预约演示
更新于：2025-05-26
Amlodipine Besylate/Olmesartan Medoxomil
奥美沙坦酯氨氯地平
更新于：2025-05-26
概要
基本信息
药物类型 小分子化药 |
别名 Azor、Ol-Vamlo、Olmersartan medoxomil/amlodipine besilate + [6] |
作用方式 拮抗剂、阻滞剂 |
作用机制 AT1R拮抗剂(血管紧张素II-1型受体拮抗剂)、VDCCs阻滞剂(电压门控性钙通道复合体阻滞剂) |
治疗领域 |
非在研适应症- |
非在研机构- |
最高研发阶段批准上市 |
首次获批日期 美国 (2007-09-26), |
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C29H30N6O6 |
InChIKeyUQGKUQLKSCSZGY-UHFFFAOYSA-N |
CAS号144689-63-4 |
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关联
51
项与 奥美沙坦酯氨氯地平 相关的临床试验CTR20244099
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CTR20242179
健康成年受试者空腹和餐后单次口服奥美沙坦酯氨氯地平片的随机、开放、单剂量、两序列、两制剂、两周期、双交叉设计的生物等效性试验
100 项与 奥美沙坦酯氨氯地平 相关的临床结果
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100 项与 奥美沙坦酯氨氯地平 相关的转化医学
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100 项与 奥美沙坦酯氨氯地平 相关的专利（医药）
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23
项与 奥美沙坦酯氨氯地平 相关的文献（医药）2023-12-12ACS nano
Azo Reductase Activated Magnetic Resonance Tuning Probe with “Switch-On” Property for Specific and Sensitive Tumor Imaging in Vivo
Article
作者: Song, Yang ; Tan, Weihong ; Zhu, Xiaokang ; Li, Linyao ; Li, Yu ; Song, Erqun ; Deng, Siyu ; Gu, Peilin
Cancer remains a threat to human health. However, if tumors can be detected in the early stage, then the effectiveness of cancer treatment could be significantly improved. Therefore, it is worthwhile to develop more sensitive and accurate cancer diagnostic methods. Herein, we demonstrated an azo reductase (AzoR)-activated magnetic resonance tuning (MRET) probe with a "switch-on" property for specific and sensitive tumor imaging in vivo. Specifically, Gd-labeled DNA1 (DNA1-Gd) and cyclodextrin-coated magnetic nanoparticles (MNP-CD) were employed as enhancer and quencher of MRET, respectively, while DNA2, an azobenzene (Azo) group-modified aptamer (AS1411), served as a linker between enhancer and quencher to construct the MRET probe of MNP@DNA(1-2)-Gd. In tumor tissues with high-level AzoR, the T1-weighted magnetic resonance signal of the MRET probe could be restored by intelligently regulating the switch from "OFF" to "ON" after activation with AzoR, thus accurately indicating the location of the tumor accurately. Moreover, the tumor with a 4 times smaller size than that of the normal tumor model could be imaged based on the proposed MRET probe. The as-proposed MRET-based magnetic resonance imaging strategy not only achieves tumor imaging accurately but also shows promise for early diagnosis of tumors, which might improve patients' survival rates and provide an opportunity for image-guided biomedical applications in the future.
2023-12-01Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie
The enhancement effect of small molecule Lyb24 reveals AzoR as a novel target of polymyxin B
Article
作者: Huang, Wei ; Hu, Chunxia ; Wang, Xiao ; Zhou, Guibao ; Cheng, Shumin ; Liu, Shiyi ; Zou, Quanming ; Sun, Longqin ; Zhang, Jinyong ; Cui, Ruiqin ; Liu, Jianhua ; Li, Jingli ; Zhao, Yan ; Huang, Ying ; Zeng, Huan
Given the important role of polymyxin B (PB) in the treatment of drug-resistant Gram-negative bacterial infections, the emergence of PB resistance poses a serious threat to public health. Adjuvant development is a supplementary strategy that can compensate for the lack of novel antibiotics by protecting PB. In this study, we found a small molecule named Lyb24 that showed weak antibacterial activity (minimum inhibitory concentration ≥ 10 μg/ml) but potentiated and revitalized the efficacy of PB against Gram-negative pathogens, including mcr-1- and mgrB-deletion-mediated PB-resistant strains. Our results showed that Lyb24 inhibits the translational levels of genes associated with the modification of lipid A. In addition, Lyb24 increases the permeability, disrupts the integrity and induces the depolarization of the membrane. We further found that both Lyb24 and PB could directly bind to AzoR and inhibit its activity. Structural analysis showed that Lyb24 binds to the isoalloxazine ring of flavin mononucleotide (FMN) through pi-pi stacking and loop η4 of AzoR. A pneumonia model was used to confirm that the activity against clinical PB-resistant Klebsiella pneumoniae was enhanced due to Lyb24 on PB. In conclusion, we provide a potential therapeutic regimen by combining Lyb24 and PB to treat Gram-negative-resistant bacterial infections. Our findings not only explain the synergistic effect of Lyb24, but also expand our knowledge on the mechanism of action of PB.
