LB Pharmaceuticals is a development stage life sciences company devoted to commercializing novel and improved versions of successful CNS treatments used extensively overseas but never developed, approved, or marketed in the United States. We believe that there are a number of ‘gold standard’ CNS therapies with excellent safety and efficacy profiles that, for various financial reasons, have never become FDA approved.

Our approach is to create a research-focused organization dedicated to generating novel intellectual property around improved versions of these former best-selling drugs. We have a low-risk, high-reward drug development business plan: invest in bringing to the US market patented, branded, first-to-market versions of standard-of-care CNS therapies currently in use worldwide. 

LB-102. LB’s lead asset, LB-102, is a novel (patented) analog of amisulpride, a drug used in Europe for decades to treat schizophrenia and low-grade depression.  LB-102 is a (low single digit nM) dopamine D2/3 and a (mid teens nM) 5-HT7 antagonist.  By methylating amisulpride we’ve designed a molecule that possesses the same key receptor binding properties while becoming more lipophilic.  In preclinical studies (ECNP 2017 ref) LB-102 was determined to be equivalent to amisulpride in: receptor binding and rodent PK profiles, and equivalent to or better than amisulpride in animal behavioral models of schizophrenia.

In a Phase 1 study, (ClinicalTrials# NCT04588129) LB-102 showed higher than expected plasma concentration compared to amisulpride and elicited EPS, a biomarker of > 80% dopamine receptor occupancy (mode of action), at substantially lower than expected doses (ECNP 2020).  A PET clinical study in humans is expected to begin dosing in Q4 2020 and a n ~300, double-blind, placebo-controlled, Phase 2 clinical study in schizophrenia patients is planned for mid 2021.

 

LB-102 LAI. Long acting injectable (LAI) medications offer several advantages, in particular in treatment compliance, for schizophrenia patients and are increasingly favored by psychiatrists.  Amisulpride is typically dosed between 400 and 800 mg per day, amounts that are too great to incorporate into a LAI formulation and be effective for more than a week.  A consequence of the potentially lower effective dose of LB-102 is that it may be feasible to generate a LAI that would be effective for a month of longer.  Work is currently underway to determine the feasibility of a LAI formulation of LB-102.

 

LB-104. LB-104 is the single R enantiomer of LB-102 (a racemic mixture).  In receptor binding studies (ECNP 2018 and ACS Omega) it was determined that LB-104 bound the 5-HT7 receptor 1000X more strongly than the S enantiomer (which binds the dopamine D2/3 receptors more strongly).  The 5-HT7 receptor has been implicated in treatment of depression (Psychopharmacology (Berl.) 2009) and may explain amisulpride’s known activity in treating negative symptoms of schizophrenia (Lancet 2019 and Am J Psychiatry 1999) as well as its efficacy in treating depression itself (J Affect Disorders 1998). Using LB-104 could allow more effective binding of the 5-HT7 receptor without the associated dopamine binding that can cause undesirable extrapyramidal symptoms.  Preclinical studies in rodents are underway to determine the utility of LB-104 to treat depression.

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