Ceftobiprole medocaril sodium
(Synonyms: 头孢比普酯钠盐; BAL5788 sodium) 目录号 : GC68005Ceftobiprole medocaril (BAL5788) sodium 是 Ceftobiprole 的胃肠外前药。Ceftobiprole 是一种非肠道吡咯烷酮头孢菌素。Ceftobiprole 是一种广谱头孢菌素，对甲氧西林 (MRSA) 和耐万古霉素葡萄球菌 (VRSA) 和耐青霉素链球菌具有高水平的体外活性。Ceftobiprole 也抑制革兰氏阳性和革兰氏阴性病原体。
Cas No.:252188-71-9
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
Ceftobiprole medocaril (BAL5788) sodium is the parenteral prodrug of Ceftobiprole . Ceftobiprole is a parenteral pyrrolidinone cephalosporin. Ceftobiprole is a broad-spectrum cephalosporin with high levels of in vitro activity against methicillin- (MRSA) and vancomycin-resistant staphylococci (VRSA) and penicillin-resistant streptococci. Ceftobiprole also inhibits gram-positive and gram-negative pathogens[1][2].
Ceftobiprole medocaril (s.c.; 3 × q12h; total daily doses of BAL9141 equivalents, 2.1, 4.2, or 8.4 mg/kg) causes ten-day cumulative survival rates ranged from 57 to 100% for female Swiss albino mice (body weight, 20 to 22 g) infected Penr Cros Ctxs strain P-15986[1].
Ceftobiprole medocaril (10, 40, 160 mg/kg; single dose; sc) has T1/2s from 20 min to 31 min, as the dose rose from 40 mg/kg to 160 mg/kg. The AUC/dose values for the escalating single doses ranges from 0.585 to 1.33, and the Cmax/dose values decreases from 1.08 to 0.90 in neutropenic thigh-infected mice[2].
[1]. E Azoulay-Dupuis, et al. Efficacy of BAL5788, a prodrug of cephalosporin BAL9141, in a mouse model of acute pneumococcal pneumonia. Antimicrob Agents Chemother. 2004 Apr;48(4):1105-11.
[2]. W A Craig, et al. In vivo pharmacodynamics of ceftobiprole against multiple bacterial pathogens in murine thigh and lung infection models. Antimicrob Agents Chemother. 2008 Oct;52(10):3492-6.
| Cas No. | 252188-71-9 | SDF | Download SDF |
| 别名 | 头孢比普酯钠盐; BAL5788 sodium | ||
| 分子式 | C26H25N8NaO11S2 | 分子量 | 712.64 |
| 溶解度 | DMSO : 250 mg/mL (350.81 mM; Need ultrasonic) | 储存条件 | 4°C, away from moisture and light |
| 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 | 1.4032 mL | 7.0162 mL | 14.0323 mL |
| 5 mM | 0.2806 mL | 1.4032 mL | 2.8065 mL |
| 10 mM | 0.1403 mL | 0.7016 mL | 1.4032 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。
Ceftobiprole medocaril
Rev Esp Quimioter 2022 Apr;35 Suppl 1(Suppl 1):25-27.PMID:35488820DOI:10.37201/req/s01.05.2022.
Ceftobiprole medocaril is a broad-spectrum 5th-generation cephalosporin with activity against Gram-positives such as methicillin-resistant Staphylococcus aureus and penicillin-resistant Streptococcus pneumoniae, and against Gram-negatives such as Pseudomonas aeruginosa. The recommended dose is 500 mg every 8 h in 2-hour infusions. Various clinical trials have demonstrated its usefulness in the treatment of community-acquired pneumonia and nosocomial pneumonia, with the exception of ventilator-associated pneumonia. In summary, it is a very useful antibiotic for the treatment of pneumonia.
Ceftobiprole medocaril in the treatment of hospital-acquired pneumonia
Future Microbiol 2015;10(12):1913-28.PMID:26573022DOI:10.2217/fmb.15.115.
