1983-LB: A Phase 1 Study of ID110521156, a Small Molecule Glucagon-Like Peptide 1 Receptor Agonist, in Healthy Subjects
Abstract
Introduction and Objective: Glucagon-like peptide-1 receptor agonists (GLP-1RAs) have emerged as effective therapeutic strategies for type 2 diabetes mellitus and obesity. To address the limitations of peptide-based GLP-1RAs, we developed ID110521156, a novel small-molecule GLP-1RA. In nonclinical studies, ID110521156 exhibited favorable pharmacokinetic property for oral administration and potent glucose-lowering efficacy with wide safety margin. Based on these findings, a first-in-human study was initiated in the Republic of Korea [NCT06063291].
Methods: A randomized, double-blind, placebo-controlled, single-ascending dose (SAD) study was conducted in healthy subjects to evaluate the safety, tolerability, and pharmacokinetics of ID110521156. Eligible subjects in the SAD cohorts (total 24, N=8/cohort) were randomly assigned to receive a single oral dose of ID110521156 or placebo in a 6:2 ratio. Additionally, a food effect study was performed in a separate cohort (N=12) using a randomized, two-sequence, crossover design to assess the effect of food on the pharmacokinetics of ID110521156.
Results: During dose escalation, systemic exposures (AUClast ) increased in a dose-proportional manner with a 95% confidence interval of 0.0623-1.0219 for the slope of the regression line. A total of 32 treatment emergent adverse events (TEAEs) were reported by 14 subjects in the SAD cohorts. Commonly reported TEAEs were gastrointestinal-related, including nausea and vomiting. No serious…
How strong is the evidence?
Evidence Hub reads this as a randomized trial, done in people. Its evidence level is 3 of 5 (Moderate · trial / cohort / secondary analysis). Trials without a large randomized design, cohorts and secondary analyses give moderate evidence. Reported size: 14 participants or records.
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