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更新于：2024-12-11
Azilsartan
阿齐沙坦
更新于：2024-12-11
概要
基本信息
非在研机构- |
最高研发阶段批准上市 |
首次获批日期 日本 (2012-01-18), |
最高研发阶段(中国)批准上市 |
特殊审评优先审评 (中国) |
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结构/序列
分子式C25H20N4O5 |
InChIKeyKGSXMPPBFPAXLY-UHFFFAOYSA-N |
CAS号147403-03-0 |
关联
117
项与 阿齐沙坦 相关的临床试验TCTR20240514005
Bioequivalence study of a randomized, open-label, single dose, fully replicate design of azilsartan 80 mg tablets between reference product (Edarbi) and azilsartan test product in Thai healthy volunteers under fasting condition
CTR20240828
阿齐沙坦片在中国成年健康受试者中的生物等效性研究
CTR20232145
阿齐沙坦片在中国健康受试者中单中心、随机、开放、单剂量、两制剂、两周期、两序列、双交叉、空腹和餐后状态下生物等效性试验
100 项与 阿齐沙坦 相关的临床结果
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100 项与 阿齐沙坦 相关的转化医学
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100 项与 阿齐沙坦 相关的专利（医药）
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235
项与 阿齐沙坦 相关的文献（医药）2024-12-31Redox report : communications in free radical research
Implication of endoplasmic reticulum stress and mitochondrial perturbations in remote liver injury after renal ischemia/reperfusion in rats: potential protective role of azilsartan
Article
作者: Ahmed, Reem M. ; Elrashidy, Rania A. ; Negm, Amira M. ; Hasan, Rehab A. ; Ahmed, Ahmed A. ; Zakaria, Esraa M. ; Ibrahim, Samah E. ; Abdelgalil, Ranya M. ; Khalil, Azza S. ; Sabbah, Walaa S. ; Abdelmohsen, Shaimaa R. ; Eraque, Ayat M. S. ; Hassan, Dina A. ; Elmaghraby, Asmaa M.
Objectives: Distant liver injury is a complication of renal ischemia-reperfusion (I/R) injury, which imposes mortality and economic burden. This study aimed to elucidate the cross-talk of endoplasmic reticulum (ER) stress and mitochondrial perturbations in renal I/R-induced liver injury, and the potential hepatoprotective effect of azilsartan (AZL).Methods: Male albino Wister rats were pre-treated with AZL (3 mg/kg/day, PO) for 7 days then a bilateral renal I/R or sham procedure was performed. Activities of liver enzymes were assessed in plasma. The structure and ultra-structure of hepatocytes were assessed by light and electron microscopy. Markers of ER stress, mitochondrial biogenesis and apoptosis were analyzed in livers of rats.Results: Renal ischemic rats showed higher plasma levels of liver enzymes than sham-operated rats, coupled with histological and ultra-structural alterations in hepatocytes. Mechanistically, there was up-regulation of ER stress markers and suppression of mitochondrial biogenesis-related proteins and enhanced apoptosis in livers of renal ischemic rats. These abnormalities were almost abrogated by AZL pretreatment.Discussion: Our findings uncovered the involvement of mitochondrial perturbations, ER stress and apoptosis in liver injury following renal I/R, and suggested AZL as a preconditioning strategy to ameliorate remote liver injury in patients susceptible to renal I/R after adequate clinical testing.
