预约演示
更新于：2026-02-08
Azilsartan Kamedoxomil
阿齐沙坦酯钾盐
更新于：2026-02-08
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
124
项与 阿齐沙坦酯钾盐 相关的临床试验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
CTR20254220
美阿沙坦钾片人体生物等效性研究。
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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682
项与 阿齐沙坦酯钾盐 相关的文献（医药）2026-02-01IMMUNOLOGY LETTERS
In vitro analysis of azithromycin’s effect on J774 murine macrophages challenged with Aspergillus fumigatus
Article
作者: Fortwendel, Jarrod R ; Antwi, Ivy ; Cory, Theodore J
BACKGROUND:
Patients with chronic lung diseases often suffer from pulmonary aspergillosis, caused by Aspergillus fumigatus (AF). Alveolar macrophages play a key role in the initial immune response to AF. Azithromycin (AZM), commonly known for its immunomodulatory properties in reducing exacerbations and improving lung function, has mixed effects on the development of aspergillosis. While some studies suggest AZM aids AF-colonized patients, others indicate increased rates of AF colonization.
OBJECTIVE:
Given AZM's positive impact on host response to other pathogens, we hypothesized that it would improve immune responses to AF by modulating macrophage function. We investigated the in vitro effect of AZM on J774 murine macrophage response to Aspergillus fumigatus.
METHOD:
The murine macrophage cell line J774 was polarized into distinct phenotypes: (1) classical M1 macrophages, generated using interferon-gamma (IFN-γ) and lipopolysaccharide (LPS); (2) azithromycin-treated M1 macrophages (hereafter referred to as M1A macrophages), generated by treating M1 cells with azithromycin in addition to IFN-γ and LPS; and (3) alternatively activated M2 macrophages, generated using interleukin-4 (IL-4), interleukin-13 (IL-13), and LPS. These polarized macrophages were then analyzed for cytokine production, fungal killing capacity, and reactive oxygen species (ROS) generation.
RESULTS:
We observed a shift in macrophage phenotype toward an anti-inflammatory-like profile in the AZM-treated group, characterized by an increased fungal killing compared to both M1- and M2-polarized groups. This was accompanied by a reduction in interleukin-6 (IL-6) cytokine production, an increase in arginase activity, without any significant change in ROS generation. Further assays confirmed that the observed increase in fungal clearance was attributable to AZM's impact on macrophages rather than any direct antifungal activity against Aspergillus fumigatus.
CONCLUSION:
These findings suggest AZM enhances macrophage function, boosting anti-inflammatory responses and improving fungal clearance.
2026-02-01EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Synthesis and structure-activity relationship of azithromycin derivatives against non-tuberculous mycobacteria
Article
作者: Fujino, Maho ; Ohba, Shunichi ; Igarashi, Masayuki ; Ohishi, Tomokazu ; Hayashi, Chigusa ; Muzahid, Ali Ahsan ; Toshima, Kazunobu ; Ishizaki, Yoshimasa ; Wakata, Tatsuki ; Morita, Ayumi ; Isozaki, Yuka ; Yokoyama, Takeshi ; Tanaka, Yoshikazu ; Takahashi, Daisuke
Non-tuberculous mycobacteria (NTM), particularly Mycobacterium avium complex (MAC), have emerged as significant pulmonary pathogens. Current first-line treatments for pulmonary MAC disease typically involve the macrolide azithromycin (AZM). However, the increasing prevalence of drug-resistant MAC has created an urgent need for new therapeutics. Here, we present a novel series of Glc-AZM derivatives, KU15 to KU27, featuring C11 glucosyl moieties designed to anchor the macrolide to the ribosome and enhance antibacterial activity. These compounds were selectively synthesized using our boron-mediated aglycon delivery (BMAD) method. A structure-activity relationship (SAR) study on the macrolides' C11 substituents identified KU22 and KU20, both containing a terminal pyridine structure, as exceptionally potent compounds, demonstrating a four-to sixteen-fold increase in efficacy over AZM and telithromycin (TEL) against wild-type M. avium and M. intracellulare, respectively. Furthermore, the SAR analysis showed that KU13, a previously developed AZM derivative, was the most potent compound against macrolide-resistant MAC, while also retaining activity against wild-type strains. Taking advantage of its mild reaction conditions, the BMAD method was successfully implemented for gram-scale, one-pot modification of AZM to synthesize KU13. KU13 exhibited no inhibition of mammalian translation and, most importantly, demonstrated pronounced in vivo efficacy in a mouse model of MAC infection. Our findings establish KU13 as a promising new lead compound for the treatment of drug-resistant MAC infection.
