预约演示
更新于：2025-08-02
Mitiglinide Calcium Hydrate
米格列奈钙
更新于：2025-08-02
概要
基本信息
药物类型 小分子化药 |
别名 Glinsuna、Mitiglinide、Mitiglinide calcium + [10] |
作用方式 阻滞剂 |
作用机制 KATP通道阻滞剂 |
治疗领域 |
在研适应症 |
非在研适应症- |
最高研发阶段批准上市 |
首次获批日期 日本 (2004-01-29), |
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C38H54CaN2O8 |
InChIKeyGJJVODCYSACLPP-UZYHXJQGSA-N |
CAS号207844-01-7 |
关联
41
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米格列奈钙片在健康人体中的随机、开放、交叉设计、四周期高脂餐后口服生物等效性试验
100 项与 米格列奈钙 相关的临床结果
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100 项与 米格列奈钙 相关的转化医学
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100 项与 米格列奈钙 相关的专利（医药）
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297
项与 米格列奈钙 相关的文献（医药）2025-04-01MOLECULAR PHARMACOLOGY
Structural similarity-based search for glinides exhibiting cis- and trans-inhibitory activity toward uric acid transporter 1
Article
作者: Sayama, Misa ; Anzai, Naohiko ; Miyauchi, Seiji ; Ishii, Itsuko ; Reien, Yoshie ; Suzuki, Takaaki
Various types of drugs can affect serum urate levels as side effects. Although these drugs are used to treat different diseases, they might share a structural component that acts on a common target to affect urate levels. Human urate transporter 1 (URAT1) plays an essential role in urate reabsorption at the renal proximal tubule and thus might be a common target for drugs that can affect serum urate levels. Our aim was to elucidate the structural requirements for a compound to show activity toward URAT1 and to identify clinically used drugs that can affect URAT1 activity. Our search was based on structural similarities in the compounds. [14C]Urate uptake by URAT1-expressing human embryonic kidney 293 (HEK-hURAT1) cells in the presence of an analog of a small molecule with known URAT1 activity suggested that structural moieties of salicylic acid can increase URAT1 cis-inhibitory activity. Therefore, we searched a database for drugs with substructures similar to salicylic acid. We were able to predict some types of loop diuretics, statins, and angiotensin receptor blockers as drug candidates that might affect URAT1. In addition, we found that glinides inhibit urate uptake by HEK-hURAT1 cells. Three glinides (nateglinide, mitiglinide, and repaglinide) all inhibited urate uptake by HEK-hURAT1 cells concentration-dependently (IC50: nateglinide, 39 μM; mitiglinide, 63 μM; repaglinide, 3.9 μM). Furthermore, glinides also showed trans-inhibition activity in URAT1-expressing Xenopus oocytes pretreated with the glinides. These findings suggest that glinides sharing a salicylic acid-like substructure might affect serum urate level by acting on URAT1. SIGNIFICANCE STATEMENT: Some types of loop diuretics, statins, angiotensin receptor blockers, and glinides were predicted to affect URAT1, based on their chemical structural similarity to salicylic acid, the structure of which allows it to interact with URAT1. Glinides in particular showed cis- and trans-inhibitory activity toward URAT1.
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.
2024-04-01Journal of diabetes investigation
Comparative effects of fixed‐dose mitiglinide/voglibose combination and glimepiride on vascular endothelial function and glycemic variability in patients with type 2 diabetes: A randomized controlled trial
Article
作者: Saito, Momo ; Tanaka, Yoshiya ; Tanaka, Kenichi ; Sonoda, Satomi ; Tomoyose, Yukiko ; Uemura, Fumi ; Hori, Yuri ; Tokutsu, Akemi ; Okada, Yosuke ; Hashimoto, Ryoma ; Kurozumi, Akira ; Umezu, Saeko ; Tateyama, Rina
ABSTRACT:
Introduction:
The aim of this study was to compare the effects of mitiglinide/voglibose with those of glimepiride on glycemic variability and vascular endothelial function in patients with type 2 diabetes.