Ceftobiprole medocaril is a fifth-generation cephalosporin approved in Europe as single-agent therapy for hospital-acquired pneumonia (HAP), excluding ventilator-associated pneumonia (VAP). It is rapidly converted to the active metabolite ceftobiprole following intravenous administration. Ceftobiprole has a broad spectrum of activity, notably against methicillin-resistant Staphylococcus aureus, ampicillin-susceptible enterococci, penicillin-resistant pneumococci and Enterobacteriaceae not producing extended-spectrum β-lactamase. Ceftobiprole is primarily excreted renally by glomerular filtration, with minimal propensity for interaction with co-administered drugs. Normal dose is ceftobiprole 500 mg, administered by 2-h intravenous infusion every 8 h, with dose adjustment according to renal function. In a pivotal Phase III trial in patients with HAP, ceftobiprole monotherapy was as efficacious as ceftazidime/linezolid for clinical and microbiological cure and was noninferior to ceftazidime/linezolid in the subgroup of patients with HAP excluding VAP. Ceftobiprole and ceftazidime/linezolid were similarly well tolerated. Ceftobiprole is an efficacious and well-tolerated option for empirical treatment of patients with HAP (excluding VAP).
Ceftobiprole medocaril: a review of its use in patients with hospital- or community-acquired pneumonia
Drugs 2014 Sep;74(13):1523-42.PMID:25117196DOI:10.1007/s40265-014-0273-x.
Ceftobiprole, the active metabolite of the prodrug Ceftobiprole medocaril (Zevtera(®)), is a new generation broad-spectrum intravenous cephalosporin with activity against methicillin-resistant Staphylococcus aureus. Ceftobiprole exhibits potent in vitro activity against a number of Gram-positive and Gram-negative pathogens associated with hospital-acquired pneumonia (HAP) and community-acquired pneumonia (CAP). It is the first cephalosporin monotherapy approved in the EU for the treatment of both HAP (excluding ventilator associated-pneumonia [VAP]) and CAP. In phase III trials, Ceftobiprole medocaril was noninferior, in terms of clinical cure rates at the test-of-cure visit, to ceftazidime plus linezolid in patients with HAP and to ceftriaxone ± linezolid in patients with CAP severe enough to require hospitalization. In patients with HAP, noninferiority of Ceftobiprole medocaril to ceftazidime plus linezolid was not demonstrated in a subset of patients with VAP. In patients with CAP, Ceftobiprole medocaril was effective in those at risk for poor outcomes (pneumonia severity index ≥91, Pneumonia Patient Outcomes Research Team score IV-V or bacteraemic pneumonia). In the phase III trials, Ceftobiprole medocaril was generally well tolerated, with ≈10 % of patients discontinuing the treatment because of adverse events. The most common treatment-related adverse events occurring in ceftobiprole recipients in the trials in patients with HAP or CAP included nausea, diarrhoea, infusion site reactions, vomiting, hepatic enzyme elevations and hyponatraemia. Therefore, Ceftobiprole medocaril monotherapy offers a simplified option for the initial empirical treatment of patients with HAP (excluding VAP) and in those with CAP requiring hospitalization.
Ceftobiprole medocaril for the treatment of community-acquired pneumonia
Expert Opin Pharmacother 2018 Sep;19(13):1503-1509.PMID:30198789DOI:10.1080/14656566.2018.1516749.
Ceftobiprole is a novel broad-spectrum cephalosporin with excellent activity against a broad range of pathogens that are important in community-acquired pneumonia (CAP), including drug-resistant pneumococci, methicillin-resistant Staphylococcus aureus, and Pseudomonas aeruginosa. Areas covered: This article reviews the spectrum of activity, the main pharmacological and pharmacodynamic characteristics of ceftobiprole as well its clinical efficacy and safety in the treatment of CAP in adult patients. Expert opinion: Taking into account that the current treatment guidelines for CAP recommend the use of an adequate empirical therapy to improve its prognosis, ceftobiprole shows a profile of antimicrobial activity that would cover most etiological agents in patients with risk factors for infection caused by multidrug resistant organisms. The results of the pivotal clinical trial of patients hospitalized with CAP treated with ceftobiprole showed a high rate of clinical cure. The clinical tolerance of ceftobiprole in clinical trials was generally very good. These findings make ceftobiprole a good parenteral therapeutic alternative for the empirical treatment of CAP that requires hospitalization, especially in patients with risk factors for CAP caused by resistant microorganisms.
