LB-102 is a benzamide anti-psychotic based on amisulpride. Benzamide antipsychotics are available in many countries throughout the world and are widely used in the UK, Italy, Germany, and others.  Amisulpride is considered the most effective benzamide approved worldwide. There are numerous peer-reviewed papers published every year on data generated in patients treated with amisulpride. Given that LB-102 is very similar to other benzamides, these papers are useful to individuals who want to learn more about this class of drugs.

Amisulpride, aripiprazole, and olanzapine in patients with
schizophrenia-spectrum disorders (BeSt InTro): a pragmatic,
rater-blind, semi-randomised trial

Published in The Lancet Psychiatry November 2020, this paper compared the safety and efficacy of amisulpride, olanzapine and aripriprazole in 144 randomized patients over 52 weeks.

Amisulpride alleviates chronic mild stress-induced cognitive deficits: Role of pre-frontal cortex microglia and Wnt/β-catenin pathway

 

Published in the European Journal of Pharmacology in August 2020 presents a deep dive into the well-known characteristic of amisulpride to treat depression and improve cognitive defects

Comparative efficacy and tolerability of 32 oral antipsychotics for the acute treatment of adults with multi-episode schizophrenia: a systematic review and network meta-analysis

 

Published in Lancet July 2019, this paper compared the efficacy and tolerability of 32 antipsychotics and showed that amisulpride was one of the most effective and best tolerated drugs with strong efficacy in the treatment of negative symptoms of schizophrenia.

Amisulpride and Olanzapine Followed by Open-Label Treatment With Clozapine in First-Episode Schizophrenia (OPTiMiSE)

 

Patients in the OPTiMiSE study received 4 weeks of open label amisulpride and those who did not achieve remission at 4 weeks were randomized to continue amisulpride or switched to olanzapine. In the open label phase I, 56% of patients on amisulpride achieved remission and 45% of phase II patients achieved remission on continued amisulpride vs 44% for olanzapine.

Clozapine Combination and Augmentation Strategies in Patients With Schizophrenia -Recommendations From an International Expert Survey Among the Treatment Response and Resistance in Psychosis (TRRIP) Working Group

 

Published in Schizophrenia Bulletin May 2020.  An international panel of experts recently recommended amisulpride as a potential adjunct to clozapine for the treatment of Clozapine Resistant Schizophrenia.

Building a translational bridge from animals to man for clinical candidate LB-102, a next-generation benzamide antipsychotic

 

Data presented at ECNP 2019 (Copenhagen) for LB-102.

Antipsychotic Benzamides Amisulpride and LB-102 Display Polypharmacy as Racemates, S Enantiomers Engage Receptors D2 and D3, while R Enantiomers Engage 5-HT7

 

Published in ACS Omega August 2019.  LB-102 antipsychotic activity is provided by targeting D2/3 receptors with the S enantiomer, while antidepressant effects are provided by targeting the 5-HT7 receptor with the R enantiomer. Based on the findings in this report, racemic LB-102 will be advanced to the clinic rather than the enantiomerically pure S LB-103.

Antipsychotic treatment of very late-onset schizophrenia-like psychosis (ATLAS): a randomised, controlled, double-blind trial

 

Published in Lancet Psychiatry in June of 2018, the ATLAS Study showed that low-dose amisulpride is effective and well-tolerated in a population of elderly (average age of 80) schizophrenia patients.

LB-102, Potential Schizophrenia Treatment, Displays Polypharmacology as a Racemate—S Enantiomer Binds D2 Receptors and R Binds 5-HT7 Receptor

 

Data presented at ECNP 2018 (Barcelona) for LB-102.

Establishing a PK-PD-E Relationship for Clinical Candidate LB-102, a Next-Generation Benzamide Antipsychotic

 

Data presented at SOBP 2018 ( New York City) for LB-102.

Pre-clinical evaluation of two novel benzamides, LB-102 and 103, for the treatment of schizophrenia

 

Data presented at ECNP 2017 (Paris) for LB-102.

Recovery in the outpatient setting: 36-month results from the Schizophrenia Outpatients Health Outcomes (SOHO) study

 

The Schizophrenia Outpatient Health Outcome Study (SOHO) showed that amisulpride was comparable to other well-known antipsychotics in recovery, remission, adequate quality of life and other important measures.

Effectiveness of antipsychotics in first-episode schizophrenia…

 

The European First Episode Schizophrenia Trial (EUFEST) enrolled a large number of patients having their first treatment with an antipsychotic. Antipsychotic naïve patients are often more sensitive to the side effects of these drugs and amisulpride was one of the best tolerated drugs in the study and had higher rates of remission than several other widely used drugs.

Comparative efficacy and tolerability of 15 antipsychotic drugs in schizophrenia: a multiple-treatments meta-analysis

 

Published in Lancet in September 2013, this paper compared the efficacy and tolerability of 15 antipsychotics and showed that amisulpride was one of the most effective and best tolerated drugs with low incidence of sedation and weight gain.

Effectiveness of sulpiride in adult patients with schizophrenia

 

In this study sulpiride patients stayed on their drug longer than haloperidol, risperidone, or olanzapine. Persistence on treatment was used as a marker for both tolerability and efficacy in this study conducted in Taiwan.

Randomized controlled trial of the effect on Quality of Life of second- vs first-generation antipsychotic drugs in schizophrenia

 

The CUtLASS (Cost Utility of the Latest Antipsychotics in Schizophrenia Study) study conducted in the UK allowed for patients to be randomized to either a 1st or 2nd generation antipsychotic. Sulpiride was included in the 1st generation arm while amisulpride was included in the second generation arm. Both drugs were well tolerated and interestingly, the 1st generation antipsychotic outperformed the 2nd generation arm possibly due to the fact that sulpiride was the most widely used drug in the 1st generation arm.

Improvement of schizophrenic patients with primary negative symptoms treated with amisulpride.

 

Several well controlled trials have found amisulpride to be useful for the predominantly negative subtype of schizophrenia characterized by social withdrawal and depressive symptoms. Amisulpride is the only antipsychotic with an approved label to address either primary or secondary negative symptoms at this time. This study found low dose amisulpride to be effective in treating predominantly negative schizophrenia.

Comparative effect of antipsychotics on risk of self-harm among patients with schizophrenia.

 

People with schizophrenia often try to harm themselves in various manners including suicide attempts. This paper looked at data on self-harm and found that amisulpride treated patients had lower rates of self-harm than patients treated with other well-known antipsychotics. As expected, clozapine patients had the lowest rates of self-harm. Sulpiride treated patients had rates of self-harm comparable to risperidone and olanzapine.

A double-blind, randomised comparative trial of amisulpride versus olanzapine in the treatment of schizophrenia: short-term results at two months.

 

Olanzapine is often considered a gold standard antipsychotic along with risperidone and clozapine. In this 2 month head to head comparison of amisulpride and olanzapine there were no differences in efficacy measures and patients on amisulpride gained significantly less weight.

Amisulpride versus fluoxetine in patients with dysthymia or major depression in partial remission: a double-blind, comparative study.

 

Many atypical antipsychotics are approved for use in depression. Amisulpride has been shown to have antidepressant effects and is used for a depressive illness called dysthymia throughout the world. Amisulpride is a 5HT-7 antagonist and also facilitates dopaminergic transmission at low doses. This study found that low dose amisulpride was as effective as fluoxetine in dysthymia and was well tolerated.

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