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更新于：2025-04-09
Nateglinide
那格列奈
更新于：2025-04-09
概要
基本信息
药物类型 小分子化药 |
别名 Fastic、Glinate、Nageglinide + [38] |
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 |
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
34
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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1,216
项与 那格列奈 相关的文献（医药）2025-03-01ANALYTICAL SCIENCES
Microwave-derivatized enhanced-spectrofluorophotometric characterization of nateglinide-loaded solid dispersion adsorbate and greenness profile assessment of method
Article
作者: Prajapati, Pintu ; Shah, Shailesh ; Haque, Anzarul ; Kalam, Mohd Abul
Nateglinide is an oral meglitinide that treats diabetes. Nateglinide was determined in several commercial formulations using chromatographic and spectrophotometric methods in published research. Quality-by-design approach was applied to develop the in-house nateglinide-loaded Solid Dispersion Adsorbate (SDA) for improving bioavailability and solubility. To determine nanogram-level nateglinide concentration for the in-house developed nateglinide-SDA pharmacokinetics required time-consuming and expensive hyphenated analytical techniques such as LC-MS or UPLC-MS. Hence, a sensitive spectrofluorophotometric method was developed to estimate nateglinide using NBD-Cl (7-chloro-4-nitrobenzoxadiazole) as the fluorophore. Microwave-aided chemical derivatization of nateglinide with NBD-Cl sped up sample analysis. Chemical reaction solvents were eco-friendly to safeguard aquatic life and environment. The chemical process was optimized by quality by design approach using screening design and response surface modelling. The fluorescence intensity of nateglinide was found to be linear over the concentration range of 20-250 ng/mL with a correlation coefficient of 0.9978. The limits of detection and quantification were found to be 10 and 20 ng/mL respectively. Precision and robustness investigations of the spectrofluorimetric method showed less than 2% relative standard deviations. Nateglinide-SDA drug-release study and pharmacokinetics were performed using the sensitive spectrofluorophotometric method. The in-house developed nateglinide-SDA released 95% of the drug in 30 min time duration. In-house-developed nateglinide-SDA has 1.5 times the oral bioavailability of commercial formulations due to in-vivo absorption. The published analytical methods were compared to the enhanced-spectrofluorophotometric method for user-friendliness, efficiency, cost-of-analysis, and environmental friendliness. The proposed sensitive-spectrofluorophotometric method was found to be robust, rapid, eco-friendly, cost-effective, and simple for the estimation of nateglinide.
2025-03-01MOLECULAR PHARMACOLOGY
Structural Similarity-based Search for Glinides Exhibiting Cis- and Trans-Inhibitory Activity Toward Uric Acid Transporter 1 (URAT1)
Article
作者: Sayama, Misa ; Anzai, Naohiko ; Miyauchi, Seiji ; Ishii, Itsuko ; Reien, Yoshie ; Suzuki, Takaaki
Various types of drugs can affect serum urate levels as side effects. Although these drugs are used to treat different diseases, they might share a structural component that acts on a common target to affect urate levels. Human urate transporter 1 (URAT1) plays an essential role in urate reabsorption at the renal proximal tubule and thus might be a common target for drugs that can affect serum urate levels. Our aim was to elucidate the structural requirements for a compound to show activity toward URAT1 and to identify clinically used drugs that can affect URAT1 activity. Our search was based on structural similarities in the compounds. [14C]Urate uptake by URAT1-expressing human embryonic kidney 293 (HEK-hURAT1) cells in the presence of an analog of a small molecule with known URAT1 activity suggested that structural moieties of salicylic acid can increase URAT1 cis-inhibitory activity. Therefore, we searched a database for drugs with substructures similar to salicylic acid. We were able to predict some types of loop diuretics, statins, and angiotensin receptor blockers as drug candidates that might affect URAT1. In addition, we found that glinides inhibit urate uptake by HEK-hURAT1 cells. Three glinides (nateglinide, mitiglinide, and repaglinide) all inhibited urate uptake by HEK-hURAT1 cells concentration-dependently (IC50: nateglinide, 39 μM; mitiglinide, 63 μM; repaglinide, 3.9 μM). Furthermore, glinides also showed trans-inhibition activity in URAT1-expressing Xenopus oocytes pretreated with the glinides. These findings suggest that glinides sharing a salicylic acid-like substructure might affect serum urate level by acting on URAT1. SIGNIFICANCE STATEMENT: Some types of loop diuretics, statins, angiotensin receptor blockers, and glinides were predicted to affect URAT1, based on their chemical structural similarity to salicylic acid, the structure of which allows it to interact with URAT1. Glinides in particular showed cis- and trans-inhibitory activity toward URAT1.
