Finafloxacin
(Synonyms: 非那沙星) 目录号 : GC33917
A fluoroquinolone antibiotic
Cas No.:209342-40-5
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Finafloxacin is a fluoroquinolone antibiotic.1 It is active against S. pneumoniae and P. aeruginosa, as well as methicillin-resistant S. aureus (MRSA) that is sensitive or resistant to fluoroquinolones (MIC90s = 2, 2, 0.125, and 4 mg/L, respectively). Finafloxacin (23.1 mg/kg) improves survival in F. tularensis- or Y. pestis-infected mice in models of tularemia or plague, respectively.2 Formulations containing finafloxacin have been used in the treatment of acute otitis externa.
1.Kocsis, B., Domokos, J., and Szabo, D.Chemical structure and pharmacokinetics of novel quinolone agents represented by avarofloxacin, delafloxacin, finafloxacin, zabofloxacin and nemonoxacinAnn. Clin. Microbiol. Antimicrob.15(1)34(2016) 2.Barnes, K.B., Richards, M.I., Laws, T.R., et al.Finafloxacin is an effective treatment for inhalational tularemia and plague in mouse models of infectionAntimicrob. Agents Chemother.65(6)e02294-02220(2021)
| Cas No. | 209342-40-5 | SDF | |
| 别名 | 非那沙星 | ||
| Canonical SMILES | O=C(C1=CN(C2CC2)C3=C(C=C(F)C(N4C[C@]5([H])OCCN[C@@]5([H])C4)=C3C#N)C1=O)O | ||
| 分子式 | C20H19FN4O4 | 分子量 | 398.39 |
| 溶解度 | DMSO : 6.4 mg/mL (16.06 mM) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.5101 mL | 12.5505 mL | 25.101 mL |
| 5 mM | 0.502 mL | 2.5101 mL | 5.0202 mL |
| 10 mM | 0.251 mL | 1.2551 mL | 2.5101 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Delafloxacin, Finafloxacin, and Zabofloxacin: Novel Fluoroquinolones in the Antibiotic Pipeline
Antibiotics (Basel) 2021 Dec 8;10(12):1506.PMID:34943718DOI:10.3390/antibiotics10121506.
Novel antimicrobial agents, approved for clinical use in past years, represent potential treatment options for various infections. In this review, we summarize the most important medical and microbiological features of three recently approved fluoroquinolones, namely delafloxacin, Finafloxacin, and zabofloxacin. Delafloxacin possesses an anionic chemical structure, and represents broad-spectrum activity, as it targets both bacterial DNA gyrase and topoisomerase IV enzymes of gram-positive and gram-negative bacteria with equal affinity. Its molecular surface is larger than that of other fluoroquinolones, and it has enhanced antibacterial efficacy in acidic environments. Delafloxacin has been approved to treat acute bacterial skin and skin-structure infections, as well as community-acquired bacterial pneumonia. Finafloxacin has a zwitterionic chemical structure, and targets both DNA gyrase and topoisomerase IV enzymes. This enables a broad antibacterial spectrum; however, Finafloxacin has so far only been approved in ear-drops to treat bacterial otitis externa. Zabofloxacin is also a broad-spectrum fluoroquinolone agent, and was first approved in South Korea to treat acute bacterial exacerbation of chronic obstructive pulmonary disease. The introduction of these novel fluoroquinolones into daily practice extends the possible indications of antibiotics into different bacterial infections, and provides treatment options in difficult-to-treat infections. However, some reports of delafloxacin resistance have already appeared, thus underlining the importance of the prudent use of antibiotics.
Efficacy of Finafloxacin in a murine model of inhalational glanders
Front Microbiol 2022 Nov 24;13:1057202.PMID:36504783DOI:10.3389/fmicb.2022.1057202.
Burkholderia mallei, the causative agent of glanders, is principally a disease of equines, although it can also infect humans and is categorized by the U.S. Centers for Disease Control and Prevention as a category B biological agent. Human cases of glanders are rare and thus there is limited information on treatment. It is therefore recommended that cases are treated with the same therapies as used for melioidosis, which for prophylaxis, is co-trimoxazole (trimethoprim/sulfamethoxazole) or co-amoxiclav (amoxicillin/clavulanic acid). In this study, the fluoroquinolone Finafloxacin was compared to co-trimoxazole as a post-exposure prophylactic in a murine model of inhalational glanders. BALB/c mice were exposed to an aerosol of B. mallei followed by treatment with co-trimoxazole or Finafloxacin initiated at 24 h post-challenge and continued for 14 days. Survival at the end of the study was 55% or 70% for mice treated with Finafloxacin or co-trimoxazole, respectively, however, this difference was not significant. However, Finafloxacin was more effective than co-trimoxazole in controlling bacterial load within tissues and demonstrating clearance in the liver, lung and spleen following 14 days of therapy. In summary, Finafloxacin should be considered as a promising alternative treatment following exposure to B. mallei.
Finafloxacin: first global approval
Drugs 2015 Apr;75(6):687-93.PMID:25808831DOI:10.1007/s40265-015-0384-z.
