Shanghai,, August 3, 2025 / Prnewswire / – Lye Pharma Group announced today that the first subject had been registered in a phase 1 clinical trial in China For its LY03021, which was deposited through China Class 1 trades for innovative drugs. Ly03021 is an inhibitor of the Noradéphrine (net) carrier, the dopamine carrier (DAT) and an allosteric modulator type A gamma-aminobutyric type A (GABA (GABA (GABA (GABA (GABA (GABA (GABAAR PAM), intended for the treatment of major depressive disorder (MDD).
MDD has a high prevalence rate, a high disability rate and a high recurrence rate. In ChinaThe life prevalence of this disease is 3.4%, and the prevalence of 12 months is 2.1%.[1] Existing antidepressants have failed to provide satisfactory response and remission rates, their beginning of action generally takes 2 to 4 weeks, [2] And patients who take them may have residual symptoms and adverse reactions. Therefore, how to quickly and effectively control the symptoms of CT and further improve the effectiveness of antidepressants and the prognosis of patients is a challenge in the development of these drugs today.
The start of CT would be closely associated with imbalances in cerebral neurotransmitters, including serotonin (5-HT), noradrenaline (NE), dopamine (DA) and gamma-aminobutyric acid (GABA). Among them, the GABA has become a key therapeutic target for psychiatric disorders. A series of studies involved critical roles in the altered Gabaergic system, the main signaling system inhibiting the central nervous system (SNC), in the pathogenesis of CT.[3] There is also evidence that the gabaergic interneurons are involved in depression behaviors and rapid antidepressive responses.[4] However, current antidepressants often excessively activate the synaptic gabaA Receiver (α subtype1B2C2), leading to undesirable effects such as excessive sedation, drowsiness and even confusion. These side effects pose challenges such as narrow therapeutic windows and dose limitations.
Developed on the new chemical / new therapeutic entity (NCE / NTE) of Luye Pharma, LY03021 acts on all three targets: net, dat and gabaAR, a new mechanism of action (MOA) which makes it a potential first class antidepressant. By targeting the synaptic gabaA Receiver (α subtype1B2C2) and Gaba ExtrasynapticA Receiver (α subtype4B3Δ) To a more appropriate connection ratio, this medication improves Gaba’s Gabaergic activationA The receptors, regulates the balance of glutamate / gaba in the brain, inhibits excessive activation of the hypothalamo-hypophyso-surrenal (HPA) axis and quickly relieves depressive symptoms. At the same time, it also increases the levels of NE and DA in the brain by inhibiting the net and the date, considerably improving central symptoms in addition to anhedonia and sexual dysfunction in TDM patients. Thanks to the effects promoting the wake of NE and DA, it also reduces undesirable effects such as sedation, drowsiness and loss of consciousness caused by the activation of GABA receptors.
Non -clinical studies have shown that LY03021 significantly inhibited depressive symptoms in animal models 24 hours after administration, and continuous administration could maintain efficiency until the end of a 21 -day study. In addition to its rapid appearance of action and sustained efficiency, this drug also has a good safety profile, because its Noael (the level of opposite effects not observed) is 50 times above its effective dose.
The phase 1 clinical trial recently launched China is a monocytoresque, randomized, double -blind, placebo -controlled study, dose climbing designed to assess the safety, tolerability and pharmacokinetic profile of LY03021 in healthy subjects.
There is a huge demand for SNC medication, including those of TDM treatment. However, the development of new drugs in this area has been relatively slow. Luye Pharma has obtained marketing authorizations for a number of internationally competitive innovative drugs and innovative formulations ChinaThe United States, Japanand other markets. Here are some examples: Erzofri® (Palperidone Palmitate) Injectable suspension for prolonged liberation and Rykindo® (Risperidone) for an injectable suspension for prolonged release, both approved for marketing in the United States; Rivastigmine twice a week transdermal, which has been approved for marketing in several European countries, JapanAnd China; and RUOXINLIN® (Toludesvenlafaxine hydrochlorhydrate hydrochloride® (Rotigotine microspheres for injection), the two were approved for marketing in China. In addition, the company also conducts clinical studies for several other survey drugs filed through China Class 1 pathway, like Ly03020, which targets TAAR1 and 5-HT2cR, LY03015, which targets vmat2 and sigma1, and ly03017, which targets 5-ht2aR and 5-HT2cR.
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[1] Yueqin Huang, Yu Wang, Hong Wang, et al. Prevalence of mental disorders in China: a transverse epidemiological study. Lancet Psychiatry. March 2019; 6 (3): 211-224. |
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[2] Guidelines for the prevention and treatment of depressive disorders in China (2nd edition). Compiled by the Chinese Psychiatry Society. Chinese medical multimedia press. |
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[3] Jiao Zou et al. The effectiveness and safety of certain new gabakines for the treatment of depression: a systematic review and a meta-analysis from randomized controlled trials. Research in psychiatry. Volume 328, October 2023, https://doi.org/10.1016/j.psychres.2023.115450 |
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[4] Manoela against Fogaça et al. The inhibition of the GABA interneurons in the MPFC is sufficient and necessary for rapid antidepressive responses. Mol Psychiatry. 2020 October 17; 26 (7): 3277–3291. DOI: 10.1038 / S41380-020-00916-Y |
About Luye Pharma Group
Luye Pharma Group is an international pharmaceutical company dedicated to the development, manufacture and sale of innovative drugs. With R&D centers in Chinathe United States, and EuropeThe company is an international leader in new medication administration systems such as microspheres, liposomes and transdermal patches. It also has several innovative products in two categories: new chemical entities and antibodies. From 2021 to 2025, the company had a total of 13 new drugs approved for marketing, each in one or more countries such as the United States, several European countries, JapanAnd China.
The company has 8 manufacturing facilities worldwide, which follow management and quality control systems comply with international and compliant with BPF. To date, the company has launched more than 30 products in the central nervous system (SNC), oncology, cardiovascular and other therapeutic areas. He leads business in more than 80 countries and regions, including the main pharmaceutical markets such as ChinaThe United States, EuropeAnd JapanAnd including fast -growing emerging markets.
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Source Luye Pharma Group