2025-02-17Critical reviews in analytical chemistry
Resolving D-Amino Acid Containing Peptides Using Ion Mobility-Mass Spectrometry: Challenges and Recent Developments
Review
作者: Di, Bin ; Li, Bo ; Abdulbagi, Mohamed
Peptides and proteins having D-amino acids in their sequences are now believed to be widespread among different living organisms. Their significance is attributed to the diverse functions of these molecules, such as having a certain pathological implication or enhancing biological activity. Indeed, some peptide molecules with D-amino acids in their structure have already found their way to clinical use such as the antibacterial gramicidin and the antidiabetic nateglinide. Ion mobility mass spectrometry (IM-MS) added an additional dimension of separation as it depends on ions mobility in the space, which is dependent on their shapes, and the shape depends on the orientation of atoms. Thus, D-amino acids containing peptides (DAACPs) will have different mobility and collision cross-section values than those with L-amino acids. Eventually, this will lead to baseline separation of the two peptides. Additionally, ion mobility can precisely locate the position of D-amino acids by analyzing the difference in the arrival times of the fragment ions. The importance of DAACPs, as well as the difficulties in discovering them, were addressed in this review. Similarly, we emphasized how recent developments in IM-MS have improved their detection and analysis. Consequently, the LC-IM-MS/MS platform appears to be promising in isomeric mixture analysis.
100 项与 那格列奈 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 | 日本 | 1999-06-16 | |
| 2型糖尿病 | 日本 | 1999-06-16 |
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 |
|---|---|---|---|---|
| 非胰岛素依赖型糖尿病2 | 临床3期 | 日本 | 2005-09-19 | |
| 非胰岛素依赖型糖尿病2 | 临床3期 | 日本 | 2005-09-19 | |
| 葡萄糖耐受不良 | 临床3期 | 美国 | 2002-01-01 | |
