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更新于：2025-01-25
Gatifloxacin
加替沙星
更新于：2025-01-25
概要
基本信息
药物类型 小分子化药 |
别名 1-cyclopropyl-6-fluoro- 8-methoxy-7-(3-methylpiperazin-1-yl)- 4-oxo-quinoline-3-carboxylic acid、Bonoq、Bonoq Uro + [99] |
作用机制 Bacterial DNA gyrase 抑制剂(细菌DNA旋转酶 抑制剂)、Bacterial top IV抑制剂(细菌拓扑异构酶IV抑制剂) |
最高研发阶段批准上市 |
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C38H50F2N6O11 |
InChIKeyRMJMZKDEVNTXHE-UHFFFAOYSA-N |
CAS号180200-66-2 |
关联
36
项与 加替沙星 相关的临床试验NCT03578276
Lessdrops™ Prophylactic Treatment After Routine Phacoemulsification Compared to Standard Drops Regimen
CTRI/2015/05/005781
Evaluation of efficacy of gatifloxacin (0.3%) in the treatment of non-perforated bacterial corneal ulcers
CTR20150066
加替沙星治疗化脓性中耳炎、中耳胆脂瘤和外耳道炎随机、单盲、阳性药平行对照并剂量探索、多中心Ⅱ期试验
100 项与 加替沙星 相关的临床结果
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100 项与 加替沙星 相关的转化医学
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100 项与 加替沙星 相关的专利（医药）
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3,836
项与 加替沙星 相关的文献（医药）2025-05-01SEPARATION AND PURIFICATION TECHNOLOGY
Radical to non-radical conversion during PMS activation triggered by optimized electronic structure: Orientational regulation of oxidation pathway for water remediation
作者: Chai, Hongxiang ; Chang, Lian ; Tan, Jianke ; Huang, Yuming ; Zhang, Xiaodan
The orientational regulation of non-radical pathways is significant in the peroxymonosulfate (PMS)-based AOP for practical potential, but remains challenge.Here, the Se-doped Co(OH)2 hollow spheres (CoHS-Se-CR) were designed for PMS activation to rapidly degrade gatifloxacin (GAT) antibiotic, with over 95% GAT removal in 20 min.DFT and exptl. trials reveal the downshift of d-band center of Co 3d and O-H bond stretch in PMS via Se doping of Co(OH)2.The active HSO.-5 generated via the breaking of O-H bond triggers the radical to the non-radical conversion of the degradation mechanism, dominated by 1O2 and assisted by electron transport process.Both oxygen vacancy and Se(VI) were involved in 1O2 generation and Co(III)/Co(II) cycle.The CoHS-Se-CR/PMS system showed high efficiency for GAT removal in a wide pH range and strong resistance to anionic interference.This work provides a new strategy for designing PMS activators to construct orientational non-radical AOP.
2025-02-01JOURNAL OF MOLECULAR STRUCTURE
Directed self-assembly with salicylic acid provides new crystalline complexes for fluoroquinolone antimicrobials to improve drug properties and synergies: Theoretical and experimental integration research
作者: Shang-Guan, Xiang-Le ; Zhao, Zhi-Long ; Zhang, Chun ; Li, Ze ; Huang, Yun-Jing ; Zhang, Jie ; Tian, Su-Yan ; Bai, Run-Chao ; Chen, Xiang-Zhu ; Wang, Shuai
To improve the physicochem. characteristics of gatifloxacin (GAT) and refine its antibacterial efficacy, a novel crystalline mol. complex combining GAT with salicylic acid (SAL), namely GAT-SAL has been successfully synthesized.Precise salt structure revealed by single crystal X-ray diffraction displayed that the entry of SAL into the GAT lattice destroyed the zwitterionic structure of GAT itself, resulting in the formation of a tetramer structure between GAT and SLA mols., thus laying a foundation for improving the physicochem. properties of GAT.The pharmaceutical research indicated that the mol. salt exhibited concurrent enhancements in both solubility and permeability surpassing the parent drug gatifloxacin.Notably, the refined physicochem. attributes bestow GAT-SAL with heightened in vitro antibacterial potency, showing larger inhibition rings and smaller MIC values.These observations can be supported by theor. studies involving theor. research based on d. functional theory (DFT) , Hirshfeld surfaces and mol. docking.The present contribution emphasizes the effectiveness of combining theory and experiment to solve the GAT problem by means of the cocrystn. approach, thus providing the new idea for the rapid screening of novel antimicrobial agents.
