LY03021同时针对NET、DAT和GABALuye Pharma (02186) announced that the group's Class 1 innovative drug LY03021 has been approved by the China National Medical Products Administration...
According to the Zhitong Finance and Economics APP, Luye Pharma (02186) announced that the group's Class 1 innovative drug LY03021 has been approved by the China National Medical Products Administration Drug Evaluation Center for clinical trials intended for treating depression.
LY03021 is a norepinephrine transporter (NET) / dopamine transporter (DA) inhibitor, and a positive allosteric modulator of γ-aminobutyric acid A receptor (GABAAR PAM). This product is independently developed based on the group's new molecular entity / new therapeutic entity technology platform (NCE / NTE), is a novel antidepressant with a triple target mechanism, and has the potential of being a first-in-class product. The company is not aware of any product with the same mechanism currently in development.
LY03021 acts on the NET, DAT, and GABAAR targets simultaneously. This product enhances GABA activation on GABAA receptor subtypes α1β2γ2 at synapses and α4β3δ at extrasynaptic sites, regulates the glutamate-GABA balance in the brain, suppresses the excessive activation of the hypothalamic-pituitary-adrenal (HPA) axis, quickly exhibits antidepressant effects. Additionally, by inhibiting NET and DAT, LY03021 increases norepinephrine (NE) and dopamine (DA) levels in the brain, significantly improving core symptoms, anhedonia, and sexual dysfunction in patients with depression, and through NE and DA's 'awakening mechanism', eliminates adverse reactions such as sedation, somnolence, and loss of consciousness caused by GABA receptor activation.
Non-clinical studies show that LY03021 significantly improves model animal depressive symptoms 24 hours after administration, and with continuous use, the efficacy can be maintained until the end of the 21-day study, demonstrating advantages of rapid onset and long-term effectiveness. Furthermore, the product has good safety, with a NOAEL (no observed adverse effect level) more than 50 times the effective dose.
Patients in CNS therapeutic areas, including depression, have a significant demand, but new drug development progresses relatively slowly. The group has a series of internationally competitive innovative drugs and formulations, becoming a leading force in this therapeutic area. The group's product portfolio in the CNS field includes: Erzofri (paliperidone palmitate extended-release suspension) and Rykindo (paliperidone palmitate extended-release microspheres injection) approved for marketing in the USA, and Ruoxinlin (tolperisone hydrochloride flupirtine maleate extended-release tablets) and Jinyouping (injection of rosuvastatin microspheres) on the market in China. In addition, the company has multiple Class 1 innovative drugs in clinical stages, including the TAAR1/5-HT2CR dual agonist (LY03020) and the VMAT2/Sigma1 dual-target new drug (LY03015).
