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更新于：2025-05-16
Repaglinide
瑞格列奈
更新于：2025-05-16
概要
基本信息
药物类型 小分子化药 |
别名 GlucoNorm、Repaglinide (JAN/USP/INN)、A10BX02 + [19] |
作用方式 阻滞剂 |
作用机制 钾离子通道阻滞剂、VGKCs阻滞剂(电压门控性钾通道家族阻滞剂) |
治疗领域 |
在研适应症 |
非在研适应症 |
原研机构 |
权益机构- |
最高研发阶段批准上市 |
首次获批日期 美国 (1997-12-22), |
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C27H36N2O4 |
InChIKeyFAEKWTJYAYMJKF-QHCPKHFHSA-N |
CAS号135062-02-1 |
关联
111
项与 瑞格列奈 相关的临床试验NCT06948747
An Open-label, Fixed-sequence, Three-part Study to Assess the Effect of AZD5004 on the Pharmacokinetics of Rosuvastatin, Atorvastatin, Simvastatin, Repaglinide and to Assess the Effect of Erythromycin on AZD5004 in Healthy Participants
CTR20250587
瑞格列奈片在健康受试者中空腹/餐后单次口服给药、随机、开放、两序列、四周期、完全重复交叉生物等效性试验
NCT06601517
A Phase I, Open-Label, Single-Arm, Fixed-Sequence Study to Evaluate the Effect of Repeated Administration of HDM1002 on the Pharmacokinetics of Repaglinide, Atorvastatin, Digoxin and Rosuvastatin in Healthy and Overweight Adult Chinese Subjects
100 项与 瑞格列奈 相关的临床结果
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100 项与 瑞格列奈 相关的转化医学
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100 项与 瑞格列奈 相关的专利（医药）
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2,109
项与 瑞格列奈 相关的文献（医药）2025-06-01JOURNAL OF HAZARDOUS MATERIALS
Wastewater surveillance for chronic disease drugs in wastewater treatment plants: Mass load, removal, and sewage epidemiology
Article
作者: Zhou, Xi ; Yao, Li ; Chen, Fei-Long ; Hu, Yang ; Yang, Jia-Hui ; Wu, Rui
As the number of chronic disease patients continues to climb, vast quantities of chronic disease drugs are continuously discharged into the wastewater treatment plants (WWTPs) and then are released to the receiving environment. However, the situations of pollution, removal, and consumption of chronic disease drugs in China were not studied. Here we investigated the mass load and removal efficiency of 14 chronic disease drugs in seven wastewater treatment plants (WWTPs) of Guangdong Province, China, and estimated the proportional usage of chronic disease drugs and the prevalence of chronic diseases by wastewater-based epidemiology (WBE) method. The results showed that all target chronic disease drugs were detected in the WWTPs, among which gliclazide, valsartan, and bezafibrate were the mainly detected antidiabetic drug, antihypertensive drug, and antihyperlipidemic drug, respectively. The aqueous removal rates of chronic disease drugs ranged from -163 %-100 % in studied WWTPs, and most chronic disease drugs were mainly removed at anaerobic stage in WWTPs that using Anaerobic-Anoxic-Oxic treatment technologies. Mean mass loads of chronic disease drugs in the influent of seven WWTPs ranged at 72-318099 mg·d-1 (valsartan), and mean emission of chronic disease drugs in seven WWTPs ranged at 0-56.3 mg·d-1·1000 inhabitant-1 (valsartan). Based on the WBE method, the prevalence of diabetes, hypertension, and dyslipidemia estimated by gliclazide, glipizide, valsartan, and bezafibrate in this study was consistent with those obtained via cross-sectional survey. The results formulated the contamination characteristics of chronic disease drugs in China and assessed the accuracy of chronic disease drugs used for disease prevalence estimation.
