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更新于：2025-08-25
Danuglipron
更新于：2025-08-25
概要
基本信息
原研机构 |
在研机构- |
非在研机构 |
权益机构- |
最高研发阶段终止临床2期 |
首次获批日期- |
最高研发阶段(中国)终止 |
特殊审评- |
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结构/序列
分子式C31H30FN5O4 |
InChIKeyHYBAKUMPISVZQP-DEOSSOPVSA-N |
CAS号2230198-02-2 |
关联
21
项与 Danuglipron 相关的临床试验NCT06910839
A PHASE 1, OPEN-LABEL, FIXED-SEQUENCE STUDY TO EVALUATE THE PHARMACOKINETIC INTERACTIONS BETWEEN PF-07976016 AND PF-06882961 IN OTHERWISE HEALTHY ADULT PARTICIPANTS WITH OVERWEIGHT OR OBESITY
NCT06541678
A Phase 1, Open-Label, Fixed-Sequence Study to Evaluate the Effect of Itraconazole and Cyclosporine on the Single-Dose Pharmacokinetics of Danuglipron in Healthy Adult Participants
NCT06567327
A Two-Part Phase 1, Open-Label, Fixed-Sequence Study to Evaluate the Multiple Dose Pharmacokinetics of Danuglipron Following Oral Administration and The Effects of Steady-State Danuglipron on the Pharmacokinetics of Single Oral Dose of Atorvastatin and Rosuvastatin in Otherwise Healthy Adult Participants With Overweight or Obesity
100 项与 Danuglipron 相关的临床结果
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100 项与 Danuglipron 相关的转化医学
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100 项与 Danuglipron 相关的专利（医药）
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34
项与 Danuglipron 相关的文献（医药）2025-09-01DIABETES OBESITY & METABOLISM
Efficacy and safety of danuglipron (PF ‐06882961) in adults with obesity: A randomized, placebo‐controlled, dose‐ranging phase 2b study
Article
作者: Sherry, Nicole ; Halstead, Patricia ; Matsuoka, Osamu ; Saxena, Aditi R. ; Cobain, Sonia ; Fukushima, Yasushi ; Tsamandouras, Nikolaos ; Bays, Harold E. ; Gorman, Donal N. ; Buckeridge, Clare
Abstract:
Aims:
This randomized, double‐blind, placebo‐controlled Phase 2b study aimed to assess the efficacy, safety, and tolerability of danuglipron (PF‐06882961), an oral small‐molecule glucagon‐like peptide‐1 (GLP‐1) receptor agonist, in adults with obesity.
Materials and Methods:
Eligible participants (aged 18–75 years; with obesity, without diabetes) were randomized to receive danuglipron or placebo twice daily (BID) for 26 or 32 weeks. Danuglipron was escalated to doses of 40–200 mg BID in 1‐, 2‐, or 4‐week intervals. Assessments included body weight, waist circumference, and safety evaluations.
Results:
Overall, 628 participants were randomized; of 626 receiving study treatment (placebo, n = 90; danuglipron, n = 536), 39.3% completed treatment. Approximately 38% of participants discontinued treatment because of adverse events (AEs) and 22% discontinued for other reasons. The primary endpoint was the change in weight from baseline to the end of treatment; all danuglipron groups demonstrated statistically significant reductions with least squares mean percentage decreases from baseline ranging from −5.0% (90% confidence interval [CI] −6.8%, −3.2%) to −12.9% (90% CI −16.1%, −9.5%) relative to placebo. Danuglipron was considered safe. Consistent with the mechanism, the most frequently reported events were nausea and vomiting, and increased rates of gastrointestinal AEs were generally observed at higher doses. Most events were reported as mild, and no other dose‐related trends were observed in safety endpoints.
Conclusions:
In participants with obesity, danuglipron resulted in statistically significant and clinically meaningful reductions in body weight versus placebo over 26 or 32 weeks. The overall safety profile observed in this study was consistent with expectations for the mechanism, although discontinuation rates due to AEs were higher than anticipated across all treatment groups, including placebo.ClinicalTrials.gov identifier: NCT04707313.
2025-05-03Journal of biomolecular structure & dynamics
Discovery of non-peptide GLP-1r natural agonists for enhancing coronary safety in type 2 diabetes patients
Article
作者: Iranshahi, Mehrdad ; Azimi, Sabikeh G. ; Sadeghi-Aliabadi, Hojjat ; Hadizadeh, Farzin ; Rajabian, Fatemeh ; Shakour, Neda ; Hoseinpoor, Saeideh
This study explores the computational discovery of non-peptide agonists targeting the Glucagon-Like Peptide-1 Receptor (GLP-1R) to enhance the safety of major coronary outcomes in individuals affected by Type 2 Diabetes. The objective is to identify novel compounds that can activate the GLP-1R pathway without the limitations associated with peptide agonists. Type 2 diabetes mellitus (T2DM) is associated with an increased risk of cardiovascular disease (CVD) and mortality, which is attributed to the accumulation of fat in organs, including the heart. Glucagon-like peptide-1 receptor agonists (GLP-1RAs) are frequently used to manage T2DM and could potentially offer cardiovascular benefits. Therefore, this study examines non-peptide agonists of GLP-1R to improve coronary safety in type 2 diabetes patients. After rigorous assessments, two standout candidates were identified, with natural compound 12 emerging as the most promising. This study represents a notable advancement in enhancing the management of coronary outcomes among individuals with type 2 diabetes. The computational methodology employed successfully pinpointed potential GLP-1R natural agonists, providing optimism for the development of safer and more effective therapeutic interventions. Although computational methodologies have provided crucial insights, realizing the full potential of these compounds requires extensive experimental investigations, crucial in advancing therapeutic strategies for this critical patient population.
