Company: LBRX
Filing Date: 2025-08-22
Form Type: S-1
Source: 0001193125-25-186467
Chunk: 174

Company: LB PHARMACEUTICALS INC
Filing Date: 2025-08-22
Form: S-1
Chunk 174
---
 with Efficacious Data to Bolster Development for a Broad Range of Indications

LB-102 is a novel, patent-protected benzamide antipsychotic drug
that was designed using amisulpride as a starting point. Amisulpride is one of the most effective and commonly used antipsychotic drugs currently approved outside the United States. Amisulpride was ranked as the second most effective antipsychotic
drug in the 2019 Lancet meta-analysis of clinical trials on antipsychotic drugs. In this meta-analysis, amisulpride was ranked the most effective antipsychotic drug in treating positive symptoms and the third most effective in addressing negative
symptoms of schizophrenia. Despite amisulpride’s efficacy and tolerability profile, it has not received regulatory approval in the United States for the treatment of any neuropsychiatric disorders, including schizophrenia, because the
development and regulatory requirements of the FDA were incompatible with patent coverage on the drug.

The modifications we incorporated
into LB-102 were designed to improve the tolerability and efficacy profile of amisulpride by addressing its shortcomings, such as limited blood-brain barrier, or BBB, permeability and dosing frequency.
Enhanced BBB permeability was expected to improve the potency of the molecule with respect to dopamine receptor binding and enable the use of lower doses compared with amisulpride. The use of

114

lower doses was hypothesized to improve the tolerability profile. We also aimed to create a new chemical entity with strong composition of matter intellectual property protection. We believe that
the methylation of amisulpride addresses these design goals, and we aimed to demonstrate in our clinical trials that LB-102’s improved BBB penetration would confer benefits over amisulpride and other
antipsychotic drugs, including lower dosing levels, a wider therapeutic window, improved tolerability, and once-daily dosing. Use of lower doses may also improve the feasibility of developing an LAI formulation.

Because amisulpride was used as the starting point in the creation of LB-102, we have conducted
preclinical head-to-head studies with the compound to determine superiority as well as to assess whether the clinical development path of amisulpride may provide a
risk-mitigated path for our development of LB-102. We have not conducted head-to-head clinical trials to date comparing LB-102 to amisulpride; however, our head-to-head preclinical studies that compared amisulpride