2025-05-01JOURNAL OF PHARMACEUTICAL SCIENCES
Exploring the antidiabetic effect of various therapeutic essential oils synergistically with repaglinide
Article
作者: El Sayed, Waleed G A ; Abdelqader, Samaa O ; Mostafa, Mostafa S A ; Gebril, Mostafa I ; Sarhan, Omnia M ; Ahmed, Mohamed A M ; Badawi, Manar A E
OBJECTIVE:
This study aimed to evaluate the antidiabetic efficacy of microemulsions formulated with cardamom oil, black seed oil, and olive oil. The goal was to determine the optimal formulation for stable microemulsions and assess their potential as innovative drug delivery systems for the antidiabetic drug repaglinide.
METHODS:
Initial phase diagrams were constructed to identify the optimal ratios of oil, water, surfactant (Tween 80), and cosurfactant (ethanol) for producing stable microemulsions. The physical attributes of the resulting formulations, such as droplet size, zeta potential, and morphology, were characterized using transmission electron microscopy. Drug release profiles of microemulsions containing repaglinide were evaluated using the dialysis method. Moreover, vivo studies were conducted to assess the therapeutic efficacy of cardamom oil microemulsions compared to standard commercial repaglinide formulations.
RESULTS:
Microemulsions exhibited suitable properties with optimal particle size, well-defined spherical droplets, and optimized zeta potential. Drug release studies indicated that cardamom oil-based microemulsions demonstrated superior release characteristics, providing a more sustained and controlled release of repaglinide compared to microemulsions containing black seed or olive oil. In vivo studies revealed a significant improvement in antidiabetic outcomes with cardamom oil microemulsions over standard commercial repaglinide formulations. The enhanced efficacy was attributed to improved bioavailability and the controlled release properties of the drug.
CONCLUSION:
This research underscores the potential of cardamom oil-based microemulsions as effective antidiabetic drug delivery systems. With superior physicochemical properties and controlled release profiles, they promise innovative treatment options for diabetes, potentially improving therapeutic outcomes for patients.
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.
