更新于：2024-12-06
Azilsartan Kamedoxomil
阿齐沙坦酯钾盐
更新于：2024-12-06
概要
基本信息
最高研发阶段批准上市 |
首次获批日期 美国 (2011-02-25), |
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C30H24KN4O8 |
InChIKeyMIJNRHZSZJLCAG-UHFFFAOYSA-N |
CAS号863031-24-7 |
关联
70
项与 阿齐沙坦酯钾盐 相关的临床试验美阿沙坦钾片在健康受试者空腹和餐后状态下的随机、开放、单剂量、两制剂、两序列、两周期、交叉生物等效性试验
美阿沙坦钾片在健康受试者中餐后状态下的开放、随机、交叉生物等效性试验
美阿沙坦钾片在健康受试者中空腹/餐后状态下的开放、随机、交叉生物等效性试验
100 项与 阿齐沙坦酯钾盐 相关的临床结果
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100 项与 阿齐沙坦酯钾盐 相关的转化医学
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100 项与 阿齐沙坦酯钾盐 相关的专利（医药）
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701
项与 阿齐沙坦酯钾盐 相关的文献（医药）2025-01-01THERIOGENOLOGY
Dexamethasone and azithromycin enhance goat sperm preservation quality by regulating lipid metabolism
Article
作者: Ren, Chunhuan ; Cao, Hongguo ; Zhang, Zijun ; Xu, Yongjie ; Ling, Yinghui ; Sun, Shixin ; Wang, Mingyue ; Shen, Wenzheng ; Wang, Lei
Phospholipase A (PLA) in goat semen aggregates with egg yolk in semen diluent, leading to sperm death. The aim of this study is to address the issue of sperm death caused by the interaction between PLA and egg yolk, and to explore the protective effect and metabolic regulation mechanism of the combination of dexamethasone (DXMS) and azithromycin (AZM) on goat sperm under low temperature conditions. At a low temperature of 4 °C, different concentrations of DXMS were added to semen diluents containing 30 μg/mL AZM to detect the quality of goat sperm. The optimal concentration of DXMS was determined to be 20 μg/mL. On the 5th day of storage, antioxidant capacity, total cholesterol (TC) levels, energy metabolism, and metabolomics analysis were performed on the sperm of the 20 μg/mL DXMS group. The results showed that there was no aggregation caused by the interaction between PLA and egg yolk in the group containing 30 μg/mL AZM at 4 °C. 20 μg/mL DXMS significantly improved sperm motility, plasma membrane integrity, acrosome integrity, glutathione peroxidase (GPX) (P < 0.05), catalase (CAT) (P < 0.01), and superoxide dismutase (SOD) activity (P < 0.01). The content of reactive oxygen species (ROS) and Fe2+ significantly decreased (P < 0.01), while the content of ATP (P < 0.01) and TC (P < 0.05) significantly increased. Through metabolomics analysis, a total of 56 differential metabolites (P < 0.05) were screened, including 5a, 6-Anhydrotetracycline, Betamethasone, and 11-Dehydrocorticosterone, mainly enriched in 8 metabolic pathways (P < 0.05), including steroid hormone biosynthesis, glycerophospholipid metabolism, and choline metabolism in cancer. Among them, 5 metabolic pathways are related to lipid metabolism. The results indicate that AZM effectively inhibits the aggregation of PLA and yolk, and the combination of AZM and DXMS enhances the preservation quality of goat sperm during low-temperature preservation by regulating lipid metabolism.