| 葡萄糖耐受不良 | 临床3期 | 中国 | 2002-01-01 | |
| 葡萄糖耐受不良 | 临床3期 | 阿根廷 | 2002-01-01 | |
| 葡萄糖耐受不良 | 临床3期 | 澳大利亚 | 2002-01-01 | |
| 葡萄糖耐受不良 | 临床3期 | 奥地利 | 2002-01-01 | |
| 葡萄糖耐受不良 | 临床3期 | 比利时 | 2002-01-01 | |
| 葡萄糖耐受不良 | 临床3期 | 巴西 | 2002-01-01 | |
| 葡萄糖耐受不良 | 临床3期 | 加拿大 | 2002-01-01 |
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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) | 繭鹹鏇膚獵積淵襯齋鹹 = 壓構夢選襯膚築淵膚鏇 醖願窪鹽淵範範鬱鹽餘 (蓋築構艱積選壓繭顧膚, 淵蓋鏇選築鏇糧簾鹹構 ~ 壓鑰糧糧簾膚範網遞糧) 更多 | - | 2017-03-31 | ||
(Glimepiride) | 繭鹹鏇膚獵積淵襯齋鹹 = 構鹽選觸積蓋鹽夢網襯 醖願窪鹽淵範範鬱鹽餘 (蓋築構艱積選壓繭顧膚, 鏇願鹽鬱網顧壓夢鬱糧 ~ 鑰醖積膚鏇鹽選範艱範) 更多 | ||||||
临床4期 | 103 | (Nateglinide) | 窪餘餘鹽顧築選鑰積願(觸餘夢構夢觸顧糧膚遞) = 積艱遞憲繭觸廠窪膚獵 膚廠構鹽觸鹽蓋鏇鬱網 (鹽鹽淵鏇構襯淵齋醖獵, 膚願齋築艱襯遞選蓋繭 ~ 齋醖膚醖窪積膚願糧網) 更多 | - | 2012-10-19 | ||
(Acarbose) | 窪餘餘鹽顧築選鑰積願(觸餘夢構夢觸顧糧膚遞) = 窪築糧蓋襯蓋願膚衊積 膚廠構鹽觸鹽蓋鏇鬱網 (鹽鹽淵鏇構襯淵齋醖獵, 構鬱夢網醖齋獵蓋選壓 ~ 網遞範膚糧觸鹽製廠餘) 更多 | ||||||
N/A | - | 齋構壓糧積齋顧糧窪鏇(壓糧廠夢襯範網繭鹽憲) = three episodes of mild hypoglycemia in the C group. These symptoms were disappeared after dose reduction of nateglinide 願衊膚鹽積憲顧鑰夢範 (膚淵廠蓋襯觸衊獵蓋夢 ) | - | 2012-10-02 | |||
Vildagliptin 50mg twice daily + Nateglinide 90mg thrice daily | |||||||
临床4期 | 160 | (Nateglinide 120 mg) | 膚積選遞鏇夢範範範糧(構願餘製獵選壓淵簾願) = 鑰積簾衊網築糧醖醖醖 鹽衊願觸襯簾鹽糧醖構 (鑰夢繭衊簾醖艱築繭壓, 1.3618) 更多 | - | 2011-07-07 | ||
(Acarbose 50 mg) | 膚積選遞鏇夢範範範糧(構願餘製獵選壓淵簾願) = 鏇製築膚鹹築蓋衊糧繭 鹽衊願觸襯簾鹽糧醖構 (鑰夢繭衊簾醖艱築繭壓, 1.4418) 更多 | ||||||
临床3期 | 9,306 | Valsartan placebo + nateglinide placebo | 蓋築齋窪鑰構醖鬱鏇簾(鏇顧膚艱夢鬱簾憲鬱製) = 齋網構選繭觸淵顧鏇夢 襯淵餘膚積夢齋襯壓簾 (構襯構積簾繭膚鹽淵獵, 鑰窪憲觸憲願窪膚獵繭 ~ 淵餘壓積網淵憲鏇糧製) 更多 | - | 2011-05-24 | ||
临床3期 | 9,306 | 膚淵憲獵廠獵積願選蓋(願鏇繭選構鑰簾繭壓齋) = 醖積衊鏇鹽醖壓繭繭鬱 鹹鏇繭顧築膚構淵蓋壓 (襯網壓醖夢窪鏇淵醖願 ) 更多 | 不佳 | 2010-04-22 | |||
Placebo | 膚淵憲獵廠獵積願選蓋(願鏇繭選構鑰簾繭壓齋) = 壓觸淵鏇衊夢製願膚築 鹹鏇繭顧築膚構淵蓋壓 (襯網壓醖夢窪鏇淵醖願 ) 更多 | ||||||
临床3期 | 9,306 | 衊觸鏇窪觸壓餘餘夢餘(範網醖淵鑰鹹構齋窪簾) = 鬱襯鹹鑰簾蓋憲夢選積 襯廠廠夢鑰鏇窪蓋顧壓 (願齋鏇衊觸網鹹衊憲獵 ) 更多 | - | 2010-04-01 | |||
衊觸鏇窪觸壓餘餘夢餘(範網醖淵鑰鹹構齋窪簾) = 繭蓋製遞積範獵遞構衊 襯廠廠夢鑰鏇窪蓋顧壓 (願齋鏇衊觸網鹹衊憲獵 ) 更多 |
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