更新于：2024-11-04
Fluvastatin Sodium
氟伐他汀钠
更新于：2024-11-04
概要
基本信息
药物类型 小分子化药 |
别名 Canef、Cranoc、Digaril + [22] |
作用机制 HMG-CoA reductase抑制剂(羟甲基戊二酰辅酶A合酶抑制剂) |
非在研适应症 |
最高研发阶段批准上市 |
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C24H26FNNaO4 |
InChIKeyCUOKYGJQSIKNFS-ZADPHQEYSA-N |
CAS号93957-55-2 |
关联
73
项与 氟伐他汀钠 相关的临床试验氟伐他汀钠缓释片人体生物等效性研究
氟伐他汀钠缓释片在健康受试者中餐后状态下的单剂量、随机、开放、四周期、两序列、重复交叉设计的生物等效性试验
氟伐他汀钠缓释片在空腹及餐后条件下的人体生物等效性试验
100 项与 氟伐他汀钠 相关的临床结果
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100 项与 氟伐他汀钠 相关的转化医学
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100 项与 氟伐他汀钠 相关的专利（医药）
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2,061
项与 氟伐他汀钠 相关的文献（医药）2025-01-01Vascular and Endovascular Surgery
Short-Term and Long-Term Fluvastatin Inhibit Effects of Thrombospondin-1 on Human Vascular Smooth Muscle Cells
Article
作者: Iwuchukwu, Chinenye ; Yuan, Helen L. ; Seymour, Keri ; Helkin, Alex ; Stein, Jeffrey J. ; Maier, Kristopher ; Ryabtsev, Boris ; Gahtan, Vivian
Introduction:
Vascular smooth muscle cells are important in intimal hyperplasia. Thrombospondin-1 is a matricellular protein involved in the vascular injury response. Statins are cholesterol lowering drugs that have beneficial cardiovascular effects. Statis have been shown to inhibit smooth muscle migration through the mevalonate pathway. This effect is thought to be mediated by small G protein Ras and Rho turnover which requires many hours. While many patients undergoing treatment for vascular disease are on statins, many are not. Thus immediate pretreatment with statins before surgery may be beneficial. We hypothesized that statins have effects independent of the mevalonate pathway and thus have an immediate effect.
Methods:
Human vascular smooth muscle cells were pretreated for 20 h (long-term) or 20 min (short-term) with fluvastatin, or mevalonolactone plus fluvastatin. Thrombospondin-1-induced migration, activation of p42/p44 extracellular signal-regulated kinase, c-Src, focal adhesion kinase and PI3 kinase was determined. The effect of fluvastatin on thrombospondin-1-induced expression of THBS1, FOS, HAS2 and TGFB2 was examined.
Results:
Both treatments inhibited thrombospondin-1-induced chemotaxis back to the control group. Mevalonolactone reversed the long-term statin effect by increasing migration but had no effect on the short-term statin response. p42/p44 extracellular signal-regulated kinase was activated by thrombospondin-1 and both treatments augmented activation. Neither treatment affected c-Src activity, but both inhibited focal adhesion kinase and PI3 kinase activity. Only long-term statin treatment inhibited THBS1 expression while both treatments inhibited FOS and TGFB2 expression. Neither treatment affected HAS2. FOS knockdown inhibited thrombospondin-1-induced HAS2 but not TGFβ2 gene expression.
Conclusion:
Long-term fluvastatin inhibited thrombospondin-1-induced chemotaxis through the mevalonate pathway while short-term fluvastatin inhibited chemotaxis through an alternate mechanism. Short-term stains have immediate effects independent of the mevalonate pathway. Acute local treatment with statins followed by longer term therapy may limit the vascular response to injury.
2024-11-01Chinese Journal of Chromatography
Preparation of chiral metal organic framework modified silica monolithic capillary column and its application in enantioseparations of chiral drugs
Article
作者: Wu, Jia-Lian ; Liao, Gan ; Huang, Lu ; Song, Rui-Ke ; Lin, Jia-Li
Metal organic frameworks (MOFs) are crystalline compounds composed of metal ions (or metal clusters) and organic ligands. Chiral MOFs have been successfully utilized as novel materials for the separation of chiral enantiomers by chromatography, demonstrating excellent chiral separation performance. In this study, a chiral MOF-modified silica monolithic capillary column was used for pressurized capillary electrochromatography. First, a chiral MOF (Co-glycyl-L-glutamic acid, Co-L-GG) was synthesized. This MOF was then used to prepare a chiral capillary monolithic column via a one-step in situ polymerization method. The optimal conditions for preparing the chiral capillary monolithic column were determined as follows: Co-L-GG amount, 5 mg; polyethylene glycol amount, 0.96 mg; tetramethoxysilane dosage, 3.6 mL; trimethoxymethylsilane dosage, 0.4 mL. Next, the effects of the separation conditions on the separation of chiral drugs were investigated. Under the conditions of an applied voltage of -20 kV and a mobile phase consisting of acetonitrile and 20 mmol/L disodium hydrogen phosphate (80∶20, v/v), six chiral drugs were separated within 3 min, with baseline separation achieved for amlodipine, fluvastatin, and tryptophan. Moreover, the prepared chiral capillary monolithic column exhibited good reproducibility and stability. Finally, molecular docking studies were conducted using AutoDock to explore the chiral recognition mechanism, and the results were analyzed using Discovery Studio. The results indicated that larger differences in binding free energy between Co-L-GG and the enantiomers of the chiral drugs were correlated with higher enantioselectivity factors. However, this correlation did not necessarily lead to an increase in resolution. Co-L-GG, which is enriched with primary amines, secondary amines, and carbonyl groups, demonstrated enantiomeric recognition capability. In conclusion, this study demonstrates that chiral MOFs can be effectively used as chiral functional monomers to prepare chiral monolithic capillary columns, highlighting their significant potential for the separation and analysis of chiral compounds. The comprehensive exploration of the synthesis, characterization, and applications of these MOFs will help provide valuable insights into the development of advanced separation technologies.
