预约演示
更新于：2025-03-25
Voglibose
伏格列波糖
更新于：2025-03-25
概要
基本信息
药物类型 小分子化药 |
别名 Glustat、Voglibose (JP17/USAN/INN)、Voglistat + [8] |
作用方式 抑制剂 |
作用机制 GANC抑制剂(glucosidase alpha, neutral C inhibitors)、MGAM抑制剂(麦芽糖酶-糖化酶抑制剂)、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- |
非在研机构 |
最高研发阶段批准上市 |
首次获批日期 日本 (1994-07-01), |
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C10H21NO7 |
InChIKeyFZNCGRZWXLXZSZ-CIQUZCHMSA-N |
CAS号83480-29-9 |
关联
62
项与 伏格列波糖 相关的临床试验CTR20244400
伏格列波糖口崩片在中国健康受试者中单次口服给药的一项单中心、随机、开放、两制剂、两序列生物等效性试验
CTR20243825
伏格列波糖片人体生物等效性研究
CTR20242708
伏格列波糖片在健康受试者中的生物等效性研究
100 项与 伏格列波糖 相关的临床结果
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100 项与 伏格列波糖 相关的转化医学
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100 项与 伏格列波糖 相关的专利（医药）
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801
项与 伏格列波糖 相关的文献（医药）2025-01-01Food Science & Nutrition
Antioxidant, Alpha‐Amylase Inhibitory and Hypoglycemic Activity of Smallanthus sonchifolius Leaves from Nepal: An Integrated In Vitro, In Vivo, and In Silico Approach
Article
作者: Pandey, Bipindra ; Rawal, Prakash ; Panta, Sushil ; Yadav, Ram Kishor
ABSTRACT:
In 2019, diabetes mellitus affected 9.3% of the global population and accounted for one in nine adult deaths. Plant‐based antioxidants neutralize harmful free radicals, mitigate oxidative stress, and significantly prevent diabetes and its complications. This study evaluated the in vitro antioxidant, alpha‐amylase inhibitory, in vivo oral hypoglycemic, and in silico antidiabetic potential of Smallanthus sonchifolius (S. sonchifolius) leaf extract. Mice (n = 25) were divided into five groups after a 16‐h fast with access to water. The groups received distilled water (normal control), metformin (100 mg/kg, standard), or S. sonchifolius ethanolic extract at 100, 250, or 500 mg/kg to compare the antidiabetic potential of the extract with that of the control. Fasting blood glucose levels were measured in tail vein blood before the experiment and at 30, 60, and 120 min post‐administration to evaluate the hypoglycemic activity of the extract and standard drug. The ethanolic extract exhibited dose‐dependent alpha‐amylase inhibition (IC50 value 0.136 mg/mL) and significant hypoglycemic effects, reducing blood glucose levels similar to those of the standard drugs voglibose and metformin. The maximum blood glucose reduction was 17.99% and 15.74% in the normal and glucose‐loaded mice, respectively, at 500 mg/kg within 120 min. In silico analysis shows, polymatin B and chlorogenic acid demonstrating the highest binding affinity of −8.2 and −7.2 kcal/mol, respectively, in PPAR‐γ (3G9E). Polymatin B and chlorogenic acid showed strong binding affinities of −7.3 and −7.5 kcal/mol, respectively, in alpha‐amylase (4W93). These findings indicate that S. sonchifolius possesses significant hypoglycemic and antioxidant properties, suggesting its potential as an antidiabetic agent, warranting further clinical research.
2025-01-01JOURNAL OF CHROMATOGRAPHY B-ANALYTICAL TECHNOLOGIES IN THE BIOMEDICAL AND LIFE SCIENCES
Non-targeted screening of illegal added hypoglycemic drugs and their derivatives in functional foods using characteristic fragment ions scanning based on liquid chromatography-high-resolution mass spectrometry
Article
作者: Liu, Yajie ; Feng, Feng ; Zhang, Feng ; Du, Rongzhu ; Wang, Xiujuan ; Feng, Xuesong
Functional foods that are illegally adulterated with chemical hypoglycemic drugs or their derivatives pose serious risks to human health. However, the detection of these compounds is a challenge due to the unknown nature of their structures, particularly as many of these compounds are newly synthesized and lack standardized references. In this study, we developed a non-targeted screening strategy for detecting illegally added hypoglycemic drugs and their derivatives in oral solution and hard capsule functional foods. This strategy utilizes a self-established characteristic fragment ions mass spectrum database based on ultrahigh-performance liquid chromatography-quadrupole/orbitrap high-resolution mass spectrometry. Nine characteristic fragment ions were identified by analyzing the mass spectrometric fragmentation patterns of hypoglycemic drugs. Meanwhile, the precursor and fragment ions of 38 known hypoglycemic drugs were collected and incorporated into the mass database. The detection limits of hypoglycemic drugs in oral solution and hard capsule samples were 0.01-10 μg/L and 0.01-50 μg/kg, respectively. Applying the non-targeted method to 20 batches of suspicious samples, we found that 3 batches of samples contained illegal added drugs. Furthermore, we identified a previously unrecorded hypoglycemic drug not present in the mass database. These results indicate that the developed strategy is a powerful tool for the rapid and highly sensitive identification of both known and unknown hypoglycemic drugs, as well as their derivatives in functional foods.
