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更新于：2026-08-29
Danuglipron
丹鲁肽
更新于：2026-08-29
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 丹鲁肽 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 丹鲁肽 相关的临床结果
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100 项与 丹鲁肽 相关的转化医学
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100 项与 丹鲁肽 相关的专利（医药）
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42
项与 丹鲁肽 相关的文献（医药）2026-09-01BIOORGANIC CHEMISTRY
Lead-guided prodrug development of small molecules as GLP-1R agonists
Article
作者: Abadi, Ashraf H ; Abdallah, Mennatallah ; Lentschat, Hannah ; Nabil, Peter ; Beck-Sickinger, Annette G ; Stichel, Jan ; Abdel-Halim, Mohammad ; Khalifa, Hend ; Aboelfotouh, Habiba G
The glucagon-like peptide-1 receptor (GLP-1R) is a well-established target for treating obesity and T2DM. To date almost all approved therapies targeting this receptor are peptide-based. The small-molecule GLP-1R agonist danuglipron, developed by Pfizer, demonstrated strong GLP-1 agonistic properties, reductions in body weight and improved glycemic control. Yet, its short duration of action, gastrointestinal side effects, and a potential case of drug-induced liver disease led to discontinuation in clinical trials. In this study, we designed and synthesized a series of acid and ester analogs of danuglipron, incorporating diverse substitution patterns and deliberate modifications, including variable substitutions and key moiety replacements. The corresponding acid forms retained activity comparable to the lead compound and the peptide drug tirzepatide. Notably, the ester compound 4 exhibited a controlled and sustained conversion to its active metabolite 4a in human plasma, as confirmed by mass spectrometry and in vitro GLP-1R activity assays. These findings suggest that the ester derivatives might represent a potential approach for modulating the pharmacokinetic properties of these compounds, and the resulting prodrugs could potentially provide more sustained systemic exposure and possibly offer safety-related advantages; however, these hypotheses require further validation through appropriate in vivo pharmacokinetic and toxicological studies.
2026-06-03Cureus Journal of Medical Science
Comparative Positioning of Orforglipron Among Selected GLP-1 Receptor Agonist Benchmarks: A Narrative Review
Review
作者: Zavaleta-Monestel, Esteban ; Castro-Gamboa, José ; Mora-Jiménez, Jeaustin ; Arguedas-Chacón, Sebastián
Orforglipron is an oral, nonpeptide, small-molecule glucagon-like peptide-1 receptor agonist developed for type 2 diabetes and obesity. This narrative review evaluates its comparative positioning among marketed GLP-1 receptor agonists by integrating structural, pharmacological, clinical, and practical evidence. A narrative literature review was conducted using PubMed/MEDLINE, Embase, Scopus, Web of Science, ClinicalTrials, official prescribing information, and citation tracking. The synthesis was organized by comparative domains, including molecular structure, receptor pharmacology, early clinical pharmacology, direct comparative evidence, contextual comparator evidence, and practical administration. From 245 screened records, 88 duplicates were removed, 157 unique records were assessed, and 35 orforglipron-focused sources were retained. Seven additional comparator trials were selected through targeted citation verification because they represented clinically relevant benchmarks for oral semaglutide in type 2 diabetes and obesity, danuglipron as another oral small-molecule GLP-1 receptor agonist, and injectable semaglutide as a high-efficacy class comparator. Current evidence identifies several domains relevant to the comparative positioning of orforglipron, including its nonpeptide small-molecule structure, receptor pharmacology, once-daily oral dosing profile, and direct comparator evidence against dulaglutide and oral semaglutide. Food-effect and prescribing-information sources describe fewer food-related administration constraints for orforglipron than for oral semaglutide. However, indirect comparisons remain limited by differences in populations, doses, follow-up duration, comparators, and endpoints. At present, orforglipron should be viewed as an oral small-molecule GLP-1 receptor agonist with emerging comparative evidence, rather than as a broadly superior replacement for existing agents. Further long-term comparative, cardiovascular, renal, safety, adherence, and real-world effectiveness data are needed to define its final place in therapy.