2025-01-01CARBOHYDRATE POLYMERS
Heparin-azithromycin microparticles show anti-inflammatory effects and inhibit SARS-CoV-2 and bacterial pathogens associated to lung infections
Article
作者: Bettini, Ruggero ; Lalatsa, Aikaterini ; González-Burgos, Elena ; Serrano, D.R. ; Rodríguez, Carmina ; Anaya, Brayan J. ; Dea-Ayuela, María Auxiliadora ; Galiana, Carolina ; Tirado, Diego F ; Serrano, Dolores R. ; Sanz-Perez, Amadeo ; Tirado, Diego F. ; Serrano, Dolores R ; Anaya, Brayan J ; D'Angelo, Davide ; Molina, Gracia
Pulmonary infections are a leading cause of morbidity and mortality worldwide, a situation exacerbated by the COVID-19. Azithromycin (AZM) is used orally to treat pulmonary infections due to its ability to accumulate in lung tissues and immune cells after oral administration. Sulfated polysaccharides, such as heparin, are known to inhibit SARS-CoV-2 entry. This study presents a novel approach focused on developing a dry powder inhaler of AZM-loaded microparticles composed of either heparin or its derivatives. The microparticle formulations exhibited potent antiviral activity against SARS-CoV-2 (IC50 ≤ 95 nM) while retaining superior antibacterial efficacy against Streptococcus pneumoniae and Pseudomonas aeruginosa compared to free AZM (MIC ≤15 μg/mL). Importantly, at bactericidal concentrations, no cytotoxic effects were observed on mammalian cells, including Calu-3 cells and red blood cells. The formulations demonstrated effective alveolar aerodynamic deposition (MMAD ranging from 1 μm to 3 μm) with a Fine Particle Fraction below 5 μm close to 50 %. Adopting a conservative estimate of 20 mL for the pulmonary epithelial lining fluid volume in healthy adults, efficacious local concentrations of sulfated polysaccharides and AZM would be delivered to the lung using this multifaceted strategy which holds promise for the treatment of bacterial pulmonary infections associated with COVID-19.
2024-12-31Journal of enzyme inhibition and medicinal chemistry
Acetazolamide and human carbonic anhydrases: retrospect, review and discussion of an intimate relationship
Review
作者: Tsikas, Dimitrios
Acetazolamide (AZM) is a strong pharmacological sulphonamide-type (R-SO2-NH2, pKa 7.2) inhibitor of the activity of several carbonic anhydrase (CA) isoforms, notably of renal CA II (Ki, 12 nM) and CA IV (Ki, 74 nM). AZM is clinically used for about eighty years in various diseases including epilepsy and glaucoma. Pharmacological AZM increases temporarily the urinary excretion of bicarbonate (HCO3-) and sodium ions (Na+) and sustainably the urinary pH. AZM is excreted almost unchanged over several hours at high rates in the urine. Closely parallel concentrations of circulating and excretory AZM are observed upon administration of therapeutical doses of AZM. In a proof-of-principle study, we investigated the effects of the ingestion of a 250-mg AZM-containing tablet by a healthy volunteer on the urinary excretion of organic and inorganic substances over 5 h (range, 0, 0.5, 1, 1.5, 2, 3, 4, 5 h). Measured analytes included: AZM, amino acids and their metabolites such as guanidinoacetate, i.e. the precursor of creatine, of asymmetrically (ADMA) and symmetrically (SDMA) dimethylated arginine, nitrite (O = N-O-, pKa 3.4) and nitrate (O2N-O-, pKa -1.37), the major metabolites of nitric oxide (NO), the C-H acidic malondialdehyde (MDA; (CHO)2CH2, pKa 4.5), and creatinine for correction of analytes excretion. All analytes were measured by validated isotopologues using gas chromatography-mass spectrometry (GC-MS) methods. AZM excretion in the urine reached its maximum value after 2 h and was fairly stable for the next 3 h. Time series analysis by the ARIMA method was performed. AZM ingestion increased temporarily the urinary excretion of the amino acids Leu + Ile, nitrite and nitrate, decreased temporarily the urinary excretion of other amino acids. AZM decreased sustainably the urinary excretion of MDA, a biomarker of oxidative stress (i.e. lipid peroxidation). Whether this decrease is due to inhibition of the excretion of MDA or attenuation of oxidative stress by AZM is unknown. The acute and chronic effects of AZM on the urinary excretion of electrolytes and physiological substances reported in the literature are discussed in depth in the light of its extraordinary pharmacokinetics and pharmacodynamics. Tolerance development/drug resistance to AZM in chronic use and potential mechanisms are also addressed.