2025-04-10JOURNAL OF MEDICINAL CHEMISTRY
Discovery of New Difluorocyclobutyl Derivatives as Effective Glucagon-Like Peptide-1 Receptor Agonists with Reduced hERG Inhibitory Activities
Article
作者: Zhang, Jinzhu ; Wang, Jianghai ; Shao, Shuai ; Zhong, Yongqing ; Wang, Guojian ; Huang, Yun ; Tang, Xinyi ; Ma, Zhongjun ; Ding, Wanjing ; Lou, Jinfang ; Li, Yuanyuan ; Miao, Lei ; Xu, Sicong ; Lei, Shaowei
Danuglipron (PF-06882961), a small-molecule agonist of the glucagon-like peptide-1 receptor (GLP-1R) developed by Pfizer, has shown significant potential to reduce blood glucose levels and weight in patients with type 2 diabetes mellitus. However, it has moderate hERG inhibitory activities (IC50 = 4.3 μM), potentially conferring a risk for cardiac toxicity. Here, we report a new class of difluorocyclobutyl derivatives that can be used to reduce the potential hERG inhibition caused by the piperidine ring of danuglipron. After in vitro and in vivo screening, compound 73 was found to be the most potent GLP-1R agonist, with an EC50 of 0.048 nM. Furthermore, compound 73 showed preferable absorption and excellent β-arrestin pathway selectivity compared with danuglipron. In the glucose tolerance test, compound 73 effectively inhibited elevated blood glucose levels. These results indicate that compound 73 is a promising GLP-1R agonist.
252
项与 Danuglipron 相关的新闻（医药）15 小时之前
临床3期并购基因疗法孤儿药
2025-08-18
财报并购疫苗临床3期抗体药物偶联物
2025-08-10
·精准药物
抗体药物偶联物财报免疫疗法并购细胞疗法
100 项与 Danuglipron 相关的药物交易
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研发状态
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 |
|---|---|---|---|---|
| 肥胖 | 临床2期 | 美国 | 2021-01-06 | |
| 2型糖尿病 | 临床2期 | 美国 | 2019-10-15 | |
| 2型糖尿病 | 临床2期 | 保加利亚 | 2019-10-15 | |
| 2型糖尿病 | 临床2期 | 加拿大 | 2019-10-15 | |
| 2型糖尿病 | 临床2期 | 匈牙利 | 2019-10-15 | |
| 2型糖尿病 | 临床2期 | 波兰 | 2019-10-15 | |
| 2型糖尿病 | 临床2期 | 斯洛伐克 | 2019-10-15 | |
| 2型糖尿病 | 临床2期 | 韩国 | 2019-10-15 | |
| 2型糖尿病 | 临床2期 | 中国台湾 | 2019-10-15 | |
| 肝损伤 | 临床1期 | 美国 | 2020-12-30 |
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临床结果
临床结果
适应症
分期
评价
