LUYE PHARMA (02186) announced that its self-developed novel drug LY03017, a next-generation 5-HT2A receptor inverse agonist and 5-HT2C receptor antagonist, has received approval from the U.S. Food and Drug Administration (FDA) to commence clinical trials. LY03017 is intended for the treatment of Alzheimer’s disease psychosis (ADP), Parkinson’s disease psychosis (PDP), and negative symptoms of schizophrenia (NSS). The FDA has waived the single ascending dose (SAD) phase in the Phase I clinical trials, allowing the drug to proceed directly to multiple ascending dose (MAD) studies and subsequent clinical trials.
Developed under the company’s New Molecular Entity/New Therapeutic Entity (NME/NTE) technology platform, LY03017 represents another innovative drug in the central nervous system (CNS) therapeutic area being developed simultaneously in China and the U.S. Currently, LY03017 is also in Phase I clinical trials in China.
Globally, only one drug has been approved by the FDA for PDP treatment, and it has not yet been approved in China. For ADP, no drugs have been approved worldwide. In the case of NSS, only a few drugs show limited efficacy. These three indications represent significant unmet medical needs.
LY03017 is a novel dual-target drug acting on 5-HT2AR and 5-HT2CR. It inhibits ventral striatal dopamine release and enhances prefrontal cortical dopamine release through 5-HT2AR inverse agonism and 5-HT2CR antagonism, potentially addressing hallucinations and delusions in PDP and ADP patients while improving NSS. Preclinical studies indicate that LY03017 demonstrates superior in vitro and in vivo pharmacological activity, tissue distribution, and cardiac safety compared to existing and investigational drugs for the same indications.
CNS therapeutics is a core strategic focus for LUYE PHARMA. The company has built a differentiated portfolio in this field, covering depression, schizophrenia, bipolar disorder, Alzheimer’s disease, and other conditions. Key products include Erzofri® (paliperidone palmitate extended-release suspension, approved in the U.S.), Rykindo® (risperidone extended-release microspheres), and rivastigmine transdermal patches (twice weekly, approved in Europe, Japan, and China), as well as Ruoxinlin® (toludesvenlafaxine hydrochloride extended-release tablets) and Jinyouping® (rotigotine microspheres for injection) in China.
Additionally, LUYE PHARMA is advancing next-generation innovative drugs, including LY03015 (a VMAT2/Sigma-1R dual-target drug), LY03020 (a TAAR1/5-HT2CR dual-target drug), and LY03021 (a NET/DAT/GABAAR triple-target drug), all in clinical development.