预约演示
更新于：2026-04-24
Azilsartan Kamedoxomil
阿齐沙坦酯钾盐
更新于：2026-04-24
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/序列
分子式C30H24KN4O8 |
InChIKeyMIJNRHZSZJLCAG-UHFFFAOYSA-N |
CAS号863031-24-7 |
关联
126
项与 阿齐沙坦酯钾盐 相关的临床试验NCT07547878
A Pilot Randomized Clinical Trial to Assess Feasibility, Safety, and Efficacy of Rapid, Simultaneous Therapy Initiation in Chronic Kidney Disease and Type 2 Diabetes: RAPID-CKD
CTR20255085
随机、开放、单剂量、两制剂、两序列、两周期、双交叉对照设计，评价餐后状态下单次口服受试制剂美阿沙坦钾片与参比制剂美阿沙坦钾片（商品名：易达比®）在中国健康受试者中的生物等效性正式试验
CTR20254332
健康受试者空腹和餐后单次口服美阿沙坦钾片的随机、开放、单剂量、两制剂、两序列、两周期、双交叉设计的生物等效性试验
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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697
项与 阿齐沙坦酯钾盐 相关的文献（医药）2026-06-01AQUATIC TOXICOLOGY
Metabolomic profiling reveals intestinal toxicity in zebrafish upon single and combined exposure to polystyrene microplastics and azithromycin
Article
作者: Tan, Jingnan ; Zhang, Le ; Ge, Lukun ; Li, Xi ; Li, Junyuan ; Sha, Haichao ; Gao, Xinwei ; Li, Qi
Polystyrene microplastics (PS-MPs) and azithromycin (AZM) are widely detected in aquatic environments, yet the mechanisms underlying their combined toxicity remain unclear. In this study, zebrafish were employed as a model organism to investigate the toxic effects of single and combined exposure to PS-MPs and AZM on intestinal health of zebrafish. Results demonstrated that the accumulation of PS-MPs in zebrafish intestines exhibited size-dependent characteristics-smaller particle sizes led to higher accumulation levels. Histopathological analysis revealed that single exposure to either PS-MPs or AZM induced intestinal structural damage. Notably, combined exposure at medium and high concentrations caused more severe damage compared to the AZM-only groups. The specific manifestations included reduced villus height, decreased goblet cell count, aggravated vacuolization, and loss of striated border. Analysis of oxidative stress indicated that PS-MPs exacerbated AZM-induced oxidative damage, intensifying intestinal oxidative stress. Additionally, the alteration of intestinal lipopolysaccharide levels reflected the modulation of gut barrier integrity and inflammatory response under combined exposure. Metabolomic analysis showed that the significantly altered metabolites induced by combined exposure to PS-MPs and AZM were mainly involved in metabolic pathways such as arginine biosynthesis, sphingolipid metabolism, purine metabolism, alanine-aspartate-glutamate metabolism, and pantothenate and CoA biosynthesis. This suggests that combined exposure significantly disrupts the metabolic homeostasis of zebrafish. This study provides key mechanistic evidence for assessing the ecological risks of combined PS-MPs and AZM pollution, reveals the interaction between oxidative stress and metabolic disturbance, clarifies the mechanism of their combined toxicity, and offers metabolomic support for evaluating the ecological risks of the synergistic effects of MPs and antibiotics.
2026-05-01INTERNATIONAL IMMUNOPHARMACOLOGY
Repurposing Azilsartan medoxomil attenuates periodontitis by targeting SERPINB9 to promote apoptosis of IL1B+ macrophages
Article
作者: Lin, Yongze ; Zhang, Hanwen ; Sun, Xueyu ; Zhao, Weiye ; Yan, Bin ; Zhang, Kejia
Periodontitis (PD) is a common chronic inflammatory disease characterized by progressive destruction of periodontal tissues and is associated with systemic disorders such as diabetes and cardiovascular disease. Despite its high global burden, current diagnostic and therapeutic strategies remain limited, highlighting the urgent need for reliable biomarkers and novel therapeutic targets. Macrophages are central to the pathogenesis of PD. Recent single-cell transcriptomic studies have identified IL1B+ macrophages as a pro-inflammatory subset closely linked to tissue destruction. However, the molecular mechanisms governing their survival remain poorly understood. In this study, we integrated multiple single-cell RNA sequencing datasets from the GEO database and applied five machine-learning algorithms to systematically identify critical regulators among differentially expressed genes in macrophages. SERPINB9 (PI9 in humans, Spi6 in mice) emerged as a key candidate, showing elevated expression in IL1B+ macrophages. Functional validation in vitro and in vivo confirmed that SERPINB9 promotes macrophage survival and sustains inflammatory responses. Furthermore, an in silico drug-repurposing screen based on FDA-approved compounds identified Azilsartan medoxomil as a potential inhibitor of SERPINB9. Pharmacological inhibition of SERPINB9 attenuated inflammatory macrophage responses and alleviated alveolar bone loss in experimental periodontitis, supporting its therapeutic potential. Collectively, these findings reveal a novel programmed cell death-related regulatory mechanism in macrophages, identifying SERPINB9 as a promising biomarker, and suggest that targeting SERPINB9 may offer a clinically translatable therapeutic strategy for periodontitis.
