By Fineline Cube 
China-based Luye Pharma Group (HKG: 2186) announced on August 3, 2025, that its self-developed Class 1 innovative drug, LY03021, has completed the enrollment of its first healthy subject in a Phase I clinical trial in China. LY03021 represents a significant advancement in the treatment of depression, leveraging a novel triple-target mechanism of action.
Mechanism of Action
LY03021 is a first-in-class antidepressant developed on Luye Pharma’s New Chemical/Therapeutic Entity (NCE/NTE) technology platform. It acts as a norepinephrine transporter (NET) and dopamine transporter (DAT) inhibitor and a positive allosteric modulator of the γ-aminobutyric acid type A receptor (GABAAR PAM). The drug is designed to enhance the activation of specific GABAAR subtypes by GABA, thereby regulating the glutamate-GABA balance and inhibiting excessive HPA axis activation. Its NET and DAT inhibitory effects also help improve anhedonia and core symptoms while reducing side effects such as sedation.
Preclinical Results
Preclinical studies have demonstrated that LY03021 is characterized by rapid onset of action, sustained efficacy, and a favorable safety profile. These attributes position LY03021 as a promising new treatment option for patients with depression.
Phase I Clinical Trial
The Phase I clinical trial is designed as a randomized, double-blind, placebo-controlled, dose-escalation study. Its primary objectives are to evaluate the safety, tolerability, and pharmacokinetic profile of LY03021 in healthy subjects.
Strategic Significance
Luye Pharma has established a strategic presence in central nervous system (CNS) therapeutics across key markets, including China, the U.S., Europe, and Japan. LY03021 is a crucial component of the company’s next-generation innovative drug strategy, reflecting its commitment to addressing unmet medical needs in the treatment of depression.-Fineline Info & Tech