Besifloxacin
目录号 : GC25135Besifloxacin is a fourth generation fluoroquinolone-type opthalmic antibiotic for the treatment of bacterial conjunctivitis.
Cas No.:141388-76-3
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Besifloxacin is a fourth generation fluoroquinolone-type opthalmic antibiotic for the treatment of bacterial conjunctivitis.
| Cas No. | 141388-76-3 | SDF | Download SDF |
| 分子式 | C19H21ClFN3O3 | 分子量 | 393.84 |
| 溶解度 | DMSO: Insoluble;Water: Insoluble; | 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 | 2.5391 mL | 12.6955 mL | 25.391 mL |
| 5 mM | 0.5078 mL | 2.5391 mL | 5.0782 mL |
| 10 mM | 0.2539 mL | 1.2696 mL | 2.5391 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。
Besifloxacin: a topical fluoroquinolone for the treatment of bacterial conjunctivitis
Clin Ther 2010 Mar;32(3):454-71.PMID:20399984DOI:10.1016/j.clinthera.2010.03.013.
Background: Besifloxacin is a topical ophthalmic fluoroquinolone that was approved by the US Food and Drug Administration (FDA) in May 2009 for the treatment of bacterial conjunctivitis caused by susceptible bacterial strains. Objective: This article provides an overview of the pharmacology, clinical efficacy, and tolerability of ophthalmic Besifloxacin when used for the treatment of bacterial conjunctivitis. Methods: Relevant reports pertaining to the pharmacology, efficacy, and tolerability of Besifloxacin were identified through a search of MEDLINE (1985-December 2009) and International Pharmaceutical Abstracts (1985-December 2009) using the terms Besifloxacin, BOL-303224-A, ophthalmic fluoroquinolones, and bacterial conjunctivitis. Additional publications were identified by reviewing the reference lists of identified articles and searching the FDA Web site. Results: Besifloxacin has potent in vitro inhibitory activity against most common ocular bacterial pathogens (MIC90 values generally < or =4 microg/mL), including Staphylococcus aureus, Streptococcus pneumoniae, and Haemophilus influenzae. In an ocular pharmacokinetic study in 64 healthy volunteers, the C(max) in tears (mean [SD], 610 [540] microg/mL) was reached 10 minutes after a single ocular instillation of Besifloxacin; concentrations > or =1.6 microg/g of tear were sustained for at least 24 hours; and the elimination t(1/2) was ~3.4 hours. In a study in 24 patients with a clinical diagnosis of bilateral bacterial conjunctivitis, systemic exposure (C(max)) after administration of Besifloxacin ophthalmic suspension 3 times daily for 5 days was <0.5 ng/mL. In 2 randomized, double-masked, vehicle-controlled clinical trials, Besifloxacin ophthalmic suspension was well tolerated and significantly more efficacious than vehicle in achieving clinical resolution (73.3% vs 43.1%, respectively, in one of the studies [P < 0.001]; 45.2% vs 33.0% in the other [P = 0.008]) and microbial eradication (88.3% vs 60.3% [P < 0.001] and 91.5% vs 59.7% [P < 0.001], respectively). In a randomized, double-masked, parallel-group, noninferiority trial comparing Besifloxacin ophthalmic suspension 0.6% with moxifloxacin ophthalmic solution 0.5%, Besifloxacin was found to be noninferior to moxifloxacin (predefined cutoff for noninferiority = -15), with no significant differences in rates of clinical resolution (58.3% and 59.4%, respectively; 95% CI, -9.48 to 7.29) or microbial eradication (93.3% and 91.1%; 95% CI, -2.44 to 6.74). Besifloxacin was generally well tolerated in these clinical trials, with the most common (> or =1.5%) ocular adverse events being nonspecific conjunctivitis (2.6%), blurred vision (2.1%), bacterial conjunctivitis (1.8%), and eye pain (1.5%). The recommended dose of Besifloxacin is 1 drop in the affected eye(s) 3 times daily (4-12 hours apart) for 7 days. Conclusion: Besifloxacin ophthalmic suspension 0.6% appeared to be well tolerated in the populations studied and was efficacious in the treatment of bacterial conjunctivitis caused by susceptible isolates.
Besifloxacin: Efficacy and Safety in Treatment and Prevention of Ocular Bacterial Infections
Ophthalmol Ther 2016 Jun;5(1):1-20.PMID:27010720DOI:10.1007/s40123-016-0046-6.
This comprehensive review summarizes the mechanism of action, pharmacokinetics, efficacy, and safety of Besifloxacin ophthalmic suspension, 0.6% and examines its role in the treatment of ocular surface bacterial infections. Besifloxacin possesses balanced activity against bacterial topoisomerase II (also called DNA gyrase) and topoisomerase IV. It has shown a low potential to select for bacterial resistance in vitro and demonstrated strong in vitro activity against many Gram-positive, Gram-negative, and anaerobic organisms, including methicillin-resistant Staphylococcus aureus and Staphylococcus epidermidis (MRSA and MRSE, respectively). Ocular pharmacokinetic studies have shown that Besifloxacin achieves high, sustained concentrations in the tear fluid and conjunctiva following topical administration, with negligible systemic exposure. Large randomized, controlled clinical trials have established the efficacy and safety of Besifloxacin administered three times daily for 5 days for treatment of acute bacterial conjunctivitis in both adults and children, with high rates of clinical resolution (up to more than 70% by day 5) and bacterial eradication (more than 90% by day 5), and a low incidence of adverse events. Additionally, Besifloxacin applied twice daily for 3 days demonstrated greater efficacy than vehicle in treating bacterial conjunctivitis. Case reports, a large retrospective chart review, and animal studies have provided supporting evidence for the efficacy of Besifloxacin in the management of acute bacterial keratitis. There is some evidence to suggest that Besifloxacin may provide an advantage over other current-generation fluoroquinolones in antimicrobial prophylaxis for ocular surgery. Besifloxacin is an appropriate option for treatment of bacterial conjunctivitis, and its use in the treatment of bacterial keratitis and lid disorders, as well as for surgical prophylaxis, appears promising and warrants further evaluation.
