China-based Luye Pharma Group (HKG: 2186) announced that it has received approval from the US Food and Drug Administration (FDA) to conduct a Phase I clinical study of its LY03015. The study will assess the safety, tolerability, and pharmacokinetics of the next-generation vesicular monoamine transporter 2 (VMAT2) inhibitor. LY03015 is under development to treat tardive dyskinesia (TD) and Huntington’s disease (HD).
Mechanism of Action and Advantages
As a next-generation VMAT2 inhibitor, LY03015 works by inhibiting the release of dopamine (DA) from presynaptic neurons, avoiding DA’s stimulation of hypersensitive D2 receptors without blocking the D2 receptors of the postsynaptic membrane. This mechanism helps mitigate symptoms of TD and HD. Compared to other VMAT2 inhibitors on the market, LY03015 avoids the risk of depression and suicide caused by off-target effects. It also has a more ideal elimination half-life, which can reduce the number of daily medications, and has a higher brain tissue distribution with lower heart distribution and lower hERG toxicity.
Clinical Trial and China Approval
The drug has obtained tacit clinical trial approval in China. The Phase I study in the US will further evaluate its safety and pharmacokinetics, paving the way for potential global development.
Current VMAT2 Inhibitors in China
According to Fineline Info & Tech data, currently approved VMAT2 inhibitors in China include reserpine, tetrabenazine, and deuterated tetrabenazine.-Fineline Info & Tech
