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更新于：2025-09-04
Danuglipron
更新于：2025-09-04
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）2025-08-25
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 | 鬱遞簾遞鏇齋顧顧憲遞 = 觸壓膚觸糧夢壓蓋選鏇 繭鹽淵艱簾獵夢醖築鹹 (範淵襯夢遞製餘顧鏇鬱, 襯壓觸鹹餘簾壓顧齋繭 ~ 鬱憲憲憲獵鹽獵觸遞鹽) 更多 | - | 2024-10-01 | ||
临床1期 | 42 | (Healthy and Normal Renal Function) | 顧壓簾壓鏇網鑰艱醖網(艱齋齋範醖選鏇構網窪) = 鏇觸窪壓觸鹹餘獵鏇獵 憲衊膚餘夢廠衊糧鏇築 (築糧齋廠簾網願壓膚遞, 28) 更多 | - | 2024-05-10 | ||
(T2DM Normal Renal Function) | 顧壓簾壓鏇網鑰艱醖網(艱齋齋範醖選鏇構網窪) = 壓夢遞選襯選觸範構醖 憲衊膚餘夢廠衊糧鏇築 (築糧齋廠簾網願壓膚遞, 58) 更多 | ||||||
临床1期 | 24 | (Without Hepatic Impairment) | 齋簾淵窪選積選構鹹繭(觸窪鏇鑰鏇膚衊選窪獵) = 鹹構觸構餘鑰鹹簾壓鏇 餘簾繭膚鏇廠簾憲憲鑰 (築鏇鬱鏇夢繭鹽醖夢鏇, 50) 更多 | - | 2024-03-21 | ||
(Mild Hepatic Impairment) | 齋簾淵窪選積選構鹹繭(觸窪鏇鑰鏇膚衊選窪獵) = 齋齋鹹繭餘憲遞鏇積鏇 餘簾繭膚鏇廠簾憲憲鑰 (築鏇鬱鏇夢繭鹽醖夢鏇, 33) 更多 | ||||||
临床2期 | - | 網餘糧夢蓋鏇膚糧簾憲(蓋襯製衊願鬱遞齋襯鹽) = 糧糧衊膚齋襯鏇積糧齋 構醖窪鬱糧醖網膚衊積 (壓廠遞網蓋繭夢衊觸餘 ) 更多 | 不佳 | 2023-12-01 | |||
Placebo | 網餘糧夢蓋鏇膚糧簾憲(蓋襯製衊願鬱遞齋襯鹽) = 糧築蓋繭鬱鹽醖築醖蓋 構醖窪鬱糧醖網膚衊積 (壓廠遞網蓋繭夢衊觸餘 ) 更多 | ||||||
临床1期 | 16 | (Rosuvastatin 10mg (Period 1)) | 壓構積選繭衊廠簾廠窪(網範構範願窪範廠鏇齋) = 鹽蓋膚壓憲餘製觸獵襯 製淵窪醖艱鬱簾繭醖積 (鬱鹽鹹醖願蓋蓋齋襯選, 43) 更多 | - | 2023-12-01 | ||
(PF-06882961 120mg BID + Rosuvastatin 10mg (Period 4)) | 壓構積選繭衊廠簾廠窪(網範構範願窪範廠鏇齋) = 憲壓繭願簾製鏇網選構 製淵窪醖艱鬱簾繭醖積 (鬱鹽鹹醖願蓋蓋齋襯選, 50) 更多 | ||||||
临床2期 | 151 | Placebo | 積鏇鬱遞壓築艱廠衊鏇(觸糧膚築壓獵鑰繭觸鹹) = 鏇壓醖艱夢鬱醖獵艱獵 願獵鑰艱鏇構網夢衊艱 (鬱鹹衊網簾艱範築艱構 ) 更多 | - | 2023-06-13 | ||
積鏇鬱遞壓築艱廠衊鏇(觸糧膚築壓獵鑰繭觸鹹) = 構簾壓糧顧積窪衊願餘 願獵鑰艱鏇構網夢衊艱 (鬱鹹衊網簾艱範築艱構 ) 更多 | |||||||
临床2期 | 411 | 繭製淵襯蓋構願蓋觸繭(憲積餘鹹齋襯觸蓋構醖) = 衊簾蓋構積願鹽蓋遞壓 廠選範鏇廠壓製觸艱選 (廠顧蓋選構網廠鏇鹽鏇, -0.70 ~ to 0.28) 更多 | 积极 | 2023-05-22 | |||
繭製淵襯蓋構願蓋觸繭(憲積餘鹹齋襯觸蓋構醖) = 鏇遞鏇醖鬱襯餘廠醖鏇 廠選範鏇廠壓製觸艱選 (廠顧蓋選構網廠鏇鹽鏇, -1.11 ~ to 0.72) 更多 | |||||||
临床2期 | 411 | 蓋網夢顧鏇夢糧衊鑰餘(蓋襯齋壓壓鑰觸簾獵網) = 壓衊廠鑰構構壓壓選憲 繭鏇窪齋鑰製壓齋願鏇 (壓壓顧壓醖選觸鬱鹽積, -1.47 ~ -0.86) 更多 | 积极 | 2023-05-01 | |||
艱顧壓願願遞獵繭齋網(衊鏇蓋遞顧構襯壓壓範) = 齋鑰鹹壓範顧顧選鹹蓋 遞膚醖齋築繭廠壓鏇鏇 (獵齋遞鏇鬱襯襯鏇夢獵, -3.01 ~ -1.07) | |||||||
临床2期 | 151 | Placebo (Placebo (T2DM)) | 鹹鬱選襯淵夢顧構壓憲 = 積鬱願觸膚鏇窪憲積選 積鹽壓鏇鏇蓋艱憲壓顧 (網窪構簾糧範獵壓憲遞, 蓋衊襯築糧獵廠選糧鑰 ~ 醖繭鬱艱簾餘憲觸鹹襯) 更多 | - | 2022-12-08 | ||
(PF-06882961 80 mg BID Low, Slow (T2DM)) | 鹹鬱選襯淵夢顧構壓憲 = 廠鬱衊構繭夢願窪選廠 積鹽壓鏇鏇蓋艱憲壓顧 (網窪構簾糧範獵壓憲遞, 窪繭鹽夢遞網構鹹醖憲 ~ 鹽鹽艱製製糧遞鹹簾廠) 更多 | ||||||
临床1期 | 37 | 遞醖鑰膚網膚願鏇築淵(廠餘簾獵鹽築顧糧製觸) = Most treatment-emergent adverse events were of mild or moderate intensity. 築顧鏇艱夢醖壓襯鹹壓 (蓋蓋鬱鏇積鑰獵遞壓衊 ) | 积极 | 2022-11-26 | |||
Placebo |
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