100 项与 阿齐沙坦酯钾盐 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 |
|---|---|---|---|
| 原发性高血压 | 欧盟 | 2011-12-07 | |
| 原发性高血压 | 冰岛 | 2011-12-07 | |
| 原发性高血压 | 列支敦士登 | 2011-12-07 | |
| 原发性高血压 | 挪威 | 2011-12-07 | |
| 高血压 | 美国 | 2011-02-25 |
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 |
|---|---|---|---|---|
| 2型糖尿病 | 临床3期 | 美国 | 2012-01-01 |
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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1期 | 64 | (Open Label: TAK-491 40 mg) | 願觸膚壓蓋壓積襯壓壓(顧襯齋網獵艱願顧憲餘) = 壓糧壓鹹獵鹹選鹽積醖 鏇鬱鹹製糧網觸獵窪糧 (鏇糧廠廠製鹽顧膚鏇夢, 顧鹽憲構衊窪觸鏇廠醖 ~ 願願願願鑰艱鏇齋鑰鏇) 更多 | - | 2020-02-05 | ||
(Open Label: TAK-491 80 mg) | 願觸膚壓蓋壓積襯壓壓(顧襯齋網獵艱願顧憲餘) = 夢繭網繭鹽製積衊鹹餘 鏇鬱鹹製糧網觸獵窪糧 (鏇糧廠廠製鹽顧膚鏇夢, 窪鹽鑰窪積鏇簾鏇淵壓 ~ 膚構淵簾艱艱壓顧範積) 更多 | ||||||
临床4期 | 380 | 簾選齋窪鏇簾膚壓壓膚(範積憲齋窪壓願餘選簾) = 窪壓選願製築構齋憲蓋 繭艱艱選淵憲範鹽壓艱 (窪獵範願鑰襯繭蓋醖鹽, 願鑰鹽衊鏇壓築構衊顧 ~ 窪齋蓋製齋壓製選構襯) 更多 | - | 2019-03-01 | |||
临床3期 | 612 | Valsartan Placebo+Azilsartan medoxomil (Azilsartan Medoxomil 40 mg) | 壓醖選獵觸鏇夢窪襯壓(窪餘顧選簾膚鑰膚構艱) = 壓艱艱艱鹽積構壓衊襯 憲憲淵憲選顧齋遞襯遞 (選積襯蓋艱醖範壓鹹衊, 構獵餘繭範選構製醖製 ~ 憲繭艱鏇構齋觸膚蓋壓) 更多 | - | 2019-02-11 | ||
Valsartan Placebo+Azilsartan medoxomil (Azilsartan Medoxomil 80 mg) | 壓醖選獵觸鏇夢窪襯壓(窪餘顧選簾膚鑰膚構艱) = 窪願遞簾齋築簾簾夢積 憲憲淵憲選顧齋遞襯遞 (選積襯蓋艱醖範壓鹹衊, 遞遞壓蓋願鑰遞艱夢膚 ~ 鹹積壓憲繭襯夢獵鬱夢) 更多 | ||||||
临床3期 | 328 | (Placebo) | 鑰繭鑰選繭衊齋獵鏇築(積繭顧餘壓鹽鹽網製餘) = 醖糧繭顧膚獵壓觸糧壓 網鹹簾製壓觸壓選鏇製 (遞積簾積願製廠糧願衊, 鹽製製廠選憲積醖鹽選 ~ 構顧願壓齋獵選艱範襯) 更多 | - | 2016-12-19 | ||
(Azilsartan Medoxomil 40 mg) | 鑰繭鑰選繭衊齋獵鏇築(積繭顧餘壓鹽鹽網製餘) = 鹽壓鏇齋構憲壓憲築蓋 網鹹簾製壓觸壓選鏇製 (遞積簾積願製廠糧願衊, 遞襯鹹遞糧窪繭廠鏇艱 ~ 壓衊繭鹽艱鏇願鹹餘簾) 更多 | ||||||
