Title:A Phase I Clinical Study of the Pharmacokinetics and Safety of Prusogliptin
Tablets in Subjects with Mild to Moderate Hepatic Insufficiency and Normal
Liver Function
Volume: 25
Issue: 2
Author(s): Huiting Zhang, Yicong Bian, Weifeng Zhao*, Liyan Miao*, Hua Zhang*, Juanjuan Cui, Xiaofang Zhang, Xueyuan Zhang and Wen Cai
Affiliation:
- Department of Infectious Diseases, the First Affiliated Hospital of Soochow University, Suzhou, China
- Institute for Interdisciplinary Drug Research and Translational
Sciences, the First Affiliated Hospital of Soochow University, Suzhou, China
- Department of Pharmacy,
the First Affiliated Hospital of Soochow University, Suzhou, China
Keywords:
Prusogliptin, DPP-4 inhibitor, hepatic impairment, phase I clinical study, pharmacokinetics, liver.
Abstract:
Background: Prusogliptin is a potent and selective DPP-4 inhibitor. In different animal models, Prusogliptin
showed potential efficacy in the treatment of type 2 diabetes. However, the knowledge of its pharmacokinetics
and safety in patients with liver dysfunction is limited.
Objectives: The present study evaluated the pharmacokinetics and safety of Prusogliptin in subjects with mild
or moderate hepatic impairment compared with healthy subjects.
Methods: According to the liver function of the subjects, we divided them into a mild liver dysfunction group,
a moderate liver dysfunction group and a normal liver function group. All subjects in three groups received a
single oral dose of Prusogliptin 100-mg tablets. Pharmacokinetics and safety index collection was carried out
before and after taking the drug. Plasma pharmacokinetics of Prusogliptin were evaluated, and geometric least-
-squares mean (GLSM) and associated 90% confidence intervals for insufficient groups versus the control
group were calculated for plasma exposures.
Results: After a single oral administration of 100 mg of Prusogliptin tablets, the exposure level of Prusogliptin
in subjects with mild liver dysfunction was slightly higher than that in healthy subjects. The exposure level of
Prusogliptin was significantly increased in subjects with moderate liver dysfunction. There were no adverse
events in this study.
Conclusion: The exposure level of Prusogliptin in subjects with liver dysfunction was higher than that in
healthy subjects. No participant was observed of adverse events. Prusogliptin tablets were safe and well tolerated
in Chinese subjects with mild to moderate liver dysfunction and normal liver function.
