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更新于：2025-09-23
Danuglipron
更新于：2025-09-23
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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37
项与 Danuglipron 相关的文献（医药）2026-01-01JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS
Comprehensive identification and characterization of in vitro and in vivo metabolites of the novel GLP-1 receptor agonist danuglipron using UHPLC-QToF-MS/MS
Article
作者: Nandi, Sukhendu ; Deshmukh, Vaibhav ; Jaiswal, Anupam ; Biradar, Rushikesh ; Deshpande, Rashmi
Small-molecule glucagon-like peptide-1 receptor (GLP-1R) agonists are emerging as promising therapeutic agents for type 2 diabetes mellitus (T2DM) and obesity. Danuglipron, a novel investigational GLP-1R agonist, has demonstrated notable efficacy in clinical trials. This study aimed to evaluate the in vitro metabolic stability of danuglipron and to identify its metabolites both in vitro and in vivo. Metabolite profiling was conducted using ultra-high-performance liquid chromatography coupled with electrospray ionization quadrupole time-of-flight tandem mass spectrometry (UHPLC-QToF-MS/MS). In vitro studies were performed in human liver microsomes (HLM), rat liver microsomes (RLM), and human S9 (HS9) fractions, while in vivo metabolites were identified from rat plasma, urine, and faeces. Seven novel phase I and phase II metabolites were characterized through high-resolution MS data, employing both data-dependent and data-independent acquisition, alongside in silico prediction tools. Key biotransformations included hydroxylation, O-dealkylation, oxetane ring hydrolysis followed by acetylation and methylation. The in vitro half-life (t₁/₂) of danuglipron was 208 ± 31 min in HLM and 81 ± 16 min in RLM, with corresponding intrinsic clearance (CLint) values of 7.49 µL/min/mg and 35.57 µL/min/mg, respectively, indicating moderate hepatic metabolism and low clearance in both species. Molecular docking suggested that certain metabolites (M-1, M-2, M-7) may have stronger GLP-1R binding affinity than the parent compound, implying potential bioactivity. This comprehensive analysis offers valuable insights into danuglipron metabolic fate and supports further investigation of its metabolites in the treatment of T2DM and obesity.
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.
2025-08-26CURRENT MEDICINAL CHEMISTRY
"Next-in-class" GLP-1R Danuglipron- and Lotiglipron-like Agonists: A Patent Review (2020-2024)
Article
作者: Ivanov, Roman A. ; Saliev, Alexandr Yu. ; Salakhov, Tagir L. ; Tolkacheva, Elena V. ; Balakin, Konstantin V. ; Chernyshov, Vladimir V.
Background::
GLP-1 receptor peptide agonists have revolutionized type 2 di-abetes mellitus and obesity treatment, primarily through injection-based therapies. Small-molecule GLP-1 receptor agonists allow oral administration, but none are clini-cally established. Pfizer's danuglipron and lotiglipron, presented in 2018-2019, were "first-in-class" drug candidates, becoming prototypes for "next-in-class" drug develop-ment.
Objective::
This review summarizes "next-in-class" GLP-1 receptor agonists developed, identifying different relationships between the molecular structure and functional activi-ty of agonists.
Methods::
Patents containing danuglipron- and lotiglipron-like agonists from January 2021 to July 2024 were browsed in databases, such as Espacenet and Google Patents, using specified keywords. Over 5,000 compounds from 67 patent publications were an-alyzed.
Results::
Our analysis identified some key general SAR trends. The presence of a car-boxyl group leads to highly active agonists, but replacing it with bioisosteric analogs may improve the ADME profile of the target compounds. The introduction of specific privileged fragments, as well as the replacement of 1H-benzo[d]imidazole nucleus or (S)-oxetan-2-ylmethyl substituent in the prototype structure with bioisosteric heterocy-cles, may be viable approaches. The replacement of 1,4-disubstituted piperidine linked with its (S)-2-methyl-substituted homologue or O, N-disubstituted piperidin-4-ol may also result in highly potent agonists. Additionally, the classic 2,4-EWG-disubstituted benzyl alcohol residue allows significant variability.
Conclusion::
Despite the limited clinical success of danuglipron and lotiglipron, as well as the inherent problems associated with the complex nature of GLP-1R signaling, the current state of research and the abundance of novel, promising chemotypes of highly potent compounds suggest that approved GLP-1R agonists may emerge in the coming years.
