Population pharmacokinetics of efpeglenatide in individuals with obesity and with type 2 diabetes
Year: 2025
Type: article
Abstract: Background: Efpeglenatide (HM11260C) is a long-acting GLP-1 receptor agonist under development for obesity. A population pharmacokinetic (PK) analysis was conducted to characterize its PK properties and evaluate covariate effects to support clinical dosing strategies. Methods: Pooled PK data from six clinical studies in participants with type 2 diabetes or obesity were analyzed using nonlinear mixed-effects modeling (NONMEM). Covariate effects, model diagnostics, and simulations were used to assess exposure and dosing strategies. Results: A two-compartment model with dual absorption pathways adequately described the data. Body weight and disease status influenced absorption and clearance; however, predicted exposure differences across weight percentiles and demographic subgroups were modest and within conventional bioequivalence limits. Simulations suggested approximately dose-proportional increases across the evaluated dose range with once-weekly administration and supported the feasibility of stepwise dose-escalation. Conclusion: Efpeglenatide PK was well characterized across type 2 diabetes and obesity populations. Although some covariates affected PK parameters, their impact on exposure was not clinically meaningful. These results support a uniform dosing strategy without routine dose adjustment and provide quantitative evidence for stepwise dose escalation in ongoing clinical development for obesity.
Source: Frontiers in Pharmacology
Authors: Seungchan Choi, Jiyoung Seo, Suemin Park, Na Young Kim, Hyeeun Kim, Hyeong-Seok Lim
Language: English
Subfield: Endocrinology, Diabetes and Metabolism
Field: Medicine
Domain: Health Sciences
Open Access status: gold
Estimated APC paid: $3,801
OpenAlex ID: W4416840857