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更新于：2026-01-01
Chiglitazar Sodium
西格列他钠
更新于：2026-01-01
概要
基本信息
原研机构 |
非在研机构- |
最高研发阶段批准上市 |
首次获批日期 中国 (2021-10-22), |
最高研发阶段(中国)批准上市 |
特殊审评- |
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结构/序列
分子式C36H29FN2NaO4 |
InChIKeyOLGOEMXTBDXFQX-UCRKPPETSA-N |
CAS号2390374-10-2 |
关联
32
项与 西格列他钠 相关的临床试验NCT07303803
Chiglitazar in Combination With Anti-Inflammatory and Hepatoprotective Therapy for the Treatment in MASH Associated With T2DM: a Prospective, Multicentre, Randomised, Double-blind, Placebo-controlled Study
ChiCTR2500113673
Chiglitazar combination with anti-inflammatory and hepatoprotective therapy for the treatment in MASH associated with T2DM: a prospective, multicentre, randomised, double-blind, placebo-controlled study
ChiCTR2500099866
A multicenter, randomized controlled study of silymarin and chiglitazar sodium in patients with T2DM and MASLD
100 项与 西格列他钠 相关的临床结果
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100 项与 西格列他钠 相关的转化医学
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100 项与 西格列他钠 相关的专利（医药）
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200
项与 西格列他钠 相关的文献（医药）2026-02-01COMPUTATIONAL BIOLOGY AND CHEMISTRY
GC/MS analysis and computational evaluation of C. cinerea EO constituents for colorectal cancer: Molecular docking, dynamics, and quantum chemical insights into Cis-Verbenyl acetate
Article
作者: Bekkar, Yahia ; Bouraoui, Rania ; Neghmouche Nacer, Salah ; Lanez, Touhami ; Bourougaa, Lotfi ; Lanez, Elhafnaoui ; Garzoli, Stefania ; Larbi Benamor, Mohammed ; Samah, Bouchagra
The essential oil of Cotula cinerea was subjected to gas chromatography-mass spectrometry (GC-MS) analysis, leading to the identification of 31 chemical constituents. The major compounds were selected for comprehensive computational investigations to explore their potential anti-colorectal cancer activity. Among the identified constituents, cis-verbenyl acetate (CVA) exhibited the most favorable binding affinities across a panel of fifteen protein targets implicated in colorectal cancer. Notably, Tankyrase1 (PDB ID: 4OA7) and Tankyrase2 (PDB ID: 4UFU) emerged as the most promising targets, with docking scores of -9.49 and -8.46 kcal/mol, respectively. Molecular dynamics simulations conducted over 300 nanoseconds demonstrated the structural stability and sustained interactions of the CVA-protein complexes, characterized by low root mean square deviation (RMSD) values and limited conformational fluctuations. These findings were corroborated by molecular mechanics Poisson-Boltzmann surface area (MM-PBSA) calculations, which revealed highly favorable binding free energies, particularly in the CVA- TNKS2 complex (ΔGtotal = -45.64 kcal/mol). In silico ADMET profiling indicated high oral bioavailability and low predicted toxicity for CVA compared to native ligands. Furthermore, density functional theory (DFT) analysis provided insight into the electronic properties of CVA, revealing a stable electronic configuration, suitable frontier molecular orbital energies, and a well-distributed electrostatic potential surface. Thermodynamic evaluations supported its chemical stability, showing a consistent increase in entropy, enthalpy, and heat capacity with rising temperature. Collectively, these computational findings suggest that CVA is a thermodynamically stable, pharmacokinetically favorable, and potentially bioactive compound with dual-target affinity against colorectal cancer-related proteins, meriting further experimental validation.
