We are leveraging our expertise in neuropsychiatry and LB-102’s mechanism of action to develop a pipeline targeting other psychiatric disorders, including mood disorders and schizophrenia with predominantly negative symptoms, and Alzheimer’s psychosis.

LB-102 for Schizophrenia: We are building a pipeline that leverages the broad therapeutic potential of our lead product candidate, LB-102, a novel, patent-protected, methylated derivative of amisulpride.

About Amisulpride: Amisulpride is a second-generation antipsychotic approved and commercialized outside the U.S. for treating schizophrenia, known for its favorable efficacy and tolerability. Despite its international use, it lacks U.S. regulatory approval due to patent incompatibility with FDA requirements. In a 2019 meta-analysis published in The Lancet, amisulpride was second only to clozapine in overall efficacy for treating schizophrenia and was most effective for positive symptoms. A 2008 head-to-head trial in The Lancet also highlighted its superior tolerability, second only to olanzapine

LB-102 Design: LB-102 is a patented benzamide designed to improve upon the safety and efficacy of amisulpride. In creating LB-102, we have added a precisely placed methyl group to the chemical structure of amisulpride with the intention of improving its permeability of the blood-brain barrier while only minimally affecting receptor binding. We believe that making this chemical change may allow LB-102 to be dosed at lower amounts than amisulpride. By dosing at a lower level, we are aiming to decrease side effects common to amisulpride and other antipsychotics while improving upon an already strong efficacy profile. We also believe this change to the chemical structure will allow us to differentiate the dosing frequency of LB-102 from that of amisulpride. We are developing LB-102 for once-daily dosing, in contrast to the typical twice-daily dosing of amisulpride. The enhanced blood-brain barrier permeability and pharmacokinetic profile of LB-102 could allow it to be formulated into the first benzamide long-acting injectable.

LB-102 Clinical Development in acute schizophrenia: Our clinical trials aim to show that LB102 can improve vs. amisulpride in key aspects

  1. Phase 1 PET imaging studies
    1. LB-102 dopamine receptor occupancy was in desired range to treat schizophrenia
    2. Showed that LB-102 reached amisulpride-like receptor occupancy at significantly lower doses
    3. Receptor occupancy persisted over 24 hours after final dose was administered under steady state conditions indicative of a compound with once daily dose potential
    4. Unique profile among anti-dopaminergic antipsychotic in that there was consistent brain dopamine occupancy over 24 hours despite low plasma levels
  2. Phase 1 safety study
    1. SAD/MAD underscores LB-102’s safety potential with no weight gain, sedation, EPS or concerning QT prolongation at Phase 2 doses

Expansion Potential

  1. Long-acting injectable
    1. LB Pharma wants to create a first-in-class benzamide LAI formulation; efforts are already underway with several prototypes
    2. Greater potency, consistent dopamine receptor engagement over 24 hours, and expected lower dose should allow LAI formulation of LB-102
    3. Potential additional novel IP
  2. Bipolar depression
    1. ~6.7M US patients
    2. Non-racemic amisulpride has shown efficacy in bipolar depression compared to placebo
    3. Amisulpride approved in Italy and other countries for dysthymia (low grade depression)
  3. Schizophrenia with predominantly negative symptoms
    1. ~1M US patients
    2. Among largest unmet needs in SCZ
    3. 2018 meta-analysis across 21 trials concluded that amisulpride is the only antipsychotic that outperformed placebo in the treatment of schizophrenia with predominantly negative symptoms