Luye Pharma Group has taken a significant step forward in the treatment of tardive dyskinesia (TD) and Huntington's disease (HD) with the submission of an investigational new drug application for LY03015, its next-generation vesicular monoamine transporter 2 (VMAT2) inhibitor, in the U.S. The Phase I clinical trial is anticipated to commence shortly, marking a pivotal moment in the development of this innovative central nervous system (CNS) drug.
TD is characterized by abnormal involuntary movements resulting from long-term use of dopamine receptor blockers, such as antipsychotics, and is known for its irreversible and disabling nature. HD, a hereditary neurodegenerative disease, presents with movement disorders, psychiatric symptoms, and cognitive impairment, severely impacting patients' quality of life and life expectancy.
VMAT2 inhibitors currently represent the sole class of drugs with proven clinical efficacy and safety for TD and HD. However, existing treatments face limitations, including a short half-life, serious adverse effects, and increased risks of depressive suicide and cardiac safety issues. LY03015 aims to address these unmet needs by inhibiting the release of presynaptic dopamine without blocking D2 receptors in the postsynaptic membrane, thereby reducing symptoms of TD and HD.
Preclinical studies have shown that LY03015 possesses superior activity, pharmacokinetic properties, and a longer half-life compared to available products, potentially lowering the required clinical dosage and minimizing adverse effects. The upcoming Phase I trial in the U.S. will be a single-center, randomized, double-blind, placebo-controlled, single-dose, dose-escalation study involving 120 healthy subjects to assess the safety, tolerability, and pharmacokinetic profile of LY03015. Concurrent clinical trials are also planned in China.
With the global market for VMAT2 inhibitors showing significant growth, LY03015 is poised to meet the high unmet needs of patients, offering improved activity, efficacy, and safety. The CNS therapeutic area remains a core focus for Luye Pharma, which continues to develop innovative drugs and formulations to address the vast unmet needs in this field, including treatments for Alzheimer's disease, schizophrenia, and bipolar disorder.