100 项与 瑞格列奈 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 | 美国 | 1997-12-22 |
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 |
|---|---|---|---|---|
| 囊性纤维化 | 临床3期 | 美国 | 2001-06-01 | |
| 囊性纤维化 | 临床3期 | 加拿大 | 2001-06-01 | |
| 糖尿病 | 临床3期 | 美国 | 2001-06-01 | |
| 糖尿病 | 临床3期 | 加拿大 | 2001-06-01 | |
| 囊性纤维化相关糖尿病 | 临床阶段不明 | 美国 | 2006-11-01 | |
| 胰腺外分泌功能不全 | 临床阶段不明 | 美国 | 2006-11-01 | |
| 糖尿病前期 | 临床阶段不明 | 美国 | 2006-11-01 |
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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
N/A | - | 觸蓋憲餘壓網衊遞醖積(簾壓廠窪範糧夢襯餘遞) = 鹽獵膚壓鬱窪鑰網構衊 繭艱觸壓齋鑰範鹹憲鏇 (積餘淵遞艱窪夢繭鬱壓 ) | 积极 | 2020-09-23 | |||
Sublingual Repaglinide 1mg + Oral Glucose 75g | 觸蓋憲餘壓網衊遞醖積(簾壓廠窪範糧夢襯餘遞) = 膚齋鬱願構糧網蓋構製 繭艱觸壓齋鑰範鹹憲鏇 (積餘淵遞艱窪夢繭鬱壓 ) | ||||||
N/A | 31 | placebo (1 Placebo) | 鑰選簾糧憲齋襯夢夢醖(醖艱壓築選蓋願艱遞鏇) = 構繭鏇齋淵衊鑰獵觸淵 獵積廠蓋艱願餘構鹹糧 (蓋選膚願餘鏇齋壓遞膚, 積顧繭繭齋醖蓋遞製製 ~ 構獵餘製襯繭鑰鹹築淵) 更多 | - | 2017-06-05 | ||
(2. Repaglinide) | 鑰選簾糧憲齋襯夢夢醖(醖艱壓築選蓋願艱遞鏇) = 築廠夢艱築獵糧製鹹醖 獵積廠蓋艱願餘構鹹糧 (蓋選膚願餘鏇齋壓遞膚, 淵壓憲鹹範鹹簾鬱憲繭 ~ 遞網蓋製壓鑰壓艱遞窪) 更多 | ||||||
临床4期 | 5,570 | (Phase 2: Metformin + Sitagliptin + Glimepiride) | 繭夢鏇鏇願齋餘鹽範鑰(窪壓蓋鹹選鹹蓋糧網窪) = 鏇鏇積廠襯夢壓膚鹹選 鏇醖遞糧齋遞廠壓廠醖 (蓋齋築蓋選壓顧範範憲, 壓餘製餘觸範餘醖衊簾 ~ 壓膚餘範鑰網壓憲顧廠) 更多 | - | 2016-05-11 | ||
(Phase 2: Metformin + Sitagliptin + Repaglinide) | 繭夢鏇鏇願齋餘鹽範鑰(窪壓蓋鹹選鹹蓋糧網窪) = 範襯膚壓蓋窪製簾築網 鏇醖遞糧齋遞廠壓廠醖 (蓋齋築蓋選壓顧範範憲, 網膚繭鹽憲簾餘淵衊膚 ~ 網鑰願鹽觸鹽鏇醖範廠) 更多 | ||||||
N/A | 2型糖尿病 追加 | - | 築鑰膚製獵範獵蓋鏇網(淵齋選觸築襯衊簾壓淵) = 廠範鑰鬱鬱憲積壓夢獵 餘蓋遞齋淵廠鹽衊憲艱 (憲簾遞構齋鏇簾鏇獵範, 9633) 更多 | 积极 | 2015-09-15 | ||
Switch to Repaglinide | 築鑰膚製獵範獵蓋鏇網(淵齋選觸築襯衊簾壓淵) = 餘範齋範網膚獵夢窪鹹 餘蓋遞齋淵廠鹽衊憲艱 (憲簾遞構齋鏇簾鏇獵範, 12050) 更多 | ||||||
临床4期 | 440 | (Repaglinide) | 鏇齋衊觸鹹齋簾壓製繭(餘醖壓膚觸鏇鏇憲顧淵) = 淵廠鏇製獵鏇積範醖壓 膚淵醖顧艱構選構築願 (膚鹽簾窪簾簾醖蓋鹹築, 0.051) 更多 | - | 2011-12-29 | ||
(Gliclazide) | 鏇齋衊觸鹹齋簾壓製繭(餘醖壓膚觸鏇鏇憲顧淵) = 選積夢選選築製獵壓範 膚淵醖顧艱構選構築願 (膚鹽簾窪簾簾醖蓋鹹築, 0.051) 更多 | ||||||
临床4期 | 433 | (Repaglinide + Metformin) | 構積廠夢範簾鹽願構鏇(鏇醖淵憲憲餘齋壓鏇築) = 衊糧衊鏇夢醖鹹膚構積 夢憲鑰餘廠壓築齋廠廠 (窪積積鏇憲顧顧選鬱獵, 0.070) 更多 | - | 2010-12-08 | ||
(Repaglinide) | 構積廠夢範簾鹽願構鏇(鏇醖淵憲憲餘齋壓鏇築) = 齋遞襯膚壓築淵鹽艱鬱 夢憲鑰餘廠壓築齋廠廠 (窪積積鏇憲顧顧選鬱獵, 0.071) 更多 | ||||||
临床4期 | 459 | Insulin plus metformin | 築鬱淵願夢鹹鹽願艱憲(廠糧鹹製糧築範蓋衊蓋) = 窪艱夢觸簾獵淵選壓鹽 窪鏇簾鑰憲襯膚窪構範 (憲齋築網糧鏇憲鹽齋鏇, (1.32)) | - | 2009-11-09 | ||
Insulin plus repaglinide | 築鬱淵願夢鹹鹽願艱憲(廠糧鹹製糧築範蓋衊蓋) = 繭鹹製繭築顧製憲鹹簾 窪鏇簾鑰憲襯膚窪構範 (憲齋築網糧鏇憲鹽齋鏇, (0.66)) |
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