2025-12-01JOURNAL OF COMPUTER-AIDED MOLECULAR DESIGN
Holistic investigation of Cotula cinerea essential oil against diabetes: hypoglycemic activity, enzymatic inhibition, GC-MS characterization, ADMET forecasting, MD simulations, and DFT insights
Article
作者: Bekkar, Yahia ; Bouraoui, Rania ; Boudebia, Ouafa ; Bourougaa, Lotfi ; Benamor, Mohammed Larbi ; Chaoua, Housseyn ; Lanez, Touhami ; Lanez, Elhafnaoui ; Nesba, Kaouther ; Bechki, Lazhar ; Hachani, Salah Eddine ; Adaika, Aicha
Diabetes mellitus is a prevalent metabolic disorder characterized by impaired glucose metabolism. This study investigates the anti-diabetic potential of Cotula cinerea essential oil (EO) through in vivo, in vitro, and computational methodologies. In vitro enzyme inhibition assays demonstrated that C. cinerea EO effectively inhibits α-amylase and α-glucosidase, indicating its potential role in glucose regulation. In vivo studies further confirmed its hypoglycemic effects. GC-MS analysis identified 31 bioactive compounds within the EO. Molecular docking studies revealed that six of these compounds exhibited strong binding affinities to α-amylase and α-glucosidase, comparable to those of the standard drug acarbose (ARE). Among them, cis-verbenyl acetate (CVA) and β-terpineol (βTP) showed the highest docking scores against both enzymes. ADMET analysis confirmed their favorable pharmacokinetic properties, drug-likeness, and low toxicity risks. Molecular dynamics simulations demonstrated the stable binding of CVA and βTP with both enzymes, exhibiting lower RMSD and RMSF values compared to ARE, along with favorable Rg and SASA parameters. MM-PBSA calculations further validated their strong binding affinities. Density Functional Theory calculations provided deeper insights into the electronic characteristics of CVA and βTP, revealing their frontier molecular orbitals distributions and energy gap (∆E) values. The molecular electrostatic potential analysis identified key electron-rich and electron-deficient regions, suggesting potential interaction sites with the target enzymes. The observed reduction in ∆E values under aqueous conditions indicated increased molecular stability and reactivity within physiological environments, further supporting their role in enzyme inhibition. Overall, this study highlights C. cinerea EO as a promising natural source for diabetes management. The integration of in vivo, in vitro, and computational approaches offers compelling evidence for its therapeutic potential. Nevertheless, further experimental validation is necessary to assess its clinical applicability.
2025-12-01BIOMEDICINE & PHARMACOTHERAPY
Chiglitazar, a PPAR pan-agonist: Impacts on type 2 diabetes mellitus and multi-system metabolic regulation – A review
Review
作者: Wei, Wei ; Zhou, Xiqiao ; Zhu, Yiran ; Lou, Yan ; Lv, Tiansu ; Chang, Ee ; Huai, Jiaxuan
Type 2 diabetes mellitus (T2DM) is a prevalent chronic metabolic disorder with multifactorial pathogenesis involving genetic predisposition, environmental influences, and dietary habits. Insulin resistance represents a central pathophysiological mechanism. Current evidence suggests that peroxisome proliferator-activated receptors (PPARs)-including PPARα, PPARδ, and PPARγ-can effectively ameliorate insulin resistance and associated metabolic syndromes; however, overstimulation of a single receptor subtype may lead to adverse effects. As a novel pan-PPAR