2026-03-09BIOMACROMOLECULES
Design of Poly-Catechol Biodynamers for Potentiation of Antibiotic Efficacy against Drug-Resistant Bacteria
Article
作者: Podlecki, Justin ; Koch, Marcus ; Zeroug-Metz, Lena ; Hirsch, Anna K. H. ; Sonntag, Philipp ; Bassil, Justine ; Buhler, Eric ; Christoulaki, Anastasia ; Lee, Sangeun ; Shehu, Kristela ; Schneider, Marc ; Kraegeloh, Annette
Catechol-modified polymers, such as DOPA-functionalized systems, have recently gained significant interest for a variety of biomedical applications, particularly in their role as antibacterial adjuvants due to their oxidative activity and ability to generate reactive oxygen species (ROS). Current catechol-functionalized polymers, however, often suffer from a restricted number of catechol groups, limited biocompatibility and solubility, and low stability due to the rapid oxidation under physiological conditions. In this study, we developed a water-soluble, biocompatible DOPA-modified biodynamer (DOPA-BD), leveraging the principles of constitutional dynamic chemistry (CDC). DOPA-BD was synthesized via polycondensation of DOPA-hydrazide and the hexaethylene glycol-conjugated carbazole dialdehyde (CA-HG), forming dynamic imine and acylhydrazone linkages between the monomers. As a result of its dynamic covalent backbone, DOPA-BD exhibits biodegradability and undergoes pH-responsive degradation under mildly acidic conditions typically found at infection sites, leading to a more than 3-fold increase in DOPA-hydrazide release compared to physiological pH. Interestingly, driven by CDC, DOPA-BD folds into a nanorod structure with a hydrodynamic diameter of ∼7.8 nm, surrounded by HG chains that offer water solubility and biocompatibility. Moreover, the incorporation of the DOPA-derivative in each repeating unit yields a polymer with exceptionally high catechol content, which remains stable and resistant to oxidation for 72 h in physiological buffer conditions. Regarding its antibacterial applicability, DOPA-BD demonstrated synergistic antibacterial activity with Azithromycin (AZM) against AZM-resistant E. coli, enhancing the antibiotic's efficacy by 4-fold. Our study indicates that DOPA-BD induces ROS production in the respective bacterial strain, suggesting ROS generation as one of the possible mechanisms contributing to the observed synergy. Overall, DOPA-BD represents a promising alternative strategy to potentiate antibacterial activity against resistant strains, holding strong potential for future antibacterial applications.
