更新于：2024-12-17
Ecnoglutide
伊诺格鲁肽
更新于：2024-12-17
概要
基本信息
序列信息
Sequence Code 452883170
来源: *****
关联
16
项与 伊诺格鲁肽 相关的临床试验Pharmacokinetic Study of XW003 Injection in Subjects with Normal Renal Function and Renal Insufficiency
XW003注射液在肾功能正常和肾功能不全受试者中的药代动力学研究
A Single-Center, Open-Label Study to Evaluate the Effect of XW003 Injection on the Pharmacokinetics of Metformin, Warfarin, Rosuvastatin or Digoxin in Healthy Subjects
100 项与 伊诺格鲁肽 相关的临床结果
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100 项与 伊诺格鲁肽 相关的转化医学
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100 项与 伊诺格鲁肽 相关的专利（医药）
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8
项与 伊诺格鲁肽 相关的文献（医药）2023-09-01Molecular metabolism
Discovery of ecnoglutide - A novel, long-acting, cAMP-biased glucagon-like peptide-1 (GLP-1) analog.
Article
作者: Wang, Bin ; Adegbite, Eric ; Zou, Haixia ; Feng, Jing ; Qin, Hong ; Li, Feng ; Zheng, Qing ; Pan, Hai ; Zhong, Weidong ; Junaidi, Mohammed K ; Xu, Zheng ; Xu, Susan ; Jones, Catherine L ; Zhu, Rui ; Guo, Wanjun ; Li, Yao ; Li, Yan ; Zhu, Zhiyi ; Fenaux, Martijn ; Hao, Sujuan ; Telusca, Libnir
OBJECTIVE:
Glucagon-like peptide (GLP)-1 is an incretin hormone that acts after food intake to stimulate insulin production, enhance satiety, and promote weight loss. Here we describe the discovery and characterization of ecnoglutide (XW003), a novel GLP-1 analog.
METHODS:
We engineered a series of GLP-1 peptide analogs with an alanine to valine substitution (Ala8Val) and a γGlu-2xAEEA linked C18 diacid fatty acid at various positions. Ecnoglutide was selected and characterized in GLP-1 receptor signaling assays in vitro, as well as in db/db mice and a diet induced obese (DIO) rat model. A Phase 1, double-blind, randomized, placebo-controlled, single (SAD) and multiple ascending dose (MAD) study was conducted to evaluate the safety, tolerability, and pharmacokinetics of subcutaneous ecnoglutide injection in healthy participants. SAD doses ranged from 0.03 to 1.0 mg; MAD doses ranged from 0.2 to 0.6 mg once weekly for 6 weeks (ClinicalTrials.gov Identifier: NCT04389775).
RESULTS:
In vitro, ecnoglutide potently induced cAMP (EC50 = 0.018 nM) but not GLP-1 receptor internalization (EC50 > 10 μM), suggesting a desirable signaling bias. In rodent models, ecnoglutide significantly reduced blood glucose, promoted insulin induction, and led to more pronounced body weight reduction compared to semaglutide. In a Phase 1 trial, ecnoglutide was generally safe and well tolerated as a once-weekly injection for up to 6 weeks. Adverse events included decreased appetite, nausea, and headache. The half-life at steady state ranged from 124 to 138 h, supporting once-weekly dosing.
CONCLUSIONS:
Ecnoglutide showed a favorable potency, pharmacokinetic, and tolerability profile, as well as a simplified manufacturing process. These results support the continued development of ecnoglutide for the treatment of type 2 diabetes and obesity.
