Phase 1, open-label, randomized study of the elecoglipron pharmacokinetic profile in healthy participants under fed and fasted conditions.

Abstract

Aims: Elecoglipron (AZD5004/ECC5004) is an oral small-molecule glucagon-like peptide-1 receptor agonist (GLP-1 RA) in development for weight management in people living with obesity or overweight and type 2 diabetes. This study aimed to characterize the pharmacokinetics (PK) profiles of two formulations of elecoglipron under fed and fasted conditions.

Methods: We assessed the PK profiles, safety and tolerability of two formulations of elecoglipron, 50 mg, under fed and fasted conditions in healthy participants in a phase 1, open-label, randomized, single-dose, fixed-sequence, crossover study.

Results: Of 23 participants screened, 14 were randomized to elecoglipron and 13 (92.9%) completed the study. The half-life for both formulations under fasted and fed conditions ranged between 20.7 and 21.2 h. Between the fed (reference) and fasted groups, geometric mean ratios (GMR) and 90% confidence intervals (CI) for the F1 formulation: area under the plasma-concentration curve (AUC) from time zero to the last measurement (AUC_0-last) was 0.96 (0.82, 1.12), AUC from time zero extrapolated to infinity (AUC_0-inf) was 0.95 (0.82, 1.11), and maximum plasma concentration (C_max) was 1.15 (0.90, 1.46). Similar results were observed for F2 in the fed and fasted groups. Safety and tolerability were comparable for the two formulations. The most common AEs were gastrointestinal (nausea, vomiting, dyspepsia, abdominal discomfort) and mostly mild in severity.

Conclusions: Elecoglipron demonstrated a PK profile supportive of once-daily dosing and may be administered under fed or fasted conditions. These findings support the continuing clinical development of elecoglipron. The trial is registered at ClinicalTrials.gov (NCT06268145). The trial was first registered on 20 February 2024.