更新于：2024-09-13
Danuglipron
更新于：2024-09-13
概要
基本信息
原研机构 |
在研机构 |
非在研机构- |
最高研发阶段临床2期 |
首次获批日期- |
最高研发阶段(中国)终止 |
特殊审评- |
结构
分子式C31H30FN5O4 |
InChIKeyHYBAKUMPISVZQP-DEOSSOPVSA-N |
CAS号2230198-02-2 |
关联
23
项与 Danuglipron 相关的临床试验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
A PHASE 1, OPEN- LABEL STUDY TO EVALUATE THE MULTIPLE DOSE PHARMACOKINETICS OF DANUGLIPRON FOLLOWING ORAL ADMINISTRATION IN OTHERWISE HEALTHY ADULT PARTICIPANTS WITH OVERWEIGHT OR OBESITY
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
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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14
项与 Danuglipron 相关的文献（医药）2024-04-01British journal of pharmacology
Newer pharmacological interventions directed at gut hormones for obesity
Review
作者: Acosta, Andres ; Camilleri, Michael
The objective is to review the newer pharmacological interventions for obesity, specifically single, dual and triple incretin receptor agonists that are either available or in the pipeline for treatment of obesity. The three incretin receptor targets are glucagon like peptide‐1 (GLP‐1), glucose‐dependent insulinotropic peptide (GIP) and glucagon. There are several approved single or dual incretin agonists which can be administered subcutaneously daily (e.g., liraglutide) or weekly (e.g., semaglutide, dulaglutide, and exenatide QW), and other experimental dual or triple incretin agonists. Analogues of amylin, peptide YY and oxyntomodulin, as well as the combination of a GLP1R agonist and GIPR antagonist also are in development. Oral semaglutide (administered daily) is approved for type 2 diabetes mellitus and is on track for regulatory review for obesity. The review includes specifically perspectives on the effects of these mechanisms and pharmacological agents on gastric emptying, which contribute to satiation and weight loss, in addition to the established evidence on effects on central mechanisms controlling appetite. In the future, it is anticipated that small molecule GLP‐1 receptor agonists (e.g., oral danuglipron) will be developed for treating obesity. These pharmacological agents are having significant impact on glycaemic control and obesity and on their co‐morbidities.
2023-10-01Diabetes, obesity & metabolism
Tolerability, safety and pharmacodynamics of oral, small-molecule glucagon-like peptide-1 receptor agonist danuglipron for type 2 diabetes: A 12-week, randomized, placebo-controlled, Phase 2 study comparing different dose-escalation schemes.
Article
作者: Andrawis, Nabil ; Birnbaum, Morris J ; Frias, Juan P ; Gorman, Donal N ; Tsamandouras, Nikolaos ; Saxena, Aditi R ; Lopez, Rene N
AIM:
To evaluate the tolerability, safety and pharmacodynamics of different dose-escalation schemes of the oral small-molecule glucagon-like peptide-1 receptor (GLP-1R) agonist danuglipron.
MATERIALS AND METHODS:
This Phase 2a, double-blind, placebo-controlled, parallel-group study randomly assigned adults with type 2 diabetes (T2D) treated with metformin to placebo or danuglipron (low [5-mg] or high [10-mg] starting dose, with 1- or 2-week dose-escalation steps, to target doses of 80, 120 or 200 mg twice daily [BID]) and adults with obesity without diabetes to placebo or danuglipron 200 mg BID.
RESULTS:
Participants with T2D (n = 123, mean glycated haemoglobin [HbA1c] 8.19%) or obesity without diabetes (n = 28, mean body mass index 37.3 kg/m2 ) were randomly assigned and treated. Discontinuation from study medication occurred in 27.3% to 72.7% of participants across danuglipron groups versus 16.7% to 18.8% for placebo, most often due to adverse events. Nausea (20.0%-47.6% of participants across danuglipron groups vs. 12.5% for placebo) and vomiting (18.2%-40.9% danuglipron vs. 12.5% placebo, respectively) were most commonly reported in participants with T2D. Gastrointestinal adverse events were generally related to danuglipron target dose and were not substantially affected by starting dose. In participants with T2D, least squares mean changes from baseline in HbA1c (-1.04% to -1.57% across danuglipron groups vs. -0.32% for placebo), fasting plasma glucose (-23.34 mg/dL to -53.94 mg/dL danuglipron vs. -13.09 mg/dL placebo) and body weight (-1.93 to -5.38 kg danuglipron vs. -0.42 kg placebo) at Week 12 were generally statistically significant for danuglipron compared with placebo (P < 0.05).
CONCLUSIONS:
Danuglipron resulted in statistically significant reductions in HbA1c, FPG and body weight over 12 weeks, in the setting of higher discontinuation rates and incidence of gastrointestinal adverse events with higher target doses.
CLINICALTRIALS:
gov identifier: NCT04617275.
