Overview
Cefobiprole is a fifth-generation cephalosporin antibiotic developed for its broad-spectrum activity against resistant bacteria, including methicillin-resistant Staphylococcus aureus (MRSA). It belongs to the beta-lactam class and is administered intravenously as its prodrug, cefobiprole medocaril. The drug was designed to address the growing need for effective treatments against multidrug-resistant pathogens. Unlike earlier cephalosporins, cefobiprole exhibits enhanced binding affinity to penicillin-binding proteins (PBPs) in Gram-positive bacteria, including MRSA, while maintaining efficacy against many Gram-negative strains. Its unique structure provides stability against certain beta-lactamases, making it a valuable option in hospital-acquired infections.
Physical and Chemical Properties
Cefobiprole is a white to off-white crystalline powder with a molecular weight of 534.57 g/mol. It is soluble in water and polar organic solvents like DMSO, facilitating its formulation for intravenous use. The drug's stability is pH-dependent, with optimal storage recommended at 2-8°C to prevent degradation. Its chemical structure includes a cephalosporin core with side chains that enhance PBP binding and beta-lactamase resistance. The prodrug, cefobiprole medocaril, is hydrolyzed in vivo to release the active compound. Analytical methods such as HPLC are commonly employed for purity testing in pharmaceutical production.
Main Applications
Cefobiprole is clinically indicated for complicated skin and soft tissue infections (cSSTI), including diabetic foot infections and wound infections involving MRSA. Its broad-spectrum activity also shows promise in treating pneumonia caused by drug-resistant Streptococcus pneumoniae and Pseudomonas aeruginosa. In hospital settings, it serves as a reserve antibiotic to reduce the risk of resistance development. Ongoing research explores its potential in bacteremia and bone/joint infections, though regulatory approvals vary by region. Combination therapies with other antibiotics are under investigation to expand its utility.
Safety and Storage
Hypersensitivity reactions, including anaphylaxis, are the primary safety concern, particularly in patients with penicillin or cephalosporin allergies. Common side effects include nausea, headache, and elevated liver enzymes. Renal function monitoring is advised due to partial renal excretion. The drug requires strict storage conditions: refrigerated (2-8°C) in original packaging to avoid light exposure. Reconstituted solutions are stable for up to 24 hours at room temperature. Disposal should follow hazardous waste protocols to minimize environmental impact.
B2B Procurement Guide
Pharmaceutical-grade cefobiprole must meet pharmacopoeial standards (USP/EP) for purity (>98%) and endotoxin levels. Buyers should verify suppliers' Good Manufacturing Practice (GMP) certifications and batch testing reports. Bulk procurement typically involves negotiations on lead times and cold-chain logistics. Prices vary by order volume and region, with generic versions increasingly available post-patent expiry. Importers must ensure compliance with local regulatory requirements, including import licenses for controlled substances. Long-term contracts with quality-focused suppliers are recommended to ensure consistency.
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