Delving into the Latest Updates on Prusogliptin with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

普卢格列汀

Target

DPP-4

Mechanism

DPP-4 inhibitors(Dipeptidyl peptidase IV inhibitors)

Therapeutic Areas

Endocrinology and Metabolic Disease

Active Indication

Diabetes Mellitus, Type 2

Inactive Indication

Liver DiseasesRenal Insufficiency

Originator Organization

National Health Research Institutes

Active Organization

CSPC Ouyi Pharmaceutical Co., Ltd.

Inactive Organization

Genovate Biotechnology Co., Ltd.

CSPC Zhongqi Pharmaceutical Technology (Tianjin) Co., Ltd.National Health Research Institutes

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Drug Highest PhaseNDA/BLA

First Approval Date-

RegulationSpecial Review Project (CN)

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Structure

Molecular FormulaC16H25FN4O2

InChIKeyVQKSCYBKUIDZEI-STQMWFEESA-N

CAS Registry1186426-66-3

Primary objective: To evaluate the effects of low-fat and standard meals on the pharmacokinetics (PK) of a single oral dose of DBPR108 tablets in healthy subjects; Secondary objective: To evaluate the effects of low-fat and standard meals on the safety and tolerability of a single oral dose of DBPR108 tablets in healthy subjects.

Start Date25 May 2022

Sponsor / Collaborator

CSPC Zhongqi Pharmaceutical Technology Shijiazhuang Co., Ltd.

NCT05146869 / CompletedPhase 1

A Randomized, Open-Label, Parallel-Cohort, Single-dose and Multiple-dose Phase I Study of DBPR108 Tablets in Type 2 Diabetes Mellitus Patients

This is a phase I study to evaluate the safety, tolerability, pharmacokinetics, and pharmacodynamics of single-dose and multiple-dose of DBPR108 tablets in Type 2 Diabetes Mellitus Patients.

Start Date30 Dec 2021

Sponsor / Collaborator

CSPC Zhongqi Pharmaceutical Technology (Tianjin) Co., Ltd.

100 Clinical Results associated with Prusogliptin

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100 Translational Medicine associated with Prusogliptin

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100 Patents (Medical) associated with Prusogliptin

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5

Literatures (Medical) associated with Prusogliptin

01 Apr 2024·Diabetes, Obesity and Metabolism

Prusogliptin (DBPR108) monotherapy in treatment‐naïve patients with type 2 diabetes: A randomized, double‐blind, active and placebo‐controlled, phase 3 study

Article

Author: Guo, Xiaohui ; Wang, Wei ; Zhang, Tianhao ; Jia, Rui ; Chen, Ling ; Ning, Tao ; Ma, Guoqing ; Zhou, Deai ; Yuan, Jing ; Huang, Yanli ; Zhang, Cheng ; Yao, Lingli ; Cao, Mengya

AbstractAimThis study aimed to assess the efficacy and safety of prusogliptin (DBPR108), a novel and highly selective dipeptidyl peptidase‐4 inhibitor, in individuals with type 2 diabetes who had not been using glucose‐lowering agents regularly for the 8 weeks before the screening period.Materials and MethodsIn this multicentre, randomized, double‐blind, phase 3 study, adult patients with type 2 diabetes were randomly assigned to receive either DBPR108 100 mg, sitagliptin 100 mg, or placebo once daily during the initial 24‐week double‐blind treatment period, followed by a 28‐week open‐label extension period during which all patients received DBPR108 100 mg once daily. The primary endpoint was the mean change in glycated haemoglobin (HbA1c) levels from baseline to week 24.ResultsIn total, 766 patients were enrolled and received DBPR108 100 mg (n = 462), sitagliptin 100 mg (n = 152), or placebo (n = 152). The mean age of all patients was 54.3 ± 10.5 years, with 58% being men. The median duration of type 2 diabetes was 0.38 (0.02, 2.65) years, and the mean HbA1c (SD) at baseline was 7.94% (0.62), 7.88% (0.61) and 7.83% (0.59) for DBPR108, sitagliptin and placebo groups, respectively. At week 24, the least square mean (SE) changes from baseline in HbA1c were −0.63% (0.04%) for DBPR108, −0.60% (0.07%) for sitagliptin and −0.02% (0.07%) for placebo. The mean treatment difference between DBPR108 and placebo was −0.61% (95% CI –0.77% to −0.44%), and between DBPR108 and sitagliptin was −0.03% (95% CI –0.19% to 0.13%). These results indicate that DBPR108 was superior to placebo and non‐inferior to sitagliptin. DBPR108 also significantly reduced fasting and postprandial plasma glucose levels and had little effect on body weight. The mean (SD) changes in HbA1c from baseline to week 52 were −0.50% (0.97%) for the DBPR108 group, −0.46% (0.96%) for the sitagliptin group and −0.41% (0.95%) for the placebo group. The incidence of adverse events was comparable across all three groups.ConclusionsDBPR108 showed superiority to placebo and non‐inferiority to sitagliptin in terms of glycaemic control over the initial 24 weeks in treatment‐naïve patients with type 2 diabetes. Furthermore, its efficacy was sustained for up to 52 weeks.

