预约演示
更新于：2026-06-27
Elecoglipron
更新于：2026-06-27
概要
基本信息
原研机构 |
非在研机构- |
最高研发阶段临床3期 |
首次获批日期- |
最高研发阶段(中国)临床3期 |
特殊审评- |
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结构/序列
分子式C48H46F2N10O5 |
InChIKeyJMKBTILBGROESC-LITSAYRRSA-N |
CAS号2758659-09-3 |
关联
23
项与 Elecoglipron 相关的临床试验NCT07662213
A Randomized, Open-label, Parallel-group Phase III Study to Evaluate the Efficacy, Safety, and Tolerability of Elecoglipron Compared With Oral Semaglutide in Adults With Type 2 Diabetes Mellitus (Eluminate-2)
NCT07662109
A Randomized, Double-blind, Parallel-group Phase III Study to Evaluate the Efficacy, Safety, and Tolerability of Elecoglipron and Dapagliflozin in Combination, Compared With Elecoglipron Alone and Dapagliflozin Alone, in Adults With Type 2 Diabetes Mellitus (Eluminate-5)
NCT07664553
A Randomized, Double-blind, Parallel-group Phase III Study to Evaluate the Efficacy, Safety, and Tolerability of Elecoglipron Compared With Placebo in Adults With Type 2 Diabetes Mellitus on Background Insulin (Eluminate-3)
100 项与 Elecoglipron 相关的临床结果
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100 项与 Elecoglipron 相关的转化医学
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100 项与 Elecoglipron 相关的专利（医药）
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2
项与 Elecoglipron 相关的文献（医药）2025-02-01DIABETES OBESITY & METABOLISM
Non‐clinical and first‐in‐human characterization of
ECC5004
/
AZD5004
, a novel once‐daily, oral small‐molecule
GLP
‐1 receptor agonist
Article
作者: Wang, Wenyu ; Zhou, Jingye ; Lindmark, Bosse ; Davies, Graeme ; Nelander, Karin ; Wang, Fan ; Xu, Jianfeng ; Chen, Wengang ; Jha, Aruni ; Van Zuydam, Natalie ; Butcher, Laurie ; Lundqvist, Sara ; Wallenius, Kristina ; Ollerstam, Anna ; Pagnussat, Sandra ; Yu, Hongtao ; Haggag, Amina Z. ; Sun, Xuefeng ; Pan, Xiaoliang ; Boianelli, Alessandro ; Liu, Haihui
Abstract:
Aims:
GLP‐1 receptor agonists (GLP‐1 RAs) are proven therapies for type 2 diabetes mellitus (T2DM) and overweight or obesity. We performed non‐clinical and first‐in‐human (FIH) evaluation of ECC5004/AZD5004, an oral small‐molecule GLP‐1 RA.
Materials and Methods:
ECC5004 was profiled in cell lines overexpressing human GLP‐1R, in glucose‐stimulated insulin secretion (GSIS) assays in a human β‐cell line and non‐human primates (NHPs). To evaluate safety, ECC5004 was orally administered to NHPs for 9 months and a phase I, double‐blind, placebo‐controlled FIH study was conducted. This study evaluated single doses of ECC5004 (1–300 mg) in healthy volunteers, and multiple daily doses (5, 10, 30 and 50 mg) in patients with T2DM for 28 days.
Results:
ECC5004 bound to the hGLP‐1R (IC
50
= 2.4 nM) augmented cAMP signalling without β‐arrestin‐2 recruitment or receptor internalization. ECC5004 potentiated GSIS in both EndoC‐βH5 cells (EC
50
= 5.9 nM) and in vivo in NHPs (EC
50
= 0.022 nM). Dose‐dependent body weight changes compared to control were seen in the 9‐month NHP toxicity study. In the first‐in‐human study, ECC5004 was well tolerated with no serious adverse events. Dose‐dependent reductions in glucose and body weight were observed with a dose‐proportional exposure at doses ≥25 mg.