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) | 廠衊餘鑰窪衊憲壓遞膚(夢餘餘築窪簾遞遞觸鬱) = 積廠壓願鑰廠簾淵齋衊 鬱築願艱積廠餘壓蓋選 (鏇繭製鏇願繭艱壓淵築, 25.0) 更多 | - | 2020-02-05 | ||
(Open Label: TAK-491 80 mg) | 廠衊餘鑰窪衊憲壓遞膚(夢餘餘築窪簾遞遞觸鬱) = 醖簾獵遞鏇蓋壓製齋蓋 鬱築願艱積廠餘壓蓋選 (鏇繭製鏇願繭艱壓淵築, 20.5) 更多 | ||||||
临床3期 | 27 | Placebo+Azilsartan (Azilsartan 2.5 - 20 mg (Weight < 50 kg)) | 鏇廠鹹願顧艱鏇遞網廠 = 鏇夢膚顧遞築廠願夢願 壓鬱遞構糧夢壓艱鹽艱 (獵夢繭壓鹹蓋簾願艱夢, 製簾鬱繭繭鑰憲窪顧鹽 ~ 壓簾壓夢醖糧衊膚膚鏇) 更多 | - | 2019-12-23 | ||
Placebo+Azilsartan (Azilsartan 5 - 40 mg (Weight ≥ 50 kg)) | 鏇廠鹹願顧艱鏇遞網廠 = 鏇夢鏇襯積窪顧鬱繭積 壓鬱遞構糧夢壓艱鹽艱 (獵夢繭壓鹹蓋簾願艱夢, 艱顧鏇鏇願築獵鬱築觸 ~ 憲憲願積鏇衊簾膚淵艱) 更多 | ||||||
临床4期 | 380 | 膚襯範膚製壓觸選齋鏇 = 蓋鏇鑰網壓鑰願糧廠齋 構淵網顧鬱鹽淵廠鬱艱 (鑰選壓製遞選築齋糧選, 顧膚網膚鬱鏇範夢獵淵 ~ 憲選願糧鬱製鹹獵憲廠) 更多 | - | 2019-03-01 | |||
临床3期 | 612 | Valsartan Placebo+Azilsartan medoxomil (Azilsartan Medoxomil 40 mg) | 艱廠淵窪積憲壓築憲構(鬱選繭範衊範築選獵齋) = 衊齋願膚築簾餘艱鹹醖 獵膚構鬱繭艱鹽餘選蓋 (蓋簾廠鬱壓鹽夢齋醖鏇, 0.5123) 更多 | - | 2019-02-11 | ||
Valsartan Placebo+Azilsartan medoxomil (Azilsartan Medoxomil 80 mg) | 艱廠淵窪積憲壓築憲構(鬱選繭範衊範築選獵齋) = 淵襯鏇襯顧餘簾築製廠 獵膚構鬱繭艱鹽餘選蓋 (蓋簾廠鬱壓鹽夢齋醖鏇, 0.5010) 更多 | ||||||
临床3期 | 551 | 鏇製築網獵遞簾繭鹹淵(襯觸餘觸窪繭齋鏇顧構) = 餘憲壓鑰糧蓋膚鬱襯鑰 餘願選壓顧鹽鏇夢構網 (鑰顧夢構鑰鏇窪願齋窪 ) | - | 2018-07-01 | |||
鏇製築網獵遞簾繭鹹淵(襯觸餘觸窪繭齋鏇顧構) = 醖醖蓋觸製獵蓋選網鹹 餘願選壓顧鹽鏇夢構網 (鑰顧夢構鑰鏇窪願齋窪 ) | |||||||
N/A | 21 | (Azilsartan Medoximil.) | 糧選艱膚夢觸膚鹹窪選(鏇餘範餘糧遞繭獵壓構) = 網鏇憲製鬱淵齋淵觸鏇 壓廠廠齋淵憲鬱顧壓願 (築窪顧選觸壓選膚積夢, 14) 更多 | - | 2017-11-09 | ||
Placebo (Placebo) | 糧選艱膚夢觸膚鹹窪選(鏇餘範餘糧遞繭獵壓構) = 糧夢襯糧憲壓鑰壓積遞 壓廠廠齋淵憲鬱顧壓願 (築窪顧選觸壓選膚積夢, 904) 更多 | ||||||
临床3期 | 328 | Azilsartan medoxomil placebo (Placebo) | 夢艱鹽顧蓋蓋窪簾襯顧(醖壓餘壓構遞壓蓋醖壓) = 夢繭廠獵壓艱鑰顧齋餘 獵製淵襯鹹簾鏇繭窪壓 (鹹憲蓋窪顧鑰構廠鹽積, 2.0039) 更多 | - | 2016-12-19 | ||
(Azilsartan Medoxomil 40 mg) | 夢艱鹽顧蓋蓋窪簾襯顧(醖壓餘壓構遞壓蓋醖壓) = 夢選齋範膚醖憲願製簾 獵製淵襯鹹簾鏇繭窪壓 (鹹憲蓋窪顧鑰構廠鹽積, 1.4117) 更多 | ||||||
临床3期 | 6 | (Azilsartan 5 mg) | 壓夢願壓積廠糧繭蓋觸(糧積淵襯鏇鹽積醖壓淵) = 餘選鹹遞簾顧壓鹽製築 齋製鹽繭淵鑰壓齋觸鬱 (鹽鏇製淵窪窪鹹衊窪廠, 2963.53) 更多 | - | 2016-04-07 | ||
(Azilsartan 10 mg) | 壓夢願壓積廠糧繭蓋觸(糧積淵襯鏇鹽積醖壓淵) = 衊繭願醖鬱憲鑰餘觸憲 齋製鹽繭淵鑰壓齋觸鬱 (鹽鏇製淵窪窪鹹衊窪廠, 893.93) 更多 | ||||||
临床3期 | 669 | chlorthalidone+azilsartan medoxomil | 壓廠鹹觸網蓋憲鹹製鑰(憲鬱製壓鹹鹹構蓋範餘) = 襯衊獵鹽選艱選蓋憲鏇 製壓願製淵襯壓遞範壓 (鹹繭願獵糧糧繭衊窪築 ) 更多 | 积极 | 2016-01-01 | ||
壓廠鹹觸網蓋憲鹹製鑰(憲鬱製壓鹹鹹構蓋範餘) = 鏇壓淵糧醖觸範製淵夢 製壓願製淵襯壓遞範壓 (鹹繭願獵糧糧繭衊窪築 ) 更多 | |||||||
临床3期 | 105 | Placebo (Placebo QD) | 鏇餘顧鬱窪淵衊構鹹鏇(艱壓蓋壓齋鹽製膚襯構) = 築獵鏇壓鬱選觸鑰廠膚 壓簾選齋範選製構鑰憲 (膚鹹鬱鹽壓糧選鑰鬱餘, 2.71) 更多 | - | 2015-05-06 | ||
(Azilsartan Medoxomil 40 mg QD) | 鏇餘顧鬱窪淵衊構鹹鏇(艱壓蓋壓齋鹽製膚襯構) = 鹽鏇製範鑰製膚構餘積 壓簾選齋範選製構鑰憲 (膚鹹鬱鹽壓糧選鑰鬱餘, 2.69) 更多 |
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