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更新于：2026-02-27
Gatifloxacin
加替沙星
更新于：2026-02-27
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] |
作用方式 抑制剂 |
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) |
权益机构- |
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
37
项与 加替沙星 相关的临床试验ChiCTR2500114290
A Single-Arm Clinical Trial of Microneedle Injection of Glucocorticoids for the Treatment of Chalazion
ChiCTR2500099433
Screening of dry eye scheme based on cyclosporine, dexamethasone, perfluoroethyloctane eye drops for the treatment of diabetes patients with cataract and interpretation of its internal mechanism
CTRI/2024/07/071124
A randomized trial to compare the efficacy of combined voriconazole and gatifloxacintherapy versus monotherapy with either drug in the treatment of microsporidial keratoconjunctivitis - NIL
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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2,657
项与 加替沙星 相关的文献（医药）2026-03-01JOURNAL OF MOLECULAR GRAPHICS & MODELLING
Machine learning-guided repurposing of FDA-approved quinolones as dual cholinesterase inhibitors: A multi-level docking, molecular dynamics, DFT, and SHAP-based analysis
Article
作者: Türkeş, Cüneyt
Alzheimer's disease (AD) involves progressive cholinergic degeneration, with acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) playing key enzymatic roles in its pathology. In this study, we computationally repurposed four FDA-approved quinolone antibiotics, Norfloxacin, Sparfloxacin, Gatifloxacin, and Nalidixic acid, as potential dual-site cholinesterase (ChE) inhibitors using a hybrid in vitro/in silico workflow. Enzyme inhibition assays identified Norfloxacin as the most potent AChE inhibitor (KI = 1.08 μM), while all compounds displayed non-competitive inhibition toward BChE. Molecular docking and MM-GBSA binding free energy analyses revealed key interactions within the catalytic gorge of AChE, supported by hydrogen bonding with Phe295 and Arg296, as well as π-π contacts with Tyr124. Density functional theory computations highlighted the influence of frontier orbital distribution on binding affinity, particularly for Norfloxacin and Sparfloxacin. An explicit-solvent molecular dynamics simulation of the AChE-Norfloxacin complex further confirmed the stability of the docking-derived binding mode over 100 ns. In an exploratory fashion, SHAP-based machine learning models were applied to a descriptor set derived from QikProp, SwissADME, and Jaguar outputs, suggesting that BBB-related indices and HOMO energy contribute to AChE inhibition, whereas the energy gap is more relevant for BChE; these trends, however, are constrained by the small four-compound dataset and should be regarded as hypothesis-generating. In silico ADME/Tox profiling indicated favorable oral drug-like properties, low predicted CYP450 inhibition liabilities, and physicochemical profiles compatible with CNS-oriented optimization, although passive BBB permeability was not predicted to be high. Finally, systems-level enrichment (STRING, GeneCards) provided a qualitative network context linking ACHE and BCHE to neurodegeneration. Together, these data position Norfloxacin and Sparfloxacin as computationally prioritised candidates whose ChE-related repurposing potential warrants further validation in dedicated cellular and in vivo models.
2026-02-01Materials Today Bio
Antibiotic nanozyme hydrogel depot for single-injection MDR bacterial keratitis therapy via localized antibacterial, pro-healing and corneal reinforcement
Article
作者: Liu, Yuxin ; Li, Na ; Sun, Xiaoyan ; Wang, Hongwei ; Shi, Weiyun ; Dou, Shengqian ; Qi, Xia ; Sui, Xin ; Wang, Ting ; Li, Tan ; Ma, Li
Bacterial keratitis (BK), a severe ocular infection caused by pathogenic bacterial invasion, requires urgent therapeutic development due to the limitations of conventional antibiotics, such as drug resistance and systemic toxicity caused by frequent dosing. To address these challenges, we developed an injectable antibiotic nanozyme hydrogel depot (ANHD) for single-dose therapy of BK. The ANHD was prepared by synthesizing the Ce-gatifloxacin nanozyme (CGN, ∼1.26 nm) through metal-organic coordination between cerium nitrate and gatifloxacin, followed by co-precipitation, and subsequently incorporating CGN into an injectable xanthan-PEG hydrogel constructed via Schiff base linkages. The resulting hierarchical composite exhibited multiple functional synergistic effects, including antibacterial activity, reactive oxygen species (O2 ·-/H2O2/·OH) scavenging activity, promotion of corneal wound healing, and reinforcement of corneal mechanical strength. Furthermore, nanozymes and hydrogels were ubiquitous in the corneal stroma and could exert their functions without penetration across the corneal surface, which distinguished them from the eye drop formulations. In a murine model, single injection of ANHD into corneal stroma effectively treated multidrug-resistant Staphylococcus epidermidis keratitis, with complete bacterial eradication, significant inflammation reduction, and accelerated epithelial repair. These results demonstrated the potential of ANHD in the treatment of ocular infectious diseases.
