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更新于：2026-03-25
Nateglinide
那格列奈
更新于：2026-03-25
概要
基本信息
药物类型 小分子化药 |
别名 Fastic、Glinate、Nageglinide + [39] |
作用方式 拮抗剂、抑制剂 |
作用机制 PPARγ拮抗剂(过氧化物酶体增长因子活化受体γ拮抗剂)、SUR1抑制剂(磺酰脲类受体1抑制剂) |
治疗领域 |
在研适应症 |
非在研适应症- |
权益机构- |
最高研发阶段批准上市 |
首次获批日期 日本 (1999-06-16), |
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C19H27NO3 |
InChIKeyOELFLUMRDSZNSF-BRWVUGGUSA-N |
CAS号105816-04-4 |
关联
37
项与 那格列奈 相关的临床试验CTR20190942
那格列奈片在健康男性和女性受试者中于餐后情况下进行的单剂量、随机、开放性、 交叉的生物等效性研究。
CTR20181442
单中心、随机开放、双周期双交叉设计评价中国健康受试者单次空腹及餐后口服那格列奈片的人体生物等效性试验
CTR20180642
那格列奈片在健康受试者中的单剂量、随机、开放性、交叉、正式、空腹及餐后生物等效性研究
100 项与 那格列奈 相关的临床结果
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100 项与 那格列奈 相关的转化医学
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100 项与 那格列奈 相关的专利（医药）
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747
项与 那格列奈 相关的文献（医药）2025-11-01BIOMEDICAL CHROMATOGRAPHY
An Isocratic RP‐HPLC Method for Simultaneous Quantification of Nateglinide and Furosemide: Application to In Vitro Caco‐2 Intestinal Permeability Studies of Nanodrugs
Article
作者: Sahin, Selma ; Kir, Fatma ; Dogan, Aysegul ; Al‐Sulaiti, Fatima Khalifa
ABSTRACT:
In the booming era of nanomedicines, Caco‐2 intestinal permeability experimental models allow characterizing intestinal permeabilities of nanopharmaceuticals and are conducted in the presence of cell culture media (CCM) and stabilizers. Methods for simultaneous quantification of furosemide (FRS) and nateglinide (NTG) in Caco‐2 experiments are lacking. We developed and validated a novel, simple, and practical reversed‐phase high‐performance liquid chromatography (RP‐HPLC) method with UV detection to simultaneously quantify FRS and NTG in the presence of CCM and stabilizers (Povidone K‐25, Pluronic F‐38) for Caco‐2 intestinal permeability experiments exploring nanoformulations. FRS and NTG nanosuspensions were prepared using high‐speed ultrasonic homogenization top–down technique. Caco‐2 cell culture studies were conducted. ICH Q2(R1) guideline requirements (i.e., selectivity, specificity, accuracy, precision, robustness, stability) were met. System suitability and linearity (FRS: 5.12–40.00 μg/mL; NTG: 7.31–50.00 μg/mL), with high determination coefficients (>0.999), and short retention times (FRS: 3.3 min; NTG: 5.3 min) were achieved. NTG and FRS in Caco‐2 samples were successfully simultaneously quantified, proving usefulness for nanodrug research applications. Varying stabilizers impact intestinal permeability. This work simulates pragmatic conditions, as cardiovascular patients are co‐administered these drugs, paving the pathway to using our novel method for a wide range of “bench‐to‐bedside” nanomedicine research designs to tackle the challenges of polypharmacy in this complex population.
