Pharmacokinetics, Pharmacodynamics, and Safety of Single-Dose Luseogliflozin (TS-071) in Japanese Children and Adolescents With Type 2 Diabetes: A Multicenter, Open-Label, Parallel-Group Phase 1 Study

Abstract

This study aimed to evaluate the pharmacokinetics, pharmacodynamics, and safety of a single dose of luseogliflozin (TS-071), a sodium–glucose cotransporter 2 (SGLT2) inhibitor, in Japanese children and adolescents with type 2 diabetes, with the goal of informing dose selection for future research. In this multicenter, open-label, parallel-group Phase 1 trial, patients aged 9-17 years received a single oral dose of luseogliflozin at 1.25, 2.5, or 5 mg. Pharmacokinetic and pharmacodynamic parameters were assessed and compared with existing adult data. In total, 19 patients completed the study. The mean age was 14.3 ± 1.9 years, and the mean body weight was 77.28 ± 25.32 kg. Plasma luseogliflozin concentrations increased in a dose-dependent manner. The maximum plasma concentration and the area under the curve were comparable to those observed in adults. Administration of luseogliflozin at all dose levels resulted in a substantial increase in urinary glucose excretion. No safety concerns emerged from the single-dose administration. Luseogliflozin demonstrated favorable pharmacokinetic, pharmacodynamic, and safety profiles in pediatric patients, consistent with adult findings. These results support the selection of 2.5- and 5-mg doses for a future Phase 3 pediatric study.