LUYE PHARMA (02186): LY03015 enrolls the first patient in Phase II clinical trial in China

LUYE PHARMA (02186) announced that the group's innovative drug LY03015 of Class 1 has enrolled the first patient in Phase II clinical trials in China. LY03015 is a VMAT2 (vesicular monoamine transporter 2) inhibitor and Sigma-1 receptor agonist, intended for the treatment of Tardive Dyskinesia (TD) and Huntington's Disease (HD). The product is being developed simultaneously in China and the United States and will further strengthen the group's product portfolio in the central nervous system (CNS) therapy field. LY03015 is a new generation VMAT2 inhibitor developed independently based on the group's new molecular entity/new therapeutic entity technology platform. By inhibiting the transport function of VMAT2, it can reduce the release of dopamine (DA) from presynaptic neurons, lower the sensitivity of DA receptors to stimulation while not blocking the D2 receptors on the postsynaptic membrane, thereby alleviating symptoms of TD and HD. Additionally, LY03015 has strong Sigma-1 receptor agonist activity, which can reduce oxidative stress response, provide neuroprotection, and improve cognition, among other benefits, thus offering better clinical treatment outcomes for TD and HD. Preclinical results indicate that compared to products on the market, LY03015 has superior in vitro and in vivo pharmacological activity and pharmacokinetic properties, with no off-target effects and better cardiac safety. Phase I clinical results demonstrate that LY03015 has good overall safety and tolerability, a longer half-life, and can be administered once daily. Unlike existing VMAT2 formulations on the market, LY03015 does not undergo metabolism by CYP2D6, reducing the risk of drug interactions. The Phase II clinical trial for LY03015 in China is a multicenter, randomized, double-blind, placebo-controlled trial conducted in TD patients.