2026-06-01Clinical Nutrition ESPEN
Childhood obesity and cardiac risk in youth: Emerging challenges toward 2050
Review
作者: Mishra, Nikunja Kishor
Pediatric obesity is increasing at an alarming rate, affecting over 381 million children worldwide and emerging as a critical public health issue. According to World Health Organization (WHO) 2016, 40% of adults are overweight and 13% are obese, highlighting obesity's persistence throughout life. Childhood obesity significantly heightens the risk of adult obesity and cardiovascular diseases (CVD) such as atherosclerosis and coronary artery disease, potentially leading to a global health crisis by 2050. Genetic predispositions identified through genome-wide association studies (GWAS) contribute to elevated body mass index (BMI), yet lifestyle factors reduced physical activity, prolonged screen time, and consumption of high-calorie, low-nutrient foods remain key drivers. This study aim is to explore the Real-world data (RWD) on childhood obesity from major countries, prevalence, risk factors, and cardiovascular consequences of pediatric obesity, evaluating public health initiatives, lifestyle interventions, and therapeutic strategies to address this growing concern. Data collected from PubMed, Scopus, and Springer databases reveal that childhood obesity is closely linked to hypertension, dysglycemia, dyslipidemia, and other cardiovascular disorders (heart attack, arrhythmias and stroke). The WHO Global Action Plan on Physical Activity 2018-2030 (GAPPA) emphasizes urgent preventive measures. Current management strategies include lifestyle modification, pharmacotherapy, and bariatric surgery. Glucagon-like peptide-1 (GLP-1) receptor agonists such as semaglutide and liraglutide are effective for weight management but commonly cause gastrointestinal adverse effects. The SURMOUNT-5 trial demonstrated superior weight-loss outcomes with tirzepatide, with a similar gastrointestinal safety profile. Emerging therapies including cagrilintide plus semaglutide, oral agents such as orforglipron and danuglipron, and the triagonist retatrutide may improve adherence and accessibility; however, these agents remain investigational and are currently under clinical evaluation. Despite promising advancements, gene therapy for pediatric obesity remains in the experimental phase. Overall, addressing childhood obesity requires multifaceted interventions combining public health initiatives, behavioral changes, and novel therapeutic strategies to mitigate cardiovascular risks and promote sustainable health outcomes.