2025-02-01JOURNAL OF MOLECULAR STRUCTURE
Dual drug molecular salt of antibacterial: Formulation, physicochemical properties study, theoretical calculations and evaluation of antibacterial activity
作者: Song, Yu-Wei ; Zhao, Zhi-Long ; Liu, Lu ; Elmidaoui, Roudaina ; Zhang, Chun ; Li, Hai-Gang ; Zhu, Xin-Ru ; Zhang, Tong-Tong ; Bai, Run-Chao ; Wang, Shuai ; Ge, Zhao-Hui
A mol. salt combined with the fluoroquinolone antibacterial gatifloxacin (GAT) and the sulfonamides antibacterial sulfamerazine (SMZ) is designed and synthesized successfully, which is the first report of the dual-drug cocrystn. of gatifloxacin.The precise structure of the acquired mol. salt GAT-SMZ has been characterized via single crystal X-ray diffraction and other techniques.Single crystal diffraction anal. displays that due to the transfer of protons from SMZ to GAT, the mol. salt of GAT-SMZ is formed, and the supramol. network is dominated by charge-assisted one-dimensional hydrogen bond chain and two-dimensional accumulation layer in the crystal.Such structural feature endows mol. salt with superior physicochem. properties, including enhanced solubility and permeability.More importantly, the superior pharmaceutical performances of the dual-drug salt resulted in enhanced antibacterial activity against the tested strains.These observations are strongly supported by theor. studies based on Hirshfeld surface and mol. docking analyses.Thus, this contribution not only highlights the validity of combining theory with experiment to drive the problem of physicochem. properties of drugs through co-crystallization methods, but also fills in the previous studies gatifloxacin dual-drug salt synergistic antibacterial research blank.
100 项与 加替沙星 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 |
|---|---|---|---|
| 睑缘炎 | 日本 | 2004-09-07 | |
| 角膜溃疡 | 日本 | 2004-09-07 | |
| 泪囊炎 | 日本 | 2004-09-07 | |
| 睑腺炎 | 日本 | 2004-09-07 | |
| 结膜炎 | 巴西 | - | 2004-03-27 |
| 细菌性结膜炎 | 美国 | 2003-03-28 | |
| 感染 | 中国 | 2002-10-29 | |
| 急性细菌性支气管炎 | 美国 | 1999-12-17 | |
| 急性鼻窦炎 | 美国 | 1999-12-17 | |
| 慢性支气管炎 | 美国 | 1999-12-17 | |
| 社区获得性肺炎 | 美国 | 1999-12-17 | |
| 淋病 | 美国 | 1999-12-17 | |
| 肾盂肾炎 | 美国 | 1999-12-17 | |
| 泌尿道感染 | 美国 | 1999-12-17 |
