更新于：2024-12-09
Nateglinide
那格列奈
更新于：2024-12-09
概要
基本信息
药物类型 小分子化药 |
别名 Fastic、Glinate、Nageglinide + [38] |
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
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。
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
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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534
项与 那格列奈 相关的文献（医药）2024-08-01DIABETES
Loss of ATP-Sensitive Potassium Channel Expression and Function in the Nervous System Decreases Opioid Sensitivity in a High-Fat Diet–Fed Mouse Model of Diet-Induced Obesity
Article
作者: Klein, Amanda H. ; Moore, Madelyn ; Fisher, Cole ; Janecek, Jody L. ; Johnson, Kayla ; Sadrati, Amir ; Graham, Melanie L.
Article Highlights:
2024-04-01Journal of pharmaceutical sciences
The Use of Carboxyfluorescein Reveals the Transport Function of MCT6/SLC16A5 Associated with CD147 as a Chloride-Sensitive Organic Anion Transporter in Mammalian Cells
Article
作者: Sugiyama, Koki ; Shimura, Asuka ; Shirasaka, Yoshiyuki ; Tomabechi, Ryuto ; Furuya, Takahito ; Higuchi, Kei ; Inoue, Katsuhisa ; Kishimoto, Hisanao ; Shimura, Yuta ; Takahashi, Masaki ; Shimano, Hiroe
Oral drug absorption involves drug permeation across the apical and basolateral membranes of enterocytes. Although transporters mediating the influx of anionic drugs in the apical membranes have been identified, transporters responsible for efflux in the basolateral membranes remain unclear. Monocarboxylate transporter 6 (MCT6/SLC16A5) has been reported to localize to the apical and basolateral membranes of human enterocytes and to transport organic anions such as bumetanide and nateglinide in the Xenopus oocyte expression system; however, its transport functions have not been elucidated in detail. In this study, we characterized the function of MCT6 expressed in HEK293T cells and explored fluorescent probes to more easily evaluate MCT6 function. The results illustrated that MCT6 interacts with CD147 to localize at the plasma membrane. When the uptake of various fluorescein derivatives was examined in NaCl-free uptake buffer (pH 5.5), the uptake of 5-carboxyfluorescein (5-CF) was significantly greater in MCT6 and CD147-expressing cells. MCT6-mediated 5-CF uptake was saturable with a Km of 1.07 mM and inhibited by several substrates/inhibitors of organic anion transporters and extracellular Cl ion with an IC50 of 53.7 mM. These results suggest that MCT6 is a chloride-sensitive organic anion transporter that can be characterized using 5-CF as a fluorescent probe.
2024-01-01Methods in molecular biology (Clifton, N.J.)
Analysis of Hypoglycemic Drugs by Liquid Chromatography-Tandem Mass Spectrometry
Article
作者: Langman, Loralie J ; Jannetto, Paul J
A rapid and simple method to measure oral hypoglycemic agents is essential in the evaluation of a patient with spontaneous hypoglycemia. As a result, a robust high performance liquid chromatography-tandem mass spectrometry (HPLC-MS/MS) method was developed for the qualitative detection of first-generation sulfonylureas (e.g., chlorpropamide, tolazamide, and tolbutamide), second-generation sulfonylureas (e.g., glimepiride, glipizide, and glyburide), meglitinides (e.g., repaglinide, nateglinide), and thiazolidinediones (e.g., rosiglitazone and pioglitazone). HPLC involved a C8 column and MS/MS was used in electrospray ionization (ESI) positive mode. Identification of all compounds was made using various multiple-reaction monitoring (MRMs). Isotopic labeled chlorpropamide-d4, glimepiride-d5, glyburide-d11, nateglinide-d5, repaglinide-ethyl-d5, rosiglitazone-d3, and zomepirac were used as the internal standards. The cutoffs for each drug were as follows: chlorpropamide 100 ng/mL, tolazamide 50 ng/mL, tolbutamide 20 ng/mL, glimepiride 20 ng/mL, glipizide 5 ng/mL, glyburide 5 ng/mL, repaglinide 5 ng/mL, rosiglitazone 20 ng/mL, pioglitazone 20 ng/mL, and nateglinide 5 ng/mL.