2024-08-01CTS-Clinical and Translational Science
Drug–drug interactions between pemafibrate and statins on pharmacokinetics in healthy male volunteers: Open‐label, randomized, 6‐sequence, 3‐period crossover studies
Article
作者: Kamimura, Tomohiro ; Suganami, Hideki ; Tanigawa, Ryohei ; Hounslow, Neil
Abstract:
Elevated triglyceride levels are associated with an increased risk of cardiovascular events despite guideline‐based statin treatment of low‐density lipoprotein cholesterol. Peroxisome proliferator‐activated receptor α (PPARα) agonists exert a significant triglyceride‐lowering effect. However, combination therapy of PPARα agonists with statins poses an increased risk of rhabdomyolysis, which is rare but a major concern of the combination therapy. Pharmacokinetic interaction is suspected to be a contributing factor to the risk. To examine the potential for combination therapy with the selective PPARα modulator (SPPARMα) pemafibrate and statins, drug–drug interaction studies were conducted with open‐label, randomized, 6‐sequence, 3‐period crossover designs for the combination of pemafibrate 0.2 mg twice daily and each of 6 statins once daily: pitavastatin 4 mg/day (n = 18), atorvastatin 20 mg/day (n = 18), rosuvastatin 20 mg/day (n = 29), pravastatin 20 mg/day (n = 18), simvastatin 20 mg/day (n = 20), and fluvastatin 60 mg/day (n = 19), involving healthy male volunteers. The pharmacokinetic parameters of pemafibrate and each of the statins were similar regardless of coadministration. There was neither an effect on the systemic exposure of pemafibrate nor a clinically important increase in the systemic exposure of any of the statins on the coadministration although the systemic exposure of simvastatin was reduced by about 15% and its open acid form by about 60%. The HMG‐CoA reductase inhibitory activity in plasma samples from the simvastatin and pemafibrate combination group was about 70% of that in the simvastatin alone group. In conclusion, pemafibrate did not increase the systemic exposure of statins, and vice versa, in healthy male volunteers.
100 项与 氟伐他汀钠 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 |
|---|---|---|---|
| 冠状动脉疾病 | 美国 | 2003-05-27 | |
| II型高脂蛋白血症 | 日本 | 1998-08-28 | |
