Unveiling the Influence of a High-Fat Meal on the Pharmacokinetics of Oral Globalagliatin, A Glucokinase Activator, in Healthy Chinese Volunteers

Globalagliatin is a novel glucokinase activator being developed to treat diabetes by helping maintain glucose homeostasis. This randomized, open-label, crossover Phase I trial in 24 healthy Chinese volunteers evaluated the effect of a high-fat meal on the single-dose pharmacokinetics and safety of oral globalagliatin, with plasma concentrations measured by LC-MS/MS and pharmacokinetic parameters derived using Phoenix WinNonlin. A high-fat meal increased Cmax, AUC0-t, and AUC0-inf by 25-35% compared with fasting conditions, and time to peak concentration was modestly delayed; globalagliatin showed favorable safety and tolerability under both conditions with no serious adverse events or hypoglycemia. The findings indicate that food intake increases globalagliatin exposure, information relevant to dosing recommendations for this investigational glucokinase activator.