Company: LBRX
Filing Date: 2025-08-22
Form Type: S-1
Source: 0001193125-25-186467
Chunk: 192

Company: LB PHARMACEUTICALS INC
Filing Date: 2025-08-22
Form: S-1
Chunk 192
---
 of
the main factors that lead to high dosing of amisulpride, compared to other antipsychotic drugs, to achieve clinically meaningful BBB penetration. The recommended dose of amisulpride for acute schizophrenia ranges from 400 mg to 800 mg per day,
which may be increased up to 1,200 mg per day. By comparison, clinically effective doses of other antipsychotic drugs with similar affinities for dopamine receptors are often much lower (e.g., 1.5 mg of Vraylar and 4 mg of Rexulti).

The high doses of amisulpride increase systemic exposure to the drug, contribute to some of its side effects, and limit its ability to be
formulated into an LAI – there are currently no LAIs approved among the benzamide class of antipsychotics. Another drawback of amisulpride is that it is typically dosed twice-daily, which can lead to lower adherence relative to therapies with
less frequent dosing schedules. Lower adherence can, in turn, lead to less efficacy of a drug in treating schizophrenia which can result in relapses.

OurSolution: LB-102for the Treatment of Schizophrenia

LB-102Overview

LB-102 is a patented benzamide designed to improve upon the safety and efficacy of amisulpride. In
creating LB-102, we have added a methyl group to the chemical structure of amisulpride with the intention of improving its permeability of BBB while only minimally affecting receptor binding. We believe that
making this chemical change allows 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. This change to the chemical
structure also allows 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.

130

The following chart shows the molecular structures of amisulpride and LB-102.

LB-102is a methylated and patented derivative of amisulpride.

In Vitro Receptor Binding of LB-102

In vitro binding of LB-102 to target central nervous system, or CNS, receptors was found to be
similar to that of amisulpride. LB-102 bound most strongly to the dopamine Dand D receptors,
with a K of