LUYE PHARMA (02186) announced that the first participant has been enrolled in the US pharmacokinetic (PK) bridging clinical trial for its self-developed new molecular entity, LY03015. This compound is the world's first vesicular monoamine transporter 2 (VMAT2) inhibitor and sigma-1 receptor (Sigma-1R) agonist, targeting the treatment of tardive dyskinesia (TD) and Huntington's disease (HD). By targeting both VMAT2 and Sigma-1R, LY03015 is designed to provide dual benefits of symptom control and pathological improvement for both conditions. On one hand, it reduces the release of dopamine from presynaptic neurons by inhibiting VMAT2 function, thereby alleviating symptoms without blocking postsynaptic D2 receptors. On the other hand, by activating Sigma-1R, it promotes the release of brain-derived neurotrophic factor and synaptic remodeling, which may repair damaged corticostriatal synaptic connections and lead to sustained symptom relief and reduced relapse rates after treatment discontinuation. The ongoing US trial is an open-label, single-dose, parallel-group bridging study designed to evaluate the safety, tolerability, and pharmacokinetic profile of LY03015 in healthy Chinese and Caucasian adult subjects. The results will provide critical data to support dose selection for subsequent Phase II and III clinical trials in the United States. LUYE PHARMA has a long-term focus on the central nervous system (CNS) therapeutic area, and LY03015 is another innovative CNS drug being developed concurrently in China and the United States. Its Phase II clinical trial in China is nearing completion. Tardive dyskinesia is an abnormal involuntary movement disorder associated with long-term use of antipsychotic drugs and other dopamine receptor blockers. Among affected individuals, 67% to 89% experience permanent involuntary movements, leading to a high disability rate. The average prevalence of TD among patients treated with antipsychotics is 25.3%. Huntington's disease is an autosomal dominant neurodegenerative disorder characterized by a triad of symptoms: choreiform involuntary movements, cognitive impairment, and psychiatric abnormalities. According to the company, VMAT2 inhibitors are currently the only class of drugs approved by the US Food and Drug Administration for treating TD and HD. There remains a significant unmet medical need in these disease areas. LUYE PHARMA plans to accelerate the clinical development of LY03015 in both China and the United States to further demonstrate its therapeutic potential and strengthen the company's competitive position in this field.
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