Safety, Tolerability, Pharmacokinetics, Pharmacodynamics, and Food Effect of Bexicaserin in Healthy Participants: A First-in-Human Randomized, Double-Blind, Placebo-Controlled Single Ascending Dose Escalation Phase 1 Study.

ABSTRACT: Bexicaserin (LP352) is a selective 5-hydroxytryptamine 2C (5-HT_2C) superagonist in development for the treatment of seizures in developmental and epileptic encephalopathies (DEEs). This double-blind, placebo-controlled, single ascending dose (SAD) Phase 1 study aimed to assess the safety, tolerability, and pharmacokinetic (PK) and pharmacodynamic (PD) profiles of single oral doses of bexicaserin and determine any relevant food effects. Forty healthy adult females were randomized to six treatment groups (1, 3, 6, 12, and 24 mg fasted; 6 mg fed) or placebo. Bexicaserin was generally safe and well tolerated: treatment-related adverse events were mild to moderate. Bexicaserin was rapidly absorbed into circulation (median T_max 1.02-1.54 h), with a mean terminal elimination

SUBMITTER: Chan R 

PROVIDER: S-EPMC12814313 | biostudies-literature | 2026 Jan

REPOSITORIES: biostudies-literature