LY03020, a dual TAAR1/5-HT2CR agonist intended to treat schizophrenia. Developed on the company’s New Chemical Entity/New Therapeutic Entity (NCE/NTE) platform, LY03020 is a next-generation antipsychotic and the world’s first agonist against both the trace amine-associated receptor 1 (TAAR1) and the 5-HT2C receptor (5-HT2CR). It is also undergoing clinical trials in China.
Schizophrenia is a severe mental disorder affecting 24 million people worldwide1, of which 3.7 million are in the U.S. 2About 30% of the treatment-resistant schizophrenia patients do not respond well to the first- and second-generation antipsychotics.3 The next-generation antipsychotics are highly anticipated to be able to address the unmet needs, as they can primarily activate the presynaptic membrane. This is a key difference in the mechanism of action (MoA) from existing antipsychotics that typically antagonize D2 and 5-HT2A receptors on the postsynaptic membrane. As a result, the next-generation antipsychotics are expected to help reduce adverse reactions such as extrapyramidal symptoms (EPS) and metabolic syndrome associated with existing antipsychotics while making significant improvements on the positive symptoms, negative symptoms and cognitive impairments common in schizophrenia.
LY03020 targets both TAAR1 and 5-HT2CR. TAAR1 is primarily expressed on the presynaptic membrane, and its activation reduces the release of monoamine neurotransmitters such as dopamine (DA) and serotonin (5-HT) into the synaptic cleft. 5-HT2CR is expressed on both pre- and post-synaptic membranes. The activation of presynaptic 5-HT2CR further lowers the release of neurotransmitters like 5-HT and enhances the inhibition of negative symptoms. The activation of postsynaptic 5-HT2CR helps to reduce metabolic syndrome such as weight gain and abnormal glucose/lipid levels.
Preclinical studies have demonstrated that LY03020 can make significant improvements on the positive and negative symptoms as well as cognitive impairments associated with schizophrenia, without noticeable risks for EPS or metabolic syndrome like weight gain and abnormal glucose/lipid levels.
Dr. Tian Jingwei, Executive Vice President of Luye Institute for Innovative Research, said: “There are huge unmet treatment needs in the Central Nervous System (CNS) therapeutic area, which includes schizophrenia, but new drug development aiming to address them has been relatively slow. We have built a differentiated CNS portfolio that is globally competitive. LY03020 is one of our investigational CNS drugs under development both in China and abroad. We are actively developing the next-generation medicines with novel mechanisms of action to stay ahead of the competition in this area and keep delivering what the patients need.”
Luye Pharma’s CNS portfolio includes Erzofri® (paliperidone palmitate) extended-release injectable suspension and Rykindo® (risperidone) for extended-release injectable suspension, both have been approved for marketing in the U.S.; and Ruoxinlin® (Toludesvenlafaxine Hydrochloride Extended-Release Tablets) and Jinyouping® (Rotigotine Microspheres for Injection), both have been launched in China. In addition, the company is conducting clinical trials for several other investigational drugs, such as LY03021, which targets NET, DAT and GABAAR, and LY03015, which targets VMAT2 and Sigma1.
###
About Luye Pharma Group
Luye Pharma Group is an international pharmaceutical company dedicated to the R&D, manufacturing, and sale of innovative medications. The company has established R&D centers in China, the U.S. and Europe, with a robust pipeline of over 30 drug candidates in China and more than 10 drug candidates in other international markets. Luye Pharma maintains high-level international standards in novel drug delivery technologies including microspheres, liposomes, and transdermal drug delivery systems. The company has achieved multiple innovations in new chemical entities and antibodies, and is also actively making strategic developments in the fields of cell therapies and gene therapies.
Luye Pharma is developing a global supply chain of 8 manufacturing sites built up around the world, with GMP quality management and control systems established in line with international standards. With more than 30 products covering oncology, the central nervous system, cardiovascular, gastroenterology, metabolism and other therapeutic areas, business is conducted in over 80 countries and regions around the world, including the largest pharmaceutical markets - China, the U.S., Europe, and Japan, as well as in fast growing emerging markets.
References：
1. World Health Organization. Available at: https://www.who.int/zh/news-room/fact-sheets/detail/schizophrenia. Accessed on January 14, 2025
2. Treatment Advocacy Center. Available at: https://www.tac.org/research-weekly-more-people-with-schizophrenia-in-the-u-s-than-previously-reported/Accessed on January 14,2025
3. Disease Analysis: Schizophrenia. www.datamonitorhealthcare.com.
