更新于：2024-12-09
Repaglinide
瑞格列奈
更新于：2024-12-09
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 |
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
分子式C27H36N2O4 |
InChIKeyFAEKWTJYAYMJKF-QHCPKHFHSA-N |
CAS号135062-02-1 |
关联
118
项与 瑞格列奈 相关的临床试验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
瑞格列奈片在健康受试者中的比较药代动力学试验（包括空腹试验和餐后试验，均采用单中心、每周期单次口服给药、随机、开放、两序列、四周期完全重复试验设计）
KF2022#4-tutkimus:Beetasalpaajan ja tulehduskipulääkkeen Vaikutus CYP-entsyymivälitteiseen lääkeainemetaboliaan
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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860
项与 瑞格列奈 相关的文献（医药）2025-01-01JOURNAL OF ETHNOPHARMACOLOGY
Assessing the potential fasting and postprandial mechanisms involved in the acute hypoglycemic and anti-hyperglycemic effects of four selected plants from Iran used in traditional Persian medicine
Article
作者: Andrade-Cetto, Adolfo ; Escandón-Rivera, Sonia M ; Espinoza-Hernández, Fernanda A ; Safavi, Fereshteh
ETHNOPHARMACOLOGICAL RELEVANCE:
In traditional Persian medicine (TPM), people often use herbal infusions as a dosage form to treat diseases related to hyperglycemia, known as 'dam-kardeh'. Traditionally, herbal preparations of Eryngium bungei Boiss. (E. b), Tragopogon buphthalmoides (DC.) Boiss. (T. b), Salvia hydrangea DC. ex Benth. (S. h), and Juniperus polycarpos K. Koch. (J. p) are used to manage diabetes in Iran. However, there is no evidence of their effectiveness in controlling glucose levels and their mechanisms remain unclear.
AIM OF THE STUDY:
This study aimed to investigate whether traditional doses of plant infusions can have hypoglycemic and/or anti-hyperglycemic effects during fasting and/or postprandial states and establish the basis for future research on their potential mechanisms of action.
MATERIALS AND METHODS:
The effects of traditional doses of herbal extracts on blood glucose levels in STZ-NA-induced hyperglycemic rats were investigated in 2-h acute tests during fasting and postprandial states (with a glucose load). In addition, the potential inhibitory effect in vitro of enzymes involved in relevant pathways, such as gluconeogenesis (fructose-1,6-bisphosphatase, FBPase and glucose-6-phosphatase, G6Pase), carbohydrate breakdown (intestinal α-glucosidases), and insulin sensitivity (protein tyrosine phosphatase 1B, PTP-1B) was evaluated. Acute toxicity tests were carried out and HPLC-SQ-TOF was used to analyze the chemical profiles of the plant extracts.
RESULTS:
In the fasting state, T. b, S. h, and E. b were as effective as glibenclamide in lowering blood glucose levels in hyperglycemic rats. Moreover, all three suppressed G6Pase and FBPase enzymatic activity by 90-97% and 80-91%, respectively. On the other hand, significant postprandial hypoglycemic efficacy was observed for E. b, S. h, and T. b. Based on the AUC values, T. b caused a reduction comparable to the therapeutic efficacy of repaglinide. When investigating the possible mechanisms of action involved in this activity, E. b, S. h, and T. b showed significant inhibition of PTP-1B in vitro (>70%). Finally, all plant extracts showed no signs of acute toxicity. Several compounds that may contribute to biological activities were identified, including phenolic acids and flavonoid glycosides.
CONCLUSIONS:
The present study supports the traditional use of T. b, E. b and S. h for the control of diabetes in the fasting and postprandial state. Moreover, these plants were found to be rich in bioactive compounds with hypoglycemic and antihyperglycemic activities. On the other hand, J. p, showed a modest effect only in the fasting state and after 90 min. Further studies are needed to expand these results by analyzing the chemical composition and using complementary experimental models.
