更新于：2024-11-04
Miglitol
米格列醇
更新于：2024-11-04
概要
基本信息
药物类型 小分子化药 |
别名 Diastabol、Miglibay、Miglitol (JP17/USAN/INN) + [12] |
作用机制 α-glucosidase抑制剂(酸性α-葡萄糖苷酶抑制剂) |
治疗领域 |
非在研适应症 |
原研机构 |
非在研机构- |
最高研发阶段批准上市 |
首次获批日期 荷兰 (1996-07-23), |
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C8H17NO5 |
InChIKeyIBAQFPQHRJAVAV-ULAWRXDQSA-N |
CAS号72432-03-2 |
关联
42
项与 米格列醇 相关的临床试验Miglitol combined with GC chemotherapy regimen to improve the efficacy of locally advanced and advanced bladder cancer
观察持证商为三和化学研究所株式会社的米格列醇片（规格：25 mg，商品名：SEIBULE®）在中国健康受试者中进行的单中心、开放、单序列、空腹、三周期、单次给药设计的药效动力学研究预试验
A single arm multicenter clinical study of miglitol in the treatment of muscle invasive bladder cancer
100 项与 米格列醇 相关的临床结果
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100 项与 米格列醇 相关的转化医学
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100 项与 米格列醇 相关的专利（医药）
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360
项与 米格列醇 相关的文献（医药）2024-12-31Journal of enzyme inhibition and medicinal chemistry
Development of iminosugar-based glycosidase inhibitors as drug candidates for SARS-CoV-2 virus via molecular modelling and in vitro studies
Article
作者: Ferjancic, Zorana ; Djurkovic, Filip ; Trmcic, Milena ; Vulovic, Bojan ; Djurdjevic Djelmas, Aleksandra ; Pavlovic, Milos ; Prodanovic, Radivoje ; Bihelovic, Filip ; Vignuzzi, Marco ; Matovic, Radomir ; Saicic, Radomir N ; Sladic, Dusan ; Kalicanin, Nevena ; Jankovic, Aleksandar ; Vallet, Thomas ; Zlatovic, Mario
We developed new iminosugar-based glycosidase inhibitors against SARS-CoV-2. Known drugs (miglustat, migalastat, miglitol, and swainsonine) were chosen as lead compounds to develop three classes of glycosidase inhibitors (α-glucosidase, α-galactosidase, and mannosidase). Molecular modelling of the lead compounds, synthesis of the compounds with the highest docking scores, enzyme inhibition tests, and in vitro antiviral assays afforded rationally designed inhibitors. Two highly active α-glucosidase inhibitors were discovered, where one of them is the most potent iminosugar-based anti-SARS-CoV-2 agent to date (EC90 = 1.94 µM in A549-ACE2 cells against Omicron BA.1 strain). However, galactosidase inhibitors did not exhibit antiviral activity, whereas mannosidase inhibitors were both active and cytotoxic. As our iminosugar-based drug candidates act by a host-directed mechanism, they should be more resilient to drug resistance. Moreover, this strategy could be extended to identify potential drug candidates for other viral infections.
2024-12-31JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
New natural protein tyrosine phosphatase 1B inhibitors from
Gynostemma pentaphyllum
Article
作者: Wu, Di ; Qin, Lin ; Wang, Jianmei ; Zhang, Qianru ; He, Yuqi ; Wu, Xingdong ; Du, Yimei ; Tan, Daopeng ; Wang, Xianting ; Xie, Jian ; Deng, Yidan
Type 2 diabetes mellitus (T2DM) is a chronic metabolic disease mainly caused by insulin resistance, which can lead to a series of complications such as cardiovascular disease, retinopathy, and its typical clinical symptom is hyperglycaemia. Glucosidase inhibitors, including Acarbose, Miglitol, are commonly used in the clinical treatment of hypoglycaemia. In addition, Protein tyrosine phosphatase 1B (PTP1B) is also an important promising target for the treatment of T2DM. Gynostemma pentaphyllum is a well-known oriental traditional medicinal herbal plant, and has many beneficial effects on glucose and lipid metabolism. In the present study, three new and nine known dammarane triterpenoids isolated from G. pentaphyllum, and their structures were elucidated by spectroscopic methods including HR-ESI-MS,1H and 13C NMR and X-ray crystallography. All these compounds were evaluated for inhibitory activity against α-glucosidase, α-amylase and PTP1B. The results suggested that compounds 7∼10 were potential antidiabetic agents with significantly inhibition activity against PTP1B in a dose-dependent manner.
2024-10-15Internal medicine (Tokyo, Japan)
Severe Acute Interstitial Nephritis Induced by α-glucosidase Inhibitor Miglitol in an Elderly Patient with Type 2 Diabetic Nephropathy
Article
作者: Nagata, Daisuke ; Imai, Toshimi ; Ono, Yuko ; Masuda, Takahiro ; Ono, Kazutoshi ; Hishida, Erika ; Akimoto, Tetsu ; Yoshizawa, Hiromichi ; Satonaka, Hiroshi
A 79-year-old male patient with type 2 diabetic nephropathy and hypertension was admitted to our hospital because of acute kidney injury with significantly elevated serum creatinine (8.12 mg/dL) and urinary β2-microglobulin (β2MG, 31,748 μg/L) levels. α-glucosidase inhibitor (α-GI) miglitol, started two weeks prior to presentation, was discontinued because drug-induced acute interstitial nephritis (AIN) was suspected. Renal biopsy revealed AIN and diabetic nephropathy. The drug-induced lymphocyte stimulation test for miglitol was also positive. After the discontinuation of miglitol, the urinary β2MG levels decreased to the normal range. This case raises the possibility that α-GI miglitol can worsen the renal function in patients with underlying renal dysfunction.
100 项与 米格列醇 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 |
|---|---|---|---|
| 糖尿病 | 日本 | 2005-10-11 | |
| 2型糖尿病 | 荷兰 | - | 1996-07-23 |
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 | 2006-06-07 | |
| 1型糖尿病 | 临床3期 | 日本 | 2005-09-13 | |
| 肥胖 | 临床2期 | 美国 | - |
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临床结果
临床结果
适应症
分期
评价
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N/A | - | - | 鹽醖憲醖鹹獵衊選憲繭(網觸憲顧糧壓構衊築夢) = 網構糧糧醖壓鏇簾築衊 顧積顧憲淵繭鏇鹽餘蓋 (餘膚範憲範壓繭醖廠餘 ) 更多 | - | 2020-06-01 | ||
鹽醖憲醖鹹獵衊選憲繭(網觸憲顧糧壓構衊築夢) = 餘鬱積願廠餘糧夢構窪 顧積顧憲淵繭鏇鹽餘蓋 (餘膚範憲範壓繭醖廠餘 ) 更多 | |||||||
N/A | 41 | 遞鹽鏇選廠鏇齋範範襯(壓獵獵衊糧餘醖壓鹹壓) = 鹽鹽製憲製選糧構蓋製 選窪蓋夢壓蓋築壓齋齋 (夢簾觸糧網糧齋鑰夢餘, 0.11) 更多 | 积极 | 2013-09-24 | |||
Sitagliptin | 遞鹽鏇選廠鏇齋範範襯(壓獵獵衊糧餘醖壓鹹壓) = 築構鹽夢觸範簾範遞選 選窪蓋夢壓蓋築壓齋齋 (夢簾觸糧網糧齋鑰夢餘, 0.17) 更多 |
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