Ceftobiprole medocaril: BAL5788, JNJ 30982081, JNJ30982081, RO 65-5788, RO 655788
Drugs R D 2006;7(5):305-11.PMID:16922591DOI:10.2165/00126839-200607050-00003.
Ceftobiprole medocaril [BAL 5788, RO 65-5788, JNJ 30982081] is a prodrug in phase III clinical development with Basilea Pharmaceutica and Cilag AG (Johnson & Johnson) for the potential treatment of serious bacterial infections, including methicillin-resistant Staphylococcus aureus (MRSA). Ceftobiprole medocaril is the water-soluble prodrug of the pyrrolidinone cephalosporin, ceftobiprole [BAL 9141, RO 63-9141]. Because of the low water solubility of ceftobiprole, its clinical application was limited and Basilea began its investigations into Ceftobiprole medocaril for further development. Ceftobiprole medocaril is being developed for IV administration and is currently undergoing phase III trials for complicated skin and skin structure infections (including MRSA) and hospital-acquired (nosocomial) pneumonia. Ceftobiprole medocaril has a broad spectrum of activity against Gram-positive bacteria (including methicillin-resistant staphylococci, penicillin-resistant pneumococci and Enterococcus faecalis) and Gram-negative bacteria. Ceftobiprole medocaril inhibits all transpeptidases, including the penicillin-binding protein (PBP) 2a, by a unique combination of features. PBP 2a is the primary enzyme responsible for beta-lactam drug resistance in MRSA; PBP 2a also acts as a key defense mechanism by interacting with the bacterial cell wall to form a chemical barricade that is impervious to antibiotics. Ceftobiprole medocaril has been designed specifically to bind to this penicillin-resistant target. Ceftobiprole medocaril is bactericidal and has not shown resistance development in vitro or in stringent animal models. Studies conducted by Basilea have demonstrated that Ceftobiprole medocaril is readily converted to ceftobiprole, and shows markedly improved water solubility. In February 2005, Basilea Pharmaceutica AG entered into an exclusive worldwide agreement with Cilag AG International (Johnson & Johnson) to develop, manufacture and market Ceftobiprole medocaril. Ortho-McNeil Pharmaceutical (Johnson & Johnson) will market Ceftobiprole medocaril in the US, and its affiliate companies, known as Janssen-Cilag, will market the product outside the US (entered as World in the Licensee table). Basilea has retained an option to co-promote Ceftobiprole medocaril in the US, major European countries, Japan and China. Johnson & Johnson Pharmaceutical Research and Development LLC will develop Ceftobiprole medocaril in collaboration with Basilea. Roche previously retained an opt-in right on Ceftobiprole medocaril. However, following Roche's decision not to exercise this right in May 2004, Basilea gained full global commercialisation rights for Ceftobiprole medocaril. Roche retains its major shareholding in Basilea. Ceftobiprole medocaril is currently in phase III trials for complicated skin and skin structure infections due to MRSA, and nosocomial pneumonia (including ventilator-associated pneumonia) due to suspected or proven MRSA, and community-acquired pneumonia. The US FDA has granted fast-track status to the compound for these two indications. Phase III results are expected in 2006 and an NDA is expected to be submitted to the FDA in 2007. An additional pivotal phase III trial (STRAUSS 2, STudy of Resistant Staphyloccocus aureus in Skin and Skin structure infections) of Ceftobiprole medocaril was initiated in October 2005 for complicated skin infections, including diabetic foot infections. This trial will be conducted in conjunction with Johnson & Johnson Pharmaceutical Research and Development.