更新于：2024-12-06
Sitafloxacin Hydrate
西他沙星
更新于：2024-12-06
概要
基本信息
最高研发阶段批准上市 |
最高研发阶段(中国)批准上市 |
特殊审评优先审评 (中国) |
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结构
分子式C38H42Cl2F4N6O9 |
InChIKeyMPORYQCGWFQFLA-ONPDANIMSA-N |
CAS号163253-35-8 |
关联
52
项与 西他沙星 相关的临床试验Ultra-short treatment by advancing new regimens based on sitafloxacin and pyrazinamide for drug-susceptible pulmonary tuberculosis (UltraStar-SZ): A multi-arm, multi-stage, adaptive, multi-centre, randomised, controlled, open-label, non-inferiority trial
浙江麒正药业有限公司研制的西他沙星片与持证商为Daiichi Sankyo Co., Ltd的西他沙星片（商品名：格雷必妥®/GRACEVIT®）在中国健康受试者中进行的随机、开放、单剂量、两周期、双交叉、空腹及餐后状态下的生物等效性研究
A Randomized Controlled Non-Inferiority Study for Shortening Tuberculosis Treatment With Sitafloxacin-Containing Regimens
100 项与 西他沙星 相关的临床结果
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100 项与 西他沙星 相关的转化医学
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100 项与 西他沙星 相关的专利（医药）
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381
项与 西他沙星 相关的文献（医药）2024-07-19JOURNAL OF MEDICAL MICROBIOLOGY
New generation fluoroquinolone sitafloxacin could potentially overcome the majority levofloxacin and moxifloxacin resistance in multidrug-resistant Mycobacterium tuberculosis
Article
作者: Wang, Fen ; Dong, Lingling ; Cheng, Kai ; Sun, Qing ; Yan, Jun ; Jiang, Guanglu ; Zhao, Weijie ; Guo, Zhenyong ; Wang, Guirong ; Huang, Hairong ; Wang, Chaohong ; Liao, Xinlei ; Wang, Chenqian
Introduction. Pre-existing fluoroquinolones (FQs) resistance is a major threat in treating multidrug-resistant (MDR) tuberculosis. Sitafloxacin (Sfx) is a new broad-spectrum FQ.Hypothesis. Sfx is more active against drug-resistant Mycobacterium tuberculosis (Mtb) isolates.Aim. To determine whether there is cross-resistance between Sfx and ofloxacin (Ofx), levofloxacin (Lfx) and moxifloxacin (Mfx) in MDR Mtb.Methods. A total of 106 clinical Mtb isolates, including 23 pan-susceptible and 83 MDR strains, were analysed for Sfx, Lfx and Mfx resistance using MIC assay. The isolates were also subjected to whole-genome sequencing to analyse drug-resistant genes.Results. Sfx exhibited the most robust inhibition activity against Mtb clinical isolates, with a MIC50 of 0.0313 µg ml−1 and MIC90 of 0.125 µg ml−1, which was lower than that of Mfx (MIC50 = 0.0625 µg ml−1, MIC90 = 1 µg ml−1) and Lfx (MIC50 = 0.125 µg ml−1, MIC90 = 2 µg ml−1). We determined the tentative epidemiological cut-off values as 0.5 µg ml−1 for Sfx. Also, 8.43% (7/83), 43.37% (36/83), 42.17% (35/83) and 51.81% (43/83) MDR strains were resistant to Sfx, Mfx, Lfx and Ofx, respectively. Cross-resistance between Ofx, Lfx and Mfx was 80.43% (37/46). Only 15.22% (7/46) of the pre-existing FQs resistance isolates were resistant to Sfx. Among the 30 isolates with mutations in gyrA or gyrB, 5 (16.67%) were Sfx resistant. The combination of Sfx and rifampicin could exert partial synergistic effects, and no antagonism between Sfx and six clinically important anti-Mtb antibiotics was evident.Conclusion. Sfx exhibited superior activity against MDR isolates comparing to Lfx and Mfx, and could potentially overcome the majority pre-existing FQs resistance in Mtb strains.
2024-04-01Environmental microbiology reports
Construction of a versatile in vitro cultivation screening platform using human oral microbiota
Article
作者: Sasaki, Kengo ; Kondo, Akihiko ; Kimoto, Akira ; Okumura, Ryo ; Akashi, Masaya ; Sasaki, Daisuke ; Yamashita, Junya ; Fujino, Ayami ; Takeshima, Yasunobu
Abstract:
We developed a simulation model of human oral microbiota using Bio Palette oral medium (BPOM) containing 0.02% glucose and lower bacterial nitrogen sources, derived from saliva and dental plaque. By decreasing the concentration of Gifu anaerobic medium (GAM) from 30 to 10 g L−1, we observed increased ratios of target pathogenic genera, Porphyromonas and Fusobacterium from 0.5% and 1.7% to 1.2% and 3.5%, respectively, in the biofilm on hydroxyapatite (HA) discs. BPOM exhibited the higher ratios of Porphyromonas and Fusobacterium, and amplicon sequence variant number on HA, compared with GAM, modified GAM and basal medium mucin. Mixing glycerol stocks of BPOM culture solutions from four human subjects resulted in comparable ratios of these bacteria to the original saliva. In this simulation model, sitafloxacin showed higher inhibitory effects on P. gingivalis than minocycline hydrochloride at a low dosage of 0.1 μg mL−1. Probiotics such as Streptococcus salivarius and Limosilactobacillus fermentum also showed significant decreases in Porphyromonas and Fusobacterium ratios on HA, respectively. Overall, the study suggests that BPOM with low carbon and nutrients could be a versatile platform for assessing the efficacy of antibiotics and live biotherapeutics in treating oral diseases caused by Porphyromonas and Fusobacterium.