2024-12-16Future Medicinal Chemistry
Synthesis of arylated tetrahydrobenzo[
H
]quinoline-3-carbonitrile derivatives as potential hits for treatment of diabetes
Article
作者: Seraj, Faiza ; Khan, Khalid Mohammed ; Baltaş, Nimet ; Taha, Muhammad ; Naz, Fouzia ; Ul-Haq, Zaheer ; Özil, Musa ; Tariq, Syeda Sumayya ; Salar, Uzma
Aim: Quinoline scaffolds are serving as the core structure for numerous antifungal, analgesic, antipyretic, anti-inflammatory drugs as well as have also been investigated for their potential antidiabetic properties. Though further exploration is required in this area as the current antidiabetic agents, such as acarbose, miglitol and voglibose, are associated with several adverse side effects. In this context, arylated tetrahydrobenzo[H]quinoline-3-carbonitrile derivatives were designed and evaluated as potential antidiabetic agents.Materials & methods: A one-pot multicomponent reaction of 6-methoxy-1-tetralone with ethyl cyanoacetate, ammonium acetate and varying aldehydes yielded a range of new arylated tetrahydrobenzo[h]quinoline-3-carbonitrile molecules 1-36.Results: Compounds 2-5, 12, 13, 19 and 32-34 showed excellent inhibition against α-amylase (IC50 = 3.42-15.14 μM) and α-glucosidase (IC50 = 0.65-9.23 μM) enzymes in comparison to the standard acarbose (IC50 = 14.35 μM). In addition, all compounds revealed significant to moderate DPPH radical scavenging activity (SC50 = 21.30-138.30 μM) compared with BHT (SC50 = 64.40 μM). Kinetic studies confirmed competitive inhibition mode, while molecular docking studies comprehend ligands' interaction with enzyme's active sites and absorption, distribution, metabolism, and excretion analysis confirms that all synthetic derivatives are nontoxic.Conclusion: This research offers a range of lead candidates to become antidiabetic agents after further advanced study.
100 项与 伏格列波糖 相关的药物交易
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研发状态
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 | 中国 | 2001-01-01 | |
| 糖尿病 | 中国 | 2001-01-01 | |
| 2型糖尿病 | 日本 | 1994-07-01 |
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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 | 494 | 遞艱窪鏇獵願艱齋製憲(憲壓鹹醖齋觸衊繭觸淵) = 繭糧積遞淵鏇鏇鬱獵構 艱艱鹹衊窪願廠顧築範 (簾觸顧鬱艱憲繭鏇構鏇, 0.0742) 更多 | - | 2019-02-04 | |||
遞艱窪鏇獵願艱齋製憲(憲壓鹹醖齋觸衊繭觸淵) = 夢膚夢膚網選繭構獵齋 艱艱鹹衊窪願廠顧築範 (簾觸顧鬱艱憲繭鏇構鏇, 0.0764) 更多 | |||||||
临床4期 | 197 | 簾襯築遞衊齋繭壓鹹鏇 = 鹽獵蓋艱願淵齋遞餘觸 願製衊鏇壓遞窪窪選繭 (艱鹽範繭淵醖蓋襯糧製, 獵簾選簾製積窪醖製鹹 ~ 憲構衊製糧顧鏇醖鹹製) 更多 | - | 2015-04-09 | |||
临床1期 | - | 22 | Metformin | 鹹醖獵糧顧鹽廠糧艱顧(衊壓襯選獵繭選選鹽鏇): geometric mean ratio = 0.99 (90% CI, 0.92 ~ 1.06), P-Value = > 0.05 更多 | - | 2014-11-01 | |
Metformin + Voglibose | |||||||
临床3期 | 133 | Sitagliptin 50 mg/day | 顧獵膚鬱襯蓋衊顧壓構(餘廠壓鏇淵網衊遞淵餘) = 窪衊鏇醖淵憲壓廠夢壓 簾憲衊築鹹餘餘範製夢 (廠鹹範壓鬱壓鏇構遞遞 ) 更多 | - | 2013-11-27 | ||
临床3期 | 319 | Sitagliptin 50 mg once daily | 夢鬱選選觸鏇窪糧築艱(鹽鹹鏇衊繭獵選鹹網顧) = 積顧鑰鏇膚觸憲積衊積 鬱鹹窪襯齋顧廠選鬱鏇 (鹽簾顧鬱憲積艱夢製鬱, -0.8 ~ -0.6) 更多 | 积极 | 2010-07-01 | ||
Voglibose 0.2 mg thrice daily | 夢鬱選選觸鏇窪糧築艱(鹽鹹鏇衊繭獵選鹹網顧) = 窪鏇鑰糧構廠廠襯壓簾 鬱鹹窪襯齋顧廠選鬱鏇 (鹽簾顧鬱憲積艱夢製鬱, -0.4 ~ -0.2) 更多 |
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