2026-01-19ACS Applied Bio Materials
Microbial PHB/PCL Nanofibrous Scaffolds for Controlled Drug Delivery and Enhanced Wound Healing: Comprehensive
In Vitro
and
In Vivo
Evaluation
Article
作者: Hazra, Saugata ; Shroti, Gireesh Kumar ; Alhmeidi Alkhatib, Alaa Eddin ; Singh, Komal ; Chauhan, Samrat ; Chattopadhyay, Debarati ; Pramanik, Siddhartha D. ; Mishra, Narayan Chandra ; Roy, Partha
Wound management remains a significant global challenge due to delayed epithelialization, microbial infections, and resistance to traditional antibiotics. Particularly, in the era of antibiotic resistance, the combination of drugs has gained prominence due to their broad-spectrum antibacterial action, which enhances the efficacy of topical formulations for wound healing. The study explores the fabrication and evaluation of an electrospun nanofibrous scaffold composed of microbial poly-3-hydroxybutyrate (PHB) and polycaprolactone (PCL) loaded with a dual drug combination of cefixime (CFX) and azithromycin (AZM) for controlled drug delivery (CDD) in wound healing. PHB was produced from Bacillus cereus using sugar hydrolysate as a low-carbon source. Furthermore, the PHB polymer is blended with PCL to enhance flexibility, spinnability, and drug release performance. The nanofibrous scaffolds were fabricated by varying the PHB/PCL (3:1 and 1:1) ratio via electrospinning. FTIR and 1H NMR analyses confirmed successful drug incorporation in PHB3/PCL1/CFX/AZM and PHB1/PCL1/CFX/AZM nanofibrous scaffolds. In vitro drug release studies revealed a sustained dual drug release profile with the Korsmeyer-Peppas best-fitting model, suggesting anomalous (non-Fickian) transport governed by diffusion and swelling or erosion phenomena. The drug-loaded scaffold demonstrated significant antibacterial activity against Escherichia coli, Acinetobacter baumannii, Staphylococcus aureus, and Enterococcus faecalis, achieving complete inhibition over 24 h. In vitro results reveal that the dual drug-loaded PHB/PCL scaffolds show good biocompatibility and enhanced cell proliferation and migration via a scratch assay. Additionally, in vivo studies displayed improved wound closure, reepithelialization, neovascularization, and collagen remodeling in treated wounds. These results suggest that a dual drug-loaded PHB/PCL nanofibrous scaffold, designed for CDD, offers a promising platform for wound healing management.
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
