LUYE PHARMA's innovative drug LY03015 (VMAT2 inhibitor/Sigma-1R agonist) completed the first subject enrollment in its US PK bridging clinical trial.

LUYE PHARMA (02186) announced that the first subject has been enrolled in the bridging clinical trial of the group's independently developed new molecular entity LY03015's pharmacokinetics (PK) in the United States. LY03015 is the world's first vesicular monoamine transporter 2 (VMAT2) inhibitor and sigma-1 receptor (Sigma-1R) agonist, targeting indications for treating Tardive Dyskinesia (TD) and Huntington's disease (HD). LY03015 aims to exert a dual effect on the two diseases in terms of "symptom control" and "pathological improvement" by targeting VMAT2 and Sigma-1R. On one hand, by inhibiting the transport function of VMAT2 to reduce the release of dopamine (DA) from presynaptic neurons, LY03015 can reduce DA stimulation of hypersensitive D2 receptors while not blocking postsynaptic D2 receptors, thereby alleviating disease symptoms. On the other hand, by stimulating Sigma-1 receptors, LY03015 can promote the release of brain-derived neurotrophic factor (BDNF) and synaptic remodeling, repairing damaged cortico-striatal synaptic connections, and potentially achieving sustained symptom relief after drug withdrawal and reducing disease recurrence rates. The clinical trial conducted in the United States is an open-label, single-dose, parallel-group bridging trial aimed at evaluating the safety, tolerability, and pharmacokinetic characteristics of LY03015 in Chinese and Caucasian healthy adult subjects to provide key evidence and scientific support for dose selection in US Phase II and III clinical trials. The group has long been focused on the central nervous system (CNS) treatment field, and LY03015, as another innovative CNS drug being simultaneously developed by the group in China and the United States, is also on the verge of completing Phase II clinical trials in China. TD is a type of abnormal involuntary movement associated with long-term use of antipsychotic drugs and other dopamine receptor blockers. Among TD patients, 67% to 89% have permanent involuntary movements with a high disability rate. The average incidence of TD in patients receiving antipsychotic drug treatment is 25.3%. HD is an autosomal dominant hereditary neurodegenerative disease with typical symptoms including chorea, cognitive impairment, and psychiatric symptoms. To the group's knowledge, VMAT2 inhibitors are currently the only class of drugs approved by the US Food and Drug Administration for treating TD and HD. There is a widespread and unmet treatment need in the related disease areas. The group will accelerate the clinical development process of LY03015 in China and the United States to further confirm the therapeutic potential of the product and continue to strengthen the group's competitive advantage in this field.