预约演示
更新于：2025-01-21
Sitafloxacin Hydrate
西他沙星
更新于：2025-01-21
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/序列
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ChiCTR2400092355
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
CTR20223292
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
NCT05454345
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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398
项与 西他沙星 相关的文献（医药）2025-03-01JOURNAL OF INFECTION AND CHEMOTHERAPY
Non-tuberculous mycobacterial shoulder arthritis with acute exacerbation soon after initiation of immune checkpoint inhibitor: A case report
Article
作者: Omori, Keitaro ; Hattori, Noboru ; Inada, Shugo ; Ohge, Hiroki ; Shigemoto, Norifumi ; Nomura, Toshihito ; Kitagawa, Hiroki
Immune checkpoint inhibitors (ICIs) have been approved for treating various cancers; however, they can cause immune-related adverse events. Generally, ICIs are not associated with an increased risk of infection, however, several reports demonstrated infections caused by non-tuberculous mycobacterium (NTM) during ICI therapy. Here, we report a case of NTM shoulder arthritis with acute exacerbation immediately after ICI initiation. A 75-year-old man was diagnosed with left shoulder arthritis caused by Mycobacterium intracellulare eight months before receiving ICI treatment and was treated with clarithromycin and ethambutol. However, the mild redness, swelling, heat, and shoulder pain persisted. The patient was diagnosed with hepatocellular carcinoma and atezolizumab and bevacizumab treatment was initiated; one day after the initiation of therapy, the patient presented with a fever and worsened shoulder symptoms. Considering the suspected worsening of NTM arthritis, sitafloxacin was additionally administered, and surgical debridement was performed. M. intracellulare was isolated through culturing shoulder synovial tissue; immunohistochemical staining analysis revealed programmed death-1 (PD-1) and programmed death ligand-1 (PD-L1) expression in granulation tissue cells. After the arthritis symptoms decreased, atezolizumab plus bevacizumab was resumed and continued with no recurrence of arthritis. The NTM exacerbation on the day after ICI administration suggests the potential involvement of the PD-1/PD-L1 pathway in the pathogenesis of NTM; moreover, adverse inflammatory reactions to NTM were possibly triggered through the blockade of this pathway.
2025-02-01JOURNAL OF ORTHOPAEDIC RESEARCH
Development of an ex vivo model to study Staphylococcus aureus invasion of the osteocyte lacuno‐canalicular network
Article
作者: Siverino, Claudia ; Metsemakers, Willem‐Jan ; Moriarty, Thomas F. ; de Mesy Bentley, Karen L. ; Vanvelk, Niels ; Verhofstad, Michael H. J.
Abstract:
Staphylococcus aureus has multiple mechanisms to evade the host's immune system and antibiotic treatment. One such mechanism is the invasion of the osteocyte lacuno‐canalicular network (OLCN), which may be particularly important in recurrence of infection after debridement and antibiotic therapy. The aim of this study was to develop an ex vivo model to facilitate further study of S. aureus invasion of the OLCN and early‐stage testing of antibacterial strategies against bacteria in this niche. The diameter of the canaliculi of non‐infected human, sheep, and mouse bones was measured microscopically on Schmorl's picrothionin stained sections, showing a large overlap in canalicular diameter. S. aureus successfully invaded the OLCN in all species in vitro as revealed by presence in osteocyte lacunae in Brown and Brenn‐stained sections and by scanning electron microscopy. Murine bones were then selected for further experiments, and titanium pins with either a wild‐type or ΔPBP4 mutant S. aureus USA300 were placed trans‐cortically and incubated for 2 weeks in tryptic soy broth. Wild‐type S. aureus readily invaded the osteocyte lacunae in mouse bones while the ΔPBP4 showed a significantly lower invasion of the OLCN (p = 0.0005). Bone specimens were then treated with gentamicin, sitafloxacin, R14 bacteriophages, or left untreated. Gentamicin (p = 0.0027) and sitafloxacin (p = 0.0280) significantly reduced the proportion of S. aureus‐occupied lacunae, whilst bacteriophage treatment had no effect. This study shows that S. aureus is able to invade the OLCN in an ex vivo model. This ex vivo model can be used for future early‐stage studies before proceeding to in vivo studies.
