Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of Multiple Ascending Doses and Dose Titration of Bexicaserin in Healthy Participants in a Randomized, Double-Blind, Placebo-Controlled Study.

ABSTRACT: Bexicaserin (LP352) is a selective superagonist of the 5-hydroxytryptamine 2C (5-HT_2C) receptor currently in development for the treatment of seizures that arise from developmental and epileptic encephalopathies. This phase 1, double-blind, placebo-controlled multiple ascending dose (MAD) study assessed the safety, tolerability, and pharmacokinetic profile of bexicaserin in healthy participants. Doses ranging from 3 to 24 mg three times daily (TID) were administered for up to 14 days. Serial blood and urine samples were collected to assess pharmacokinetics, and prolactin was assessed as a pharmacodynamic biomarker. Bexicaserin was generally safe and well-tolerated, rapidly absorbed, metabolized to three circulatory pharmacologically inactive metabolites, and had a median T_m

SUBMITTER: Williams J 

PROVIDER: S-EPMC12814314 | biostudies-literature | 2026 Jan

REPOSITORIES: biostudies-literature