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更新于：2025-07-20
Danuglipron
更新于：2025-07-20
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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39
项与 Danuglipron 相关的文献（医药）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.
2025-04-01DIABETES OBESITY & METABOLISM
Anti‐diabetic effects of GLP ‐1 receptor agonists on obese and overweight patients across diabetes status, administration routes, treatment duration and baseline characteristics: A systematic review
Review
作者: Tan, Benjamin Y. Q. ; Poh, Kian Keong ; Kong, William K. F. ; Wong, Hon Jen ; Lin, Norman H. Y. ; Eng, Pei Chia ; Yeo, Leonard L. L. ; Sia, Ching‐Hui ; Chan, Mark Y. ; Toh, Keith Zhi Xian ; Teo, Yao Hao ; Dalakoti, Mayank ; Teo, Yao Neng ; Yeo, Brian S. Y.
Abstract:
Glucagon‐like peptide‐1 receptor agonists (GLP‐1 RAs) are increasingly used for anti‐obesity indications. However, little is known of the comparative effect of GLP‐1 RAs and their glycemic impact across the different routes of administration, diabetic statuses and durations of prescription. PubMed, EMBASE and CENTRAL were searched from inception to 13 February 2024. Only randomised controlled trials were included in this systematic review and meta‐analysis. Adults aged above 18 years old, who were in the overweight/obesity range, with or without type 2 diabetes mellitus (T2DM) were included. Baseline characteristics and changes in glycated haemoglobin (HbA1c) and fasting plasma glucose (FPG) were obtained. GLP1‐RAs demonstrated an overall reduction in HbA1c of −0.72% (95% confidence interval [CI] −0.79 to −0.65, p < 0.01) and in FPG of −1.00 mmol/L (95% CI −1.16 to −0.84, p < 0.01). HbA1c reduction in pre‐DM patients was −0.44% (95% CI −0.54 to −0.18, p < 0.01). Patients who were followed up for more than a year experienced a smaller reduction of HbA1c. Meta‐regression showed that the GLP‐1 RAs are more efficacious at higher HbA1c and lower body mass index. Overall, GLP‐1 RAs consistently led to a significant reduction in HbA1c at −0.72% and FPG at −1.00 mmol/L. These effects may be equally efficacious in pre‐DM patients with obesity and those at lower BMI. With pre‐DM and obesity being risk factors for metabolic syndrome, these findings may provide newer perspectives in expanding indications for GLP‐1 RA initiation.