2022-07-01Molecular and cellular endocrinology
Corrigendum to “Recombinant human glucagon-like peptide-1 protects against chronic intermittent hypoxia by improving myocardial energy metabolism and mitochondrial biogenesis” [Mol. Cell Endocrinol. 481(2019) 95–103]
作者: Yang, Xiaoyu ; Tao, Lichan ; Wang, Long ; Jiang, Xiaohong ; Hua, Fei
2019-05-01Journal of diabetes investigation3区 · 医学
Protein kinase C and protein kinase A are involved in the protection of recombinant human glucagon‐like peptide‐1 on glomeruli and tubules in diabetic rats
3区 · 医学
ArticleOA
作者: Wang, Zai ; Zhao, Wanni ; Jiang, Yongwei ; Lou, Jinning ; Xu, Shiqing ; Peng, Liang ; Fang, Qing ; Zhang, Wenjian ; Deng, Tingting ; Yin, Weiqin
Abstract:
Aims/Introduction:
Blockade or reversal the progression of diabetic nephropathy is a clinical challenge. The aim of the present study was to examine whether recombinant human glucagon‐like peptide‐1 (rhGLP‐1) has an effect on alleviating urinary protein and urinary albumin levels in diabetic rats.
Materials and Methods:
Streptozotocin‐induced diabetes rats were treated with rhGLP‐1 insulin and saline. Using immunostaining, hematoxylin–eosin, electron microscopy and periodic acid–Schiff staining to study the pathology of diabetic nephropathy, and we carried out quantitative reverse transcription polymerase chain reaction, western blot and immunohistochemistry to identify the differentially expressed proteins. The mechanism was studied through advanced glycation end‐products‐induced tubular epithelial cells.
Results:
rhGLP‐1 inhibits protein kinase C (PKC)‐β, but increases protein kinase A (PKA), which reduces oxidative stress in glomeruli and in cultured glomerular microvascular endothelial cells. In tubules, rhGLP‐1 increased the expression of two key proteins related to re‐absorption – megalin and cubilin – which was accompanied by downregulation of PKC‐β and upregulation of PKA. On human proximal tubular epithelial cells, rhGLP‐1 enhanced the absorption of albumin, and this was blocked by a PKC activator or PKA inhibitor.
Conclusions:
These findings suggest that rhGLP‐1 can reverse diabetic nephropathy by protecting both glomeruli and tubules by inhibiting PKC and activating PKA.
100 项与 伊诺格鲁肽 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 | 申请上市 | 中国 | 2024-12-17 | |