Conclusion:
ECC5004 engaged the GLP‐1R across the therapeutic dose range tested and had a safety and tolerability profile consistent with other GLP‐1 RAs, along with a pharmacokinetic profile compatible with once‐daily oral dosing. These data support continued development of ECC5004 as a potential therapy for T2DM and overweight or obesity.
Clinical trial registration
: NCT05654831.
SCIENTIA PHARMACEUTICA
Oral Small-Molecule GLP-1 Receptor Agonists: Mechanistic Insights and Emerging Therapeutic Strategies
作者: Muciño-Galicia, Axel Eduardo ; Briseño-Díaz, Paola ; Vargas-Camacho, Jorge Arturo ; León-Cabrera, Sonia ; Castañeda-Ramírez, Ari Evelyn ; Saldívar-Cerón, Héctor Iván ; Díaz-Domínguez, María Regina
Small-molecule glucagon-like peptide-1 receptor agonists (GLP-1RAs) represent an innovative advancement in oral therapeutics, addressing key limitations associated with injectable peptide-based incretin therapies. These nonpeptidic agents exert their actions primarily through non-canonical binding orthosteric sites within the GLP-1 receptor transmembrane domain, enabling selective G protein (Gs)-biased signaling with reduced β-arrestin-mediated adverse effects. Orforglipron has notably advanced through Phase 3 clinical development, demonstrating significant reductions in hemoglobin A1c and body weight (up to 7.9%) with favorable tolerability. Conversely, promising candidates such as danuglipron and lotiglipron were discontinued due to hepatotoxicity, underscoring critical safety concerns intrinsic to small-molecule GLP-1RA development. Current clinical candidates, including GSBR-1290, CT-996, and ECC5004, continue to offer substantial potential due to their oral bioavailability, simplified dosing regimens, and favorable gastrointestinal tolerability. Nevertheless, challenges persist regarding hepatic safety, pharmacodynamic variability, and limited long-term outcome data. This review integrates current structural, pharmacological, and clinical evidence, highlights key mechanistic innovations—including biased agonism, covalent binding strategies, and allosteric modulation—and discusses future directions for this rapidly evolving therapeutic class in metabolic disease management.
335
项与 Elecoglipron 相关的新闻（医药）2026-06-26
·医药笔记
抗体药物偶联物临床3期临床2期临床成功临床结果
100 项与 Elecoglipron 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 |
|---|---|---|---|---|
| 2型糖尿病 | 临床3期 | 美国 | 2026-07-06 | |
| 2型糖尿病 | 临床3期 | 中国 | 2026-07-06 | |
| 2型糖尿病 | 临床3期 | 日本 | 2026-07-06 | |
| 2型糖尿病 | 临床3期 | 阿根廷 | 2026-07-06 | |
| 2型糖尿病 | 临床3期 | 澳大利亚 | 2026-07-06 | |
| 2型糖尿病 | 临床3期 | 巴西 | 2026-07-06 | |
| 2型糖尿病 | 临床3期 | 保加利亚 | 2026-07-06 | |
| 2型糖尿病 | 临床3期 | 加拿大 | 2026-07-06 | |
| 2型糖尿病 | 临床3期 | 智利 | 2026-07-06 | |
| 2型糖尿病 | 临床3期 | 捷克 | 2026-07-06 |
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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 | - | - | 選蓋蓋壓夢願鏇簾網遞(膚壓淵顧窪蓋窪襯餘夢) = Dose‐dependent body weight changes compared to control were seen in the 9‐month NHP toxicity study 築糧顧築範網壓構蓋淵 (鏇壓淵憲獵獵遞廠醖蓋 ) 更多 | 积极 | 2025-02-01 | ||
临床1期 | - | AZD5004 50mg | 築齋網願鹹鹹窪觸積鏇(獵獵遞顧蓋製獵鑰醖顧): Difference = -76.6 mg/dL 更多 | 积极 | 2024-11-04 | ||
Placebo | |||||||
临床1期 | - | 願範網齋憲範顧鏇積廠(廠衊築築積製衊鹹壓餘) = None 醖顧鏇遞夢網膚築觸餘 (選淵蓋構網淵遞網艱鹽 ) 更多 | 积极 | 2024-11-04 |
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