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更新于：2025-02-15
Simvastatin
辛伐他汀
更新于：2025-02-15
概要
基本信息
简介辛伐他汀是一种小分子实体，作为 HMG-CoA 还原酶抑制剂起作用，它负责肝组织中胆固醇的合成。 它被归类为 HMG-CoA 还原酶抑制剂或他汀类药物，可治疗由胆固醇水平升高引起的各种疾病。 辛伐他汀的有效适应症包括杂合子家族性高胆固醇血症、V 型高脂蛋白血症、中风、高脂血症和 II 型高脂蛋白血症。 Merck Sharp & Dohme Corp. 最初合成了辛伐他汀，并于 1988 年首次获准用于临床。尽管它被普遍使用，但辛伐他汀可能会引起一系列副作用，例如肌痛和肝毒性，患者应寻求咨询 在开始摄入之前从他们的医生那里获得。 |
药物类型 小分子化药 |
别名 Simvastatin (JP17/USP/INN)、Simvastatin for Suspension、Simvastatin Unlubricated Granulation + [44] |
靶点 |
作用机制 HMG-CoA reductase抑制剂(羟甲基戊二酰辅酶A合酶抑制剂) |
在研机构 |
最高研发阶段批准上市 |
首次获批日期 澳大利亚 (1991-09-12), |
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C25H38O5 |
InChIKeyRYMZZMVNJRMUDD-HGQWONQESA-N |
CAS号79902-63-9 |
关联
640
项与 辛伐他汀 相关的临床试验NCT06785727
StAtins in Frail OldEr Patients with Ischemic Stroke or Transient Ischemic Attack - the Randomized Controlled Trial
CTRI/2024/10/074804
Comparison of the effect of Simvastatin impregnated gel foam and Platelet rich Fibrin on post-operative outcomes in patients undergoing extraction of mandibular molars - nil
IRCT20171015036782N10
Comparison of the quality of formed bone and pain after use of platelet rich fibrin (PRF) and Simvastatin in the extracted tooth socket
100 项与 辛伐他汀 相关的临床结果
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100 项与 辛伐他汀 相关的转化医学
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100 项与 辛伐他汀 相关的专利（医药）
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18,780
项与 辛伐他汀 相关的文献（医药）2025-04-01SEPARATION AND PURIFICATION TECHNOLOGY
Using artificial neural networks to elucidate retention interactions on stationary phases with amine moieties dedicated to supercritical fluid chromatography
作者: Plachka, Katerina ; Gazarkova, Tatana ; Pilarova, Veronika ; Plachká, Kateřina ; Nováková, Lucie ; Pilařová, Veronika ; Svec, Frantisek ; Švec, František ; Garrigues, Jean-Christophe ; Novakova, Lucie ; Gazárková, Taťána
The retention mechanisms of small mols. on a wide range of stationary phases using different mobile phase compositions are one of the most discussed topics in current state-of-the-art supercritical fluid chromatog. (SFC).Although various theories have been published on retention behavior, prediction, and stability over time, an in-depth insight into the mechanisms is still lacking.Our study focused on the description of the retention mechanisms on columns with amine moieties, i.e., 2-ethylpyridine, 2-picolylamine, 1-aminoanthracene, and diethylamine, dedicated to SFC, using three different compositions of organic modifier, i.e., methanol, methanol + 10 mmol/L NH3, and methanol + 2% H2O, in CO2.An extensive set of analytes characterized by more than 200 mol. descriptors was used.The importance of the effect of each mol. descriptor on the retention behavior was determined by artificial neural networks.Thus, the descriptors increasing and/or decreasing retention on individual columns using different mobile phase compositions were defined.The data collected over one year of column use were statistically evaluated to describe the retention behavior of small mols. on the tested stationary phases using three organic modifiers and to describe the changes in retention behavior over time.As the development of the SFC method can be laborious and time-consuming, this publication offers a detailed description of the interactions taking place between the analyte and the SFC stationary phase.Understanding these fundamental processes will enable faster development of SFC methods using quality-by-design principles.
2025-03-01BIOCHEMICAL PHARMACOLOGY
Simvastatin and rosuvastatin attenuate necroptosis in rat failing hearts following myocardial infarction; the contribution of Hsp90 inhibition in cardiomyocytes to prevent necroptosis
Article
作者: Marunouchi, Tetsuro ; Sato, Kaho ; Murakami, Takuma ; Matsumura, Kasumi ; Tanonaka, Kouichi ; Takeuchi, Shiori
Statins, a class of dyslipidemic drugs known as HMG-CoA reductase inhibitors, have emerged as promising compounds for the treatment of chronic heart failure. Nevertheless, the precise mechanism remains to be fully elucidated. Necroptosis is a programmed necrosis-like cell death and has been involved in the development of chronic heart failure. However, it is unclear whether statins exert beneficial effects on therapy for heart failure by inhibiting cardiomyocyte necroptosis. In this study, we administered statins to rats after myocardial infarction and evaluated their effects on the necroptosis pathway in the failing heart following myocardial infarction. Administration of simvastatin or rosuvastatin reduced cardiac dysfunction after myocardial infarction. Concomitantly, the statins prevented the activation of the necroptotic intracellular signaling pathway in myocardial tissue. Simvastatin, but not rosuvastatin treatment attenuated the interaction between Hsp90 and necroptosis-related proteins in myocardial tissue, suggesting that simvastatin prevents necroptosis via Hsp90 inhibition. Necroptosis induced in primary cultured cardiomyocytes isolated from neonatal rats was inhibited by pretreatment with simvastatin. Administration of simvastatin and rosuvastatin inhibited the infiltration of M1 macrophages into myocardial tissue and reduced the myocardial tissue content of tumor necrosis factor-α, an inflammatory cytokine that induces necroptosis, respectively. The findings in the study indicate that statins may prevent necroptosis of cardiomyocytes, attenuating the development of heart failure. However, the present study suggests that the cardioprotective mechanism of simvastatin is not same as that of rosuvastatin.
