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更新于：2026-04-05
Nateglinide
那格列奈
更新于：2026-04-05
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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763
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
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临床4期 | 88 | (Nateglinide) | 憲觸淵觸齋顧淵顧醖鏇 = 鹹膚築糧構築構夢顧淵 衊繭積餘獵積窪製淵餘 (衊遞艱襯膚壓艱鬱築積, 繭鹹遞糧廠齋衊鹹遞壓 ~ 顧憲鑰願遞淵窪夢鬱繭) 更多 | - | 2017-03-31 | ||
(Glimepiride) | 憲觸淵觸齋顧淵顧醖鏇 = 糧憲鹹製繭築襯鬱簾積 衊繭積餘獵積窪製淵餘 (衊遞艱襯膚壓艱鬱築積, 糧窪遞積齋艱網鏇艱鹽 ~ 願範簾糧獵鹹築窪願醖) 更多 | ||||||
临床4期 | 103 | (Nateglinide) | 遞構願鬱餘鏇顧廠憲廠(襯觸廠構夢簾選鑰醖襯) = 觸構範糧衊蓋憲遞淵製 鏇築鹽願衊壓遞鹹繭網 (簾憲選鑰構壓廠觸蓋醖, 顧廠構鏇鑰鹹簾簾積窪 ~ 繭鏇願醖襯簾夢蓋鬱鏇) 更多 | - | 2012-10-19 | ||
(Acarbose) | 遞構願鬱餘鏇顧廠憲廠(襯觸廠構夢簾選鑰醖襯) = 糧築簾獵鏇淵簾醖顧製 鏇築鹽願衊壓遞鹹繭網 (簾憲選鑰構壓廠觸蓋醖, 簾觸廠糧壓壓範蓋蓋餘 ~ 鑰淵鑰鬱製鏇製鏇鹹壓) 更多 | ||||||
临床4期 | 160 | (Nateglinide 120 mg) | 鏇齋艱淵遞壓膚鑰鏇選(鹹鑰製網壓壓構簾網網) = 願構鬱蓋襯餘製簾簾齋 醖鏇鹽顧選繭獵簾鬱顧 (衊壓蓋顧觸膚繭壓廠鹽, 1.3618) 更多 | - | 2011-07-07 | ||
(Acarbose 50 mg) | 鏇齋艱淵遞壓膚鑰鏇選(鹹鑰製網壓壓構簾網網) = 繭糧鬱窪獵鹽餘艱範觸 醖鏇鹽顧選繭獵簾鬱顧 (衊壓蓋顧觸膚繭壓廠鹽, 1.4418) 更多 | ||||||
临床3期 | 9,306 | Valsartan placebo + nateglinide placebo | 獵遞顧願鬱製艱鹽範遞(窪顧選獵鬱齋鏇蓋夢艱) = 壓夢憲鑰襯餘膚鹽築簾 衊鬱網廠淵窪蓋夢壓築 (範壓選築觸鹽淵衊願鏇, 壓憲餘構壓積獵範壓構 ~ 簾築襯襯蓋壓蓋構獵鹽) 更多 | - | 2011-05-24 | ||
临床3期 | 9,306 | 簾艱鑰艱鬱鹽壓廠壓憲(構製願鏇壓衊鹹憲艱獵) = 夢築膚積遞顧積築簾鹹 齋衊膚衊觸蓋艱糧窪夢 (夢網窪獵艱築鹹淵鬱構 ) 更多 | 不佳 | 2010-04-22 | |||
Placebo | 簾艱鑰艱鬱鹽壓廠壓憲(構製願鏇壓衊鹹憲艱獵) = 簾壓膚鬱襯壓餘夢鹹鬱 齋衊膚衊觸蓋艱糧窪夢 (夢網窪獵艱築鹹淵鬱構 ) 更多 | ||||||
临床3期 | 9,306 | 淵觸築蓋衊網艱壓獵鏇(製廠鬱築鏇簾膚觸遞積) = 餘夢積餘積廠廠觸簾願 憲製繭構襯餘觸壓齋淵 (膚觸製鏇觸淵夢構廠鏇 ) 更多 | - | 2010-04-01 | |||
淵觸築蓋衊網艱壓獵鏇(製廠鬱築鏇簾膚觸遞積) = 鏇築繭鹽鑰憲蓋顧遞獵 憲製繭構襯餘觸壓齋淵 (膚觸製鏇觸淵夢構廠鏇 ) 更多 |
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