01 Feb 2024·Current Drug Metabolism

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

Article

Author: Miao, Liyan ; Zhang, Hua ; Zhang, Xueyuan ; Bian, Yicong ; Zhang, Xiaofang ; Cai, Wen ; Zhang, Huiting ; Cui, Juanjuan ; Zhao, Weifeng

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.

01 Nov 2022·Diabetes, Obesity and Metabolism

Efficacy and safety of DBPR108 (prusogliptin) as an add‐on to metformin therapy in patients with type 2 diabetes: A 24‐week, multi‐centre, randomized, double‐blind, placebo‐controlled, superiority, phase III clinical trial

Article

Author: Ling, Hongwei ; Geng, Jianlin ; Zheng, Huiping ; Xu, Jianping ; Niu, Huikun ; Xiao, Xinhua ; Yuan, Jing ; Investigators ; Zhang, Tianhao ; Xie, Ying ; Huang, Yanli

AbstractAimTo evaluate the efficacy and safety of DBPR108 (prusogliptin), a novel dipeptidyl peptidase‐4 (DPP‐4) inhibitor, as an add‐on therapy in patients with type 2 diabetes (T2D) that is inadequately controlled with metformin.Materials and MethodsIn this 24‐week, multi‐centre, randomized, double‐blind, placebo‐controlled, superiority, phase III study, adult T2D patients with HbA1c levels ranging from 7.0% to 9.5% on stable metformin were enrolled and randomized (2:1) into the DBPR108 + metformin and placebo + metformin groups. The primary endpoint was the change from baseline in HbA1c at week 24 of DBPR108 versus placebo as an add‐on therapy to metformin.ResultsAt week 24, the least‐square mean (standard error) change from baseline in HbA1c was significantly greater in the DBPR108 group (−0.70% [0.09%]) than in the placebo group (−0.07% [0.11%]) (P < .001), with a treatment difference of −0.63% (95% confidence interval: −0.87%, −0.39%) on the full analysis set. A higher proportion of patients achieved an HbA1c of 6.5% or less (19.7% vs. 8.5%) and an HbA1c of 7.0% or less (50.0% vs. 21.1%) at week 24 in the DBPR108 + metformin group. Furthermore, add‐on DBPR108 produced greater reductions from baseline in fasting plasma glucose and 2‐hour postprandial plasma glucose without causing weight gain. The overall frequency of adverse events was similar between the two groups.ConclusionsDBPR108 as add‐on therapy to metformin offered a significant improvement in glycaemic control, was superior to metformin monotherapy (placebo) and was safe and well‐tolerated in patients with T2D that is inadequately controlled with metformin.

100 Deals associated with Prusogliptin

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R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Diabetes Mellitus, Type 2	NDA/BLA	CN	CSPC Ouyi Pharmaceutical Co., Ltd.	26 Apr 2023
Liver Diseases	Preclinical	CN	CSPC Zhongqi Pharmaceutical Technology Shijiazhuang Co., Ltd.	09 Jun 2021
Renal Insufficiency	Preclinical	CN	CSPC Zhongqi Pharmaceutical Technology Shijiazhuang Co., Ltd.	07 Jun 2021
Diabetes Mellitus	Preclinical	TW	Genovate Biotechnology Co., Ltd.	22 Nov 2012

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT04218734 (NEWS) Manual	Phase 3	Diabetes Mellitus, Type 2	1,000	Metformin+Prusogliptin	(ylpdilvyko) = DBPR108片组显著优于安慰剂组 kxyeankbaz (dlmhglygal )	Positive	22 Aug 2022
				Metformin+Placebo
NCT01650324 (CTgov)	Phase 1	Diabetes Mellitus, Type 2	32	placebo+DBPR108 (Placebo)	tmsdbvnulb(rvgufeihwh) = ncibfnyrqy imhrowlxll (ffzjgivonu, aikhjadydg - alaogfwelq) View more	-	28 Aug 2014
				DBPR108 (DBPR108 25 mg)	tmsdbvnulb(rvgufeihwh) = nzxksfsykx imhrowlxll (ffzjgivonu, kwjibrwxhg - alfeyybqoc) View more