LB-102

LB-102 is an N-methylated analogue of amisulpride being developed as a potential first-in-class benzamide antipsychotic in the United States. It has demonstrated promising efficacy and safety in clinical trials, particularly for treating acute schizophrenia. LB-102 works primarily as a dopamine D2/D3 receptor antagonist with additional 5HT7 antagonism. Unlike many commonly prescribed antipsychotics in the U.S., LB-102 has low off-target binding, which reduces the risk of unwanted side effects such as anti-cholinergic burden and excessive sedation. Its improved blood-brain barrier permeability allows for lower dosing while maintaining strong clinical response. The drug has completed Phase 2 clinical trials with positive results. In the NOVA-1 trial, LB-102 achieved its primary endpoint of clinically meaningful change in Positive and Negative Syndrome Scale (PANSS) total score at week 4 with statistical significance across all tested doses (50mg, 75mg, and 100mg). The drug also showed positive results in the Clinical Global Impression of Severity (CGI-S) scores. LB-102 demonstrated a favorable safety profile with: low incidence of extrapyramidal symptoms (EPS), limited clinical adverse events associated with elevated prolactin, minimal QT interval prolongation, average placebo-adjusted weight gain of 2 kg, and only one case of sedation reported across 251 dosed subjects. Phase 3 clinical trials for acute schizophrenia are expected to begin in Q4 2025. LB-102 offers several potential advantages over existing antipsychotics: once-daily dosing without food effect, simplifying treatment regimen; improved blood-brain barrier penetration allowing for lower doses; potential efficacy for both positive and negative symptoms of schizophrenia; low binding to 5-HT2C, Alpha-1, or H1 receptors, which helps avoid side effects like weight gain and sedation. LB Pharmaceuticals is also exploring the drug's potential in additional psychiatric indications, including bipolar depression.

Other names

N-MethylamisulprideN′-Methylamisulpride(R)-N-Methyl AmisulprideAmisulpride impurity HNM73EV997HNM-73EV997HNM 73EV997HGWW586C64DGWW-586C64DGWW 586C64D