更新于：2024-09-06
Sitafloxacin Hydrate
西他沙星
更新于：2024-09-06
概要
基本信息
非在研机构 |
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
50
项与 西他沙星 相关的临床试验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
A Multicenter, Randomized, Open-Label, Parallel-Controlled Clinical Study to Evaluate the Efficacy and Safety of Sitafloxacin in Adult Subjects With Acute Exacerbation of Chronic Obstructive Pulmonary Disease
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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369
项与 西他沙星 相关的文献（医药）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.
2023-11-01Heliyon
Comparison of the in vitro antibacterial activity of ofloxacin, levofloxacin, moxifloxacin, sitafloxacin, finafloxacin, and delafloxacin against Mycobacterium tuberculosis strains isolated in China
Article
作者: Geng, Zhi ; Gu, Yuzhen ; Qi, Zhenyan ; Huang, Hairong ; Jiang, Xiaoyi ; Kong, Yaoyao ; Yu, Xia ; Chu, Naihui ; Jiang, Guanglu ; Wang, Fen ; Jia, Junnan
Objective:
The resistance of Mycobacterium tuberculosis (Mtb) to currently available fluoroquinolones (FQs), namely ofloxacin (OFX), levofloxacin (LFX), and moxifloxacin (MFX), renders the treatment of TB infections less successful. In this study, we aimed to evaluate the susceptibility and intracellular killing assay of Mtb to next-generation FQs in vitro and determine the correlation of FQs resistance and newly detected mutations in gyrB by molecular docking.
Methods:
Antimicrobial susceptibility test was performed to determine the minimum inhibitory concentrations (MICs) of six FQs, including currently available FQs (OFX, LFX, and MFX) and next-generation FQs, i.e., sitafloxacin (SFX), finafloxacin (FIN) and delafloxacin (DFX) against Mtb clinical isolates obtained in 2015 and 2022, respectively. Quinolone-resistance-determining regions of gyrA and gyrB were subjected to DNA sequencing and the correlation of FQs resistance and new mutations in gyrB were determined by molecular docking. Furthermore, the intracellular antibacterial activity of the six FQs against Mtb H37Rv in THP-1 cells was evaluated.
Results:
SFX exhibited the highest antibacterial activity against Mtb isolates (MIC90 = 0.25 μg/mL), whereas DFX and OFX exhibited comparable activity (MIC90 = 8 μg/mL). A statistically significant difference was observed among the MICs of the new generation FQs (SFX, P = 0.002; DFX, P = 0.008). Additionally, a marked increase in MICs was found in strains isolated in 2022 compared with those isolated in 2015. There might be correlation between FQs resistance and mutations in gyrB G520T and G520A. Cross-resistance rate between SFX and MFX was 40.6 % (26/64). At a concentration of 1 μg/mL, SFX exhibited high intracellular antibacterial activity (96.6 % ± 1.5 %) against the Mtb H37Rv, comparable with that of MFX at a concentration of 2 μg/mL.
Conclusion:
SFX exhibits the highest inhibitory activity against Mtb in vitro and THP-1 cell lines, which exhibits partial-cross resistance with MFX. There might be correlation between FQs resistance and mutations in gyrB G520T and G520A.Our findings provide crucial insights into the potential clinical application of SFX and DFX in the treatment of Mtb infections.
2023-08-15Internal medicine (Tokyo, Japan)
A Vonoprazan, Clarithromycin, and Metronidazole Regimen as <i>Helicobacter pylori</i> Eradication Therapy for Patients with Penicillin Allergy in Light of Clarithromycin Resistance
Article
作者: Kasugai, Kunio ; Izawa, Shinya ; Nagao, Kazuhiro ; Yoshimine, Takashi ; Sasaki, Makoto ; Kato, Shunsuke ; Adachi, Kazunori ; Funaki, Yasushi ; Koshino, Akira ; Yamaguchi, Yoshiharu ; Ohashi, Wataru ; Ogasawara, Naotaka ; Sugiyama, Tomoya ; Ebi, Masahide
Objective Vonoprazan (VPZ), clarithromycin (CAM), metronidazole (MNZ) and VPZ, MNZ, and sitafloxacin (STFX) regimen are all established Helicobacter pylori eradication therapies for patients with penicillin allergy in Japan. However, no study has assessed the efficacy of a VPZ, CAM, and MNZ (VCM) regimen in patients with clarithromycin resistance (CAM-R). We therefore assessed the efficacy of a VCM regimen for treating H. pylori infection in patients with CAM-R and penicillin allergy. Methods Fifty-three patients with penicillin allergy who received H. pylori eradication therapy were retrospectively analyzed. Eight patients received a 7-day proton-pump inhibitor, CAM, and MNZ (PCM) regimen; 35 patients [11 CAM-R, and 10 with clarithromycin sensitivity (CAM-S)] received 7-day VCM regimens; and 10 patients received 7-day VPZ, MNZ, and STFX (VMS) regimens. A 13C-urea breath test was used to determine eradication. The efficacy of eradication was evaluated via both intention-to-treat (ITT) and per-protocol (PP) analyses. Results According to ITT and PP analyses, eradication rates (ERs) with PCM, VCM, and VMS therapies were 50.0% and 50.0%, 94.3% and 100%, and 90% and 90%, respectively. Treatment was successful in all patients with CAM-S. For patients with CAM-R, treatment was successful in 10 patients, and 1 patient discontinued treatment owing to an adverse event. According to ITT and PP analyses, ERs were 90.9% and 100% in CAM-R, and were 100% and 100% in CAM-S, respectively. Conclusion The VCM regimen for H. pylori eradication may be a viable candidate therapy for patients with penicillin allergy, regardless of CAM-R.
100 项与 西他沙星 相关的药物交易
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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 |
未上市
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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 | |
| 扁桃体炎 | 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 | |
| 慢性阻塞性肺疾病 | 临床3期 | 中国 | 2015-10-23 | |
| 肾盂肾炎 | 临床3期 | 中国 | 2015-10-23 |
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N/A | 114 | 製鹹廠範製餘淵範選鹹(蓋鹽繭淵鏇構範衊蓋餘) = 鹹選製鏇艱選鹹糧蓋構 繭衊選壓鬱築願積鹹蓋 (製糧膚獵築製蓋構構衊 ) | - | 2022-01-01 | |||
N/A | 感染 维持 | - | 鹽獵壓壓糧鬱膚鬱襯膚(齋鹹壓糧齋鏇襯醖壓築) = 鏇壓製鬱鏇艱遞繭願艱 鏇淵選蓋蓋鏇窪鑰淵範 (鹹餘顧蓋餘願鬱選選壓 ) 更多 | 积极 | 2012-10-30 | ||
鹽獵壓壓糧鬱膚鬱襯膚(齋鹹壓糧齋鏇襯醖壓築) = 觸廠齋蓋網蓋壓衊衊製 鏇淵選蓋蓋鏇窪鑰淵範 (鹹餘顧蓋餘願鬱選選壓 ) 更多 |
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