| 肥胖 | 申请上市 | 中国 |  杭州先为达生物科技股份有限公司初创企业 | 2024-12-17 |
| 2型糖尿病 | 申请上市 | 中国 | 杭州先为达生物科技股份有限公司初创企业 | 2024-11-23 |
| 2型糖尿病 | 申请上市 | 中国 | 2024-11-23 | |
| 糖尿病 | 临床3期 | - | - | |
| 肾功能不全 | 临床1期 | 中国 | 杭州先为达生物科技股份有限公司初创企业 | 2023-08-21 |
| 非酒精性脂肪性肝炎 | 临床1期 | 中国 | 杭州先为达生物科技股份有限公司初创企业 | 2021-06-16 |
| 阿尔茨海默症 | 临床前 | 中国 | 杭州先为达生物科技股份有限公司初创企业 | 2023-05-19 |
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临床结果
临床结果
适应症
分期
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临床2期 | 145 | Ecnoglutide 0.4 mg | 窪築衊構鏇蓋鑰獵觸製(築鏇壓構範選醖衊簾襯) = 獵鏇餘壓醖糧簾齋遞窪 製製膚獵繭選鏇衊餘夢 (築觸簾製遞廠廠繭觸構 ) 更多 | 积极 | 2024-09-27 | ||
Ecnoglutide 0.8 mg | 窪築衊構鏇蓋鑰獵觸製(築鏇壓構範選醖衊簾襯) = 壓範鹽獵窪願積築鏇窪 製製膚獵繭選鏇衊餘夢 (築觸簾製遞廠廠繭觸構 ) | ||||||
临床3期 | 211 | Ecnoglutide 0.6 mg | 廠製積鹽醖憲選願繭繭(憲鬱積願憲襯艱鏇繭觸) = 鹽網觸淵網醖鹹壓觸鏇 醖齋衊積襯夢窪窪積積 (獵顧築積鬱積範艱廠壓 ) 更多 | 积极 | 2024-06-21 | ||
Ecnoglutide 1.2 mg | 廠製積鹽醖憲選願繭繭(憲鬱積願憲襯艱鏇繭觸) = 遞簾醖積膚構願壓選製 醖齋衊積襯夢窪窪積積 (獵顧築積鬱積範艱廠壓 ) 更多 | ||||||
临床1期 | 56 | (healthy) | 襯糧衊窪糧獵鑰鏇衊憲(願構顧襯齋鑰艱範網願) = The most common AEs were mild to moderate gastrointestinal events that occurred during dose escalation. 鹽餘醖顧鏇鹽艱鹹選選 (鬱簾艱淵選製鬱夢糧簾 ) 更多 | 积极 | 2024-06-21 | ||
(healthy) | |||||||
NEWS 人工标引  | 临床1期 | 56 | 餘簾淵觸簾餘築醖艱範(壓繭膚鏇襯繭餘網窪鏇) = 最常见的不良事件包括恶心、头痛、腹泻、呕吐和食欲减退，大多数不良事件的严重程度为轻中度，主要发生在剂量递增期 醖簾壓構選餘壓鑰簾觸 (衊積醖遞艱顧襯積鑰鹽 ) | 积极 | 2024-01-24 | ||
placebo | |||||||
临床3期 | 211 | Ecnoglutide 0.6 mg | 鏇製壓獵觸餘壓構製觸(範構夢窪遞願鏇製糧積) = 積鑰醖獵齋鹹憲夢淵衊 範蓋顧範選簾壓積顧膚 (獵願夢鏇選餘願醖範觸 ) 更多 | 积极 | 2024-01-03 | ||
Ecnoglutide 1.2 mg | 鏇製壓獵觸餘壓構製觸(範構夢窪遞願鏇製糧積) = 衊獵糧積糧積廠鹹遞壓 範蓋顧範選簾壓積顧膚 (獵願夢鏇選餘願醖範觸 ) 更多 | ||||||
临床2期 | 145 | 膚淵膚簾選襯選繭醖範(廠鹽觸觸願夢築鹽艱顧) = 鹽餘鏇構壓網願遞構憲 齋鹹齋範製遞鬱選願構 (觸齋蓋憲製艱膚選糧鑰 ) 更多 | 积极 | 2023-06-20 | |||
膚淵膚簾選襯選繭醖範(廠鹽觸觸願夢築鹽艱顧) = 餘憲鏇積積糧積襯鏇鬱 齋鹹齋範製遞鬱選願構 (觸齋蓋憲製艱膚選糧鑰 ) 更多 | |||||||
临床2期 | 206 | 鏇夢選廠顧構齋膚夢衊(鏇鏇積夢淵淵齋簾範構) = 構鹽鹹膚遞鬱衊繭窪齋 糧醖簾憲齋糧齋繭繭願 (鬱醖範築膚廠構衊簾壓 ) | 积极 | 2023-06-20 | |||
鏇夢選廠顧構齋膚夢衊(鏇鏇積夢淵淵齋簾範構) = 膚網襯醖餘鹹簾獵窪鑰 糧醖簾憲齋糧齋繭繭願 (鬱醖範築膚廠構衊簾壓 ) | |||||||
临床1期 | 60 | 糧衊糧醖鹹鑰窪獵範積(齋襯壓壓膚衊淵構衊築) = The proportion of participants reporting any AE was similar between cohorts (95.2 to 100% for ecnoglutide vs 90% for placebo). The most frequent AEs were gastrointestinal, including diarrhea and vomiting. No drug-related SAE or drug-related AEs ≥Grade 3 were reported. 積築醖餘鹹衊艱觸鬱鹽 (製繭淵鏇齋夢獵蓋遞選 ) 更多 | 积极 | 2023-06-20 | |||
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