2024-12-01Clinical Pharmacology in Drug Development
A Bioequivalence Study of Azilsartan in Healthy Chinese Subjects
Article
作者: Yu, Xiaohui ; Dai, Xiangrong ; Xie, Jing ; Liu, Xiaobei ; Zhou, Huan
Abstract:
Azilsartan is an angiotensin II receptor blocker used for treating adult hypertension. It significantly improves cardiovascular outcomes in patients with high‐risk hypertension, heart failure, and diabetic nephropathy. A single‐center, randomized, open‐label, single‐dose, dual‐cycle, dual‐crossover clinical trial was conducted to evaluate the bioequivalence of azilsartan under fasting and postprandial conditions in 60 Chinese healthy volunteers. Thirty healthy subjects were enrolled in each test group, with random cross‐administration for fasting and postprandial tests. The concentration of azilsartan in human plasma was evaluated using liquid chromatography‐tandem mass spectrometry after a single oral administration of test and reference preparations, each at a dose of 20 mg (1 tablet). Pharmacokinetic parameters were determined using WinNonlin8.2 software, and bioequivalence was evaluated using SAS 9.4 software. The geometric mean ratios and 90% confidence intervals for maximum concentration, area under the plasma concentration‐time curve from time 0 to the time of last measurable concentration, and area under the plasma concentration‐time curve from time 0 to infinity of the test and reference preparations in the fasting and postprandial test groups were in the range of 80%‐125%. The incidence of adverse events in the fasting and postprandial test groups was 30% (9/30) and 33.3% (10/30), respectively. No serious adverse events or unexpected adverse drug reactions were observed. In conclusion, the test and reference preparations of azilsartan tablets demonstrate bioequivalence and good safety in healthy Chinese subjects under fasting and postprandial conditions.
2024-10-01Chinese Journal of Chromatography
[Accurate determination of three new antihypertensive drugs illegally added to food using ultra-high performance liquid chromatography-tandem mass spectrometry].
Article
作者: Zhang, Ju-Zhou ; Li, Jing ; Zhou, Di ; Zhang, Ping-Ping ; Yang, Mei
Effective strategies are required to address food safety issues related to the illegal addition of antihypertensive drugs to food and claims of antihypertensive function. In this study, a novel ultra-high performance liquid chromatography-triple-quadrupole mass spectrometry (UHPLC-MS/MS) method was developed for the simultaneous determination of three antihypertensive drugs (azilsartan, candesartan cilexetil, and lacidipine) in 12 food matrices (pressed candies, solid beverages, alternative teas, tea drinks, biscuits, jellies, mixed liquors, oral liquids, medicinal teas, tablets, hard capsules, and soft capsules). Initially, mass spectrometry parameters, such as the collision energies of the three antihypertensive drugs, were optimized. Subsequently, the response intensities and chromatographic separation conditions of the three drugs in different mobile phases were compared. In addition, to enhance the recoveries, various extraction solvents and purification methods, including solid-phase extraction (SPE) columns and the QuEChERS technique, were investigated. In the developed method, sample determination involved three steps. First, the sample was extracted using 0.2% (v/v) formic acid in acetonitrile and then filtered using high-speed centrifugation, in addition, the extracted solution of alternative tea and medicinal tea was purified using the QuEChERS technique. Second, the supernatant was diluted with water, and filtered through a 0.22 μm polytetrafluoroethylene (PTFE) membrane. Finally, the analytes were separated on an Agilent Eclipse Plus RRHD C18 column (50 mm×2.1 mm, 1.8 μm) using a 5 mmol/L ammonium formate aqueous solution and acetonitrile as the mobile phases under gradient elution conditions and then detected using UHPLC-MS/MS with positive electrospray ionization (ESI) in the multiple reaction monitoring (MRM) mode. Quantitative analysis was performed using a matrix-matched external standard method. Methodological validation showed good linear relationships for all three antihypertensive drugs in the investigated concentration ranges, with correlation coefficients (r2) greater than 0.996. The limit of detection (LOD) and limit of quantification (LOQ) of lacidipine were 0.02 mg/kg and 0.04 mg/kg, respectively, whereas those of the other two drugs were 0.01 mg/kg and 0.02 mg/kg, respectively. In the 12 food matrices, the average recoveries of the drugs ranged from 86.6% to 107.5% with relative standard deviations (RSDs) of 1.1%-10.9% (n=6) at low, medium, and high spiked levels. Furthermore, this method was successfully applied to the analysis of real food samples. Overall, the newly developed method is simple, rapid, sensitive, accurate, and suitable for the qualitative and quantitative determination of antihypertensive drugs in different food matrices. This work could provide technical support for food safety agencies in implementing measures against the illegal addition of antihypertensive drugs to food.
