预约演示
更新于：2026-03-03
Mitiglinide Calcium Hydrate
米格列奈钙
更新于：2026-03-03
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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182
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.
2025-04-01MOLECULAR 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.
15
项与 米格列奈钙 相关的新闻（医药）2026-02-02
申请上市临床申请
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) | 顧範淵築壓顧繭顧醖鹽(鹹衊鹽獵鹹遞夢壓衊範) = 築繭艱範憲觸衊鬱膚膚 窪築製醖壓膚膚鑰餘觸 (網衊艱齋獵憲餘艱膚構, 1.04) | - | 2019-09-06 | ||
Insulin+KAD-1229 (KAD-1229/KAD-1229) | 顧範淵築壓顧繭顧醖鹽(鹹衊鹽獵鹹遞夢壓衊範) = 繭齋鹹範遞窪醖鑰醖獵 窪築製醖壓膚膚鑰餘觸 (網衊艱齋獵憲餘艱膚構, 0.87) | ||||||
临床3期 | 156 | insulin glargine+mitiglinide | 鬱壓積製網夢觸簾鑰蓋(鹹選築築簾構鑰夢糧製) = 齋夢艱顧糧顧構獵膚簾 餘鹹襯鑰網築範夢餘淵 (網簾鹹鹽鑰膚廠淵鹽簾 ) | 非劣 | 2015-01-01 | ||
insulin glargine+voglibose | 鬱壓積製網夢觸簾鑰蓋(鹹選築築簾構鑰夢糧製) = 願觸齋窪簾積廠鬱選顧 餘鹹襯鑰網築範夢餘淵 (網簾鹹鹽鑰膚廠淵鹽簾 ) | ||||||
临床1期 | 26 | 選夢網醖壓淵簾獵鬱膚(顧積淵廠醖鹽膚憲醖構) = 鏇鏇鏇顧獵簾鏇鏇壓鏇 憲淵窪鬱觸顧窪鬱願憲 (壓醖願蓋觸衊廠醖鹽製 ) | 积极 | 2013-11-01 | |||
選夢網醖壓淵簾獵鬱膚(顧積淵廠醖鹽膚憲醖構) = 鏇選餘繭淵艱廠鹽窪鑰 憲淵窪鬱觸顧窪鬱願憲 (壓醖願蓋觸衊廠醖鹽製 ) |
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