Luye Pharma completes U.S. bridging trial for VMAT2/Sigma-1R dual-acting drug LY03015

Bulletin Express08-05

Luye Pharma Group Ltd. announced the successful completion of a U.S. bridging clinical study for LY03015, an in-house small-molecule targeting both VMAT2 inhibition and Sigma-1R activation for the treatment of tardive dyskinesia (TD) and Huntington’s disease-related chorea.

The open-label, single-dose trial enrolled 24 healthy volunteers—12 Chinese and 12 Caucasian—each receiving a 20 mg oral dose. Pharmacokinetic parameters were comparable between ethnic groups. All treatment-emergent adverse events were mild, with no serious adverse events recorded. Safety and tolerability were notably better in Caucasian subjects, reflected in TEAE incidence rates of 33.33% versus 83.33% in Chinese subjects.

Data from a prior multicenter, randomized, double-blind, placebo-controlled phase II study in China (n = 121) demonstrated a 76.50% AIMS ≥50% response in the 20 mg dose cohort after six weeks, nearly double historical response levels of current first-line therapies. Building on these findings, the company plans a simplified fixed-dose regimen for the forthcoming U.S. efficacy study, positioning LY03015 for differentiated clinical value in efficacy, onset, and dosing convenience.

Luye Pharma’s central nervous system pipeline also features: • LY03017 – next-generation 5-HT2A inverse agonist/5-HT2C antagonist in phase II (China) for multiple neuropsychiatric indications. • LY03020 – first agonist of both TAAR1 and 5-HT2C, in phase II (China) for schizophrenia and Alzheimer’s disease-related psychosis. • LY03021 – first-in-class GABAAR PAM and NET/DAT inhibitor in phase I (China) for major depressive disorder.

The board stated that the bridging results support immediate initiation of a U.S. efficacy trial for LY03015.

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