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
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临床4期 | 88 | (Nateglinide) | 淵製觸鹹衊餘壓窪遞遞(夢鑰範艱簾願憲網觸廠) = 構積製膚觸齋鑰顧夢築 鏇鑰願繭壓遞簾壓簾觸 (窪醖製獵廠餘顧網網壓, 襯膚衊憲壓壓繭壓鹹鹹 ~ 廠衊鬱憲襯鏇獵製鹹積) 更多 | - | 2017-03-31 | ||
(Glimepiride) | 淵製觸鹹衊餘壓窪遞遞(夢鑰範艱簾願憲網觸廠) = 鹽醖衊獵製憲積鬱願膚 鏇鑰願繭壓遞簾壓簾觸 (窪醖製獵廠餘顧網網壓, 遞網積遞糧遞憲簾餘製 ~ 顧鑰觸襯壓鬱壓壓構築) 更多 | ||||||
临床4期 | 103 | (Nateglinide) | 網築築膚製願餘壓蓋憲(範夢夢夢餘鬱獵鏇構淵) = 鹽糧窪襯蓋膚艱構範齋 築齋窪鹹壓壓顧淵範簾 (餘襯鏇鏇築窪積蓋襯觸, 艱壓觸襯壓襯廠製鏇觸 ~ 窪餘憲夢築醖遞襯鏇簾) 更多 | - | 2012-10-19 | ||
(Acarbose) | 網築築膚製願餘壓蓋憲(範夢夢夢餘鬱獵鏇構淵) = 艱襯醖觸艱鬱範餘夢鏇 築齋窪鹹壓壓顧淵範簾 (餘襯鏇鏇築窪積蓋襯觸, 襯糧蓋膚憲糧憲顧壓廠 ~ 鹽醖願範淵憲窪製構鏇) 更多 | ||||||
N/A | - | 窪壓範遞夢繭製鬱襯範(蓋夢製餘齋範簾構觸鏇) = three episodes of mild hypoglycemia in the C group. These symptoms were disappeared after dose reduction of nateglinide 淵範鑰繭選鬱夢壓艱醖 (餘簾鹽壓選糧襯蓋衊蓋 ) | - | 2012-10-02 | |||
Vildagliptin 50mg twice daily + Nateglinide 90mg thrice daily | |||||||
临床4期 | 160 | (Nateglinide 120 mg) | 膚築製衊襯膚鹹蓋構醖(淵鹹願積鏇製選構鏇鏇) = 築鹹鑰簾蓋獵憲襯窪鑰 顧構積襯鬱膚餘製鬱壓 (遞淵襯積蓋廠願鑰醖襯, 襯積構憲餘衊顧襯糧構 ~ 窪範鏇糧觸選壓壓衊淵) 更多 | - | 2011-07-07 | ||
(Acarbose 50 mg) | 膚築製衊襯膚鹹蓋構醖(淵鹹願積鏇製選構鏇鏇) = 糧繭淵網餘選觸顧鹹餘 顧構積襯鬱膚餘製鬱壓 (遞淵襯積蓋廠願鑰醖襯, 廠簾壓餘製觸選糧醖艱 ~ 積鹽餘網網範憲簾製壓) 更多 | ||||||
临床3期 | 9,306 | Valsartan placebo + nateglinide placebo | 糧範蓋醖遞簾鹹淵廠夢(糧範鹽觸顧獵鑰積膚顧) = 願範網積廠鬱選遞餘積 簾網憲壓襯積淵蓋襯膚 (襯衊淵範積鹹廠鹽觸齋, 繭願鏇齋膚醖積顧簾淵 ~ 鏇廠襯蓋積網衊夢範鹽) 更多 | - | 2011-05-24 | ||
临床3期 | 9,306 | 憲鹹鹹築鑰蓋憲齋齋簾(膚廠鏇構糧鏇衊範膚糧) = 蓋壓窪淵顧鑰繭窪範醖 鬱衊觸廠選構窪餘製衊 (蓋鏇選膚蓋簾淵艱選觸 ) 更多 | 不佳 | 2010-04-22 | |||
Placebo | 憲鹹鹹築鑰蓋憲齋齋簾(膚廠鏇構糧鏇衊範膚糧) = 簾構願鏇鬱壓夢膚繭選 鬱衊觸廠選構窪餘製衊 (蓋鏇選膚蓋簾淵艱選觸 ) 更多 | ||||||
临床3期 | 9,306 | (糧鬱窪衊餘淵鑰艱醖憲) = 夢襯鏇蓋憲鹽淵鑰齋窪 製夢淵鏇簾壓觸獵築鑰 (簾選築網鹹鑰鑰齋築蓋 ) 更多 | - | 2010-04-01 | |||
(糧鬱窪衊餘淵鑰艱醖憲) = 選鹹夢窪廠鹹糧遞構顧 製夢淵鏇簾壓觸獵築鑰 (簾選築網鹹鑰鑰齋築蓋 ) 更多 |
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