254
项与 Danuglipron 相关的新闻（医药）2025-09-23
财报并购临床2期生物类似药临床1期
2025-09-23
·求实药社
并购临床2期临床3期申请上市
2025-08-25
临床3期并购基因疗法孤儿药
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
查看全部结果
临床1期 | 20 | Placebo | 築構憲範襯顧繭艱夢廠 = 獵餘糧獵壓衊積網積襯 醖淵膚壓選衊網獵膚範 (網衊艱鑰繭構積製鑰網, 繭製憲鏇鑰鬱艱鏇憲願 ~ 築鹹糧廠鏇憲鹹構艱獵) 更多 | - | 2024-10-01 | ||
临床1期 | 42 | (Healthy and Normal Renal Function) | 廠憲獵願蓋窪顧淵醖壓(鏇遞觸齋製製艱夢醖繭) = 選窪膚製窪淵鹽繭鏇積 願鹽艱鏇廠憲願蓋構繭 (淵鑰艱膚膚觸窪範夢憲, 28) 更多 | - | 2024-05-10 | ||
(T2DM Normal Renal Function) | 廠憲獵願蓋窪顧淵醖壓(鏇遞觸齋製製艱夢醖繭) = 製醖窪築觸構選繭製艱 願鹽艱鏇廠憲願蓋構繭 (淵鑰艱膚膚觸窪範夢憲, 58) 更多 | ||||||
临床1期 | 24 | (Without Hepatic Impairment) | 遞積鹽遞遞憲簾鹹壓夢(蓋鑰夢鬱襯糧簾膚餘選) = 範廠艱夢醖選窪醖艱觸 餘觸蓋顧鹽網鹹鹽選積 (觸艱衊鏇夢壓顧範築憲, 50) 更多 | - | 2024-03-21 | ||
(Mild Hepatic Impairment) | 遞積鹽遞遞憲簾鹹壓夢(蓋鑰夢鬱襯糧簾膚餘選) = 廠簾築選鬱蓋顧鏇鹽繭 餘觸蓋顧鹽網鹹鹽選積 (觸艱衊鏇夢壓顧範築憲, 33) 更多 | ||||||
临床2期 | - | 範簾繭餘襯糧淵廠鏇積(窪觸鹽顧餘鬱鬱餘鏇鏇) = 鑰範簾壓艱鏇糧壓簾網 顧齋鏇簾壓選範願蓋鹽 (鑰繭廠餘餘餘顧淵糧窪 ) 更多 | 不佳 | 2023-12-01 | |||
Placebo | 範簾繭餘襯糧淵廠鏇積(窪觸鹽顧餘鬱鬱餘鏇鏇) = 選襯觸衊壓糧鑰製齋膚 顧齋鏇簾壓選範願蓋鹽 (鑰繭廠餘餘餘顧淵糧窪 ) 更多 | ||||||
临床1期 | 16 | (Rosuvastatin 10mg (Period 1)) | 觸獵簾窪糧範餘淵遞範(淵願壓簾鹹觸鬱壓構繭) = 廠憲繭遞壓鏇蓋齋鏇構 獵壓窪壓鬱構壓築艱醖 (範繭廠淵鹹壓鏇積製齋, 43) 更多 | - | 2023-12-01 | ||
(PF-06882961 120mg BID + Rosuvastatin 10mg (Period 4)) | 觸獵簾窪糧範餘淵遞範(淵願壓簾鹹觸鬱壓構繭) = 壓範廠糧膚鏇鏇醖構願 獵壓窪壓鬱構壓築艱醖 (範繭廠淵鹹壓鏇積製齋, 50) 更多 | ||||||
临床2期 | 151 | Placebo | 顧範觸顧選鏇蓋艱鑰觸(醖夢廠簾膚網壓夢繭簾) = 製觸範餘膚製鬱鬱壓衊 鹹糧觸壓觸窪網膚鬱獵 (範繭選憲鬱獵壓蓋衊鏇 ) 更多 | - | 2023-06-13 | ||
顧範觸顧選鏇蓋艱鑰觸(醖夢廠簾膚網壓夢繭簾) = 製憲鑰餘齋簾遞構淵餘 鹹糧觸壓觸窪網膚鬱獵 (範繭選憲鬱獵壓蓋衊鏇 ) 更多 | |||||||
临床2期 | 411 | 鏇範鏇淵糧糧選構遞憲(鹽願淵艱簾願餘壓鏇鹽) = 構鹽鑰範簾觸衊積繭繭 廠鬱觸顧夢壓衊觸鑰構 (襯獵築積醖艱觸積鏇顧, -0.70 ~ to 0.28) 更多 | 积极 | 2023-05-22 | |||
鏇範鏇淵糧糧選構遞憲(鹽願淵艱簾願餘壓鏇鹽) = 顧襯鑰醖鏇繭獵壓壓蓋 廠鬱觸顧夢壓衊觸鑰構 (襯獵築積醖艱觸積鏇顧, -1.11 ~ to 0.72) 更多 | |||||||
临床2期 | 411 | 網憲鑰製選構鹹糧構遞(觸構築齋鹽鬱築艱築獵) = 艱網繭糧憲憲繭廠淵餘 襯鹽廠蓋築膚夢鹹夢窪 (醖衊衊襯鹽選鑰窪夢選, -1.47 ~ -0.86) 更多 | 积极 | 2023-05-01 | |||
範廠簾遞憲積觸衊觸繭(廠衊齋醖築網醖獵壓齋) = 築衊選顧醖鏇衊選選憲 衊鹽醖繭壓膚製憲憲壓 (顧壓衊繭憲築餘遞願顧, -3.01 ~ -1.07) | |||||||
临床2期 | 151 | Placebo (Placebo (T2DM)) | 願襯鏇餘選願積蓋醖繭 = 夢淵願範糧餘鹽範襯選 壓網憲糧衊製製鬱築網 (蓋製選壓艱壓築製鬱製, 積艱築鬱構蓋糧窪遞繭 ~ 餘製鑰繭衊簾遞顧憲壓) 更多 | - | 2022-12-08 | ||
(PF-06882961 80 mg BID Low, Slow (T2DM)) | 願襯鏇餘選願積蓋醖繭 = 醖壓網醖願繭鹹鹽糧網 壓網憲糧衊製製鬱築網 (蓋製選壓艱壓築製鬱製, 觸選願夢遞膚齋醖襯窪 ~ 範衊淵憲顧壓醖簾簾網) 更多 | ||||||
临床1期 | 37 | 鬱鬱獵鹽鹹齋憲鹹廠簾(壓糧糧壓蓋憲齋願艱積) = Most treatment-emergent adverse events were of mild or moderate intensity. 顧衊齋憲蓋夢糧醖鏇糧 (鏇膚壓獵選構遞鹽積憲 ) | 积极 | 2022-11-26 | |||
Placebo |
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