2025-01-07Microbiology Spectrum
Early bactericidal activity of sitafloxacin against pulmonary tuberculosis
Article
作者: Nie, Lihui ; Wu, Zhangjun ; Wang, Yufeng ; Xu, Yuanhong ; Gao, Mengqiu ; Tong, Jing ; Rao, Youyi ; Shang, Yuanyuan ; Du, Juan ; Ren, Yi ; Wu, Guihui ; Pang, Yu
ABSTRACT:
Sitafloxacin is a quinolone broad-spectrum antimicrobial agent, and its pharmacologic properties and
in vitro
data demonstrate that sitafloxacin has a potent killing effect against
Mycobacterium tuberculosis
, including drug-resistant strains, which is superior to that of other available quinolones. However, its efficacy in patients with primary-sensitive tuberculosis is unclear. This study aims to evaluate the early bactericidal activity (EBA) of sitafloxacin in patients with primary drug-susceptible tuberculosis. In this early bactericidal activity study, 30 patients with primary smear-positive tuberculosis were randomized to the once-daily oral administration of 200 mg sitafloxacin, 500 mg levofloxacin, or 300 mg isoniazid (INH) for 7 days. Sputum for quantitative culture was collected 2 days before the study of drug administration, followed by 16 hours of overnight sputum collected daily for 7 days of monotherapy. Colony-forming units (CFU) of
Mycobacterium tuberculosis
were counted from the collected overnight sputum on agar plates to calculate the EBA, defined as log
10
CFU/mL sputum/day. The bactericidal activity was measured by measuring the first 2 days (early bactericidal activity 0–2) and the last 5 days (prolonged early bactericidal properties 2–7) of study drug administration. The EBA 0–2 of INH (0.39 ± 0.22 log
10
CFU/mL/day) was higher than that of levofloxacin (0.26 ± 0.27 log10CFU/mL/day) and sitafloxacin (0.22 ± 0.25 log
10
CFU/mL/day), with no statistically significant difference (
P
= 0.08). EBA 0–2 was similar for the three drugs. INH prolonged early bactericidal activity (2–7) (0.17 ± 0.16 log
10
CFU/mL/day) was higher than levofloxacin (0.14 ± 0.10 log
10
CFU/mL/day) and lower than sitafloxacin (0.26 ± 0.31 log
10
CFU/mL/day), with no statistically significant difference (
P
= 0.59). The EBA 2–7 of sitafloxacin showed higher activity than INH and levofloxacin. Sitafloxacin exhibits comparable early bactericidal activity and higher extended early bactericidal activity relative to levofloxacin. In addition, this novel fluoroquinolone has a good safety profile. The study data highlights the potential of sitafloxacin in the clinical management of drug-susceptible tuberculosis, as well as drug-resistant tuberculosis.
IMPORTANCE:
Sitafloxacin is a quinolone broad-spectrum antimicrobial agent, and its pharmacologic properties and
in vitro
data demonstrate that sitafloxacin has a potent killing effect against
Mycobacterium tuberculosis
. However, its efficacy in patients with primary-sensitive tuberculosis is unclear. We investigated the early bactericidal activity of sitafloxacin in primary susceptible tuberculosis. The results showed that sitafloxacin exhibited comparable early bactericidal activity and higher extended early bactericidal activity relative to levofloxacin. In addition, this novel fluoroquinolone has a good safety profile. Our study data highlights the potential of sitafloxacin in the clinical management of drug-susceptible tuberculosis, as well as drug-resistant tuberculosis.
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 |
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 | |
| 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
查看全部结果
N/A | 114 | 夢餘衊構積廠鹽鹹鹽繭(鬱遞鏇齋鑰襯憲淵簾顧) = 鹹廠獵簾願壓糧鹹製鹹 製糧繭壓襯齋窪製窪觸 (壓築鹽鏇憲網製獵積積 ) | - | 2022-01-01 | |||
N/A | 一线 | 二线 | 三线 | 180 | Sitafloxacin-based regimen | 製鏇膚築鹽積餘壓網網(夢獵鏇膚鑰壓齋觸繭獵) = one patient experienced appearance of nettle rash/hives and dropped out from this study 觸鹽廠範蓋範衊醖觸糧 (艱壓鑰蓋廠廠廠積窪鏇 ) | 积极 | 2015-10-01 | |
N/A | 感染 维持 | - | 鹹鹹憲繭窪糧網鏇繭選(觸築蓋築製夢鏇艱衊獵) = 憲壓鏇製觸艱選糧窪艱 築網淵鏇鹹衊襯淵顧觸 (夢艱鑰餘艱窪願積獵顧 ) 更多 | 积极 | 2012-10-30 | ||
鹹鹹憲繭窪糧網鏇繭選(觸築蓋築製夢鏇艱衊獵) = 淵簾糧範夢觸鏇製觸製 築網淵鏇鹹衊襯淵顧觸 (夢艱鑰餘艱窪願積獵顧 ) 更多 |
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