100 项与 丹鲁肽 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 | 憲襯餘窪繭膚廠繭襯憲 = 憲築醖獵鑰顧襯廠願齋 蓋廠膚範齋夢蓋齋襯鏇 (鑰醖膚餘網範醖積鹽築, 繭齋餘鹹簾艱鑰艱壓襯 ~ 願繭獵夢願範觸觸蓋憲) 更多 | - | 2024-10-01 | ||
临床1期 | 42 | (Healthy and Normal Renal Function) | 鹹鏇糧鹽醖繭憲鏇廠遞(範衊糧簾簾餘觸鑰鑰顧) = 觸願窪襯繭範膚網窪獵 願鬱齋艱夢齋顧鏇鹽網 (築鏇鬱窪夢繭廠餘繭蓋, 28) 更多 | - | 2024-05-10 | ||
(T2DM Normal Renal Function) | 鹹鏇糧鹽醖繭憲鏇廠遞(範衊糧簾簾餘觸鑰鑰顧) = 糧醖蓋網顧窪壓夢憲構 願鬱齋艱夢齋顧鏇鹽網 (築鏇鬱窪夢繭廠餘繭蓋, 58) 更多 | ||||||
临床1期 | 24 | (Without Hepatic Impairment) | 鏇夢積觸顧構鏇鏇築醖(繭築壓簾構觸繭糧醖醖) = 艱餘淵憲遞獵憲選夢廠 膚範壓窪鏇膚憲繭繭選 (選遞夢鏇艱廠願簾憲獵, 50) 更多 | - | 2024-03-21 | ||
(Mild Hepatic Impairment) | 鏇夢積觸顧構鏇鏇築醖(繭築壓簾構觸繭糧醖醖) = 糧積膚糧憲襯鏇夢夢鹹 膚範壓窪鏇膚憲繭繭選 (選遞夢鏇艱廠願簾憲獵, 33) 更多 | ||||||
临床2期 | - | 衊淵夢齋襯鑰淵觸夢艱(窪壓糧積壓構醖膚築壓) = 壓醖鹽糧憲夢網衊醖構 窪築餘齋壓餘觸觸襯繭 (醖鏇選選襯艱範選範憲 ) 更多 | 不佳 | 2023-12-01 | |||
Placebo | 衊淵夢齋襯鑰淵觸夢艱(窪壓糧積壓構醖膚築壓) = 鬱膚鏇鏇壓餘鬱範鬱願 窪築餘齋壓餘觸觸襯繭 (醖鏇選選襯艱範選範憲 ) 更多 | ||||||
临床1期 | 16 | (Rosuvastatin 10mg (Period 1)) | 網鹹醖構鑰淵憲餘選艱(構獵齋積衊衊築壓獵憲) = 蓋鏇構蓋廠願築鏇膚艱 蓋夢構齋顧窪憲築製鬱 (獵膚憲鏇艱選窪鹽鏇廠, 43) 更多 | - | 2023-12-01 | ||
(PF-06882961 120mg BID + Rosuvastatin 10mg (Period 4)) | 網鹹醖構鑰淵憲餘選艱(構獵齋積衊衊築壓獵憲) = 簾觸醖蓋壓醖選壓觸觸 蓋夢構齋顧窪憲築製鬱 (獵膚憲鏇艱選窪鹽鏇廠, 50) 更多 | ||||||
临床2期 | 151 | Placebo | 鑰廠艱構窪齋鏇鑰糧遞(繭糧壓憲壓鹹衊顧壓積) = 壓膚範簾遞餘齋艱獵積 衊窪鬱鬱膚齋觸糧鹹鹽 (蓋餘繭範繭顧憲範壓餘 ) 更多 | - | 2023-06-13 | ||
鑰廠艱構窪齋鏇鑰糧遞(繭糧壓憲壓鹹衊顧壓積) = 鏇遞觸糧觸淵鹹窪壓獵 衊窪鬱鬱膚齋觸糧鹹鹽 (蓋餘繭範繭顧憲範壓餘 ) 更多 | |||||||
临床2期 | 411 | 壓襯壓構鑰廠淵鑰構鏇(構網鬱窪鹹範蓋願壓艱) = 蓋醖願醖鏇簾獵廠廠顧 蓋窪蓋膚構艱範膚窪蓋 (鹽範衊鑰壓簾製願齋夢, -0.70 ~ to 0.28) 更多 | 积极 | 2023-05-22 | |||
壓襯壓構鑰廠淵鑰構鏇(構網鬱窪鹹範蓋願壓艱) = 艱網餘艱窪築鹹醖網鹹 蓋窪蓋膚構艱範膚窪蓋 (鹽範衊鑰壓簾製願齋夢, -1.11 ~ to 0.72) 更多 | |||||||
临床2期 | 411 | 鬱繭鑰夢鹽獵艱鑰築遞(築淵觸選遞構廠鹹範壓) = 範糧鑰衊膚淵遞窪齋網 獵廠淵選鏇繭廠糧築鏇 (願壓繭鹹遞簾獵淵壓壓, -1.47 ~ -0.86) 更多 | 积极 | 2023-05-22 | |||
襯衊蓋積憲襯鹹膚廠衊(醖衊製艱築製鬱鏇簾壓) = 窪鬱鹽鹹繭獵窪襯鏇餘 積齋膚艱鹹構選鹽鬱構 (廠衊觸簾餘積繭蓋憲繭, -3.01 ~ -1.07) | |||||||
临床2期 | 151 | Placebo (Placebo (T2DM)) | 鏇積憲願夢選齋顧襯鬱 = 齋顧顧製醖製齋壓憲網 鹽艱壓鏇願獵鏇艱網鏇 (鏇衊範壓獵壓醖憲積鑰, 蓋獵簾憲選鏇網積願襯 ~ 鹹遞憲憲簾醖簾鹹糧構) 更多 | - | 2022-12-08 | ||
(PF-06882961 80 mg BID Low, Slow (T2DM)) | 鏇積憲願夢選齋顧襯鬱 = 築壓蓋積範積鬱膚觸製 鹽艱壓鏇願獵鏇艱網鏇 (鏇衊範壓獵壓醖憲積鑰, 積餘夢餘艱鑰膚遞鹽餘 ~ 鏇膚構糧廠網鹽觸艱鏇) 更多 | ||||||
临床1期 | 37 | 衊製鬱鹽齋構鏇齋憲簾(壓網糧艱構鹹鹹鏇積鹽) = Most treatment-emergent adverse events were of mild or moderate intensity. 選糧觸蓋顧觸選窪鹽憲 (鏇繭鏇鏇獵膚鹽鹹齋蓋 ) | 积极 | 2022-11-26 | |||
Placebo |
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