2023-10-01Bioorganic & medicinal chemistry letters
6-Azaspiro[2.5]octanes as small molecule agonists of the human glucagon-like peptide-1 receptor.
Article
作者: Curto, John M ; Wei, Liuqing ; Bagley, Scott W ; Piotrowski, David W ; Limberakis, Chris ; Genovino, Julien ; Aspnes, Gary E ; Mathiowetz, Alan M ; Coffey, Steven B ; Rose, Colin R ; Conn, Edward L ; Jiao, Wenhua ; Ruggeri, Roger B ; Edmonds, David J ; Ingle, Gajendra ; Griffith, David A
Activation of the glucagon-like peptide-1 (GLP-1) receptor stimulates insulin release, lowers plasma glucose levels, delays gastric emptying, increases satiety, suppresses food intake, and affords weight loss in humans. These beneficial attributes have made peptide-based agonists valuable tools for the treatment of type 2 diabetes mellitus and obesity. However, efficient, and consistent delivery of peptide agents generally requires subcutaneous injection, which can reduce patient utilization. Traditional orally absorbed small molecules for this target may offer improved patient compliance as well as the opportunity for co-formulation with other oral therapeutics. Herein, we describe an SAR investigation leading to small-molecule GLP-1 receptor agonists that represent a series that parallels the recently reported clinical candidate danuglipron. In the event, identification of a benzyloxypyrimidine lead, using a sensitized high-throughput GLP-1 agonist assay, was followed by optimization of the SAR using substituent modifications analogous to those discovered in the danuglipron series. A new series of 6-azaspiro[2.5]octane molecules was optimized into potent GLP-1 agonists. Information gleaned from cryogenic electron microscope structures was used to rationalize the SAR of the optimized compounds.
177
项与 Danuglipron 相关的新闻（医药）2024-09-13
·药融云
临床3期临床2期临床结果
2024-09-11
·药融云
临床2期临床1期
2024-09-11
·药融圈
临床结果临床2期临床1期
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 |
|---|---|---|---|---|
| 超重 | 临床2期 | 比利时 | 2021-07-19 | |
| 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 |
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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1期 | 42 | (Healthy and Normal Renal Function) | 鹹夢壓顧憲鏇繭餘醖願(鹹範壓窪鑰餘積鑰艱積) = 製壓壓繭鑰鹹鹹獵觸顧 壓憲襯鏇鹹鹽鑰鏇鏇鏇 (醖餘鹹艱願憲願壓獵選, 廠夢鑰廠遞壓淵鑰襯鬱 ~ 鹹鏇範壓蓋網鬱願鏇遞) 更多 | - | 2024-05-10 | ||
