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, designed to be 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, 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 lower than expected doses. A PET study in humans is expected to begin dosing in Q4.

Molecule
Preclinical
Phase 1
Phase 2
Phase 3
KarXT
Schizophrenia
LB-102
Schizophrenia
LB-102 LAI
Depression
LB-104
*Preclinically, LB is working on development of a long-acting form of LB-102 (impossible with amisulpride due to dose used) as well as LB-104 as a potential treatment for depression.

Publications

ACNP 2021 American College of Neuropsychopharmacology Poster – “PET clinical study of novel antipsychotic LB-102 demonstrates unexpectedly prolonged dopamine receptor engagement”

ECNP 2021 European College of Neuropsychopharmacology Poster – “LB-102 displays superior dopamine receptor occupancy compared to amisulpride in mouse and human PET studies”

ECNP 2020 European College of Neuropsychopharmacology Poster – “Safety, pharmacokinetics, and pharmacodynamics of LB-102, a selective D2/5-HT7 antagonist, in healthy volunteers”

ECNP 2019 European College of Neuropsychopharmacology Poster – “Building a translational bridge from animals to man for clinical candidate LB-102, a next-generation benzamide antipsychotic”

ACS Omega 2019 Peer-reviewed Publication – Antipsychotic Benzamides Amisulpride and LB-102 Display Polypharmacy as Racemates, S Enantiomers Engage Receptors D2 and D3, while R Enantiomers Engage 5‑HT7

ECNP 2018 European College of Neuropsychopharmacology Poster –LB-102, Potential Schizophrenia Treatment, Displays Polypharmacology as a Racemate—S Enantiomer Binds D2 Receptors and R Binds 5-HT7Receptor”

SOBP May 2018 Society of Biological Psychiatry Poster – “Establishing a PK-PD-E Relationship for Clinical Candidate LB-102, a Next-Generation Benzamide Antipsychotic”

ECNP Sept 2017  European College of Neuropsychopharmacology Poster – “Pre-clinical Evaluation of Two Novel Benzamides LB-102 and 103 for the Treatment of Schizophrenia”