LUYE PHARMA - VOLUNTARY ANNOUNCEMENT FIRST SUBJECT ENROLLED IN THE U.S. PK BRIDGING CLINICAL TRIAL OF THE GROUP'S INNOVATIVE DRUG LY03015 (VMAT2 INHIBITOR/SIGMA-1R AGONIST)
LUYE PHARMA - VOLUNTARY ANNOUNCEMENT
FIRST SUBJECT ENROLLED IN THE U.S. PK BRIDGING CLINICAL TRIAL OF THE GROUP'S INNOVATIVE DRUG LY03015 (VMAT2 INHIBITOR/SIGMA-1R AGONIST)
LUYE PHARMA GROUP LTD.
綠叶制药集团有限公司
(Incorporated in Bermuda with limited liability)
(Stock Code: 02186)
VOLUNTARY ANNOUNCEMENT
FIRST SUBJECT ENROLLED IN THE U.S. PK BRIDGING CLINICAL TRIAL OF THE GROUP'S INNOVATIVE DRUG LY03015
(VMAT2 INHIBITOR/SIGMA-1R AGONIST)
The board of directors (the "Board") of Luye Pharma Group Ltd. (the "Company", together with its subsidiaries, the "Group") announces that the first subject has been enrolled in the U.S. pharmacokinetic (PK) clinical trial of the Group's in-house developed new molecular entity LY03015. This is the world's first investigational drug designed to inhibit vesicular monoamine transporter 2 (VMAT2) and activate sigma-1 receptor (Sigma-1R). It is intended for the treatment of tardive dyskinesia (TD) and Huntington's disease (HD).
By targeting VMAT2 and Sigma-1R, LY03015 is designed to control the symptoms of both TD and HD and potentially modify their pathologies. On the one hand, it reduces the release of presynaptic neuronal dopamine (DA) by inhibiting the function of VMAT2, thereby reducing the stimulation of supersensitive D2 receptors by DA without blocking postsynaptic D2 receptors, which may help alleviate symptoms. On the other hand, by activating Sigma-1R, it may also stimulate the release of brain-derived neurotrophic factor (BDNF) and promote synaptic remodeling to help restore the impaired corticostriatal synaptic connectivity, with the potential to provide a sustained symptom relief and reduce recurrence following treatment discontinuation.
The clinical trial being conducted in the U.S. is an open-label, single-dose and parallel-group bridging study designed to evaluate the safety, tolerability, and pharmacokinetic profile of LY03015 in healthy Chinese and Caucasian adults, providing key evidence to support dose selection for subsequent U.S. Phase II and Phase III clinical trials. The Group has a longestablished presence in the central nervous system (CNS) therapeutic area. Being another investigational CNS drug under development in both China and the U.S., LY03015 is expected to complete a Phase II clinical trial in China soon.
TD is a movement disorder characterized by abnormal involuntary movements associated with the long-term use of dopamine receptor-blocking agents, including antipsychotic medications. Approximately 67% to 89% of the patients with TD experience permanent involuntary movements, resulting in a high rate of disability. Among patients receiving antipsychotic medications, the average prevalence of TD is approximately 25.3%. HD is an autosomal dominant neurodegenerative disorder, with typical symptoms including choreiform involuntary movements, cognitive impairment, and psychiatric or behavioral abnormalities.
To the Group's knowledge, VMAT2 inhibitors remain the only class of drugs approved by the U.S. Food and Drug Administration (FDA) for the treatment of TD and HD to date. There is a substantial unmet need in treating these two diseases. The Group will accelerate the clinical development of LY03015 in both China and the U.S. to further validate its therapeutic potential and enhance the Group's competitive edge in this field.
The CNS therapeutic area is a strategic focus for the Group. The Group has built a differentiated product portfolio targeting multiple conditions such as depression, schizophrenia, bipolar disorder, and Alzheimer's disease. This portfolio includes Erzofri® (paliperidone palmitate) extended-release injectable suspension and Rykindo® (risperidone) for extended-release injectable suspension, both approved for marketing in the U.S.; the Rivastigmine Twice Weekly Transdermal Patch, which was approved for marketing in Japan, China, and several European countries; and Ruoxinlin® (Toludesvenlafaxine Hydrochloride Sustained-Release Tablets), which was approved for marketing in China. The Group is also conducting clinical trials for several other investigational drugs, including LY03017 which targets 5-HT R/5-HT R, LY03020 which targets TAAR1/5-HT R, and LY03021 which
2A 2C 2C
targets GABA R/NET/DAT.
A
By Order of the Board
LUYE PHARMA GROUP LTD. Liu Dian Bo
Chairman
Hong Kong, 20 April 2026
As at the date of this announcement, the executive directors of the Company are Mr. LIU Dian Bo, Mr. YANG Rong Bing, Mr. YUAN Hui Xian and Ms. ZHU Yuan Yuan; the nonexecutive directors of the Company are Mr. SONG Rui Lin and Mr. HUANG Liming; and the independent non-executive directors of the Company are Mr. ZHANG Hua Qiao, Professor LO Yuk Lam, Mr. LEUNG Man Kit, Mr. CHOY Sze Chung Jojo and Ms. XIA Lian.