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

This is an open-label, randomized, three-period, crossover, single-dose study to evaluate the effects of a low-fat meal and a standard meal on the pharmacokinetics of DBPR108 and the safety and tolerability of DBPR108 under different fed states in healthy adult subjects.

开始日期2022-05-29

申办/合作机构

石药集团中奇制药技术（天津）有限公司

NCT05146869

/ Completed临床1期

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.

开始日期2021-12-30

申办/合作机构

石药集团中奇制药技术（天津）有限公司

NCT05072028

/ Completed临床1期

A Clinical Study to Evaluate the Absorption, Metabolism, and Excretion of [14C]DBPR108 in Chinese Healthy Adult Male Subjects- Mass Balance and Biotransformation Study of [14C]DBPR108 in Human

This is a single-center, open-label phase I clinical study to evaluate the mass balance and biotransformation pathways of [14C]DBPR108 in Chinese healthy adult male subjects, to reveal the overall pharmacokinetic characteristics of DBPR108 in human body, and to provide a reference for the rational administration.

开始日期2021-11-16

申办/合作机构

石药集团中奇制药技术（天津）有限公司

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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项与普卢格列汀相关的文献（医药）

2025-05-01·CLINICAL PHARMACOKINETICS

Pharmacokinetics and Pharmacodynamics of Prusogliptin (DBPR108), a Once-Daily Dipeptidyl Peptidase-4 Inhibitor, in Patients with Type 2 Diabetes

Article

作者: Yao, Lingli ; Wang, Juan ; Lin, Yang ; Li, Xiaoli ; Yang, Kexu ; Qi, Huanhuan ; Jing, Shan ; Jia, Rui ; Zhou, Huan ; Liu, Wenfang ; Zhang, Tianhao ; Zhang, Xiaofang ; Lu, Chunyan ; Liu, Jingyi

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.

2024-06-01·EUROPEAN 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.

2024-04-01·Diabetes, 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 ; Wang, Wei ; Zhou, Deai ; 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.