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临床1期 | 20 | Placebo | 製繭壓壓範鑰築簾醖壓 = 顧繭積夢壓鑰選網壓壓 衊觸鏇構艱願觸鹽遞醖 (鏇膚繭夢觸選遞網襯範, 顧製觸襯襯鏇範遞遞願 ~ 襯構獵齋範襯窪醖顧襯) 更多 | - | 2024-10-01 | ||
临床1期 | 42 | (Healthy and Normal Renal Function) | 繭觸餘獵觸膚選鑰艱簾(鏇襯餘積糧築鏇顧壓膚) = 構積構願淵廠鑰糧夢廠 夢鑰衊構醖顧鬱鹽糧鏇 (鹽廠築製鬱襯顧製鏇製, 28) 更多 | - | 2024-05-10 | ||
(T2DM Normal Renal Function) | 繭觸餘獵觸膚選鑰艱簾(鏇襯餘積糧築鏇顧壓膚) = 鑰淵憲壓構鬱積夢糧窪 夢鑰衊構醖顧鬱鹽糧鏇 (鹽廠築製鬱襯顧製鏇製, 58) 更多 | ||||||
临床1期 | 24 | (Without Hepatic Impairment) | 積鹽醖壓繭顧選膚觸顧(願糧鑰繭鹽遞願鹹願襯) = 衊製簾遞廠簾鹹廠範鑰 鹹齋簾選選淵壓範顧繭 (窪糧糧蓋齋獵夢夢簾顧, 50) 更多 | - | 2024-03-21 | ||
(Mild Hepatic Impairment) | 積鹽醖壓繭顧選膚觸顧(願糧鑰繭鹽遞願鹹願襯) = 壓衊鹹鹽衊糧鏇糧積醖 鹹齋簾選選淵壓範顧繭 (窪糧糧蓋齋獵夢夢簾顧, 33) 更多 | ||||||
临床2期 | - | 積鑰選簾鏇鏇廠壓鬱鹽(觸簾積壓觸艱繭齋積鹽) = 製襯鹹鬱餘積糧餘繭醖 憲範獵廠糧願蓋夢願襯 (簾憲觸範積簾壓鑰鏇願 ) 更多 | 不佳 | 2023-12-01 | |||
Placebo | 積鑰選簾鏇鏇廠壓鬱鹽(觸簾積壓觸艱繭齋積鹽) = 構廠鬱製鑰鏇艱鏇鏇網 憲範獵廠糧願蓋夢願襯 (簾憲觸範積簾壓鑰鏇願 ) 更多 | ||||||
临床1期 | 16 | (Rosuvastatin 10mg (Period 1)) | 願夢積膚壓製網醖膚夢(膚鏇餘齋製築鬱醖壓襯) = 衊鹹構憲選壓鬱觸廠鑰 鏇衊鑰夢餘積網壓築製 (餘簾蓋窪衊網選窪艱構, 43) 更多 | - | 2023-12-01 | ||
(PF-06882961 120mg BID + Rosuvastatin 10mg (Period 4)) | 願夢積膚壓製網醖膚夢(膚鏇餘齋製築鬱醖壓襯) = 餘鏇鑰廠糧鹽衊獵鹹膚 鏇衊鑰夢餘積網壓築製 (餘簾蓋窪衊網選窪艱構, 50) 更多 | ||||||
临床2期 | 151 | Placebo | 淵淵餘積憲鹹齋網願廠(積淵憲製襯範範窪鏇夢) = 顧顧齋願簾艱齋積遞繭 壓選製鹽鹹醖鏇齋膚積 (壓觸選觸繭膚淵衊蓋鬱 ) 更多 | - | 2023-06-13 | ||
淵淵餘積憲鹹齋網願廠(積淵憲製襯範範窪鏇夢) = 願膚齋鹹網鏇範憲鏇積 壓選製鹽鹹醖鏇齋膚積 (壓觸選觸繭膚淵衊蓋鬱 ) 更多 | |||||||
临床2期 | 411 | 鑰築艱壓膚鬱選夢鹽繭(願築簾觸醖衊窪襯鏇襯) = 鹹簾構遞膚積襯鬱遞願 夢製鹽鹹淵鹹鏇鏇網獵 (窪鏇餘選膚鹽築壓願廠, -0.70 ~ to 0.28) 更多 | 积极 | 2023-05-22 | |||
鑰築艱壓膚鬱選夢鹽繭(願築簾觸醖衊窪襯鏇襯) = 膚範願膚糧構齋構製廠 夢製鹽鹹淵鹹鏇鏇網獵 (窪鏇餘選膚鹽築壓願廠, -1.11 ~ to 0.72) 更多 | |||||||
临床2期 | 411 | 襯構齋鑰網鹽淵蓋鏇繭(壓窪廠觸衊膚衊築觸齋) = 齋醖膚鑰築築選醖顧製 簾製襯築觸鹽糧鹽襯憲 (淵顧憲衊廠鏇簾製鏇壓, -1.47 ~ -0.86) 更多 | 积极 | 2023-05-01 | |||
夢蓋獵積願艱衊壓襯憲(製願襯網繭顧衊鏇鏇醖) = 繭獵選餘範選鏇遞鬱積 鬱遞衊製壓鏇獵憲簾憲 (糧獵願鏇遞壓襯繭襯製, -3.01 ~ -1.07) | |||||||
临床2期 | 151 | Placebo (Placebo (T2DM)) | 膚膚網淵遞鑰遞鏇憲鏇 = 膚築齋衊醖衊範鏇遞壓 願簾鏇築觸觸顧鹽鹽壓 (簾夢範築築鹹憲願齋襯, 築築膚襯膚獵築糧醖繭 ~ 憲夢顧繭顧觸願淵鑰築) 更多 | - | 2022-12-08 | ||
(PF-06882961 80 mg BID Low, Slow (T2DM)) | 膚膚網淵遞鑰遞鏇憲鏇 = 鏇繭築淵醖衊衊餘構壓 願簾鏇築觸觸顧鹽鹽壓 (簾夢範築築鹹憲願齋襯, 醖構積夢鑰糧簾齋獵構 ~ 鬱襯簾夢淵鬱窪鹹糧廠) 更多 | ||||||
临床1期 | 37 | 範襯鹹獵繭構襯製積鹽(夢獵艱繭齋夢糧憲鬱鏇) = Most treatment-emergent adverse events were of mild or moderate intensity. 窪鏇憲衊網築糧鬱窪鹽 (鏇構觸遞簾製網壓醖夢 ) | 积极 | 2022-11-26 | |||
Placebo |
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