(T2DM Normal Renal Function) | 鹹夢壓顧憲鏇繭餘醖願(鹹範壓窪鑰餘積鑰艱積) = 艱窪襯淵窪糧築構醖鏇 壓憲襯鏇鹹鹽鑰鏇鏇鏇 (醖餘鹹艱願憲願壓獵選, 醖蓋衊醖淵壓鑰鹽觸糧 ~ 網鹽網顧築鹹築憲願願) 更多 | ||||||
临床2期 | - | 餘艱選醖獵蓋壓獵憲獵(鹹顧襯選廠淵鏇壓淵鬱) = 糧糧襯鑰襯醖遞淵觸鏇 選網觸襯糧艱鬱構齋願 (顧鏇憲糧遞鹽選餘憲衊 ) 更多 | 不佳 | 2023-12-01 | |||
Placebo | 餘艱選醖獵蓋壓獵憲獵(鹹顧襯選廠淵鏇壓淵鬱) = 選願鑰簾鬱繭窪餘遞壓 選網觸襯糧艱鬱構齋願 (顧鏇憲糧遞鹽選餘憲衊 ) 更多 | ||||||
临床1期 | 16 | (Rosuvastatin 10mg (Period 1)) | 觸膚壓衊鹹膚選醖網廠(製廠壓構獵衊獵憲鹹壓) = 築積窪齋製鹹壓膚窪鏇 齋窪製襯鏇艱製鬱願壓 (遞鹹憲廠鑰淵窪築築製, 願憲顧鏇繭鹹獵獵繭築 ~ 範夢製窪壓醖糧夢鹹網) 更多 | - | 2023-12-01 | ||
(PF-06882961 120mg BID + Rosuvastatin 10mg (Period 4)) | 觸膚壓衊鹹膚選醖網廠(製廠壓構獵衊獵憲鹹壓) = 顧網簾糧鹹繭糧鹹壓衊 齋窪製襯鏇艱製鬱願壓 (遞鹹憲廠鑰淵窪築築製, 壓壓顧鏇製餘網構蓋積 ~ 蓋構鹽窪餘製鑰糧鹹衊) 更多 | ||||||
临床2期 | 151 | Placebo | 築衊鏇鑰憲獵簾範膚簾(糧築選製鹽築醖廠範獵) = 構鑰齋鏇顧壓衊鹹窪糧 衊顧蓋艱簾憲襯醖鑰製 (顧餘網窪壓膚憲築構窪 ) 更多 | - | 2023-06-13 | ||
築衊鏇鑰憲獵簾範膚簾(糧築選製鹽築醖廠範獵) = 積鹹構醖選觸獵餘餘觸 衊顧蓋艱簾憲襯醖鑰製 (顧餘網窪壓膚憲築構窪 ) 更多 | |||||||
临床2期 | 411 | 願繭鑰範齋齋鏇艱膚鹹(廠顧餘醖夢網遞繭鏇鹹) = 鹽膚膚窪鬱鏇壓積鹽遞 壓餘願製憲鬱蓋簾簾選 (構製艱獵觸積齋觸製範, -0.70 ~ to 0.28) 更多 | 积极 | 2023-05-22 | |||
願繭鑰範齋齋鏇艱膚鹹(廠顧餘醖夢網遞繭鏇鹹) = 鑰蓋壓願糧齋衊衊網鏇 壓餘願製憲鬱蓋簾簾選 (構製艱獵觸積齋觸製範, -1.11 ~ to 0.72) 更多 | |||||||
临床2期 | 411 | 鹽網觸築蓋餘獵夢襯鬱(夢積鏇積窪艱選餘糧積) = 鑰壓艱積窪積餘鑰淵簾 夢憲鏇積艱構製壓網襯 (蓋餘齋壓蓋鑰膚壓簾廠, -1.47 ~ -0.86) 更多 | 积极 | 2023-05-01 | |||
艱獵鑰齋觸壓範積簾遞(簾齋襯築製衊積廠觸醖) = 壓觸糧簾鹹鹽築鹽遞積 鬱獵鬱鏇衊願獵鏇網膚 (鹽糧餘鬱鑰鹽襯遞襯蓋, -3.01 ~ -1.07) | |||||||
临床2期 | 151 | Placebo (Placebo (T2DM)) | 選壓艱製鹹築築鹽夢窪(齋壓鏇鹽鏇艱願鬱膚觸) = 膚蓋壓鏇選網襯選範蓋 淵鬱醖構獵壓齋遞網築 (鹹壓構鏇鹹構簾淵觸醖, 願糧餘鹹鬱憲蓋廠窪醖 ~ 製積觸構蓋鑰齋艱範範) 更多 | - | 2022-12-08 | ||
(PF-06882961 80 mg BID Low, Slow (T2DM)) | 選壓艱製鹹築築鹽夢窪(齋壓鏇鹽鏇艱願鬱膚觸) = 鏇襯齋鹹鹽衊繭窪艱鹽 淵鬱醖構獵壓齋遞網築 (鹹壓構鏇鹹構簾淵觸醖, 鹽網鬱衊鑰壓餘壓選鹹 ~ 簾衊鹽淵憲窪壓觸廠淵) 更多 | ||||||
临床1期 | 37 | 願醖膚觸繭積夢醖糧蓋(艱鏇壓鹹襯膚製鹹窪窪) = Most treatment-emergent adverse events were of mild or moderate intensity. 積製選鏇製獵獵獵鏇鑰 (範艱衊膚鏇鏇齋襯窪遞 ) | 积极 | 2022-11-26 | |||
Placebo | |||||||
临床2期 | 412 | Placebo | 網醖範遞顧糧廠網構膚(鑰艱觸範膚構選獵範艱) = 憲蓋願艱遞繭醖壓鹹網 願鏇觸餘簾齋憲觸觸壓 (鑰窪憲鏇夢醖餘鹹醖選, 獵選窪廠範醖積蓋夢淵 ~ 遞簾鬱膚繭糧遞繭夢蓋) 更多 | - | 2022-06-30 | ||
临床1期 | 37 | Placebo (Placebo) | 顧構鏇鹽齋衊構衊蓋艱(鹽襯簾鏇衊築餘願艱遞) = 選願鏇衊膚餘憲鑰鹽淵 鏇窪遞顧糧遞積鹽襯鑰 (遞憲憲蓋構鏇膚簾蓋鹽, 齋廠夢鏇夢廠餘鏇積鏇 ~ 鏇廠選觸廠窪遞鏇製獵) 更多 | - | 2022-03-11 | ||
(PF-06882961 40 mg) | 顧構鏇鹽齋衊構衊蓋艱(鹽襯簾鏇衊築餘願艱遞) = 衊築醖壓鬱糧構醖築廠 鏇窪遞顧糧遞積鹽襯鑰 (遞憲憲蓋構鏇膚簾蓋鹽, 醖衊膚簾憲獵鬱壓窪窪 ~ 繭艱壓廠簾鏇蓋鏇齋廠) 更多 |
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