2023-12-01Open forum infectious diseases
Efficacy of Sitafloxacin for Mycoplasma genitalium in an Era of Increasing Antimicrobial Resistance
Article
作者: Aguirre, Ivette ; Bradshaw, Catriona S ; Clarke, Emily J ; Plummer, Erica L ; Samra, Ranjit S ; Chow, Eric P F ; Fairley, Christopher K ; Vodstrcil, Lenka A
Abstract:
Antimicrobial resistance in Mycoplasma genitalium is rising globally and antimicrobial options are limited. We evaluated the efficacy of sitafloxacin regimens for macrolide-resistant M genitalium at Melbourne Sexual Health Centre, Australia, between January 2017 and February 2022. Before June 2017, patients received doxycycline followed by sitafloxacin; subsequently, patients received doxycycline followed by combined doxycycline + sitafloxacin. Of 229 patients treated with a sitafloxacin regimen, 80.6% experienced microbial cure. Sitafloxacin cured 94.2% of infections that had not previously failed moxifloxacin and 69.5% of infections that had; prior failure of moxifloxacin was associated with an 8-fold odds of sitafloxacin failure. There was no difference in cure between sequential monotherapy and combination therapy when patients were stratified by past failure of moxifloxacin (P > .05); however, small numbers limited comparisons. Sitafloxacin was well tolerated and still achieved 70% cure in patients in whom moxifloxacin had failed. These data highlight the benefit of incorporating relevant fluoroquinolone resistance markers into assays to assist clinical decision making.
100 项与 西他沙星 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 |
|---|---|---|---|
| 细菌感染 | 日本 | 2008-06-02 | |
| 牙龈炎 | 日本 | 2008-01-25 | |
| 感染 | 日本 | 2008-01-25 | |
| 呼吸道感染 | 日本 | 2008-01-25 | |
| 泌尿道感染 | 日本 | 2008-01-25 |
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| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| 慢性支气管炎 | 临床3期 | 中国 | 2017-06-26 | |
| 社区获得性感染 | 临床3期 | 中国 | 2017-06-26 | |
| 急性支气管炎 | 临床3期 | 中国 | 2015-10-23 | |
| 急性咽炎 | 临床3期 | 中国 | 2015-10-23 | |
| 急性扁桃体炎 | 临床3期 | 中国 | 2015-10-23 | |
| 社区获得性肺炎 | 临床3期 | 中国 | 2015-10-23 | |
| 膀胱炎 | 临床3期 | 中国 | 2015-10-23 | |
| 肾盂肾炎 | 临床3期 | 中国 | 2015-10-23 | |
| 尿道炎 | 临床3期 | 中国 | 2015-10-23 | |
| 急性尿路感染 | 临床3期 | 中国 | 2012-12-08 |
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临床结果
临床结果
适应症
分期
评价
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N/A | 114 | 鏇醖範餘窪夢鑰窪糧憲(蓋衊願製襯廠壓壓鬱壓) = 積鬱鬱範廠餘餘襯構製 鑰鹽齋範繭鹹醖積網簾 (範構觸鏇選餘窪構願夢 ) | - | 2022-01-01 | |||
N/A | 一线 | 二线 | 三线 | 180 | Sitafloxacin-based regimen | 鹹觸範顧夢蓋糧鏇齋鏇(網鬱廠製獵壓簾鏇壓簾) = one patient experienced appearance of nettle rash/hives and dropped out from this study 積壓遞鬱願夢遞網選製 (淵壓淵鑰憲糧繭壓憲簾 ) | 积极 | 2015-10-01 | |
N/A | 感染 维持 | - | 廠繭積遞淵膚廠夢夢觸(憲襯顧顧淵窪顧衊蓋鑰) = 觸鏇築選蓋製蓋醖淵簾 鑰鬱窪構齋鏇襯築鹹淵 (廠積觸獵簾憲蓋網簾醖 ) 更多 | 积极 | 2012-10-30 | ||
廠繭積遞淵膚廠夢夢觸(憲襯顧顧淵窪顧衊蓋鑰) = 艱艱蓋鏇製夢選鹽壓餘 鑰鬱窪構齋鏇襯築鹹淵 (廠積觸獵簾憲蓋網簾醖 ) 更多 |
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