2021-08-12The Journal of antimicrobial chemotherapy2区 · 医学
Role of AzoR, a LysR-type transcriptional regulator, in SmeVWX pump-mediated antibiotic resistance in Stenotrophomonas maltophilia
2区 · 医学
Article
作者: Lin, Yi-Tsung ; Yang, Tsuey-Ching ; Tsai, Yu-Chieh ; Li, Li-Hua ; Lu, Hsu-Feng
Abstract:
Background:
The SmeVWX efflux pump of Stenotrophomonas maltophilia contributes to menadione (MD) tolerance and resistance to chloramphenicol, quinolones and tetracycline. The components of the SmeVWX efflux pump are encoded by a five-gene operon, smeU1VWU2X. We have previously demonstrated that the smeU1VWU2X operon is intrinsically unexpressed and inducibly expressed by MD via a SoxR- and SmeRv-involved regulatory circuit in S. maltophilia KJ. We also inferred that there should be other regulator(s) involved in MD-mediated smeU1VWU2X expression in addition to SoxR and SmeRv.
Objectives:
To identify novel regulator(s) involved in the regulation of MD-mediated smeU1VWU2X expression and elucidate the regulatory circuit.
Methods:
A possible regulator candidate involved in the regulation of MD-mediated smeU1VWU2X expression was identified by a homologue search using the helix-turn-helix domain of SmeRv as a query. Gene expression was assessed using the promoter-xylE transcriptional fusion assay and quantitative RT–PCR. The impact of the regulator on SmeVWX pump-mediated functions was investigated via mutant construction and functional tests (antibiotic susceptibility and MD tolerance).
Results:
AzoR (Smlt3089), a LysR-type transcriptional regulator, was investigated. In unstressed logarithmically grown cells, AzoR was abundantly expressed and functioned as a repressor, inhibiting the expression of the smeU1VWU2X operon. MD challenge attenuated azoR expression, thus derepressing the expression of the smeU1VWU2X operon in S. maltophilia KJ. AzoR down-regulation-mediated smeU1VWU2X expression was observed in quinolone-resistant and SmeVWX-overexpressing S. maltophilia clinical isolates.
Conclusions:
AzoR negatively regulates the expression of the smeU1VWU2X operon and SmeVWX pump-mediated antibiotic resistance in S. maltophilia.
100 项与 奥美沙坦酯氨氯地平 相关的药物交易
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研发状态
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 | 中国 | 2018-07-12 | |
| 高血压 | 美国 | 2007-09-26 |
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临床结果
临床结果
适应症
分期
评价
查看全部结果
临床4期 | 600 | Olmesartan/Amlodipine 40/10 mg | 糧繭憲膚壓願積築衊觸(鏇繭顧襯艱製餘範簾膚) = 鹹膚窪窪鬱繭蓋顧積構 齋餘繭糧襯醖醖製鏇憲 (餘夢簾構製廠淵製鹹製 ) 更多 | 积极 | 2013-12-01 | ||
Perindopril/Amlodipine 8/10 mg | 糧繭憲膚壓願積築衊觸(鏇繭顧襯艱製餘範簾膚) = 衊築鑰襯鑰獵獵醖淵齋 齋餘繭糧襯醖醖製鏇憲 (餘夢簾構製廠淵製鹹製 ) 更多 | ||||||
N/A | 292 | 鹽齋築製範繭夢艱窪獵(鹽壓顧繭衊鏇淵糧鬱窪) = Incidence of study drug related adverse events was comparable in monotherapy and combination therapy group (2.77% vs 2.17%) 鏇網網繭繭範衊鬱鏇範 (餘積鏇構憲製範憲糧糧 ) | 积极 | 2012-09-01 | |||
临床3期 | 2,204 | (Olmesartan(OLM) 40 Mg-Amlodipine(AML) 10 mg) | 構襯願網構範鹹網廠淵(製膚憲夢窪觸醖顧鹹遞) = 糧餘衊淵艱窪糧構齋齋 築鑰簾觸願壓齋糧顧壓 (餘鏇網鹽壓鹹糧鑰願願, 0.55) 更多 | - | 2011-11-22 | ||
(OLM 40-AML 10-Hydrochlorothiazide (HCTZ) 12.5) | 構襯願網構範鹹網廠淵(製膚憲夢窪觸醖顧鹹遞) = 獵網衊觸網鑰餘鹽繭製 築鑰簾觸願壓齋糧顧壓 (餘鏇網鹽壓鹹糧鑰願願, 0.55) 更多 | ||||||
临床4期 | 999 | Hydrochlorothiazide+Amlodipine+Olmesartan Medoxomil | 範齋範鹽壓遞鏇衊築範 = 構簾鹹壓醖網鑰網膚繭 齋範淵製醖憲餘觸觸餘 (廠構鬱鑰網選網憲餘廠, 鏇遞齋鑰艱構夢膚廠蓋 ~ 製糧廠網構觸壓鹽膚遞) 更多 | - | 2010-09-29 | ||
临床4期 | 207 | 齋鬱觸艱觸鏇夢鑰夢顧(襯觸網網鑰艱繭獵艱夢) = 簾糧鬱積淵積構艱憲淵 獵齋糧築網獵網願鹹襯 (製簾簾壓鏇壓鑰顧醖獵, 0.76) 更多 | - | 2010-07-02 |
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