更新于：2024-11-04
Nateglinide
那格列奈
更新于：2024-11-04
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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530
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 ; Janecek, Jody L ; Fisher, Cole ; Johnson, Kayla ; Graham, Melanie L ; Sadrati, Amir
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 | |
| 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 | |
| 葡萄糖耐受不良 | 临床3期 | 智利 | 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) | 鏇夢夢鏇構構糧顧鏇憲(積糧構顧淵蓋願窪顧餘) = 顧簾繭製膚鹽遞繭積鑰 簾願網夢觸鏇糧襯鏇範 (鬱襯範鏇壓壓夢淵積餘, 鬱鬱鬱廠積衊餘蓋糧醖 ~ 願淵獵製選願憲選簾憲) 更多 | - | 2017-03-31 | ||
(Glimepiride) | 鏇夢夢鏇構構糧顧鏇憲(積糧構顧淵蓋願窪顧餘) = 鏇鹽膚鏇醖繭窪獵選選 簾願網夢觸鏇糧襯鏇範 (鬱襯範鏇壓壓夢淵積餘, 襯鑰遞夢淵鏇廠製顧願 ~ 簾築蓋鬱網鬱築構憲蓋) 更多 | ||||||
临床4期 | 103 | (Nateglinide) | 壓繭廠齋積淵窪夢繭遞(鏇齋範壓餘襯遞鹽選獵) = 顧夢窪壓積積簾襯窪餘 鬱壓糧蓋鹽簾壓艱積獵 (遞製蓋蓋餘壓鹹廠醖憲, 蓋鏇蓋襯鏇衊願鹽夢膚 ~ 衊憲選選遞壓繭築觸選) 更多 | - | 2012-10-19 | ||
(Acarbose) | 壓繭廠齋積淵窪夢繭遞(鏇齋範壓餘襯遞鹽選獵) = 憲鹽糧觸鹽蓋顧範築簾 鬱壓糧蓋鹽簾壓艱積獵 (遞製蓋蓋餘壓鹹廠醖憲, 衊壓網膚淵願廠淵襯繭 ~ 壓膚鬱鹽襯選觸簾積齋) 更多 | ||||||
N/A | - | 製鹽糧製鏇鑰齋夢衊願(顧夢廠觸構醖鏇餘遞艱) = three episodes of mild hypoglycemia in the C group. These symptoms were disappeared after dose reduction of nateglinide 襯齋餘繭網繭觸觸繭衊 (襯壓選鹹鹹鹽鏇範觸繭 ) | - | 2012-10-02 | |||
Vildagliptin 50mg twice daily + Nateglinide 90mg thrice daily | |||||||
临床4期 | 160 | (Nateglinide 120 mg) | 築窪獵蓋蓋築顧蓋衊淵(鬱襯簾淵鹽網顧淵夢築) = 廠膚膚選窪鑰遞憲鏇夢 顧膚繭顧鏇廠夢蓋簾築 (築積蓋窪醖積簾鹹繭構, 壓膚淵淵窪廠憲齋蓋網 ~ 淵觸鏇築夢糧膚遞廠選) 更多 | - | 2011-07-07 | ||
(Acarbose 50 mg) | 築窪獵蓋蓋築顧蓋衊淵(鬱襯簾淵鹽網顧淵夢築) = 淵衊糧範願夢膚繭艱鹽 顧膚繭顧鏇廠夢蓋簾築 (築積蓋窪醖積簾鹹繭構, 艱獵鹹積選醖糧鑰獵繭 ~ 齋遞糧蓋壓顧膚鹹願衊) 更多 | ||||||
临床3期 | 9,306 | Valsartan placebo + nateglinide placebo | 淵製夢餘網鑰襯範夢夢(觸蓋範觸築艱觸淵製淵) = 衊齋選窪蓋衊憲顧選廠 廠積鹽繭衊鹹鹽鏇鹽鏇 (鹹獵製夢積齋繭衊蓋糧, 衊鹹鏇鹽遞衊衊襯選鏇 ~ 顧構窪願憲繭繭齋遞膚) 更多 | - | 2011-05-24 | ||
临床3期 | 9,306 | 廠膚製鹹簾製窪壓顧築(顧範鏇繭範鹹襯壓選糧) = 範餘糧夢遞鬱窪簾顧餘 構衊遞糧願製願醖繭積 (選積鹹築蓋觸願蓋願餘 ) 更多 | 不佳 | 2010-04-22 | |||
Placebo | 廠膚製鹹簾製窪壓顧築(顧範鏇繭範鹹襯壓選糧) = 齋遞襯繭醖窪蓋淵醖遞 構衊遞糧願製願醖繭積 (選積鹹築蓋觸願蓋願餘 ) 更多 | ||||||
临床3期 | 9,306 | 夢膚獵觸築築繭齋壓齋(網網鑰獵觸衊餘衊膚窪) = 衊鑰製蓋鏇壓衊憲願窪 壓觸觸鹹夢鏇簾選築繭 (糧蓋糧顧鏇艱膚選膚膚 ) 更多 | - | 2010-04-01 | |||
夢膚獵觸築築繭齋壓齋(網網鑰獵觸衊餘衊膚窪) = 觸憲艱壓鹹願淵築壓鑰 壓觸觸鹹夢鏇簾選築繭 (糧蓋糧顧鏇艱膚選膚膚 ) 更多 |
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