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 |
|---|---|---|---|---|
| 中耳炎 | 临床3期 | 美国 | - | |
| 中耳胆脂瘤 | 临床2期 | 中国 | - | 2013-10-08 |
| 外耳炎 | 临床2期 | 中国 | - | 2013-10-08 |
| 化脓性中耳炎 | 临床2期 | 中国 | - | 2013-10-08 |
| 细菌性角膜炎 | 临床2期 | 美国 | 2003-10-01 | |
| 细菌性角膜炎 | 临床2期 | 印度 | 2003-10-01 | |
| 炎症 | 临床1期 | - | - | 2013-10-08 |
| 炭疽 | 临床前 | 美国 | - |
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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4期 | 35 | (LessDrops) | 鑰鏇範遞願壓襯簾簾夢(鬱構膚鹹膚築壓鏇憲壓) = 壓蓋鹽淵範繭簾糧顧夢 膚衊顧夢廠夢衊構淵簾 (顧顧衊網窪蓋簾艱糧製, 窪膚衊願鹽餘憲膚膚選 ~ 膚繭獵願築鬱選壓餘簾) 更多 | - | 2022-06-10 | ||
鑰鏇範遞願壓襯簾簾夢(鬱構膚鹹膚築壓鏇憲壓) = 築淵鏇簾廠網窪網齋壓 膚衊顧夢廠夢衊構淵簾 (顧顧衊網窪蓋簾艱糧製, 遞壓壓淵衊衊淵遞襯遞 ~ 觸構觸鹽艱繭觸衊鑰簾) 更多 | |||||||
临床3期 | - | (Standard 6-month treatment) | 簾醖壓觸獵淵夢襯餘顧(廠淵淵齋夢鏇憲襯積築) = 膚夢窪窪夢淵繭製蓋淵 淵餘獵積憲壓淵膚鏇廠 (憲艱衊鬱齋壓積構憲選 ) 更多 | - | 2017-07-01 | ||
Test regimen with gatifloxacin, rifampin, and isoniazid | 簾醖壓觸獵淵夢襯餘顧(廠淵淵齋夢鏇憲襯積築) = 鹹簾廠膚壓遞選夢構糧 淵餘獵積憲壓淵膚鏇廠 (憲艱衊鬱齋壓積構憲選 ) 更多 | ||||||
N/A | - | 願選夢齋觸醖糧襯構蓋(鏇蓋願窪餘蓋窪獵鑰網) = 願築艱願淵鑰醖憲憲顧 鬱範衊壓餘網衊範蓋淵 (壓蓋淵鑰憲繭顧繭繭糧, 0.02) | - | 2015-11-15 | |||
Polymyxin-trimethoprim | 願選夢齋觸醖糧襯構蓋(鏇蓋願窪餘蓋窪獵鑰網) = 夢鑰繭範醖齋齋艱選艱 鬱範衊壓餘網衊範蓋淵 (壓蓋淵鑰憲繭顧繭繭糧, 0.02) | ||||||
N/A | - | - | 夢窪顧艱艱膚繭餘襯鬱(餘蓋壓顧觸壓壓構簾願) = 餘鏇醖醖觸選繭選製壓 壓製顧襯蓋構艱窪構憲 (繭廠製構顧齋遞襯襯築 ) | - | 2015-06-01 | ||
临床4期 | 60 | 鹽觸鑰鹽衊顧憲夢窪衊(獵餘簾鑰範襯選範鑰繭) = 製襯鬱齋廠願艱齋網憲 鏇襯壓夢遞醖鹹蓋窪繭 (觸壓繭觸網齋觸憲鹹網, 艱窪鑰繭糧選製鬱範齋 ~ 窪蓋廠窪鏇壓鬱獵網廠) 更多 | - | 2015-01-29 | |||
临床3期 | 1,437 | 醖觸獵願淵遞壓構顧觸(鬱壓鹹憲積襯壓餘鬱衊) = AEs were reported by 11.6% and 13.3% of patients in the gatifloxacin 0.5% and vehicle safety populations, respectively 簾鏇觸齋廠觸構顧獵遞 (蓋願願蓋鏇選網鹹鬱淵 ) 更多 | - | 2014-12-01 | |||
Vehicle | |||||||
临床3期 | 1,836 | 4-month gatifloxacin-containing regimen | 窪糧築網網築艱憲觸觸(淵蓋膚鏇壓膚淵膚築糧) = 觸糧遞製淵餘蓋憲窪範 顧窪醖獵襯積築膚糧獵 (鏇齋膚夢壓選膚鏇廠簾 ) 更多 | 不佳 | 2014-10-23 | ||
standard regimen | 窪糧築網網築艱憲觸觸(淵蓋膚鏇壓膚淵膚築糧) = 壓願鬱網鏇願鏇鑰鏇獵 顧窪醖獵襯積築膚糧獵 (鏇齋膚夢壓選膚鏇廠簾 ) 更多 | ||||||
临床4期 | - | 129 | 艱遞鏇窪膚鏇壓築襯願(膚製鏇衊獵廠淵顧憲廠) = 鹽製齋餘醖窪選鏇鹽衊 願衊願積鹽艱觸選壓窪 (淵觸膚築憲願築鑰鏇網, 製鏇鹽糧鬱憲積鏇範願 ~ 蓋繭構廠淵廠淵願製憲) 更多 | - | 2014-06-12 | ||
临床3期 | 169 | 糧糧簾餘網膚簾網憲糧(網衊壓築獵獵鹽淵夢遞) = 獵膚觸製選獵鑰衊顧襯 壓淵選選鑰選製鹹遞積 (顧獵獵鏇顧淵製糧膚積, -90.5% ~ +61.5%) | - | 2013-09-01 | |||
N/A | 627 | 衊鑰繭膚遞夢鹽遞顧範(鏇繭選製築簾蓋醖製衊): HR = 0.81 (95% CI, 0.25 ~ 2.65), P-Value = 0.73 更多 | 不佳 | 2013-01-01 | |||
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