| 高脂血症 | 法国 | 1997-10-21 | |
| 动脉粥样硬化 | 美国 | 1993-12-31 | |
| 高胆固醇血症 | 美国 | 1993-12-31 |
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 |
|---|---|---|---|---|
| 勃起功能障碍 | 临床3期 | 德国 | 2006-10-01 | |
| 家族性混合型高脂血症 | 临床3期 | 中国 | 2005-06-01 | |
| 原发性高胆固醇血症 | 临床3期 | 中国 | 2005-06-01 | |
| 杂合子家族性高胆固醇血症 | 临床3期 | 瑞士 | 2001-10-01 |
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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
临床2期 | 局限性前列腺癌 新辅助 | 33 | 窪餘選構艱鹽糧築選齋(餘艱積襯憲築範鬱鬱糧) = 範鹽膚鹽簾鬱齋憲遞膚 齋膚選蓋壓製窪繭鬱築 (醖醖醖憲積衊範窪構願, 1.9 ~ 5.0) 更多 | - | 2020-03-13 | ||
临床4期 | 436 | (Fluvastatin Sodium Extended Release Tablet) | 獵積蓋簾蓋鹹壓齋夢鏇(繭壓鹽獵衊鏇網蓋鑰構) = 餘鏇蓋鏇壓鑰觸齋積醖 簾顧鬱醖窪艱餘齋鏇構 (壓蓋蓋鹽醖壓構鏇蓋糧, 鑰淵餘簾憲繭鑰衊壓淵 ~ 簾夢鹽蓋網壓鹽蓋襯遞) 更多 | - | 2014-06-11 | ||
(Fluvastatin Sodium Immediate Release Capsule) | 獵積蓋簾蓋鹹壓齋夢鏇(繭壓鹽獵衊鏇網蓋鑰構) = 鹹製鑰積簾積簾築憲憲 簾顧鬱醖窪艱餘齋鏇構 (壓蓋蓋鹽醖壓構鏇蓋糧, 衊廠積鹽鏇顧繭艱觸網 ~ 願築鬱積廠網積艱繭鬱) 更多 | ||||||
N/A | 14 | 築衊齋襯顧壓顧膚簾齋(願艱膚衊鬱願淵選廠襯) = 鬱襯簾製齋鏇蓋築膚願 襯蓋築齋範築淵齋鑰窪 (觸夢鑰膚觸構繭醖簾餘 ) 更多 | 积极 | 2012-05-01 | |||
Statin | 築衊齋襯顧壓顧膚簾齋(願艱膚衊鬱願淵選廠襯) = 製鑰窪淵襯鬱觸衊簾窪 襯蓋築齋範築淵齋鑰窪 (觸夢鑰膚觸構繭醖簾餘 ) 更多 | ||||||
临床4期 | - | 蓋鏇鏇鹹獵簾網簾艱簾(廠簾艱鏇遞網餘選艱製) = 鏇廠餘壓憲艱鬱鑰築鹹 範選廠醖廠糧夢願獵憲 (築壓積醖鹽齋網齋選淵 ) | 积极 | 2010-05-25 | |||
Placebo | 蓋鏇鏇鹹獵簾網簾艱簾(廠簾艱鏇遞網餘選艱製) = 糧糧網窪壓憲願繭膚願 範選廠醖廠糧夢願獵憲 (築壓積醖鹽齋網齋選淵 ) | ||||||
临床2期 | 45 | 膚觸築獵繭繭壓鹽蓋憲(襯獵夢製齋築積艱遞獵) = 餘積憲蓋夢襯構鏇選襯 艱淵壓築構選齋構艱網 (窪艱鹹網醖膚鬱糧範糧 ) | - | 2010-01-01 | |||
膚觸築獵繭繭壓鹽蓋憲(襯獵夢製齋築積艱遞獵) = 簾觸壓襯鬱鏇廠觸鹹襯 艱淵壓築構選齋構艱網 (窪艱鹹網醖膚鬱糧範糧 ) | |||||||
临床4期 | 793 | Placebo (Placebo) | 製鏇醖艱遞艱積襯選簾(廠構醖築簾餘糧願獵齋) = 蓋顧製鹹獵鹹網膚蓋餘 選艱鬱觸顧繭淵築衊鹹 (鑰鏇網夢憲構製鹽餘餘, 夢繭糧醖鹽築鑰衊鹹壓 ~ 鏇淵構網範鑰蓋築構艱) 更多 | - | 2009-09-14 | ||
(Acetaminophen) | 製鏇醖艱遞艱積襯選簾(廠構醖築簾餘糧願獵齋) = 衊範鏇蓋餘醖選築觸齋 選艱鬱觸顧繭淵築衊鹹 (鑰鏇網夢憲構製鹽餘餘, 獵齋廠餘選鬱壓範淵獵 ~ 襯遞鏇築簾齋積簾艱願) 更多 | ||||||
N/A | - | - | 鏇願築觸觸鬱鬱製齋鑰(鹹獵膚願網獵範範鹹鹹): hazard ratio = 0.55 (95% CI, 0.34 ~ 0.88), P-Value = 0.01 | 积极 | 2009-09-03 | ||
Placebo | |||||||
临床4期 | 89 | 範餘鑰選齋窪願糧蓋醖(簾憲蓋壓築願襯壓網願) = 齋繭蓋觸網夢壓範遞餘 觸壓糧蓋膚廠鬱願餘選 (壓遞糧鹹網網鑰窪艱廠 ) 更多 | 积极 | 2008-07-15 | |||
Placebo | 範餘鑰選齋窪願糧蓋醖(簾憲蓋壓築願襯壓網願) = 膚醖鑰範網製築願觸醖 觸壓糧蓋膚廠鬱願餘選 (壓遞糧鹹網網鑰窪艱廠 ) 更多 | ||||||
N/A | 系统性硬皮病 一线 | 20 | 餘遞艱廠衊夢鬱簾鑰蓋(鬱壓艱願鹹積遞壓顧窪) = 製襯簾鏇顧網製廠壓餘 築獵壓鹽顧簾衊網願鏇 (顧願醖壓膚遞範觸餘襯 ) 更多 | - | 2006-06-21 | ||
Control (no therapy) | 餘遞艱廠衊夢鬱簾鑰蓋(鬱壓艱願鹹積遞壓顧窪) = 衊簾廠繭獵齋憲淵築淵 築獵壓鹽顧簾衊網願鏇 (顧願醖壓膚遞範觸餘襯 ) 更多 |
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