Segal Trials Leads Phase 2 Schizophrenia Trial of LB-102 Toward Primary Endpoint

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LB-102, also known as N-Methylamisulpride, is an investigational drug being developed for the treatment of schizophrenia A. Its mechanism of action (MOA) involves acting as a dopamine D2 and D3 receptor antagonist, as well as a serotonin 5-HT2B and 5-HT7 receptor antagonist A.

By blocking these receptors, LB-102 helps to regulate neurotransmitter activity in the brain, which can help alleviate symptoms of schizophrenia A. It’s designed to have improved lipophilicity and blood-brain barrier permeability compared to amisulpride, potentially leading to better efficacy and fewer side effects A.

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Is it like brilaroxazine?

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It’s a methylated version of Amisulpride if I’m honest I’m not sure what advantage methylating the drug provides. Hold on I’ll look it up.

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N-Methylamisulpride (NMA), a derivative of amisulpride, offers some advantages over regular amisulpride due to its distinct pharmacological profile. Here are some key differences:

  1. Improved Blood-Brain Barrier Penetration:
    N-Methylamisulpride exhibits greater ability to cross the blood-brain barrier compared to amisulpride, which enhances its central nervous system (CNS) activity. This means it can achieve therapeutic effects at lower doses.
  2. Selective Dopamine Receptor Targeting:
    Both drugs act as dopamine D2/D3 receptor antagonists, but NMA may have a more favorable receptor binding profile, potentially contributing to enhanced efficacy and reduced side effects.
  3. Lower Risk of Prolactin Elevation:
    Amisulpride is associated with significant prolactin elevation, which can lead to side effects such as galactorrhea and sexual dysfunction. N-Methylamisulpride may have a lower tendency to increase prolactin levels, improving tolerability.
  4. Potentially Fewer Extrapyramidal Symptoms (EPS):
    By reducing off-target dopamine blockade in certain brain regions, NMA may carry a lower risk of motor side effects like EPS, which are common with antipsychotics.
  5. Faster Onset of Action:
    Due to better pharmacokinetic properties, NMA may act more quickly than amisulpride, which can be beneficial in acute psychiatric episodes.
  6. Improved Efficacy in Certain Disorders:
    N-Methylamisulpride has shown potential efficacy in conditions like depression and anxiety, in addition to psychosis. Some research suggests it may work better for mood symptoms compared to amisulpride.

These differences make N-Methylamisulpride an attractive alternative to amisulpride in some clinical settings. However, its use may depend on availability, cost, and specific patient needs.

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Could be wrong but I’d guess they can do this with every ap.

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Thanks for the information. I think there is not much difference in terms of the mechanism of action.

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Yeah, seems that way. I know I asked you this somewhat recently but did they conclude that evenamide trial near you? I wanna try that drug bad lol

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The trial with Evenamide has already ended. I will ask the doctor if I can participate in an individual trial when he comes back from vacation.

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Wow! I wish I had that option. I would do it. I know you struggle with aps but I think you’d be able to function on a minimal dose with evenamide.

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He told me that evenamide is taken as a supplement, it cannot be taken alone. That is why I refused to participate in the trial. I wish I could take it alone.