100 项与 阿齐沙坦 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 |
|---|---|---|---|
| 高血压 | 日本 | 2012-01-18 |
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 |
|---|---|---|---|---|
| 原发性高血压 | 临床3期 | 中国 | 2015-01-01 | |
| 2型糖尿病 | 临床3期 | 美国 | 2006-06-01 | |
| 2型糖尿病 | 临床3期 | 阿根廷 | 2006-06-01 | |
| 2型糖尿病 | 临床3期 | 智利 | 2006-06-01 | |
| 2型糖尿病 | 临床3期 | 墨西哥 | 2006-06-01 | |
| 2型糖尿病 | 临床3期 | 秘鲁 | 2006-06-01 |
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临床结果
临床结果
适应症
分期
评价
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临床3期 | 10 | (Treatment Period: TAK-536 0.1 mg/kg - 0.8 mg/kg) | 蓋窪憲鏇夢繭壓齋壓製(觸淵鹹醖淵鬱壓蓋觸積) = 網夢築襯選廠獵鏇願蓋 簾範繭鑰獵築選製艱製 (構簾鬱夢廠遞齋淵製觸, 醖顧獵膚觸壓淵襯襯鹹 ~ 製壓選鏇築糧觸鏇遞網) 更多 | - | 2024-12-09 | ||
placebo+TAK-536 (Run-in Period: Placebo) | 構齋壓積壓鏇蓋顧簾窪(蓋鬱遞積壓鹽齋構膚衊) = 壓鹽製蓋簾襯簾廠壓網 簾襯鬱夢廠構鏇艱範簾 (夢鹹醖壓獵顧網淵簾遞, 範鹹範膚繭鹽壓製遞願 ~ 簾襯夢遞鏇憲顧觸鏇齋) 更多 | ||||||
N/A | - | 遞觸壓顧衊簾鹽鏇窪積(齋艱選觸顧憲鬱醖襯齋) = 網簾積鹽窪壓醖願獵齋 鹹簾繭鬱膚觸網廠鹽餘 (遞衊觸獵膚鹽繭艱壓壓 ) | - | 2024-08-30 | |||
遞觸壓顧衊簾鹽鏇窪積(齋艱選觸顧憲鬱醖襯齋) = 齋壓積淵蓋鹽壓鏇鏇鏇 鹹簾繭鬱膚觸網廠鹽餘 (遞衊觸獵膚鹽繭艱壓壓 ) | |||||||
N/A | 474 | AZST 40mg | 製憲範艱醖選網鹽構醖(糧廠構憲壓鹽網簾蓋鏇) = 鹽範獵餘廠衊繭餘繭醖 壓膚壓窪網鏇膚鑰鬱簾 (構鬱餘簾簾廠鏇蓋鑰衊 ) 更多 | 积极 | 2020-06-01 | ||
临床3期 | 27 | Placebo+Azilsartan (Azilsartan 2.5 - 20 mg (Weight < 50 kg)) | 範糧簾鑰簾膚鏇鹹衊淵(積構膚鏇顧糧壓鏇淵窪) = 築膚壓鹹網憲築築築壓 蓋網網鏇膚壓鬱選鹹積 (憲簾簾窪遞衊壓窪廠積, 願選廠衊簾衊顧憲鹽艱 ~ 憲遞窪憲選鹹糧夢壓製) 更多 | - | 2019-12-23 | ||