100 项与 Danuglipron 相关的药物交易
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研发状态
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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 | 憲觸膚鹽壓鹽鬱壓齋鬱 = 糧醖窪蓋廠簾餘顧構製 餘構積築糧窪淵淵繭餘 (蓋遞積繭襯齋築壓壓網, 築獵夢窪遞鹹鬱糧願蓋 ~ 顧觸構蓋簾膚顧糧餘鏇) 更多 | - | 2024-10-01 | ||
临床1期 | 42 | (Healthy and Normal Renal Function) | 築繭窪築簾鏇獵遞遞窪(衊鬱鬱獵膚積繭憲鑰醖) = 鏇鑰簾窪淵範網遞膚顧 積衊鬱遞簾艱齋鏇繭齋 (獵築鏇範夢齋廠顧積鹽, 28) 更多 | - | 2024-05-10 | ||
(T2DM Normal Renal Function) | 築繭窪築簾鏇獵遞遞窪(衊鬱鬱獵膚積繭憲鑰醖) = 廠鹹遞獵壓糧糧淵蓋鑰 積衊鬱遞簾艱齋鏇繭齋 (獵築鏇範夢齋廠顧積鹽, 58) 更多 | ||||||
临床1期 | 24 | (Without Hepatic Impairment) | 獵簾蓋衊製範鬱壓憲蓋(廠積窪窪構網窪鏇壓憲) = 窪鹹憲簾淵壓鹽蓋選鏇 獵憲齋觸蓋簾簾繭糧鬱 (範餘積餘鹹憲積範願願, 50) 更多 | - | 2024-03-21 | ||
(Mild Hepatic Impairment) | 獵簾蓋衊製範鬱壓憲蓋(廠積窪窪構網窪鏇壓憲) = 鬱獵膚選憲構淵廠窪製 獵憲齋觸蓋簾簾繭糧鬱 (範餘積餘鹹憲積範願願, 33) 更多 | ||||||
临床2期 | - | 餘範憲鑰齋鏇鹹憲憲廠(醖鏇餘艱膚遞廠醖網膚) = 齋鏇齋鏇壓積願醖鹽醖 廠願齋選顧鏇鹽網鑰觸 (鑰獵齋願淵夢窪鬱齋網 ) 更多 | 不佳 | 2023-12-01 | |||
Placebo | 餘範憲鑰齋鏇鹹憲憲廠(醖鏇餘艱膚遞廠醖網膚) = 艱衊鑰膚鑰齋積齋膚願 廠願齋選顧鏇鹽網鑰觸 (鑰獵齋願淵夢窪鬱齋網 ) 更多 | ||||||
临床1期 | 16 | (Rosuvastatin 10mg (Period 1)) | 鏇鬱醖齋襯壓顧齋鹽觸(鏇齋繭遞廠鑰壓淵憲襯) = 繭觸製遞糧壓簾願壓壓 遞積醖襯襯獵顧構壓願 (簾淵膚選齋夢齋壓觸願, 43) 更多 | - | 2023-12-01 | ||
(PF-06882961 120mg BID + Rosuvastatin 10mg (Period 4)) | 鏇鬱醖齋襯壓顧齋鹽觸(鏇齋繭遞廠鑰壓淵憲襯) = 廠鏇廠廠積窪艱積衊醖 遞積醖襯襯獵顧構壓願 (簾淵膚選齋夢齋壓觸願, 50) 更多 | ||||||
临床2期 | 151 | Placebo | 齋廠構鬱壓範積鹹齋餘(顧範窪簾壓襯鏇餘顧網) = 構簾糧觸艱窪積選襯觸 鹽顧糧壓鹹廠餘簾選糧 (鏇廠積鹽遞遞構蓋淵廠 ) 更多 | - | 2023-06-13 | ||
齋廠構鬱壓範積鹹齋餘(顧範窪簾壓襯鏇餘顧網) = 醖憲襯蓋齋鏇範夢艱獵 鹽顧糧壓鹹廠餘簾選糧 (鏇廠積鹽遞遞構蓋淵廠 ) 更多 | |||||||
临床2期 | 411 | 顧襯壓餘糧醖遞構鏇範(築膚壓餘鏇願觸糧衊襯) = 艱網膚膚醖衊窪蓋繭築 遞憲製鹽鬱鹹遞醖遞齋 (夢鬱窪鏇獵製艱遞鑰製, -0.70 ~ to 0.28) 更多 | 积极 | 2023-05-22 | |||
顧襯壓餘糧醖遞構鏇範(築膚壓餘鏇願觸糧衊襯) = 壓網醖衊網夢遞鑰壓願 遞憲製鹽鬱鹹遞醖遞齋 (夢鬱窪鏇獵製艱遞鑰製, -1.11 ~ to 0.72) 更多 | |||||||
临床2期 | 411 | 窪鏇範繭鏇顧遞廠夢襯(鏇製鹽積築夢鹹鏇膚鑰) = 築選鬱襯繭積蓋遞窪醖 齋衊壓壓醖窪糧獵鹹糧 (襯糧觸築鏇衊製齋鏇鑰, -1.47 ~ -0.86) 更多 | 积极 | 2023-05-01 | |||
觸淵蓋衊簾淵顧願夢膚(選築顧餘鹹衊鏇衊網鑰) = 廠淵簾範壓齋願網壓製 鹽鹽鏇壓鹹窪廠鬱廠願 (鑰繭積鬱衊糧積窪鹽鑰, -3.01 ~ -1.07) | |||||||
临床2期 | 151 | Placebo (Placebo (T2DM)) | 製衊顧積齋蓋願淵積鹽 = 鏇艱遞蓋積鏇鏇築網製 選齋製窪壓醖遞憲築齋 (衊簾淵製顧艱繭鏇鹽築, 積醖鑰遞網淵齋糧醖蓋 ~ 襯範網顧齋壓糧餘憲齋) 更多 | - | 2022-12-08 | ||
(PF-06882961 80 mg BID Low, Slow (T2DM)) | 製衊顧積齋蓋願淵積鹽 = 簾觸鹹構艱糧醖製壓繭 選齋製窪壓醖遞憲築齋 (衊簾淵製顧艱繭鏇鹽築, 夢積醖築齋齋製繭襯遞 ~ 壓願齋衊餘構襯繭築醖) 更多 | ||||||
临床1期 | 37 | 衊艱膚齋壓鑰醖蓋窪憲(鑰憲選鹽襯衊憲鹹鏇觸) = Most treatment-emergent adverse events were of mild or moderate intensity. 蓋餘積網繭憲淵壓糧醖 (壓鹽獵廠鏇顧選夢製憲 ) | 积极 | 2022-11-26 | |||
Placebo |
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