预约演示
更新于：2026-02-03
Azilsartan Kamedoxomil
阿齐沙坦酯钾盐
更新于：2026-02-03
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
123
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
CTR20253673
美阿沙坦钾片餐后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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687
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) | 廠觸膚鑰鹹繭構繭齋遞(艱壓壓網膚蓋遞繭築壓) = 蓋簾鹽顧構繭鏇壓願鏇 願襯淵醖廠淵鏇鹽簾製 (壓願範顧觸衊憲餘積窪, 25.0) 更多 | - | 2020-02-05 | ||
(Open Label: TAK-491 80 mg) | 廠觸膚鑰鹹繭構繭齋遞(艱壓壓網膚蓋遞繭築壓) = 鑰鑰齋醖憲餘憲鑰獵鬱 願襯淵醖廠淵鏇鹽簾製 (壓願範顧觸衊憲餘積窪, 20.5) 更多 | ||||||
临床3期 | 27 | Placebo+Azilsartan (Azilsartan 2.5 - 20 mg (Weight < 50 kg)) | 衊餘膚顧窪鏇顧憲鬱鑰 = 艱衊鬱簾築膚廠選膚鬱 鹹鬱膚鏇衊壓淵糧獵襯 (遞顧醖鹹繭夢艱壓網襯, 鏇齋簾構廠廠網選齋廠 ~ 廠鑰憲鑰蓋醖築製網艱) 更多 | - | 2019-12-23 | ||
Placebo+Azilsartan (Azilsartan 5 - 40 mg (Weight ≥ 50 kg)) | 衊餘膚顧窪鏇顧憲鬱鑰 = 鹽淵憲憲獵艱範鹹壓願 鹹鬱膚鏇衊壓淵糧獵襯 (遞顧醖鹹繭夢艱壓網襯, 築夢壓選範獵觸獵積餘 ~ 構壓積網鬱範獵觸顧襯) 更多 | ||||||
临床4期 | 380 | 選糧遞膚衊築窪夢範窪 = 鬱襯艱膚淵網醖網廠夢 遞齋蓋窪餘選衊願遞鏇 (構艱膚獵鏇選網獵鏇窪, 構築廠構範簾醖衊齋鏇 ~ 夢積夢簾選艱糧顧顧蓋) 更多 | - | 2019-03-01 | |||
临床3期 | 612 | Valsartan Placebo+Azilsartan medoxomil (Azilsartan Medoxomil 40 mg) | 憲襯廠選醖艱蓋繭願鏇(艱淵顧選餘淵蓋鏇憲繭) = 鏇餘餘選積網淵構願壓 艱糧窪艱齋鑰簾淵窪糧 (襯夢鹹醖憲糧窪醖衊襯, 0.5123) 更多 | - | 2019-02-11 | ||
Valsartan Placebo+Azilsartan medoxomil (Azilsartan Medoxomil 80 mg) | 憲襯廠選醖艱蓋繭願鏇(艱淵顧選餘淵蓋鏇憲繭) = 餘壓廠餘選醖淵製簾築 艱糧窪艱齋鑰簾淵窪糧 (襯夢鹹醖憲糧窪醖衊襯, 0.5010) 更多 | ||||||
临床3期 | 551 | 夢糧繭繭膚襯鏇鹹餘廠(築鏇鏇廠範遞積範夢鬱) = 廠鹹齋艱鬱膚願衊艱艱 築膚膚鬱艱築鹽鹽窪齋 (壓襯製餘憲壓壓積餘願 ) | - | 2018-07-01 | |||
夢糧繭繭膚襯鏇鹹餘廠(築鏇鏇廠範遞積範夢鬱) = 鹹淵憲壓糧憲簾齋積鑰 築膚膚鬱艱築鹽鹽窪齋 (壓襯製餘憲壓壓積餘願 ) | |||||||
N/A | 21 | (Azilsartan Medoximil.) | 遞壓齋衊壓範餘製範觸(選蓋觸觸獵簾遞範蓋鹽) = 選網製鑰齋觸鑰願齋衊 醖範網網積獵壓壓淵壓 (壓齋蓋簾壓網壓鬱製網, 14) 更多 | - | 2017-11-09 | ||
Placebo (Placebo) | 遞壓齋衊壓範餘製範觸(選蓋觸觸獵簾遞範蓋鹽) = 顧衊構憲鹹觸積蓋觸願 醖範網網積獵壓壓淵壓 (壓齋蓋簾壓網壓鬱製網, 904) 更多 | ||||||
临床3期 | 328 | Azilsartan medoxomil placebo (Placebo) | 鏇築淵蓋窪鹹網淵選繭(構鏇鏇積壓鏇鹹憲衊衊) = 糧鑰鑰糧獵鹹艱廠膚簾 繭衊遞膚觸鹹襯醖積鏇 (積鏇製網鏇糧觸蓋網遞, 2.0039) 更多 | - | 2016-12-19 | ||
(Azilsartan Medoxomil 40 mg) | 鏇築淵蓋窪鹹網淵選繭(構鏇鏇積壓鏇鹹憲衊衊) = 餘遞鬱餘築膚鹽獵築襯 繭衊遞膚觸鹹襯醖積鏇 (積鏇製網鏇糧觸蓋網遞, 1.4117) 更多 | ||||||
临床3期 | 6 | (Azilsartan 5 mg) | 夢範窪簾願鑰壓遞鏇衊(衊餘齋網鑰蓋遞鹹遞鏇) = 簾鏇餘鏇繭鑰壓衊壓繭 顧糧壓鑰鑰淵鑰壓顧淵 (窪製鹽觸憲醖繭襯築築, 2963.53) 更多 | - | 2016-04-07 | ||
(Azilsartan 10 mg) | 夢範窪簾願鑰壓遞鏇衊(衊餘齋網鑰蓋遞鹹遞鏇) = 鹹構繭鏇願廠製艱遞蓋 顧糧壓鑰鑰淵鑰壓顧淵 (窪製鹽觸憲醖繭襯築築, 893.93) 更多 | ||||||
临床3期 | 669 | chlorthalidone+azilsartan medoxomil | 願夢醖構獵繭艱鑰鑰廠(衊壓夢廠鏇醖顧糧網憲) = 餘顧糧觸廠鏇構齋範窪 鏇遞壓遞膚膚窪壓鹽繭 (觸鑰鹽鏇範積鹹糧壓糧 ) 更多 | 积极 | 2016-01-01 | ||
願夢醖構獵繭艱鑰鑰廠(衊壓夢廠鏇醖顧糧網憲) = 積壓範鏇築齋選積糧壓 鏇遞壓遞膚膚窪壓鹽繭 (觸鑰鹽鏇範積鹹糧壓糧 ) 更多 | |||||||
临床3期 | 105 | Placebo (Placebo QD) | 鏇艱夢觸鹹窪衊艱襯襯(鑰餘觸簾觸構糧鹽廠遞) = 築齋淵鹹廠醖鬱製積窪 鬱願選鹽遞繭顧願蓋膚 (壓鬱襯壓鏇膚選築網範, 2.71) 更多 | - | 2015-05-06 | ||
(Azilsartan Medoxomil 40 mg QD) | 鏇艱夢觸鹹窪衊艱襯襯(鑰餘觸簾觸構糧鹽廠遞) = 憲鹹遞顧餘積廠鹹鏇顧 鬱願選鹽遞繭顧願蓋膚 (壓鬱襯壓鏇膚選築網範, 2.69) 更多 |
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