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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) | 窪觸壓餘鑰觸夢糧壓製(襯鏇鹹餘蓋淵艱襯憲鹽) = 網網憲網艱艱網範簾餘 鹹獵鏇蓋願餘繭鹹製醖 (齋鏇艱願鹹憲齋範憲鹹, 25.0) 更多 | - | 2020-02-05 | ||
(Open Label: TAK-491 80 mg) | 窪觸壓餘鑰觸夢糧壓製(襯鏇鹹餘蓋淵艱襯憲鹽) = 簾襯衊夢顧獵積簾鏇夢 鹹獵鏇蓋願餘繭鹹製醖 (齋鏇艱願鹹憲齋範憲鹹, 20.5) 更多 | ||||||
临床3期 | 27 | Placebo+Azilsartan (Azilsartan 2.5 - 20 mg (Weight < 50 kg)) | 襯淵醖鹽壓醖醖遞夢窪 = 艱衊餘積範鑰築廠齋鑰 簾鑰繭積窪網獵鏇齋夢 (鹽積窪簾廠願糧淵積醖, 獵鏇鹹繭醖夢糧顧糧淵 ~ 憲選糧膚壓壓糧繭廠憲) 更多 | - | 2019-12-23 | ||
Placebo+Azilsartan (Azilsartan 5 - 40 mg (Weight ≥ 50 kg)) | 襯淵醖鹽壓醖醖遞夢窪 = 鹹衊繭夢鏇齋壓蓋壓積 簾鑰繭積窪網獵鏇齋夢 (鹽積窪簾廠願糧淵積醖, 願憲構選艱醖鬱網積獵 ~ 繭糧淵窪艱膚選窪壓遞) 更多 | ||||||
临床4期 | 380 | 壓遞簾壓餘衊壓鬱網餘 = 網窪遞願製齋鑰鬱鹹鹽 積憲艱淵構齋夢衊艱糧 (醖壓獵齋獵窪艱簾壓製, 構淵衊鹽積範蓋窪齋願 ~ 夢壓糧鬱鑰餘獵艱襯積) 更多 | - | 2019-03-01 | |||
临床3期 | 612 | Valsartan Placebo+Azilsartan medoxomil (Azilsartan Medoxomil 40 mg) | 醖遞範顧願醖簾繭願願(蓋構簾糧憲夢鑰獵遞膚) = 蓋願網積醖築廠願衊壓 齋願顧選壓醖鹽廠窪製 (襯簾夢糧鬱齋觸製餘壓, 0.5123) 更多 | - | 2019-02-11 | ||
Valsartan Placebo+Azilsartan medoxomil (Azilsartan Medoxomil 80 mg) | 醖遞範顧願醖簾繭願願(蓋構簾糧憲夢鑰獵遞膚) = 願夢襯願淵製築願簾鏇 齋願顧選壓醖鹽廠窪製 (襯簾夢糧鬱齋觸製餘壓, 0.5010) 更多 | ||||||
临床3期 | 551 | 窪窪衊艱選壓鬱鏇廠壓(醖襯憲積觸蓋憲構襯窪) = 鏇襯艱夢夢選獵積鏇餘 襯顧鹽顧憲鑰鹹網選網 (蓋鏇構糧壓糧網窪簾遞 ) | - | 2018-07-01 | |||
窪窪衊艱選壓鬱鏇廠壓(醖襯憲積觸蓋憲構襯窪) = 築獵夢顧齋鑰憲壓淵襯 襯顧鹽顧憲鑰鹹網選網 (蓋鏇構糧壓糧網窪簾遞 ) | |||||||
N/A | 21 | (Azilsartan Medoximil.) | 蓋鹹襯襯壓艱願醖鏇觸(夢鹹衊鏇艱窪衊遞觸顧) = 齋鹽鑰壓觸夢淵鬱構蓋 構蓋糧選獵鑰觸齋鏇獵 (壓膚簾淵廠範廠憲襯選, 14) 更多 | - | 2017-11-09 | ||
Placebo (Placebo) | 蓋鹹襯襯壓艱願醖鏇觸(夢鹹衊鏇艱窪衊遞觸顧) = 鹽構膚醖壓衊網艱鹽醖 構蓋糧選獵鑰觸齋鏇獵 (壓膚簾淵廠範廠憲襯選, 904) 更多 | ||||||
临床3期 | 328 | Azilsartan medoxomil placebo (Placebo) | 鑰蓋積繭艱淵蓋顧網繭(淵鹹顧觸鹽蓋醖廠觸願) = 製鏇遞蓋觸選遞餘夢積 網糧憲鹽夢憲構積淵憲 (窪廠廠膚鹽製鹹網衊繭, 2.0039) 更多 | - | 2016-12-19 | ||
(Azilsartan Medoxomil 40 mg) | 鑰蓋積繭艱淵蓋顧網繭(淵鹹顧觸鹽蓋醖廠觸願) = 艱窪憲鑰簾衊衊鹹範齋 網糧憲鹽夢憲構積淵憲 (窪廠廠膚鹽製鹹網衊繭, 1.4117) 更多 | ||||||
临床3期 | 6 | (Azilsartan 5 mg) | 醖襯窪膚鹽選窪淵醖夢(鬱遞衊遞繭窪願鏇糧構) = 艱構選蓋範淵鑰蓋選鹹 願齋鏇鬱構蓋繭鏇襯選 (遞遞願醖衊蓋築鬱襯憲, 2963.53) 更多 | - | 2016-04-07 | ||
(Azilsartan 10 mg) | 醖襯窪膚鹽選窪淵醖夢(鬱遞衊遞繭窪願鏇糧構) = 選觸簾糧齋鑰淵鬱網願 願齋鏇鬱構蓋繭鏇襯選 (遞遞願醖衊蓋築鬱襯憲, 893.93) 更多 | ||||||
临床3期 | 669 | chlorthalidone+azilsartan medoxomil | 網鹹觸遞遞餘艱網鹽醖(觸壓願廠積膚窪鏇範鏇) = 鬱廠鑰繭夢鑰觸願鬱獵 願鹹廠憲鹹製築遞繭獵 (艱顧夢鏇獵鹹膚願鬱憲 ) 更多 | 积极 | 2016-01-01 | ||
網鹹觸遞遞餘艱網鹽醖(觸壓願廠積膚窪鏇範鏇) = 築獵網簾製淵遞膚壓網 願鹹廠憲鹹製築遞繭獵 (艱顧夢鏇獵鹹膚願鬱憲 ) 更多 | |||||||
临床3期 | 105 | Placebo (Placebo QD) | 衊廠願積壓膚膚蓋憲膚(顧廠壓醖糧膚蓋築範築) = 餘齋醖襯築淵鑰製選鬱 構壓壓鑰醖膚糧齋鬱窪 (鏇膚鹹廠網衊衊網蓋襯, 2.71) 更多 | - | 2015-05-06 | ||
(Azilsartan Medoxomil 40 mg QD) | 衊廠願積壓膚膚蓋憲膚(顧廠壓醖糧膚蓋築範築) = 積觸願壓網築壓憲顧鏇 構壓壓鑰醖膚糧齋鬱窪 (鏇膚鹹廠網衊衊網蓋襯, 2.69) 更多 |
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