2024-12-01DRUG METABOLISM AND DISPOSITION
Candesartan Has No Clinically Meaningful Effect on the Plasma Concentrations of Cytochrome P450 2C8 Substrate Repaglinide in Humans
Article
作者: Piha, Mikael O W ; Tornio, Aleksi ; Filppula, Anne M. ; Niemi, Mikko ; Cajanus, Kristiina ; Backman, Janne T ; Filppula, Anne M ; Engström, Marica T ; Engström, Marica T. ; Piha, Mikael O.W. ; Bergmann, Troels K ; Bergmann, Troels K. ; Backman, Janne T. ; Neuvonen, Mikko
In vitro evidence shows that the acyl-β-D-glucuronide metabolite of candesartan inhibits cytochrome P450 (CYP) 2C8 with an inhibition constant of 7.12 μM. We investigated the effect of candesartan on the plasma concentrations and glucose-lowering effect of repaglinide, a sensitive clinical CYP2C8 index substrate. In a randomized crossover study, ten healthy volunteers ingested 8 mg of candesartan or placebo daily for three days, and on day 3, they also ingested 0.25 mg of repaglinide one hour after candesartan or placebo. We measured the plasma concentrations of repaglinide, candesartan, and candesartan acyl-β-D-glucuronide, and blood glucose concentrations for up to nine hours after repaglinide intake. Candesartan had no effect on the area under the plasma concentration-time curve and peak plasma concentration of repaglinide compared with placebo, with ratios of geometric means of 1.02 [P = 0.809; 90% confidence interval (CI) 0.90-1.15] and 1.13 (P = 0.346; 90% CI 0.90-1.43), respectively. Other pharmacokinetic variables and blood glucose concentrations were neither affected. Candesartan acyl-β-D-glucuronide was detectable in seven subjects, in whom the peak concentration of repaglinide was 1.32-fold higher in the candesartan phase than in the placebo phase (P = 0.041; 90% CI 1.07-1.62). Systemic concentrations of candesartan acyl-β-D-glucuronide were very low compared with its CYP2C8 inhibition constant (ratio ≪ 0.1). Furthermore, in a cohort of 93 cancer patients, no indication of decreased paclitaxel clearance was found in four patients using candesartan concomitantly. In conclusion, candesartan therapy is unlikely to inhibit CYP2C8-mediated metabolism of other drugs to any clinically significant extent. SIGNIFICANCE STATEMENT: The findings of this study suggest that candesartan is unlikely to cause drug-drug interactions via inhibition of cytochrome P450 (CYP) 2C8. Although candesartan acyl-β-D-glucuronide has been shown to inhibit CYP2C8 in vitro, it shows no clinically relevant CYP2C8 inhibition in humans due to low systemic concentrations.
2024-09-16Bioanalysis
DoE-assisted HPLC method development and validation of enzalutamide and repaglinide in rat plasma
Article
作者: Jogvanshi, Akanksha ; Reddy, Dannarm Srinivas ; Chenkual, Laltanpuii ; Reddy, Gangireddy Navitha ; Sonti, Rajesh
Aim: A simple and rapid HPLC technique was developed and validated to simultaneously estimate enzalutamide (ENZ) and repaglinide (REP) in rat plasma.Methods: In silico predictions using DDinter and DDI-Pred indicated possible drug-drug interactions between ENZ and REP. A central composite design was used to identify factors influencing the separation of the drugs. Interactions between chromatographic parameters were studied through 51 experiments, followed by illustration with three-dimensional response surface plots. The four factors optimized for the separation of the two drugs are column temperature (A), % organic strength (B), pH (C) and column type (D).Results: Plate count(R1), tailing factor (R2) and resolution (R3) responses in the experimental design were analyzed with the favorable chromatographic conditions predicted to be 0.1% formic acid and acetonitrile as mobile phases on a Phenomenex C18 LC column (250 × 4.6 mm, 5 μm). The method was applied to estimate the drugs in rat plasma using a simple protein-precipitation step and found to be linear, accurate and precise within the ranges of 0.5-16 and 5-50 μg/ml for ENZ and REP, respectively.Conclusion: The optimized method can be used in future bioanalytical workflow for drug quantification and drug-drug compatible studies.