项与普卢格列汀相关的新闻（医药）

2025-04-25

·石药集团

石药集团1类创新药普卢格列汀上市会隆重召开，引领多重用药安全变革

4月20日，石药集团普卢格列汀片（商标名：善泽平®）上市会在湖南长沙隆重召开，业内多位权威专家及学者展开专业探讨，会议现场吸引了众多临床一线工作者的广泛参与。上市会伊始，石药集团执行总裁王振国先生发表致辞，对莅临上市会的各位专家学者及临床医务工作者表示热烈欢迎和诚挚问候。他表示，普卢格列汀是石药集团在糖尿病领域上市的第一个1类创新药；未来，石药集团将以普卢格列汀为起点，全面布局糖尿病产品管线。作为我国自主研发的新一代DPP-4抑制剂，普卢格列汀在化学结构中引入氟原子，显著提高活性与选择性，从而实现对DPP-4表现出高选择性和强抑制性1。在中国开展的两项多中心III期临床试验（普卢格列汀单药III期试验、普卢格列汀联合二甲双胍III期试验）均取得积极结果，充分展现了普卢格列汀优异的降糖疗效和良好的安全性2,3，尤其在T2DM患者多重用药管理中具有独特优势。普卢格列汀在中国的成功上市为糖尿病治疗领域注入全新动力，也标志着国内广大T2DM患者迎来了有效、安全的治疗新选择，普卢格列汀临床应用前景可期！普卢格列汀如何破解多重用药困局T2DM管理调挑战升级：多重用药显著增加药物相互作用风险（DDI）中国糖尿病患病率仍在持续攀升，预计2050年中国患病人群将达到1.68亿4。从治疗现状来看，糖尿病的生理机制复杂，不论是“早期联合”还是“阶梯治疗”，采用不同作用机制的药物联合治疗已成为血糖控制的必经之路。然而，目前更为棘手的是，作为糖尿病的高发人群，老年患者往往多病共存，多重用药现象日益普遍。除多种降糖药外，许多患者还需要接受降压药、调脂药、抗血小板药等治疗5-8。据统计，64%的老年T2DM患者需同时使用5种以上药物9。北京协和医院肖新华教授强调，多重用药致使DDI风险显著增加，这给T2DM综合管理带来新的挑战，因为DDI不仅对血糖控制产生不利影响，还可能增加患者住院甚至死亡风险，进一步加重患者负担10-12。DPP4抑制剂新成员——普卢格列汀：多重用药患者的安全新选择面对这一严峻的临床挑战，新型DPP-4抑制剂普卢格列汀通过优化代谢途径，提供了有效解决方案。DPP-4抑制剂具有低血糖发生率低、体重影响中性、胃肠道反应少等特点，已成为老年糖尿病患者的一线用药13。目前国内已有多种DPP-4抑制剂类药物上市，虽然机制相同，但不同药物的代谢途径并不相同。CYP450酶、P糖蛋白（P-pg）是介导代谢性DDI发生的两大主要途径14，普卢格列汀的优势之一在于其不经过CYP450酶代谢，且非P-pg底物，因此DDI风险更小1。并且，普卢格列汀不与格列本脲及临床常用心血管药物（包括缬沙坦、辛伐他汀、华法林、地高辛）发生相互作用，联用时普卢格列汀及上述药物均不需要调整剂量1。因此，普卢格列汀的上市为多重用药患者提供了一种安全、便捷的治疗新选择。从降糖效果来看，由北京大学第一医院郭晓蕙教授牵头的普卢格列汀单药治疗未经治疗的T2DM患者的III期研究显示，普卢格列汀100mg QD治疗24周后，糖化血红蛋白（HbA1c）水平显著降低，降幅达0.61%（去除安慰剂效应，p<0.001)，48%的患者血糖达标（HbA1c≤7%），患者空腹血糖（FPG）和餐后2h血糖（2h-PPG）也实现有效改善2。图1.T2DM患者应用善泽平100mg QD治疗24周后HbA1c的变化另一项普卢格列汀联合二甲双胍治疗T2DM患者的III期研究由北京协和医院肖新华教授牵头，在中国30个中心进行。结果显示，普卢格列汀100mg QD+二甲双胍治疗24周后，HbA1c水平降幅达0.63%（去除安慰剂效应，p<0.001)， 50.0%的患者血糖达标（HbA1c≤7%）， FPG和2h-PPG也均明显降低3。图2.T2DM患者应用善泽平100mg QD+二甲双胍治疗24周后HbA1c的变化普卢格列汀降糖疗效确切，低血糖发生率低2,3，能够满足患者长期用药需求，尤其有助于多重用药患者实现更佳的治疗体验。结语普卢格列汀作为国家“重大新药创制”专项成果，其上市不仅是中国糖尿病创新药物研发的又一里程碑，也标志着我国糖尿病药物研发迈入新的国际前沿。其通过优化化学结构和代谢途径，显著提高药物活性及选择性，并减轻糖尿病患者多重用药风险，使患者合并用药更安心、临床治疗更便捷。未来，普卢格列汀的广泛应用将进一步丰富糖尿病治疗手段，助力患者实现更好、更安全的长期血糖管理。参考文献：1.普卢格列汀研究者手册2.Wang W, et al. Diabetes Obes Metab. 2024 Apr;26(4):1321-1332.3.Xu J, et al. Diabetes Obes Metab. 2022 Nov;24(11):2232-2240.4.International Diabetes Federation. (2025). IDF diabetes atlas (11th ed.).5.国家重点研发项目(2018YFC2002400)课题组.高龄老年共病患者多重用药安全性管理专家共识[J].中华保健医学杂志,2021,23(05):548-554.6.殷立新,张立辉.特殊人群用药指导丛书:老年人用药指导[M].北京:人民卫生出版社，2012.7.陶立群.我国老年慢性病现状及发展趋势[J].老龄问题研究,2006(3):17-29.8.沈杰,等.老年人多重用药评估与管理中国专家共识(2024)[J].中华老年医学杂志, 2024, 43(03):269-278.9.Remelli F, et al. 2022 Sep;34(9):1969-1983.10.Hammad MA, et al. J Pharm Bioallied Sci 2017.9(4): p. 221-22811.Cai R, et al. Artif Intell Med 2017,76:7-15.12.Moura CS, et al. J Pharm Pharm Sci 2009,12(3):266-272.13.国家老年医学中心,中华医学会老年医学分会,中国老年保健协会糖尿病专业委员会.中国老年糖尿病诊疗指南(2024版)[J].中华糖尿病杂志, 2024, 16(02):147-189.14.王崇,刘克辛.外排型转运体与CYP450酶所介导的药物相互作用[J].药学学报, 2014, 49(5):6.【声明】1、本新闻旨在分享研究成果，非广告用途；2、本资料仅供医药专业人士参考，非产品推荐依据，也不应被视为诊疗建议。