Finafloxacin is a fluoroquinolone antimicrobial agent that exhibits optimum efficacy in slightly acidic environments. It is being developed by MerLion Pharmaceuticals to treat serious bacterial infections associated with an acidic environment, including urinary tract infections and Helicobacter pylori infections. An otic suspension of Finafloxacin (Xtoro™), developed by Alcon (a division of Novartis), was recently approved in the USA for the treatment of acute otitis externa, and a Common Technical Document for this indication was also filed in Canada. Oral and/or intravenous formulations are in phase I and II evaluation in uncomplicated urinary tract infections (Germany and Singapore), complicated urinary tract infections and pyelonephritis (Germany and Poland) and H. pylori infection (Germany). This article summarizes the milestones in the development of Finafloxacin leading to this first approval for otitis externa.
Treatment of urinary tract infections in the era of antimicrobial resistance and new antimicrobial agents
Postgrad Med 2020 Apr;132(3):234-250.PMID:31608743DOI:10.1080/00325481.2019.1680052.
Urinary tract infections (UTIs) caused by antibiotic-resistant Gram-negative bacteria are a growing concern due to limited treatment options. Knowledge of the common uropathogens in addition to local susceptibility patterns is essential in determining appropriate empiric antibiotic therapy of UTIs. The recommended first-line empiric antibiotic therapy for acute uncomplicated bacterial cystitis in otherwise healthy adult nonpregnant females is a 5-day course of nitrofurantoin, a 3-g single dose of fosfomycin tromethamine, or a 5-day course of pivmecillinam. High rates of resistance for trimethoprim-sulfamethoxazole and ciprofloxacin preclude their use as empiric treatment of UTIs in several communities, particularly if patients who were recently exposed to them or in patients who are at risk of infections with extended-spectrum β-lactamases (ESBLs)-producing Enterobacteriales. Second-line options include oral cephalosporins such as cephalexin or cefixime, fluoroquinolones and β-lactams, such as amoxicillin-clavulanate. Current treatment options for UTIs due to AmpC- β -lactamase-producing Enterobacteriales include nitrofurantoin, fosfomycin, pivmecillinam, fluoroquinolones, cefepime, piperacillin-tazobactam and carbapenems. Treatment oral options for UTIs due to ESBLs-E coli include nitrofurantoin, fosfomycin, pivmecillinam, amoxicillin-clavulanate, Finafloxacin, and sitafloxacin while pivmecillinam, fosfomycin, Finafloxacin, and sitafloxacin are treatment oral options for ESBLs- Klebsiella pneumoniae. Parenteral treatment options for UTIs due to ESBLs-producing Enterobacteriales include piperacillin-tazobactam (for ESBL-E coli only), carbapenems including meropenem/vaborbactam, imipenem/cilastatin-relebactam, and sulopenem, ceftazidime-avibactam, ceftolozane-tazobactam, aminoglycosides including plazomicin, cefiderocol, fosfomycin, sitafloxacin, and Finafloxacin. Ceftazidime-avibactam, meropenem/vaborbactam, imipenem/cilastatin-relebactam, colistin, fosfomycin, aztreonam and ceftazidime-avibactam, aztreonam and amoxicillin-clavulanate, aminoglycosides including plazomicin, cefiderocol, tigecycline are treatment options for UTIs caused by carbapenem-resistant Enterobacteriales (CRE). Treatment options for UTIs caused by multidrug resistant (MDR)-Pseudomonas spp. include fluoroquinolones, ceftazidime, cefepime, piperacillin-tazobactam, carbapenems including imipenem-cilastatin/relebactam, meropenem, and fosfomycin, ceftolozane-tazobactam, ceftazidime-avibactam, aminoglycosides including plazomicin, aztreonam and ceftazidime-avibactam, cefiderocol, and colistin. It is important to use the new antimicrobials wisely for treatment of UTIs caused by MDR-organisms to avoid resistance development.
Finafloxacin for the treatment of urinary tract infections
Expert Opin Investig Drugs 2015;24(7):957-63.PMID:26068714DOI:10.1517/13543784.2015.1052401.
Introduction: In the past decade, the indiscriminate use of fluoroquinolones in the prophylaxis and treatment of urinary tract infections (UTIs) has led to an increase of antibiotic resistance patterns. Finafloxacin is a new generation fluoroquinolone with interesting preclinical characteristics and pH-related efficacy. Areas covered: This review summarizes Finafloxacin's safety profile and prospectively evaluates its specific use in the treatment of UTIs. This article was based on a Medline English literature search. Expert opinion: In vitro and in vivo studies have shown that Finafloxacin expresses its full antibacterial activity in acidic environments and is able to exert significant bactericidal effects in difficult-to-treat infections. Finafloxacin has a broad antibacterial spectrum and efficient pharmacokinetic absorption. Moreover, it undergoes extensive tissue distribution, resulting in good antibacterial activity for daily dosages from 400 to 800 mg. This novel compound has also been successfully tested on biofilm-related Escherichia coli. Finafloxacin has demonstrated a good safety and tolerability profile in humans when administered orally or intravenously and is thus an interesting compound for the treatment of UTIs. However, further prospective randomized clinical trials will be necessary to confirm these preliminary results before definitive conclusions can be made.