LYUE PHARMA (02186) innovative drug LY03015 (VMAT2 inhibitor/Sigma-1R agonist) has achieved positive results in the Phase II clinical trial for the treatment of delayed onset movement disorders in China.

LUYE PHARMA (02186) announced that the Phase II clinical trial of the Group's independently developed innovative drug LY03015 for the treatment of Tardive Dyskinesia (TD) in China has been completed, achieving positive results and meeting the primary endpoint. LY03015 is the world's first vesicle monoamine transporter 2 (VMAT2) and Sigma-1R dual-target innovative drug to enter clinical trials, targeting indications for TD and chorea associated with Huntington's disease (HD). TD is a hyperkinetic movement disorder that occurs after long-term use of antipsychotic drugs, characterized by involuntary, rhythmic, repetitive stereotyped movements, including abnormal movements of facial or trunk muscles. The symptoms often persist even after discontinuation of the causative drugs, severely affecting the mental health and quality of life of patients. According to global data, the average incidence of TD among patients receiving antipsychotic drug treatment is approximately 25.3%. The Cortellis database shows that the market size of drugs for the treatment of this disease is approximately $5 billion/year and is growing rapidly. Public information shows that existing treatment drugs either have serious safety risks due to off-target effects of metabolites or through CYP2D6 metabolism inactivation with evident genetic polymorphism. Results from double-blind clinical trials of existing treatment drugs show that about 60% of patients still cannot achieve a clinically meaningful improvement rate (proportion of improvement in the Abnormal Involuntary Movement Scale [AIMS] score of 1-7 by 50%) after treatment with a single-target VMAT2 inhibitor, indicating inadequate effectiveness and significant unmet treatment needs. Through its independently established AI drug design platform, the Group has designed a novel small molecule drug, LY03015, which not only addresses the safety risks mentioned above but also targets VMAT2 and Sigma-1R with high activity, exerting a dual action of "symptom control" and "pathological improvement." On one hand, inhibiting the transport function of VMAT2 reduces the release of dopamine (DA) from presynaptic neurons, decreasing the sensitivity of DA to D2 receptor stimulation and thus relieving disease symptoms. On the other hand, stimulation of Sigma-1R can promote the release of brain-derived neurotrophic factor (BDNF) and synaptic remodeling, repairing damaged cortico-striatal synaptic connections, potentially achieving sustained symptom relief and reducing the rate of disease recurrence.