预约演示
更新于：2025-02-09
Prusogliptin
普卢格列汀
更新于：2025-02-09
概要
基本信息
原研机构 |
在研机构 |
非在研机构 |
最高研发阶段批准上市 |
首次获批日期 中国 (2025-01-08), |
最高研发阶段(中国)批准上市 |
特殊审评特殊审批 (中国) |
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结构/序列
分子式C16H25FN4O2 |
InChIKeyVQKSCYBKUIDZEI-STQMWFEESA-N |
CAS号1186426-66-3 |
关联
27
项与 普卢格列汀 相关的临床试验NCT05150626
An Open-label, Randomized, Three-period, Crossover, Single-dose Study to Evaluate the Effect of a Low-fat Meal and a Standard Meal on the Pharmacokinetics of DBPR108 in Healthy Subjects
CTR20213110
在健康受试者中评价低脂餐和标准餐对DBPR108片药代动力学影响的单剂量、随机、开放、三序列、三周期、交叉临床研究
NCT05146869
A Randomized, Open-Label, Parallel-Cohort, Single-dose and Multiple-dose Phase I Study of DBPR108 Tablets in Type 2 Diabetes Mellitus Patients
100 项与 普卢格列汀 相关的临床结果
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100 项与 普卢格列汀 相关的转化医学
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100 项与 普卢格列汀 相关的专利（医药）
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8
项与 普卢格列汀 相关的文献（医药）2024-06-01EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Synthesis and clinical application of representative small-molecule dipeptidyl Peptidase-4 (DPP-4) inhibitors for the treatment of type 2 diabetes mellitus (T2DM)
Review
作者: Shao, Dong-Wei ; Zhao, Li-Jie ; Sun, Jin-Feng
Diabetes mellitus is a chronic metabolic disorder characterized by high blood glucose levels, which can cause many diseases, including osteoporosis, fractures, arthritis, and foot complications. The inhibitors of dipeptidyl peptidase-4 (DPP-4), an enzyme involved in glucose metabolism regulation, are essential for managing Type 2 Diabetes Mellitus (T2DM). The inhibition of DPP-4 has become a promising treatment approach for T2DM because it can increase levels of active glucagon-like peptide-1 (GLP-1), leading to improved insulin secretion in response to glucose and reduced release of glucagon. The review commences by elucidating the role of DPP-4 in glucose homeostasis and its significance in T2DM pathophysiology. Furthermore, it presents the mechanism of action, preclinical pharmacodynamics, clinical efficacy, and toxicity profiles of small-molecule DPP-4 inhibitors across various clinical stages. This comprehensive review provides valuable insights into the synthesis and clinical application of DPP-4 inhibitors, serving as an invaluable resource for researchers, clinicians, and pharmaceutical professionals interested in diabetes therapeutics and drug development.
2024-04-01Diabetes, obesity & metabolism
Prusogliptin (DBPR108 ) monotherapy in treatment‐naïve patients with type 2 diabetes: A randomized, double‐blind, active and placebo‐controlled, phase 3 study
Article
作者: Yao, Lingli ; Cao, Mengya ; Zhang, Cheng ; Zhou, Deai ; Wang, Wei ; Guo, Xiaohui ; Ning, Tao ; Ma, Guoqing ; Zhang, Tianhao ; Chen, Ling ; Yuan, Jing ; Jia, Rui ; Huang, Yanli
Abstract:
Aim:
This 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 Methods:
In 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.
Results:
In 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.
Conclusions:
DBPR108 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.
2024-02-01Current 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
作者: Zhang, Huiting ; Cai, Wen ; Zhang, Xueyuan ; Bian, Yicong ; Zhang, Hua ; Cui, Juanjuan ; Zhang, Xiaofang ; Miao, Liyan ; 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.
100 项与 普卢格列汀 相关的药物交易
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研发状态
批准上市
10 条最早获批的记录, 后查看更多信息
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| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| 2型糖尿病 | 中国 | 2025-01-08 |
未上市
10 条进展最快的记录, 后查看更多信息
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| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| 肾功能不全 | 临床1期 | 中国 | 2021-06-15 | |
| 肝病 | 临床1期 | 中国 | 2021-06-09 | |
| 糖尿病 | 临床1期 | 中国台湾 | 2012-11-22 |
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临床结果
临床结果
适应症
分期
评价
查看全部结果
临床3期 | 1,000 | Metformin+Prusogliptin | 鹹廠簾糧夢築願鏇顧鏇(壓網構繭網鏇遞構顧廠) = DBPR108片组显著优于安慰剂组 顧網壓廠衊構鹽齋窪膚 (衊襯憲網構簾願選鏇鏇 ) | 积极 | 2022-08-22 | ||
Metformin+Placebo | |||||||
临床2期 | 276 | 鹽膚衊窪餘簾齋網醖艱(糧糧簾願襯糧壓獵壓製) = 鬱蓋顧願鬱簾淵醖顧繭 鏇膚積蓋衊糧築鏇繭壓 (襯鬱築淵膚築簾顧糧選 ) 更多 | 积极 | 2020-07-01 | |||
鹽膚衊窪餘簾齋網醖艱(糧糧簾願襯糧壓獵壓製) = 構夢鏇窪範範襯鏇蓋壓 鏇膚積蓋衊糧築鏇繭壓 (襯鬱築淵膚築簾顧糧選 ) 更多 | |||||||
临床1期 | 32 | placebo+DBPR108 (Placebo) | 醖膚衊遞壓簾獵鑰醖範(淵觸蓋鹹顧簾膚繭願簾) = 鹽艱觸蓋餘糧遞願製繭 鹽夢簾窪鬱憲鏇憲襯範 (衊鬱鹹積襯鹽獵膚鹹廠, 齋廠憲網願膚鏇網願簾 ~ 願鹽鬱繭憲窪壓顧顧願) 更多 | - | 2014-08-28 | ||
(DBPR108 25 mg) | 醖膚衊遞壓簾獵鑰醖範(淵觸蓋鹹顧簾膚繭願簾) = 鹽襯範壓艱構選願鏇鹽 鹽夢簾窪鬱憲鏇憲襯範 (衊鬱鹹積襯鹽獵膚鹹廠, 簾網鹹憲壓鹹繭繭範夢 ~ 遞淵選膚構鹽餘膚簾網) 更多 |
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