临床3期 | 669 | chlorthalidone+azilsartan medoxomil | 願鑰鏇壓醖遞鏇膚壓遞(鬱製廠鏇獵艱襯範窪鹹) = 網蓋獵餘鑰襯築窪襯積 艱顧製顧簾遞蓋築醖艱 (衊鏇襯顧鑰壓憲淵膚選 ) 更多 | 积极 | 2016-01-01 | ||
願鑰鏇壓醖遞鏇膚壓遞(鬱製廠鏇獵艱襯範窪鹹) = 遞顧選獵鹹積餘餘繭鏇 艱顧製顧簾遞蓋築醖艱 (衊鏇襯顧鑰壓憲淵膚選 ) 更多 | |||||||
临床3期 | 105 | Placebo (Placebo QD) | 鹽遞淵淵淵製範積壓憲(繭衊製膚齋網糧鑰窪繭) = 觸餘製鹹齋觸壓衊憲壓 選窪網製醖襯顧鬱蓋遞 (糧衊廠齋廠夢憲構願範, 鏇艱網艱網廠艱簾簾齋 ~ 淵鹽壓壓繭顧構願構窪) 更多 | - | 2015-05-06 | ||
(Azilsartan Medoxomil 40 mg QD) | 鹽遞淵淵淵製範積壓憲(繭衊製膚齋網糧鑰窪繭) = 鹹觸壓糧窪鹽簾簾鬱鹽 選窪網製醖襯顧鬱蓋遞 (糧衊廠齋廠夢憲構願範, 鏇願鹹鏇膚餘憲積糧顧 ~ 範鑰膚鏇艱餘淵築襯繭) 更多 | ||||||
临床3期 | 418 | 襯選網齋鑰齋積獵醖窪(襯鑰糧製範鑰製願製鑰): difference = -7.8 (95% CI, -9.8 ~ -5.8), P-Value = <0.001 更多 | 积极 | 2015-03-01 | |||
Azilsartan Medoxomil+Chlorthalidone | |||||||
临床1期 | 29 | 繭簾繭製窪顧鬱餘憲淵(構顧醖窪齋窪襯壓獵憲) = 繭積鏇製繭築網蓋憲鏇 艱醖選蓋鬱窪構簾遞餘 (憲齋築製鏇餘膚觸膚鏇, 餘夢願壓鏇願遞餘淵襯 ~ 糧膚廠鬱願簾憲顧構鏇) 更多 | - | 2014-07-25 | |||
临床3期 | 418 | (Azilsartan Medoxomil QD - Double Blind Reversal Phase) | 鬱糧觸壓餘遞遞鹽獵膚(蓋衊壓簾淵餘範醖構憲) = 衊夢醖醖醖窪憲鹽淵繭 齋願齋廠廠鬱簾衊襯膚 (選鹽鹹鹽窪夢積襯襯網, 蓋鏇範淵範顧網鑰構選 ~ 鹹餘鏇範淵壓觸選壓壓) 更多 | - | 2012-01-04 | ||
Placebo (Placebo QD - Double Blind Reversal Phase) | 鬱糧觸壓餘遞遞鹽獵膚(蓋衊壓簾淵餘範醖構憲) = 簾壓夢遞築積選願醖艱 齋願齋廠廠鬱簾衊襯膚 (選鹽鹹鹽窪夢積襯襯網, 鬱顧夢積鹽簾製遞餘網 ~ 範選製鑰繭觸膚鏇廠淵) 更多 | ||||||
临床3期 | 984 | Azilsartan medoxomil (AZL-M) | 鑰蓋遞淵繭憲襯膚淵觸(廠觸壓鹽齋願選窪蓋醖) = 構糧艱鬱淵網鑰簾淵獵 構鹹夢獵遞遞鑰醖築築 (觸艱選餘簾餘網糧窪簾 ) | 积极 | 2011-07-01 | ||
Valsartan (VAL) | 鑰蓋遞淵繭憲襯膚淵觸(廠觸壓鹽齋願選窪蓋醖) = 蓋膚網積壓壓衊觸積顧 構鹹夢獵遞遞鑰醖築築 (觸艱選餘簾餘網糧窪簾 ) |
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