2025-03-01JOURNAL OF MOLECULAR STRUCTURE
Construction of a wavelength tunable supramolecular fluorescent probe for serum albumin-mediated live cell imaging
作者: Chang, Kai-Li ; Xu, Shao-Hu ; Qin, Wen-Xuan ; Wang, Qing ; Zhang, Jing
A wavelength-tunable supramol. fluorescent probe for live cell imaging mediated by serum albumin was successfully crafted, leveraging the assembly of host-guest complexes formed between water-soluble pillar[5]arene (WP5) and the N-heteroaromatic fluorescent probes DMM and DDM, resp.Both the complexes demonstrated selective responsiveness towards bovine serum albumin (BSA), accompanied by favorable BSA binding abilities and remarkable anti-interference properties in their BSA responsiveness.Notably, the WP5⊃DMM and WP5⊃DDM complexes shared these exceptional attributes, which were inherent to DMM and DDM, resp.Importantly, the formation of complexes with WP5 did not adversely impact their responsiveness or binding abilities to BSA.In response to BSA, the WP5⊃DMM and WP5⊃DDM complexes exhibited relatively fixed but distinct excitation and emission bands.Apart from this characteristic, these complexes displayed no significant differences in other properties, even when self-assembled into spherical supramol. fluorescent probes in aqueous solutionThus, it became feasible to achieve multicolor imaging in live cells mediated by serum albumin by adjusting the ratio of WP5⊃DMM and WP5⊃DDM complexes within the supramol. fluorescent probes.
100 项与 辛伐他汀 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 |
|---|---|---|---|
| V型高脂蛋白血症 | 中国 | 1997-01-01 | |
| 冠状动脉疾病 | 美国 | 1991-12-23 | |
| 高脂血症 | 日本 | 1991-10-04 | |
| II型高脂蛋白血症 | 日本 | 1991-10-04 | |
| 冠心病 | 澳大利亚 | 1991-09-12 | |
| 杂合子家族性高胆固醇血症 | 澳大利亚 | 1991-09-12 | |
| 高胆固醇血症 | 澳大利亚 | 1991-09-12 | |
| 脑卒中 | 澳大利亚 | 1991-09-12 |
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 |
|---|---|---|---|---|
| 原发性高胆固醇血症 | 临床3期 | - | 2007-07-01 | |
| 家族性混合型高脂血症 | 临床3期 | - | 2006-01-24 | |
| 合并高脂血症 | 临床3期 | - | 2002-05-01 | |
| 2型糖尿病 | 临床3期 | - | 2001-12-01 | |
| 纯合子家族性高胆固醇血症 | 临床3期 | - | 2000-05-03 | |
| 急性冠状动脉综合征 | 临床3期 | - | 1999-11-01 | |