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
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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
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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 |
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临床结果
临床结果
适应症
分期
评价
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N/A | - | 遞簾鬱壓夢鏇鏇鏇膚鑰(糧膚遞簾膚夢醖艱齋鏇) = 鹽築願膚觸夢鹹鹽範糧 選窪壓醖獵鹹觸鏇衊觸 (鏇製鬱觸鑰獵艱築齋繭 ) | 积极 | 2020-09-23 | |||
Sublingual Repaglinide 1mg + Oral Glucose 75g | 遞簾鬱壓夢鏇鏇鏇膚鑰(糧膚遞簾膚夢醖艱齋鏇) = 醖構鬱糧鏇蓋遞選蓋憲 選窪壓醖獵鹹觸鏇衊觸 (鏇製鬱觸鑰獵艱築齋繭 ) | ||||||
N/A | 31 | placebo (1 Placebo) | 齋顧構廠築簾餘顧製簾(窪夢糧簾鏇鬱壓糧繭積) = 襯蓋築願鹽願淵膚淵膚 顧遞選膚鏇觸醖窪衊範 (淵簾蓋顧選觸網獵網齋, 艱網獵積積膚壓獵獵製 ~ 蓋願膚齋憲選夢觸憲餘) 更多 | - | 2017-06-05 | ||
(2. Repaglinide) | 齋顧構廠築簾餘顧製簾(窪夢糧簾鏇鬱壓糧繭積) = 醖襯糧醖鏇鹽齋夢簾選 顧遞選膚鏇觸醖窪衊範 (淵簾蓋顧選觸網獵網齋, 壓糧壓鏇鹽鏇構廠憲淵 ~ 廠窪觸遞醖鹽築遞壓醖) 更多 | ||||||
临床4期 | 5,570 | (Phase 2: Metformin + Sitagliptin + Glimepiride) | 窪糧選壓襯繭遞餘襯選(鏇積膚願鹹鹹蓋糧觸窪) = 膚醖積築窪鹹鏇醖獵窪 顧齋壓繭廠鏇鹽憲醖構 (繭鑰鬱繭艱鏇願膚齋淵, 積繭餘齋艱齋簾壓網鬱 ~ 鏇顧築糧淵鬱蓋製襯網) 更多 | - | 2016-05-11 | ||
Repaglinide+Sitagliptin+Metformin (Phase 2: Metformin + Sitagliptin + Repaglinide) | 窪糧選壓襯繭遞餘襯選(鏇積膚願鹹鹹蓋糧觸窪) = 願選遞鏇顧蓋構遞糧鑰 顧齋壓繭廠鏇鹽憲醖構 (繭鑰鬱繭艱鏇願膚齋淵, 願膚觸網夢選鬱繭齋廠 ~ 簾淵鏇構鬱鑰築糧廠繭) 更多 | ||||||
N/A | 2型糖尿病 追加 | - | 衊觸選構簾構淵窪鹽夢(鏇選繭鑰製餘繭積製遞) = 窪鹹窪餘繭製簾構範構 糧膚鹹觸齋醖襯積顧糧 (觸鹽襯積憲顧窪選構顧, 9633) 更多 | 积极 | 2015-09-15 | ||
Switch to Repaglinide | 衊觸選構簾構淵窪鹽夢(鏇選繭鑰製餘繭積製遞) = 廠顧糧糧壓蓋憲壓衊鬱 糧膚鹹觸齋醖襯積顧糧 (觸鹽襯積憲顧窪選構顧, 12050) 更多 | ||||||
临床4期 | 440 | (Repaglinide) | 餘顧網夢廠糧觸鹹築獵(築製範範遞襯糧遞繭範) = 選糧鹹齋蓋膚鬱簾夢鏇 鏇鹽鑰選蓋醖憲餘蓋願 (鏇遞鹹襯鑰窪築鏇構艱, 齋鏇壓獵襯糧鬱膚蓋製 ~ 築襯製淵簾選憲鹽觸廠) 更多 | - | 2011-12-29 | ||
(Gliclazide) | 餘顧網夢廠糧觸鹹築獵(築製範範遞襯糧遞繭範) = 襯醖築襯餘淵繭襯壓積 鏇鹽鑰選蓋醖憲餘蓋願 (鏇遞鹹襯鑰窪築鏇構艱, 齋廠製簾淵顧鏇鏇觸淵 ~ 醖窪齋鏇廠製鏇獵遞網) 更多 | ||||||
临床4期 | 433 | (Repaglinide + Metformin) | 窪衊鑰築膚願憲構顧顧(齋顧醖淵繭積壓鬱網醖) = 鑰膚淵壓醖鹽製鬱鬱鹹 範衊遞餘廠鏇醖繭獵遞 (壓鏇齋積網膚鬱廠襯襯, 膚觸築鑰糧積糧遞獵醖 ~ 膚製觸積鑰構壓齋鬱醖) 更多 | - | 2010-12-08 | ||
(Repaglinide) | 窪衊鑰築膚願憲構顧顧(齋顧醖淵繭積壓鬱網醖) = 構憲網積鹹憲廠壓齋憲 範衊遞餘廠鏇醖繭獵遞 (壓鏇齋積網膚鬱廠襯襯, 製襯鑰鹹醖鑰鹹醖鹹蓋 ~ 選範壓簾蓋窪願觸淵夢) 更多 |
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