临床3期申请上市

2025-04-23

·Pharma CMC

石药集团「普卢格列汀二甲双胍缓释片」获批临床

4月22日，石药集团发布公告，集团开发的普卢格列汀二甲双胍缓释片获得国家药监局批准，可在中国开展临床试验。该产品为全球首款获批临床的由普卢格列汀和盐酸二甲双胍组成的新复方制剂。普卢格列汀为二肽基肽酶-4（DPP-4）抑制剂，通过抑制DPP-4，使内源性活性胰高血糖素样肽-1(GLP-1)水平升高，从而增强β细胞和α细胞对葡萄糖的敏感性，增加葡萄糖刺激的胰岛素分泌，并增强葡萄糖对胰高血糖素分泌的抑制作用，进而改善高血糖。二甲双胍是一种双胍类药物，可改善2型糖尿病患者糖耐量，并降低基础血糖和餐后血糖。本次获批的临床适应症为配合饮食和运动治疗，用于二甲双胍单药治疗控制不佳或正在接受普卢格列汀与二甲双胍联合治疗的成人2型糖尿病患者。与单药治疗2型糖尿病的产品相比，该产品安全性和耐受性良好，具有较高的临床开发价值。

临床结果上市批准临床申请CSCO会议

2025-04-23

·石药集团

石药集团普卢格列汀二甲双胍缓释片获临床试验批准

4月22日，石药集团（1093.HK）宣布，本集团开发的普卢格列汀二甲双胍缓释片（下称：该产品）已获中华人民共和国国家药品监督管理局批准，可在中国开展临床试验。该产品为全球首款获批临床的由普卢格列汀和盐酸二甲双胍组成的新复方制剂。普卢格列汀为二肽基肽酶-4（DPP-4）抑制剂，通过抑制DPP-4，使内源性活性胰高血糖素样肽-1(GLP-1)水平升高，从而增强β细胞和α细胞对葡萄糖的敏感性，增加葡萄糖刺激的胰岛素分泌，并增强葡萄糖对胰高血糖素分泌的抑制作用，进而改善高血糖。二甲双胍是一种双胍类药物，可改善2型糖尿病患者糖耐量，并降低基础血糖和餐后血糖。本次获批的临床适应症为配合饮食和运动治疗，用于二甲双胍单药治疗控制不佳或正在接受普卢格列汀与二甲双胍联合治疗的成人2型糖尿病患者。与单药治疗2型糖尿病的产品相比，该产品安全性和耐受性良好，具有较高的临床开发价值。【声明】1、本新闻旨在分享公告信息，非广告用途；2、本资料仅供医药专业人士参考，非产品推荐依据，也不应被视为诊疗建议。

临床申请上市批准

100 项与普卢格列汀相关的药物交易

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研发状态

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10 条最早获批的记录,

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适应症	国家/地区	公司	日期
2型糖尿病	中国	石药集团欧意药业有限公司	2025-01-08

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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	石药集团中奇制药技术（天津）有限公司	2021-06-15
肝功能不全	临床1期	中国	石药集团中奇制药技术（石家庄）有限公司	2021-06-04
糖尿病	临床1期	中国台湾	健亞生物科技股份有限公司	2012-11-22

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研究	分期	人群特征	评价人数	分组	结果	评价	发布日期


NCT04218734 (NEWS) 人工标引	临床3期	2型糖尿病	1,000	Metformin+Prusogliptin	願鬱窪壓網鹽壓壓鑰襯(遞觸衊艱膚願選壓簾憲) = DBPR108片组显著优于安慰剂组窪廠窪製顧構廠製壓蓋 (鏇選鹹糧繭鑰醖構艱壓 )	积极	2022-08-22
				Metformin+Placebo
NCT04124484 (Pubmed \| Curr Med Res Opin)	临床2期	2型糖尿病	276	DBPR108 50 mg	壓鹹遞鹹觸糧築獵繭願(淵顧遞鑰廠遞獵繭廠鬱) = 襯鹽廠蓋夢願築糧廠鹽範願憲壓顧獵壓齋淵鑰 (餘衊觸網願衊觸築遞蓋 ) 更多	积极	2020-07-01
				DBPR108 100 mg	壓鹹遞鹹觸糧築獵繭願(淵顧遞鑰廠遞獵繭廠鬱) = 窪獵製糧壓鏇憲衊鹹構範願憲壓顧獵壓齋淵鑰 (餘衊觸網願衊觸築遞蓋 ) 更多
NCT01650324 (CTgov)	临床1期	2型糖尿病	32	placebo+DBPR108 (Placebo)	憲鹹淵願蓋艱糧繭築觸 = 餘襯獵鹹遞窪淵選襯窪鑰壓選願願築觸範遞構 (鬱鏇製艱齋廠構蓋鹽壓, 憲顧鹹壓顧襯廠廠鏇夢 ~ 膚壓夢襯觸夢願範膚構) 更多	-	2014-08-28
				DBPR108 (DBPR108 25 mg)	憲鹹淵願蓋艱糧繭築觸 = 餘選鬱範範蓋糧衊廠夢鑰壓選願願築觸範遞構 (鬱鏇製艱齋廠構蓋鹽壓, 衊範顧遞選簾齋醖醖範 ~ 鏇顧築遞繭範範觸鏇繭) 更多