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LY03020 is a novel, oral small molecule antipsychotic developed by Luye Pharma. It is the world’s first dual agonist of trace amine-associated receptor 1 (TAAR1) and serotonin 5-HT2C receptor (5-HT2CR). Unlike existing antipsychotics that typically antagonize D2 and 5-HT2A receptors on the postsynaptic membrane, LY03020 acts as an agonist at TAAR1 and 5-HT2CR—primarily on presynaptic membranes. Activation of TAAR1 reduces the release of monoamine neurotransmitters such as dopamine and serotonin into the synaptic cleft. Activation of presynaptic 5-HT2CR further lowers neurotransmitter release, enhancing inhibition of negative symptoms; activation of postsynaptic 5-HT2CR helps reduce metabolic syndrome risks like weight gain and abnormal glucose/lipid levels. Preclinical studies show significant improvements in positive/negative symptoms and cognitive impairments associated with schizophrenia without notable extrapyramidal or metabolic side effects. The drug is being developed for schizophrenia and Alzheimer’s disease psychosis[1][3][4][6].

Other names

LY03020LY-03020LY 03020LPM787000048 maleateLPM-787000048 maleateLPM 787000048 maleate