预约演示
更新于：2026-02-01
Mitiglinide Calcium Hydrate
米格列奈钙
更新于：2026-02-01
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
40
项与 米格列奈钙 相关的临床试验CTR20234251
米格列奈钙片随机、开放、交叉设计在中国健康受试者中的生物等效性正式试验
CTR20213240
米格列奈钙片(10mg)在健康受试者中的生物等效性试验
CTR20220245
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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184
项与 米格列奈钙 相关的文献（医药）2025-12-01Journal of Advanced Research
High-throughput screening identifies FDA approved drug mitiglinide as a novel pyroptosis inhibitor and therapeutic agent for osteoarthritis
Article
作者: Zhou, Yifei ; Zhao, Shiying ; Zhuo, Nanfang ; Zhang, Xiaolei ; Zhu, Zongxin ; Yu, Tanxin ; Lin, Shihan ; Zhang, Youli ; Wu, Aimin ; Wang, Jiangning ; Zhang, Hanwen ; Yu, Huilin
INTRODUCTION:
Osteoarthritis (OA), a leading cause of joint dysfunction, is characterized by progressive cartilage degradation linked to chondrocyte pyroptosis, yet disease-modifying therapies remain elusive. In this study, we conducted the first systematic drug repurposing screen in chondrocytes, aiming at identifying drugs that may suppress pyroptosis and verifying the therapeutic effects on OA.
METHODS:
Mitiglinide's effects on chondrocyte viability were quantified via CCK-8 assays and live/dead staining. Pyroptosis inhibition, extracellular matrix (ECM) homeostasis, and NF-κB activation were measured by western blot and immunofluorescence. Network pharmacology analysis and molecular docking were applied to predict the interacting protein of mitiglinide, while Nrf2 was knocked down by siRNAs to confirm its role in mitiglinide regulated pyroptosis and ECM. In vivo, destabilization of the medial meniscus (DMM) model -induced OA mice received mitiglinide for 8 weeks, with efficacy evaluated through X-ray, OARSI-graded histopathology, immunohistochemistry, Hematoxylin-Eosin and Safranin O-Fast green staining.
RESULTS:
Through high-throughput screening (HTS) of 1,228 FDA-approved drugs, we identified a list of pyroptosis inhibitors, and mitiglinide was suggested as one of the most potent pyroptosis inhibitors in chondrocyte. Mechanistic studies demonstrated that mitiglinide may directly target Nrf2 and suppress its downstream NF-κB-driven NLRP3 inflammasome activation; it may also promote ECM homeostasis in chondrocytes. In vivo study showed that mitiglinide may effectively attenuate OA pathology in mice.
CONCLUSION:
Mitiglinide, identified via FDA-drug-library screening, alleviates OA progression by suppressing NLRP3 inflammasome activation and ECM degradation via activation of the Nrf2/HO-1 signaling pathway. This positions mitiglinide as a repurposed disease-modifying OA drug candidate.
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: Satomi Sonoda ; Yuri Hori ; Yukiko Tomoyose ; Yosuke Okada ; Momo Saito ; Saeko Umezu ; Fumi Uemura ; Ryoma Hashimoto ; Kenichi Tanaka ; Akemi Tokutsu ; Rina Tateyama ; Yoshiya Tanaka ; Akira Kurozumi
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.
14
项与 米格列奈钙 相关的新闻（医药）2026-01-30
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
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 | 2004-01-29 |
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 |
|---|---|---|---|---|
| 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) | 鏇齋觸膚鏇鬱製製夢鑰(憲築窪憲窪衊衊廠鏇淵) = 窪醖鏇觸鏇鏇鑰鹽鬱願 觸築遞膚膚鏇艱構夢構 (窪觸網壓壓遞衊鏇憲選, 1.04) | - | 2019-09-06 | ||
Insulin+KAD-1229 (KAD-1229/KAD-1229) | 鏇齋觸膚鏇鬱製製夢鑰(憲築窪憲窪衊衊廠鏇淵) = 淵夢餘網鬱繭顧餘築簾 觸築遞膚膚鏇艱構夢構 (窪觸網壓壓遞衊鏇憲選, 0.87) | ||||||
临床3期 | 156 | insulin glargine+mitiglinide | 廠網餘製鑰顧蓋觸鹹鹹(繭淵蓋範餘繭製窪齋醖) = 窪淵淵積蓋艱膚鹽膚積 夢窪願遞簾範構醖憲遞 (築膚齋願築蓋壓膚壓繭 ) | 非劣 | 2015-01-01 | ||
insulin glargine+voglibose | 廠網餘製鑰顧蓋觸鹹鹹(繭淵蓋範餘繭製窪齋醖) = 齋製範襯艱艱憲鹹範構 夢窪願遞簾範構醖憲遞 (築膚齋願築蓋壓膚壓繭 ) | ||||||
临床1期 | 26 | 膚鬱齋鬱鹹獵觸衊製艱(糧壓鏇構鬱糧襯淵觸鏇) = 願淵觸膚壓憲遞網壓網 築淵繭憲糧糧襯製鏇淵 (選餘齋廠艱願窪製鑰積 ) | 积极 | 2013-11-01 | |||
膚鬱齋鬱鹹獵觸衊製艱(糧壓鏇構鬱糧襯淵觸鏇) = 鹹艱顧顧鏇顧膚憲範壓 築淵繭憲糧糧襯製鏇淵 (選餘齋廠艱願窪製鑰積 ) |
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