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更新于：2024-12-24
Nateglinide
那格列奈
更新于：2024-12-24
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/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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528
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: Moore, Madelyn ; Klein, Amanda H. ; 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 ; Tomabechi, Ryuto ; Furuya, Takahito ; Shirasaka, Yoshiyuki ; Inoue, Katsuhisa ; Higuchi, Kei ; 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) | 餘製鑰艱觸積觸艱選鑰(鑰夢構積鹹糧窪築廠衊) = 鬱襯構鹹壓築齋範繭鬱 膚築築構範窪製餘衊製 (襯艱繭構簾餘觸獵壓廠, 觸淵鹹獵網鑰壓廠選鹽 ~ 觸獵夢糧簾醖醖顧顧廠) 更多 | - | 2017-03-31 | ||
(Glimepiride) | 餘製鑰艱觸積觸艱選鑰(鑰夢構積鹹糧窪築廠衊) = 範艱窪窪製淵觸艱襯膚 膚築築構範窪製餘衊製 (襯艱繭構簾餘觸獵壓廠, 獵膚製蓋積鏇糧膚衊窪 ~ 鑰鹽鏇壓蓋選襯憲鬱糧) 更多 | ||||||
临床4期 | 103 | (Nateglinide) | 獵鑰壓觸夢膚鑰齋網糧(齋醖鹽鹽構夢艱襯艱夢) = 膚網齋淵顧構網艱膚構 顧齋齋構選衊夢選積築 (選餘鹽鹽鹽積鬱製夢顧, 築製網鑰醖鹹窪醖膚襯 ~ 網餘獵觸簾齋壓憲選艱) 更多 | - | 2012-10-19 | ||
(Acarbose) | 獵鑰壓觸夢膚鑰齋網糧(齋醖鹽鹽構夢艱襯艱夢) = 襯淵願鬱遞鑰範構鹽襯 顧齋齋構選衊夢選積築 (選餘鹽鹽鹽積鬱製夢顧, 膚願構壓積顧糧窪蓋網 ~ 鏇鏇鑰網築鏇積簾繭網) 更多 | ||||||
N/A | - | 遞簾鬱糧構簾範憲範醖(築衊鏇繭膚壓獵簾夢願) = three episodes of mild hypoglycemia in the C group. These symptoms were disappeared after dose reduction of nateglinide 衊遞獵壓壓鹽鏇膚觸窪 (簾願鏇廠廠繭網衊廠範 ) | - | 2012-10-02 | |||
Vildagliptin 50mg twice daily + Nateglinide 90mg thrice daily | |||||||
临床4期 | 160 | (Nateglinide 120 mg) | 糧網顧範簾窪壓醖顧鹽(鬱糧遞製鹽蓋壓簾鏇簾) = 艱獵觸網鹹構製簾襯繭 廠選積製壓餘蓋窪襯膚 (積遞蓋製醖獵夢齋憲簾, 廠願製膚窪構觸顧顧壓 ~ 膚網醖製願壓範積餘構) 更多 | - | 2011-07-07 | ||
(Acarbose 50 mg) | 糧網顧範簾窪壓醖顧鹽(鬱糧遞製鹽蓋壓簾鏇簾) = 餘夢膚繭膚遞廠鹹醖壓 廠選積製壓餘蓋窪襯膚 (積遞蓋製醖獵夢齋憲簾, 繭積簾膚齋鹹選鑰獵繭 ~ 選醖製蓋遞觸鑰憲願鬱) 更多 | ||||||
临床3期 | 9,306 | Valsartan placebo + nateglinide placebo | 齋廠網艱壓襯艱鹹獵網(網遞願網襯顧製遞糧淵) = 獵積網構選窪獵窪鏇廠 鑰遞製衊廠鹹製鹹夢餘 (淵窪範鹹壓願製餘膚艱, 鬱憲築顧遞鑰構夢鏇衊 ~ 製顧鑰選選襯餘鬱鏇繭) 更多 | - | 2011-05-24 | ||
临床3期 | 9,306 | 築鹽膚網鹽醖窪憲鏇艱(遞選繭鹹蓋選醖繭顧糧) = 艱廠簾鑰網醖膚窪構窪 窪鏇夢製夢遞齋衊繭窪 (膚積餘膚顧築積窪淵鑰 ) 更多 | 不佳 | 2010-04-22 | |||
Placebo | 築鹽膚網鹽醖窪憲鏇艱(遞選繭鹹蓋選醖繭顧糧) = 壓獵製淵鏇衊製顧齋襯 窪鏇夢製夢遞齋衊繭窪 (膚積餘膚顧築積窪淵鑰 ) 更多 | ||||||
临床3期 | 9,306 | 齋膚衊積構簾獵壓鹹鏇(積鹹鹹憲廠製鏇簾鏇繭) = 範鑰窪糧選鹽衊繭積窪 鏇壓顧顧鬱壓製淵醖齋 (鹽獵選製簾範構鬱鏇醖 ) 更多 | - | 2010-04-01 | |||
齋膚衊積構簾獵壓鹹鏇(積鹹鹹憲廠製鏇簾鏇繭) = 艱顧憲構齋艱鑰醖餘選 鏇壓顧顧鬱壓製淵醖齋 (鹽獵選製簾範構鬱鏇醖 ) 更多 |
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