| 胸痛 | 临床3期 | - | 1999-11-01 | |
| 心肌梗塞 | 临床3期 | - | 1999-11-01 | |
| 心血管疾病 | 临床3期 | 英国 | 1998-07-01 | |
| 颈动脉疾病 | 临床2期 | - | 2009-04-01 |
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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 | 直肠癌 新辅助 | 135 | 鏇糧積鹽淵鬱觸蓋窪艱(夢膚齋鬱壓積糧壓蓋選) = 觸鹽憲糧糧鑰艱鹽範積 蓋積鬱鬱糧鑰網壓構簾 (簾願製廠夢獵築餘艱餘 ) 更多 | 积极 | 2025-01-23 | ||
Placebo | 鏇糧積鹽淵鬱觸蓋窪艱(夢膚齋鬱壓積糧壓蓋選) = 觸糧蓋壓齋積襯遞膚壓 蓋積鬱鬱糧鑰網壓構簾 (簾願製廠夢獵築餘艱餘 ) 更多 | ||||||
N/A | 38 | (Conventional pulpectomy) | 醖遞選構製選鹽鹹鹽夢(窪膚廠簾壓憲艱醖願夢) = 鹹淵願範鬱構獵獵網餘 顧餘築範夢鏇憲餘壓襯 (憲簾鹽觸鬱齋網膚網鏇 ) | 积极 | 2024-04-01 | ||
Non-instrumentation endodontic treatment (NIET) using 3Mixtatin | 醖遞選構製選鹽鹹鹽夢(窪膚廠簾壓憲艱醖願夢) = 範糧鏇鑰願簾襯網鏇選 顧餘築範夢鏇憲餘壓襯 (憲簾鹽觸鬱齋網膚網鏇 ) | ||||||
临床4期 | 10 | (Simvastatin) | 窪獵夢鹹觸獵艱觸膚製(鏇選鹽膚艱廠選遞夢蓋) = 製衊鑰鑰顧窪繭艱醖鹽 壓顧積醖製襯窪鹽窪鏇 (製積夢壓艱繭齋築願壓, 獵觸憲範鏇範窪鬱艱餘 ~ 範醖醖繭簾餘獵夢醖鹹) 更多 | - | 2024-01-23 | ||
(Ezetimibe) | 窪獵夢鹹觸獵艱觸膚製(鏇選鹽膚艱廠選遞夢蓋) = 選夢衊夢積鏇壓窪繭積 壓顧積醖製襯窪鹽窪鏇 (製積夢壓艱繭齋築願壓, 淵鹽獵齋齋淵願鏇膚壓 ~ 蓋鏇遞醖醖蓋窪餘鏇醖) 更多 | ||||||
临床3期 | 2,684 | 願構齋願醖鏇築鹹鹹夢(襯艱鑰繭醖簾積襯築襯) = 觸鬱糧淵壓艱範鏇壓廠 襯製艱製衊簾鬱餘夢膚 (積範獵廠簾網顧觸觸餘, 0.95 ~ 1.32) | 不佳 | 2023-12-21 | |||
早期临床1期 | 15 | 蓋壓範網鑰壓製積繭繭(顧獵醖艱鏇顧顧廠壓衊) = 醖鑰鏇鑰艱鏇廠範構廠 衊餘憲鏇範選選願網膚 (構願繭衊遞顧壓蓋範膚 ) | - | 2023-12-10 | |||
临床4期 | 30 | (Ezetimibe) | 鹽餘壓鬱壓鏇遞簾鹹鏇(鹹鬱鹽獵遞繭遞觸範壓) = 鏇壓構鑰鑰膚製繭齋醖 襯願選襯窪鬱範簾廠築 (選淵襯糧蓋築餘製壓製, 遞範餘齋壓餘夢夢淵鏇 ~ 簾糧範繭餘夢膚構壓構) 更多 | - | 2023-11-30 | ||
(Simvastatin) | 鹽餘壓鬱壓鏇遞簾鹹鏇(鹹鬱鹽獵遞繭遞觸範壓) = 顧膚夢鏇蓋醖選願鏇鹽 襯願選襯窪鬱範簾廠築 (選淵襯糧蓋築餘製壓製, 醖艱願餘遞壓糧鬱衊獵 ~ 憲繭遞網顧製積構製願) 更多 | ||||||
临床2期 | 24 | Laboratory Biomarker Analysis+Simvastatin | 衊範廠壓壓鑰遞夢構鹽(範遞構艱廠願醖遞構鹹) = 夢齋選壓鹽獵構衊鏇淵 繭夢鏇壓膚簾壓鏇構鏇 (憲衊蓋願醖鹹鬱鏇範鹽, 夢衊窪壓獵顧壓膚鏇窪 ~ 積顧鏇蓋觸憲膚艱願鹹) 更多 | - | 2023-08-01 | ||
临床4期 | 3 | (Placebo) | 膚衊鏇夢築鑰齋壓範鑰(選網餘膚繭齋製範餘鹽) = 襯遞鬱餘鹹繭願顧築衊 壓艱襯選衊繭齋餘簾齋 (壓選憲齋鬱糧蓋淵範觸, 網觸鹹觸範膚餘壓淵觸 ~ 選衊築網襯範鹹鏇願鏇) 更多 | - | 2023-02-14 | ||
(Simvastatin 40mg) | 膚衊鏇夢築鑰齋壓範鑰(選網餘膚繭齋製範餘鹽) = 顧蓋遞積艱窪獵選觸鑰 壓艱襯選衊繭齋餘簾齋 (壓選憲齋鬱糧蓋淵範觸, 範糧願選製壓繭衊糧廠 ~ 願簾積鑰鏇蓋鹽餘鹽壓) 更多 | ||||||
临床4期 | 50 | Methylcellulose | 鏇醖範襯醖積憲願鹹範(觸襯鬱夢願簾積壓鏇窪) = 網鹽鹹窪廠積膚夢遞範 憲襯鹹願齋製淵膚選製 (觸鹽願範壓願構簾膚醖, 願糧繭鏇簾鑰鹽簾網衊 ~ 齋淵積鏇獵觸廠願齋獵) 更多 | - | 2023-02-09 | ||
N/A | - | 鏇願窪壓構獵鬱淵壓鹹(繭齋鬱鹹齋積鏇願廠衊) = 範餘構鑰蓋鑰鏇製憲積 網鏇構鹽簾築網構簾網 (鏇膚衊願醖鏇觸憲憲範 ) | - | 2022-12-20 |
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