Besifloxacin, a new ophthalmic fluoroquinolone for the treatment of bacterial conjunctivitis
Expert Opin Pharmacother 2009 Oct;10(15):2545-54.PMID:19743941DOI:10.1517/14656560903213413.
Besifloxacin is a new fluoroquinolone anti-infective developed for ophthalmic use. Besifloxacin ophthalmic suspension 0.6% (Besivance) was recently approved for the treatment of bacterial conjunctivitis. The objective of this article is to provide a comprehensive overview of microbiological, pharmacokinetic/pharmacodynamic and clinical studies with Besifloxacin. Microbiological studies have demonstrated that Besifloxacin has wide-spectrum and potent activity against common ocular pathogens, including Gram-negative and Gram-positive pathogens associated with bacterial conjunctivitis, and retained activity against fluoroquinolone-resistant staphylococci and multidrug-resistant strains. In preclinical and human studies, topically applied Besifloxacin had a prolonged ocular concentration and minimal systemic exposure. In clinical studies, patients randomized to Besifloxacin ophthalmic suspension 0.6% experienced significantly higher rates of clinical resolution and microbial eradication than patients randomized to vehicle. Besifloxacin ophthalmic suspension 0.6% was also found to be as effective and well tolerated as moxifloxacin ophthalmic solution 0.5%. The low minimum inhibitory concentrations and high attainment of pharmacodynamic targets with Besifloxacin may contribute to a lower risk for the emergence of bacterial resistance, although further studies are needed. These data indicate that Besifloxacin ophthalmic suspension 0.6% is an important new option for the treatment of bacterial conjunctivitis.
Besifloxacin in the management of bacterial infections of the ocular surface
Can J Ophthalmol 2015 Jun;50(3):184-91.PMID:26040217DOI:10.1016/j.jcjo.2014.12.013.
Acute bacterial conjunctivitis is a common infection of the ocular surface. Increasing rates of bacterial resistance have prompted the development of new antibiotics with improved activity against the bacterial species most often found in this disease. Besifloxacin is the first topical chlorofluoroquinolone developed solely for ophthalmic use. Studies have attested to its in vitro potency against a broad range of bacteria, as well as its efficacy in clinical studies of bacterial conjunctivitis when dosed 2 or 3 times a day. This review provides an up-to-date summary of studies on causative pathogens in acute bacterial conjunctivitis; recent geographic trends in bacterial resistance among ocular pathogens, including that of methicillin-resistant Staphylococcus aureus; the efficacy of Besifloxacin in preclinical and clinical studies; its safety; and the role of Besifloxacin in combating resistant strains. Further, this review provides a brief update on bacterial keratitis, causative pathogens, the development of resistance among those pathogens, and the potential role of Besifloxacin in the treatment of bacterial keratitis.
The role of Besifloxacin in the treatment of bacterial conjunctivitis
Ann Pharmacother 2014 May;48(5):616-25.PMID:24566460DOI:10.1177/1060028014524175.
Objective: To evaluate the role of Besifloxacin in bacterial conjunctivitis treatment. Data sources: Searches were made on MEDLINE/PubMed and EMBASE (January 2007 to January 2014) using the terms Besifloxacin and Besivance. References from these publications were reviewed for additional resources. Additional information was collected from Bausch & Lomb, the manufacturer of Besivance; www.clinicaltrials.gov; and American Academy of Ophthalmology. Study selection and data extraction: English-language documents were reviewed for pharmacology, pharmacokinetics, efficacy, and safety, with priority on clinical trials. Data synthesis: Three large randomized controlled clinical trials established the safety and efficacy of Besifloxacin ophthalmic suspension 0.6% compared with placebo or active comparator (moxifloxacin ophthalmic solution 0.5%) given 3 times a day for 5 days for acute bacterial conjunctivitis (BC) treatment. Compared with placebo, Besifloxacin had clinically superior bacterial eradication rates and was noninferior to moxifloxacin. Besifloxacin was compared with placebo in 2 randomized, placebo-controlled trials, dosed twice a day for 3 days. Superior efficacy was seen compared with placebo, which supports the shorter dosing schedule. Ophthalmic Besifloxacin is well tolerated; the most common adverse effect (conjunctival redness) occurred in 2% of patients. Adverse effects in 1% to 2% of patients included blurred vision, eye pain, eye irritation, eye pruritus, and headache. Conclusion: Besifloxacin 0.6% ophthalmic suspension 3 times a day for 5 days is safe and effective for BC. Twice-a-day dosing for 3 days was also effective-a simplified regimen compared with other fluoroquinolones. Disadvantages include price and lack of a generic. Further evaluation is needed to evaluate comparative efficacy among other ocular fluoroquinolones and unlabeled uses.