PET clinical study of novel antipsychotic LB-102 demonstrates unexpectedly prolonged dopamine receptor target engagement.

ABSTRACT: Regulation of dopamine activity has important clinical consequences, most notably in schizophrenia. LB-102, N-methyl amisulpride, is a novel dopamine D_2/3/5-HT₇ inhibitor being developed as a treatment for schizophrenia and other psychiatric disorders. The characteristic that is common to all current antipsychotics is their engagement of D₂ dopamine receptors. The goal of this study was to measure the dopamine receptor occupancy of orally administered LB-102 at three different doses (50, 75, and 100 mg as single doses and 50 and 100 mg as multiple doses) and at different timepoints in healthy volunteers using positron emission tomography (PET) with ¹¹C raclopride as a radiotracer. Results of this study (NCT04588129) showed that steady-state once

SUBMITTER: Wong DF 

PROVIDER: S-EPMC11632090 | biostudies-literature | 2024 Dec

REPOSITORIES: biostudies-literature