Luye Pharma Group today announced that the investigational new drug application for its in-house developed next-generation vesicular monoamine transporter 2 (VMAT2) inhibitor, LY03015, has been submitted in the U.S., with Phase I clinical trial expected to begin soon. LY03015 is used for the treatment of tardive dyskinesia (TD) and Huntington's disease (HD). It is an innovative central nervous system (CNS) drug developed by Luye Pharma on the company’s New Chemical Entity / New Therapeutic Entity(NCE/NTE) Technology Platform.
TD is an extrapyramidal disorder featuring abnormal involuntary movements such as sedentary inability, myoclonus and convulsions, which occurs late after long-term use of dopamine receptor blockers such as antipsychotics. The disease is irreversible and disabling, with each bout of symptoms persisting for extended periods. HD is a hereditary neurodegenerative disease with clinical manifestations of movement disorders, psychiatric symptoms and cognitive impairment. As HD progresses, the advanced stages of the disease are characterized by stiffness and low-activity Parkinson's-like symptoms, which may be accompanied by focal dystonia, severely affecting patients’ quality of life and life expectancy.
VMAT2 inhibitors are the only drugs with validated clinical efficacy and safety for the treatment of TD and HD, but there are still high unmet needs that current marketed VMAT2 inhibitor products cannot address. These include a short half-life, risks of serious adverse effects due to off-target effects, drug instructions labeled with black box warnings for increased risk of depressive suicide, and increased cardiac safety risk.
As a new generation VMAT2 inhibitor, LY03015 can reduce the symptoms of TD and HD by inhibiting the release of presynaptic dopamine (DA), preventing the stimulation of supersensitive D2 receptors by DA without blocking D2 receptors in the postsynaptic membrane.
The results of preclinical studies indicate that LY03015 is more active, has better pharmacokinetic properties and a longer half-life than commercially available products. These properties are expected to reduce the required clinical dosage and thus reduce cardiac safety risk and other adverse effects.
The Phase I clinical trial of LY03015 in the U.S. will consist of a single-center, randomized, double-blind, placebo-controlled, single-dose, dose-escalation trial designed to evaluate the safety, tolerability and pharmacokinetic profile of a single oral dose of LY03015 in healthy subjects, with a planned enrollment of 120 subjects. In addition to the U.S. clinical trials for LY03015 will also be conducted simultaneously in China.
In the future, based on further validation of the product features in clinical trials, LY03015 is expected to address the unmet treatment needs of patients using commercially available VMAT2 inhibitors, in terms of activity, efficacy and safety, and have broader market prospects. Public financial data shows that three VMAT2 inhibitors approved by the U.S. Food and Drug Administration (FDA) had combined global sales of approximately US $1.659 billion in 2020, an increase of 37.9% over 2019, indicating significant market potential.
The CNS therapeutic area, where LY03015 is applied, is one of Luye Pharma’s core therapeutic areas. The company offers several innovative drugs and formulations worldwide targeting the vast unmet needs in this area. Among them, Rivastigmine multi-day transdermal patch for Alzheimer’s disease is eligible for marketing authorization in several EU countries. Commercialization agreements for the drug in Japan, Germany, Italy, Portugal, Greece and other markets have been reached with partners. Meanwhile, Seroquel (quetiapine fumarate, immediate release, IR) and Seroquel XR (extended release formulation), for schizophrenia and bipolar disorder, are sold in 51 countries and regions worldwide.
The company currently has a number of new drugs under development, several of which are now in the late clinical stage and new drug application (NDA) stage in China, the US, Europe and other countries and regions, covering a variety of diseases such as depression and Parkinson’s disease, forming a rich product portfolio in the CNS treatment field.
Luye Pharma Group today announced that the investigational new drug application for its in-house developed next-generation vesicular monoamine transporter 2 (VMAT2) inhibitor, LY03015, has been submitted in the U.S., with Phase I clinical trial expected to begin soon. LY03015 is used for the treatment of tardive dyskinesia (TD) and Huntington's disease (HD). It is an innovative central nervous system (CNS) drug developed by Luye Pharma on the company’s New Chemical Entity / New Therapeutic Entity(NCE/NTE) Technology Platform.
TD is an extrapyramidal disorder featuring abnormal involuntary movements such as sedentary inability, myoclonus and convulsions, which occurs late after long-term use of dopamine receptor blockers such as antipsychotics. The disease is irreversible and disabling, with each bout of symptoms persisting for extended periods. HD is a hereditary neurodegenerative disease with clinical manifestations of movement disorders, psychiatric symptoms and cognitive impairment. As HD progresses, the advanced stages of the disease are characterized by stiffness and low-activity Parkinson's-like symptoms, which may be accompanied by focal dystonia, severely affecting patients’ quality of life and life expectancy.
VMAT2 inhibitors are the only drugs with validated clinical efficacy and safety for the treatment of TD and HD, but there are still high unmet needs that current marketed VMAT2 inhibitor products cannot address. These include a short half-life, risks of serious adverse effects due to off-target effects, drug instructions labeled with black box warnings for increased risk of depressive suicide, and increased cardiac safety risk.
As a new generation VMAT2 inhibitor, LY03015 can reduce the symptoms of TD and HD by inhibiting the release of presynaptic dopamine (DA), preventing the stimulation of supersensitive D2 receptors by DA without blocking D2 receptors in the postsynaptic membrane.
The results of preclinical studies indicate that LY03015 is more active, has better pharmacokinetic properties and a longer half-life than commercially available products. These properties are expected to reduce the required clinical dosage and thus reduce cardiac safety risk and other adverse effects.
The Phase I clinical trial of LY03015 in the U.S. will consist of a single-center, randomized, double-blind, placebo-controlled, single-dose, dose-escalation trial designed to evaluate the safety, tolerability and pharmacokinetic profile of a single oral dose of LY03015 in healthy subjects, with a planned enrollment of 120 subjects. In addition to the U.S. clinical trials for LY03015 will also be conducted simultaneously in China.
In the future, based on further validation of the product features in clinical trials, LY03015 is expected to address the unmet treatment needs of patients using commercially available VMAT2 inhibitors, in terms of activity, efficacy and safety, and have broader market prospects. Public financial data shows that three VMAT2 inhibitors approved by the U.S. Food and Drug Administration (FDA) had combined global sales of approximately US $1.659 billion in 2020, an increase of 37.9% over 2019, indicating significant market potential.
The CNS therapeutic area, where LY03015 is applied, is one of Luye Pharma’s core therapeutic areas. The company offers several innovative drugs and formulations worldwide targeting the vast unmet needs in this area. Among them, Rivastigmine multi-day transdermal patch for Alzheimer’s disease is eligible for marketing authorization in several EU countries. Commercialization agreements for the drug in Japan, Germany, Italy, Portugal, Greece and other markets have been reached with partners. Meanwhile, Seroquel (quetiapine fumarate, immediate release, IR) and Seroquel XR (extended release formulation), for schizophrenia and bipolar disorder, are sold in 51 countries and regions worldwide.
The company currently has a number of new drugs under development, several of which are now in the late clinical stage and new drug application (NDA) stage in China, the US, Europe and other countries and regions, covering a variety of diseases such as depression and Parkinson’s disease, forming a rich product portfolio in the CNS treatment field.