Materials and Methods:
It was a multicenter, open‐label, randomized, crossover study. Hospitalized patients received either mitiglinide/voglibose (three times daily administration of 10 mg mitiglinide and 0.2 mg voglibose) or glimepiride (once‐daily 2 mg) in random order, each for 5 days. The reactive hyperemia index (RHI) and the mean amplitude of glycemic excursions (MAGE) were measured as co‐primary endpoints using reactive hyperemia peripheral arterial tonometry and continuous glucose monitoring.
Results:
The analysis included 30 patients (15 in each group). The RHI was 1.670 ± 0.369 during treatment with mitiglinide/voglibose and 1.716 ± 0.492 during treatment with glimepiride, with no significant difference between the two. MAGE was significantly lower in the mitiglinide/voglibose group (47.6 ± 18.5 mg/dL) than in the glimepiride group (100.6 ± 32.2 mg/dL). Although the mean blood glucose levels over the entire 24 h period were comparable between the two groups, the use of mitiglinide/voglibose was associated with a lower standard deviation of mean glucose, coefficient of variation, and mean postprandial glucose excursion compared with glimepiride. The time below range (<70 mg/dL) and the time above range (>180, >200, and 250 mg/dL) were lower in the mitiglinide/voglibose group, while the time in range (70–180 mg/dL) was higher.
Conclusions:
In our short‐duration randomized crossover study, although not impacting vascular endothelial function, mitiglinide/voglibose demonstrated potential benefits in reducing glycemic variability, postprandial hyperglycemia, and hypoglycemia in patients with type 2 diabetes.
100 项与 米格列奈钙 相关的药物交易
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研发状态
批准上市
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| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| 2型糖尿病 | 日本 | 2004-01-29 |
未上市
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| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| 内分泌系统疾病 | 临床1期 | 中国 | 2012-11-14 |
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临床结果
临床结果
适应症
分期
评价
查看全部结果
临床4期 | 178 | Insulin+KAD-1229 (Placebo/KAD-1229) | 艱鹹廠餘簾網鹹膚蓋膚(糧衊糧膚壓製製廠鑰廠) = 鏇廠齋齋齋構艱衊鑰獵 衊膚顧遞艱蓋壓願鏇齋 (夢壓獵簾選築鹹簾鬱簾, 1.04) | - | 2019-09-06 | ||
Insulin+KAD-1229 (KAD-1229/KAD-1229) | 艱鹹廠餘簾網鹹膚蓋膚(糧衊糧膚壓製製廠鑰廠) = 觸構構繭衊蓋願鏇範夢 衊膚顧遞艱蓋壓願鏇齋 (夢壓獵簾選築鹹簾鬱簾, 0.87) | ||||||
临床3期 | 156 | insulin glargine+mitiglinide | 餘蓋製積製製壓艱網遞(鬱憲願簾獵構構構範簾) = 齋蓋壓鹹蓋艱觸憲鬱齋 餘膚廠膚鹹積繭構膚鬱 (遞壓廠顧鑰膚餘繭衊願 ) | 非劣 | 2015-01-01 | ||
insulin glargine+voglibose | 餘蓋製積製製壓艱網遞(鬱憲願簾獵構構構範簾) = 網齋鏇壓廠積醖膚膚積 餘膚廠膚鹹積繭構膚鬱 (遞壓廠顧鑰膚餘繭衊願 ) | ||||||
临床1期 | 26 | 構願範艱顧窪糧製觸糧(襯鬱遞製構蓋鏇蓋醖製) = 鏇構積膚膚鬱衊積構鏇 鹽獵製獵鹽淵淵衊襯範 (廠淵範齋襯鑰築齋鏇膚 ) | 积极 | 2013-11-01 | |||
Sitagliptin alone | 構願範艱顧窪糧製觸糧(襯鬱遞製構蓋鏇蓋醖製) = 窪夢窪淵鹹鑰淵窪艱繭 鹽獵製獵鹽淵淵衊襯範 (廠淵範齋襯鑰築齋鏇膚 ) |
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