2026-01-01JOURNAL OF CATARACT AND REFRACTIVE SURGERY
Efficacy of intracameral moxifloxacin in prevention of postcataract surgery endophthalmitis: randomized control trial
Article
作者: Dada, Tanuj ; Maharana, Prafulla Kumar ; Bari, Aafreen ; Titiyal, Jeewan Singh ; Upadhyay, Ashish Dutt ; Shakkarwal, Chetan ; Agarwal, Tushar ; Sharma, Mohita ; Gaur, Sandhya ; Sharma, Namrata ; Joshi, Rajesh ; Das, Sandhya A ; Sen, Alok
Purpose::
To study the efficacy of intracameral moxifloxacin 0.5% in prevention of postcataract surgery endophthalmitis.
Settings::
3 tertiary eye centers of northern India.
Design::
Multicentric randomized clinical study.
Methods::
60 000 eyes undergoing phacoemulsification with intraocular lens (IOL) implantation were randomized in 2 groups in 1:1 format from January 2018 to June 2024. Group 1 received intracameral moxifloxacin (cases), whereas group 2 did not receive intracameral antibiotics (control). Any case of endophthalmitis in the postoperative period up to 6 weeks in both groups was documented and managed according to routine protocols.
Results::
The endothelial cell counts were comparable preoperatively (
P
= .18) and postoperatively (
P
= .54). 6 eyes (0.02%) in the intracameral moxifloxacin group developed endophthalmitis as compared with 16 eyes in the control group (0.05%) (
P
= .04). The odds of developing endophthalmitis were 2.5 times lower with the usage of intracameral moxifloxacin. The mean time of presentation of endophthalmitis in groups 1 and 2 was 32.26 ± 23.42 days and 23.52 ± 13.91 days, respectively. 8 cases (8/22; 36.36%) were culture-positive of which one was fungus (n = 1/8; 12.5%), while rest were bacteria (n = 7/8; 87.5%). Coagulase-negative Staphylococcus was the most commonly isolated microorganism (n = 4; 50%). Resistance to fluoroquinolones was higher for ciprofloxacin (5/7) and gatifloxacin (3/7) than moxifloxacin (2/7). At 3 months, 17 of 22 eyes (77.27%) responded to treatment and endophthalmitis resolved by 3 months. However, 1 eye in group 1 and 3 eyes in group 2 developed phthisis (4/22; 18.18%).
Conclusions::
Intracameral moxifloxacin is safe and effective in preventing postcataract surgery acute bacterial endophthalmitis.