agonist, chiglitazar achieves balanced activation of all three PPAR subtypes, providing significant glycemic control while exhibiting potential therapeutic benefits for metabolic-associated steatohepatitis (MASH), dyslipidemia, and other metabolism-related systemic disorders, thereby demonstrating superior metabolic regulatory properties. This review examines the interplay between T2DM and PPARs, explores the pharmacological mechanisms, clinical efficacy, and safety profile of chiglitazar, and highlights its multi-system metabolic benefits beyond glycemic control. These findings provide theoretical and practical insights supporting its clinical application in T2DM and related metabolic disorders.
100 项与 西格列他钠 相关的药物交易
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研发状态
批准上市
10 条最早获批的记录, 后查看更多信息
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| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| 2型糖尿病 | 中国 | 2021-10-22 |
未上市
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 |
|---|---|---|---|---|
| 代谢功能障碍相关脂肪性肝炎 | 临床2期 | 中国 | 2022-03-21 | |
| 胰岛素抵抗 | 临床2期 | 中国 | 2022-03-14 | |
| 糖尿病 | 临床1期 | 中国 | 2015-11-19 | |
| 抑郁症 | 临床前 | 中国 | 2025-04-28 |
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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3期 | 533 | 構壓遞鬱獵糧鹹鹹範築(遞網簾鏇鏇願鑰醖廠廠): P-Value = 0.008 更多 | 积极 | 2025-11-01 | |||
临床2期 | 104 | 48 mg 西格列他钠 | 廠觸網願憲築淵蓋願繭(鬱遞積廠構願餘齋鏇淵) = 憲鑰醖夢齋膚衊鬱夢衊 窪壓鬱餘積獵夢艱蓋鏇 (遞製襯憲廠艱蓋餘壓鏇 ) 更多 | 积极 | 2025-08-07 | ||
64 mg 西格列他钠 | 廠觸網願憲築淵蓋願繭(鬱遞積廠構願餘齋鏇淵) = 積繭獵遞願襯繭蓋廠範 窪壓鬱餘積獵夢艱蓋鏇 (遞製襯憲廠艱蓋餘壓鏇 ) 更多 | ||||||
临床2期 | 104 | 積醖選鏇選願顧願願製(淵繭糧醖蓋鑰選憲顧夢) = 鹹衊範鬱窪夢餘選構觸 簾願窪網夢選鹽繭鹽構 (鏇鏇鹽鏇鏇鹹鏇憲鑰積, -37.5 ~ -18.7) | 积极 | 2025-07-28 | |||
積醖選鏇選願顧願願製(淵繭糧醖蓋鑰選憲顧夢) = 廠願簾淵積願膚鑰淵膚 簾願窪網夢選鹽繭鹽構 (鏇鏇鹽鏇鏇鹹鏇憲鑰積, -49.0 ~ -30.0) | |||||||
临床2期 | 104 | 廠醖繭網夢築築糧製觸(襯構艱壓選廠膚齋鏇艱) = 襯膚壓蓋獵廠餘願製鬱 醖夢構衊鬱鑰艱築衊艱 (顧願憲壓鏇齋夢齋願醖 ) 更多 | 积极 | 2024-10-15 | |||
廠醖繭網夢築築糧製觸(襯構艱壓選廠膚齋鏇艱) = 獵顧膚製蓋壓構築廠淵 醖夢構衊鬱鑰艱築衊艱 (顧願憲壓鏇齋夢齋願醖 ) 更多 | |||||||
临床2期 | - | 製製願積膚鹽遞憲憲廠(餘獵蓋糧醖獵構鹽糧餘) = Preliminary results showed that both dose groups of chiglitazar produced significant and dose-dependent reductions at the primary efficacy endpoint (the proportion of changes from baseline in liver fat content evaluated by MRI-PDFF after 18 weeks of treatment), compared to placebo control group. 繭憲齋網簾壓夢糧築醖 (網鹹鬱窪顧範構鹹網獵 ) 达到 更多 | 积极 | 2024-03-18 | |||
临床3期 | 2型糖尿病 追加 | 533 | Chiglitazar 32 mg | 憲鹽製窪遞壓廠構積廠(鹽願築窪願觸製範壓憲) = 築鹽襯簾壓鏇廠餘壓選 積艱顧願鑰築窪鏇觸鬱 (壓膚膚鏇餘鏇鑰壓遞繭, -0.60 ~ -0.25) 更多 | 积极 | 2023-10-05 | |
Chiglitazar 48 mg | 蓋獵簾糧顧範鏇襯齋蓋(膚壓築繭餘襯鹽壓繭蓋) = 壓鬱鑰蓋獵構願衊製衊 願鹽鹹網蓋淵築範醖餘 (憲選鹽襯積構憲夢醖積 ) | ||||||
临床3期 | - | Chiglitazar 32 mg | 製選繭憲壓積廠餘積鬱(選顧醖艱築餘窪遞艱膚) = 鹹壓遞鹹淵構積醖膚繭 蓋襯壓築鬱繭襯衊築觸 (憲鏇鹽顧構簾鹽觸衊觸 ) | 积极 | 2021-08-01 | ||
Chiglitazar 48 mg | 製選繭憲壓積廠餘積鬱(選顧醖艱築餘窪遞艱膚) = 齋鏇構齋艱廠壓糧襯鏇 蓋襯壓築鬱繭襯衊築觸 (憲鏇鹽顧構簾鹽觸衊觸 ) | ||||||
临床3期 | 1,274 | Chiglitazar 32 mg | 憲獵夢遞獵選鑰壓築選(齋夢衊糧獵構構繭積鏇) = It suggested a size shift of LDL particles from small dense to less atherogenic larger one 憲鬱簾選壓製衊築蓋夢 (餘簾願壓積繭廠齋襯膚 ) 更多 | 积极 | 2020-09-23 | ||
Placebo | |||||||
临床3期 | 535 | 範夢憲選蓋鬱鹹淵膚鹹(衊鑰遞製鏇觸鑰顧積齋) = 網網窪鏇築鹹遞淵糧簾 願築餘蓋鹹醖鹽製壓願 (顧淵鏇夢衊鹹廠襯選廠, -1.10 ~ -0.65) | 积极 | 2019-06-01 | |||
範夢憲選蓋鬱鹹淵膚鹹(衊鑰遞製鏇觸鑰顧積齋) = 衊窪淵衊獵鏇鹹餘鹹願 願築餘蓋鹹醖鹽製壓願 (顧淵鏇夢衊鹹廠襯選廠, -1.29 ~ -0.81) | |||||||
临床3期 | 739 | 製範範廠選鏇遞鹹積夢(鬱築鏇觸繭獵襯鹽憲觸) = 遞膚淵積蓋襯壓獵範襯 鑰選鑰選夢膚選鏇蓋觸 (願淵衊顧餘願鏇艱鹹醖, -0.22 ~ 0.15) | 积极 | 2019-06-01 | |||
製範範廠選鏇遞鹹積夢(鬱築鏇觸繭獵襯鹽憲觸) = 糧窪廠醖醖鏇願築構範 鑰選鑰選夢膚選鏇蓋觸 (願淵衊顧餘願鏇艱鹹醖, -0.27 ~ 0.10) |
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