2025-09-01CHEMISTRY & BIODIVERSITY
Discovery of Hypoglycemic and Cardiovascular Drugs as Effective Inhibitors on Human Pancreatic Lipase
Article
作者: Liang, Bing‐Jie ; Zou, Li‐Wei ; Wang, Dan‐Dan ; Yu, Yang ; Dong, Le‐Xuan ; Wang, Shu‐Xia ; He, Wen‐Yao ; Zhang, Jing
ABSTRACT:
Obesity is closely related to the occurrence and development of many diseases, such as diabetes, hypertension, and hyperlipidemia. As an important digestive enzyme, human pancreatic lipase (hPL) is involved in the metabolism and absorption of dietary fat and is a key target of overweight and obesity. Therefore, the inhibition of hPL enzyme is a feasible strategy for the prevention and treatment of obesity. In this study, we collected a series of marketed hypoglycemic and cardiovascular drugs and evaluated their inhibitory activity against hPL. Among them, ticagrelor (HC‐14), prasugrel (HC‐18), amlodipine (HC‐26), simvastatin (HC‐32), and lovastatin (HC‐33) had strong inhibitory activity against hPL. In order to further clarify the inhibition mechanism, inhibition kinetics and molecular docking were carried out, and results revealed that HC‐14 was a mixed inhibitory manner on hPL activity. HC‐14 also showed similar inhibitory effect on human carboxylesterase 2 (hCES2), but poor inhibitory effect on other five serine hydrolases. Further studies showed that HC‐14 significantly inhibited hPL activity in AR42J cells, resulting in dose‐dependent inhibition. Overall, the above results suggest that ticagrelor is a cardiovascular drug that inhibits hPL, which also provides an important reference for the search and development of other drugs for the treatment of obesity.
2025-06-18CRYSTAL GROWTH & DESIGN
Relaxation of Nateglinide-Pyridinecarboxamide Coamorphous Systems to Cocrystals: Synthon Competition with Acid, Amide, and Pyridine Groups
作者: Juszyńska-Gałązka, Ewa ; Drzewicz, Anna ; Pereira Silva, Pedro S. ; Piedade, M. Fátima M. ; Gałązka, Mirosław ; Rosado, Mário T. S. ; Silva, Manuela R. ; Eusébio, M. Ermelinda S. ; Silva, Joana F. C.
Amide-amide, acid-amide, and acid-pyridine synthons are among the most effective hydrogen-bonded building blocks in multicomponent drug systems.In this work, a conformationally flexible compound with prolific polymorphism was chosen as a carboxylic acid model drug, combined with three pyridinecarboxamide positional isomers as co-formers - picolinamide, nicotinamide, and isonicotinamide.Quench-cooling molten mixtures with different molar ratios produced binary coamorphous systems.Their thermal stability was dependent on the heating rate, relaxing to equimolar cocrystals with picolinamide and isonicotinamide, also obtained by mechanochem.Contrarily, both methods could only produce phys. mixtures with nicotinamide.Thermal anal. and X-ray diffraction were used to characterize the crystalline phases.Furthermore, the mol. dynamics of the pure compounds and binary phases were studied by dielec. spectroscopy, while the main intermol. interactions were investigated by FTIR-ATR and computational methods based on DFT calculations-mol. electrostatic potential, NBO, and IGM-δg analyses.The acid hydroxyl group was the strongest hydrogen bond donor, and the amide carbonyl group was the best acceptor.However, the synthon competition outcome was found to depend on the pyridinecarboxamide isomer, with picolinamide having a more different behavior because of electronic and steric effects.Exptl. and computational results suggest an acid-amide synthon in the nateglinide-picolinamide cocrystal, which was fully confirmed by single-crystal X-ray diffraction.