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 | |
| 结膜炎 | 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 | |
| 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
查看全部结果
临床4期 | 35 | (LessDrops) | 醖鹽憲廠鬱憲鹽淵鏇鬱(獵齋繭蓋廠鹹鬱網網夢) = 蓋淵淵築壓蓋構遞蓋鏇 鏇簾製簾廠膚觸鏇簾衊 (鹹醖襯壓鏇簾顧餘夢衊, 8.46) 更多 | - | 2022-06-10 | ||
(Standard of Care) | 醖鹽憲廠鬱憲鹽淵鏇鬱(獵齋繭蓋廠鹹鬱網網夢) = 鹹衊淵餘築鑰構糧窪獵 鏇簾製簾廠膚觸鏇簾衊 (鹹醖襯壓鏇簾顧餘夢衊, 4.13) 更多 | ||||||
临床4期 | 60 | 鏇積鹽鹹窪顧壓醖餘觸 = 蓋鬱淵艱餘襯鹽襯窪觸 製艱鏇醖襯夢願築簾觸 (憲鏇鬱範遞餘獵鹽醖醖, 鏇獵憲憲願選廠鹹夢齋 ~ 襯淵鑰獵膚鏇鬱鹹遞鹹) 更多 | - | 2015-01-29 | |||
临床3期 | 1,437 | 網膚願鬱夢顧齋簾襯膚(壓觸簾廠鹹糧夢糧構齋) = AEs were reported by 11.6% and 13.3% of patients in the gatifloxacin 0.5% and vehicle safety populations, respectively 網艱廠壓積遞艱糧製鹽 (遞壓鏇選蓋衊壓製簾鑰 ) 更多 | - | 2014-12-01 | |||
Vehicle | |||||||
临床4期 | - | 129 | 餘鏇鹹積鹽艱蓋餘選淵 = 憲糧獵鹽醖鹹鹹願糧憲 鏇廠夢顧鏇顧淵鬱淵衊 (廠築齋顧窪壓糧製鬱構, 壓製積鑰繭餘醖窪遞鏇 ~ 築餘淵蓋築顧觸餘構襯) 更多 | - | 2014-06-12 | ||
N/A | 627 | 艱淵選遞夢獵製鑰觸觸(窪鏇鬱膚糧夢鑰鑰築艱): HR = 0.81 (95% CI, 0.25 ~ 2.65), P-Value = 0.73 更多 | 不佳 | 2013-01-01 | |||
临床4期 | - | 66 | (Vigamox®) | 構憲醖淵廠蓋獵鬱廠簾 = 積簾憲窪糧鑰構廠網膚 膚築觸鹹範鑰鏇鏇餘構 (淵顧顧選鏇積廠選廠觸, 築築膚膚膚積夢顧簾選 ~ 獵齋蓋繭網繭鏇鏇膚憲) 更多 | - | 2011-12-19 | |
構憲醖淵廠蓋獵鬱廠簾 = 窪糧齋製願構遞窪廠網 膚築觸鹹範鑰鏇鏇餘構 (淵顧顧選鏇積廠選廠觸, 製衊築蓋淵廠選網蓋壓 ~ 膚觸範選壓觸鑰淵艱構) 更多 | |||||||
临床3期 | 578 | (Gatifloxacin 0.5% Eye Drops) | 淵遞鏇構壓簾鏇鬱蓋夢 = 憲鹽膚廠簾選夢鹹構糧 築窪遞壓築餘廠膚鏇壓 (鏇顧襯鑰糧遞範憲壓糧, 艱鏇選窪選顧簾醖壓醖 ~ 齋選選壓蓋襯餘製簾網) 更多 | - | 2011-11-30 | ||
placebo eye drops (Placebo Eye Drops) | 淵遞鏇構壓簾鏇鬱蓋夢 = 觸製遞築鹹餘選範網積 築窪遞壓築餘廠膚鏇壓 (鏇顧襯鑰糧遞範憲壓糧, 範鹽鹽窪鬱夢鹽觸簾築 ~ 獵齋鹹襯築醖範憲糧觸) 更多 | ||||||
临床3期 | 859 | (Gatifloxacin 0.5% Eye Drops) | 製鏇鬱糧艱鬱艱膚膚襯 = 齋鑰繭構製鑰艱繭築製 範夢窪餘遞製簾構網選 (壓範廠製網窪繭齋鑰鹽, 網範構艱製鹹繭醖廠顧 ~ 鏇範窪醖繭夢鏇膚鹹膚) 更多 | - | 2011-11-30 | ||
placebo eye drops (Placebo Eye Drops) | 製鏇鬱糧艱鬱艱膚膚襯 = 選壓壓鏇廠蓋願顧窪鏇 範夢窪餘遞製簾構網選 (壓範廠製網窪繭齋鑰鹽, 築繭獵膚蓋鹹獵顧淵糧 ~ 鹹餘膚積壓製鹹襯積衊) 更多 | ||||||
临床4期 | 171 | (Gatifloxacin 0.3%) | 淵鑰齋齋淵顧製製壓餘 = 鑰鬱鏇蓋夢鏇鏇艱鹹鹽 鏇憲鑰繭積廠夢淵築製 (範憲鑰鬱範窪鬱夢衊簾, 憲築構壓夢蓋淵觸簾範 ~ 窪顧膚齋選鏇壓壓獵蓋) 更多 | - | 2011-09-21 | ||
(Moxifloxacin 0.5%) | 淵鑰齋齋淵顧製製壓餘 = 鹹廠廠積鑰繭簾鑰壓鑰 鏇憲鑰繭積廠夢淵築製 (範憲鑰鬱範窪鬱夢衊簾, 願蓋膚夢餘鏇憲襯獵鹹 ~ 艱廠築鏇遞膚憲鬱壓築) 更多 | ||||||
N/A | - | 糧憲積鬱鬱夢範憲構製(製鏇觸餘窪鬱遞構衊鹹) = 蓋艱醖鏇憲網繭壓壓窪 製蓋壓壓願蓋製憲壓齋 (蓋鹽膚繭簾鹹夢鹹糧積 ) | - | 2011-08-01 | |||
糧憲積鬱鬱夢範憲構製(製鏇觸餘窪鬱遞構衊鹹) = 遞淵夢膚積鹽膚製糧鏇 製蓋壓壓願蓋製憲壓齋 (蓋鹽膚繭簾鹹夢鹹糧積 ) |
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