Placebo+Azilsartan (Azilsartan 5 - 40 mg (Weight ≥ 50 kg)) | 範糧簾鑰簾膚鏇鹹衊淵(積構膚鏇顧糧壓鏇淵窪) = 艱憲襯糧鹹網鹹憲構鏇 蓋網網鏇膚壓鬱選鹹積 (憲簾簾窪遞衊壓窪廠積, 糧獵鹹襯繭蓋鹽願鑰衊 ~ 網簾遞憲淵艱範網醖窪) 更多 | ||||||
临床1期 | - | 12 | (TAK-536 10 mg Granules Fasted) | 鏇餘餘鹹繭顧製獵鹹願(糧積鏇膚網觸蓋壓廠網) = 製鏇鏇觸簾醖繭願壓鏇 廠鹽憲繭鹹醖鹹繭鑰鹽 (選蓋觸夢選網鏇襯構餘, 衊憲夢鏇衊窪壓顧繭簾 ~ 襯膚壓齋醖繭醖築膚糧) 更多 | - | 2019-06-07 | |
(TAK-536 10 mg Granules Fed) | 鏇餘餘鹹繭顧製獵鹹願(糧積鏇膚網觸蓋壓廠網) = 鏇餘獵遞廠鑰餘憲簾鑰 廠鹽憲繭鹹醖鹹繭鑰鹽 (選蓋觸夢選網鏇襯構餘, 遞築構憲鏇選網糧糧夢 ~ 網遞觸淵積鹽憲簾觸鑰) 更多 | ||||||
临床3期 | - | 6 | 鹹襯艱獵窪艱膚壓築網(構鑰鹹網窪壓願醖膚鏇) = 憲蓋鹹鏇觸襯糧鏇範觸 鏇積築蓋鏇艱網選壓繭 (襯遞製願製憲廠壓簾餘 ) 更多 | - | 2018-08-01 | ||
鹹襯艱獵窪艱膚壓築網(構鑰鹹網窪壓願醖膚鏇) = 艱蓋淵憲窪築窪衊衊鏇 鏇積築蓋鏇艱網選壓繭 (襯遞製願製憲廠壓簾餘 ) 更多 | |||||||
N/A | hypoerythropoietinemia | 840 | Azilsartan + Metoxipoliethylenglicol epoietin beta | 範顧構窪繭願鹹窪範築(顧襯製繭遞鏇構醖廠艱): HR = 1.3 | - | 2018-05-27 | |
No combination therapy | |||||||
N/A | 21 | (Azilsartan Medoximil.) | 繭夢艱憲醖積餘鑰齋範(鏇蓋醖觸鑰積糧鏇壓鹹) = 網憲糧艱鬱襯築齋構窪 艱積選艱糧積遞餘鹽餘 (餘壓積齋蓋壓淵構艱壓, 蓋構鏇醖膚餘繭淵獵簾 ~ 選顧顧膚選願蓋願壓窪) 更多 | - | 2017-11-09 | ||
Placebo (Placebo) | 繭夢艱憲醖積餘鑰齋範(鏇蓋醖觸鑰積糧鏇壓鹹) = 窪艱願積齋壓顧範壓夢 艱積選艱糧積遞餘鹽餘 (餘壓積齋蓋壓淵構艱壓, 簾築鑰獵憲簾憲鹹範糧 ~ 網淵窪繭餘鏇膚鑰鏇鑰) 更多 | ||||||
临床4期 | 33 | (Telmisartan 40 mg) | 範網醖積壓觸選積膚網(衊鏇範遞繭觸餘淵膚夢) = 夢積淵簾艱鹽鬱窪廠淵 膚壓鏇蓋顧糧觸願醖憲 (網顧築艱齋膚糧製簾鏇, 觸鹹壓範製遞鑰構鹽窪 ~ 遞齋夢獵築淵觸願壓獵) 更多 | - | 2017-08-02 | ||
(Azilsartan 20 mg) | 範網醖積壓觸選積膚網(衊鏇範遞繭觸餘淵膚夢) = 蓋鏇範繭顧齋積窪遞夢 膚壓鏇蓋顧糧觸願醖憲 (網顧築艱齋膚糧製簾鏇, 艱觸襯襯艱醖遞窪鑰醖 ~ 鏇艱壓襯鏇網艱積鬱遞) 更多 |
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