100 项与 那格列奈 相关的药物交易
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研发状态
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 | 日本 | 1999-06-16 | |
| 2型糖尿病 | 日本 | 1999-06-16 |
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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4期 | 88 | (Nateglinide) | 糧廠顧構膚齋網膚蓋餘 = 衊鏇蓋鹹衊簾觸範衊獵 艱簾廠積齋簾獵選衊鑰 (簾齋製鏇廠築鬱淵鑰齋, 鹽鹽願衊選構淵遞選鑰 ~ 餘鑰醖鏇製夢構繭鑰衊) 更多 | - | 2017-03-31 | ||
(Glimepiride) | 糧廠顧構膚齋網膚蓋餘 = 積選製襯構製築鑰壓醖 艱簾廠積齋簾獵選衊鑰 (簾齋製鏇廠築鬱淵鑰齋, 襯觸壓鏇窪範鑰築鏇遞 ~ 糧遞糧餘齋簾夢鬱鏇觸) 更多 | ||||||
临床4期 | 103 | (Nateglinide) | 憲淵遞鹹廠選鏇艱鏇積(壓觸夢鹽獵糧齋壓蓋鹽) = 顧網範餘繭鹽壓醖齋醖 鏇餘淵鬱觸鑰齋願顧廠 (鏇鑰繭選製憲窪鬱鏇襯, 餘艱繭簾醖鑰獵夢襯鏇 ~ 衊製獵簾簾鹽餘願範襯) 更多 | - | 2012-10-19 | ||
(Acarbose) | 憲淵遞鹹廠選鏇艱鏇積(壓觸夢鹽獵糧齋壓蓋鹽) = 淵簾範餘窪築餘繭獵觸 鏇餘淵鬱觸鑰齋願顧廠 (鏇鑰繭選製憲窪鬱鏇襯, 蓋蓋醖鏇餘廠廠夢艱獵 ~ 餘顧製齋蓋鑰鑰艱齋窪) 更多 | ||||||
临床4期 | 160 | (Nateglinide 120 mg) | 鏇廠範艱鏇鹽壓糧網艱(範餘糧壓築鏇選築遞觸) = 廠醖淵鹹構築憲積壓鏇 蓋網簾壓選襯淵窪膚選 (齋衊築膚壓衊簾築觸壓, 1.3618) 更多 | - | 2011-07-07 | ||
(Acarbose 50 mg) | 鏇廠範艱鏇鹽壓糧網艱(範餘糧壓築鏇選築遞觸) = 選鹽獵憲醖蓋糧選鏇壓 蓋網簾壓選襯淵窪膚選 (齋衊築膚壓衊簾築觸壓, 1.4418) 更多 | ||||||
临床3期 | 9,306 | Valsartan placebo + nateglinide placebo | 繭鏇醖鏇構顧顧鬱獵網(顧築願壓獵衊構製網艱) = 範壓壓願餘衊醖構築夢 蓋廠齋築廠獵築觸餘築 (顧襯齋蓋顧範鏇憲窪廠, 蓋構窪獵壓夢積糧選窪 ~ 願淵衊獵夢顧遞範窪鏇) 更多 | - | 2011-05-24 | ||
临床3期 | 9,306 | 繭鹽蓋淵襯繭艱壓壓鹹(觸鏇糧構觸膚積蓋範遞) = 鏇淵艱願餘夢憲範膚範 遞鹽齋窪襯顧艱簾艱觸 (顧餘繭餘夢餘願壓窪鏇 ) 更多 | 不佳 | 2010-04-22 | |||
Placebo | 繭鹽蓋淵襯繭艱壓壓鹹(觸鏇糧構觸膚積蓋範遞) = 鏇醖糧糧願遞積鬱鹽選 遞鹽齋窪襯顧艱簾艱觸 (顧餘繭餘夢餘願壓窪鏇 ) 更多 | ||||||
临床3期 | 9,306 | 範獵壓糧壓顧餘鏇廠窪(醖壓廠艱壓觸鹽糧鏇壓) = 顧壓製選獵鏇襯壓廠窪 鏇簾醖選夢範鏇遞鹽鏇 (製廠窪構鏇鑰築淵夢鑰 ) 更多 | - | 2010-04-01 | |||
範獵壓糧壓顧餘鏇廠窪(醖壓廠艱壓觸鹽糧鏇壓) = 窪範鹹繭鏇醖鑰鬱襯製 鏇簾醖選夢範鏇遞鹽鏇 (製廠窪構鏇鑰築淵夢鑰 ) 更多 |
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