- 2025-04-19
- Clinical pharmacokinetics 64(5)
- Wenfang Liu
- Kexu Yang
- Yang Lin
- Chunyan Lu
- Jingyi Liu
- Huan Zhou
- Juan Wang
- Tianhao Zhang
- Lingli Yao
- Huanhuan Qi
- Xiaofang Zhang
- Rui Jia
- Xiaoli Li
- Shan Jing
Study Design
- Type
- Randomized Controlled Trial (RCT)
- Sample size
- n = 30
- Population
- Chinese adults with type 2 diabetes, glycated hemoglobin of 7.0-9.5%, and body mass index of 19-35 kg/m^2
- Methods
- Randomized, parallel-group, open-label, phase I study, once-daily DBPR108 50-, 100-, or 200-mg tablet groups
- Blinding
- Open-label
- Funding
- Unclear
Background and objective
DBPR108 (prusogliptin) is a novel, orally bioavailable dipeptidyl peptidase-4 (DPP-4) inhibitor. This study investigated the pharmacokinetics and pharmacodynamic characteristics of DBPR108 tablets in patients with type 2 diabetes.Methods
In this randomized, parallel-group, open-label, phase I study, Chinese adults with type 2 diabetes, glycated hemoglobin of 7.0-9.5%, and body mass index of 19-35 kg/m2 were randomized 1:1:1 to once-daily DBPR108 50-, 100-, or 200-mg tablet groups. The primary endpoints included pharmacokinetic and pharmacodynamic characteristics after a single dose and multiple doses of DBPR108.Results
In total, 30 patients were randomized with 10 patients in each group. DBPR108 was quickly absorbed with median time to reach the maximum plasma concentration of 1.5-4 h at steady state. Exposure to DBPR108 at steady-state increased dose proportionally with mean maximum steady-state plasma DBPR108 concentration during dosage intervals of 119, 256, and 567 ng/mL in the 50-, 100-, and 200-mg groups, respectively. Accumulation ratio of DBPR108 ranged from 0.85 to 1.3, and steady state was reached after four continuous daily doses. After multiple doses of DBPR108, maximum inhibitory efficacy of DPP-4 increased with higher dose levels ranging from 62.1 to 89.4%. Active glucagon-like peptide-1 levels increased after DBPR108 administration. In addition, six patients experienced treatment-emergent adverse events without leading to treatment interruption or discontinuation.Conclusions
DBPR108 was well tolerated in Chinese patients with type 2 diabetes, and both the pharmacokinetic and pharmacodynamic profiles support once-daily dosage regimens of DBPR108 in future studies.Trial registration
ClinicalTrials.gov (NCT05146869); registered 23 November 2021.