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CAS NO:
1286218-63-0
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Basic Info
CAS Number
1286218-63-0
Pharmacopoeia
ChP
Grade
In-house Standards
Is Manufacturer
YES
Packaging & Delivery
Minimum Order Quantity
Any
Delivery Cycle
Negotiable
Product Description
Reference Standards &Impurity
AI Product Description
*The following content is generated by AI and is for reference only.
Ceftaroline fosamil is a novel intravenous cephalosporin antibiotic belonging to the fifth-generation class, specifically designed to combat methicillin-resistant Staphylococcus aureus (MRSA) and other multidrug-resistant Gram-positive pathogens. As a prodrug, ceftaroline fosamil itself possesses no antibacterial activity; upon intravenous administration, it undergoes rapid enzymatic hydrolysis by plasma esterases to release the active moiety, ceftaroline. The molecular formula of the active drug ceftaroline is C24H28N6O7S3, while the fosamil salt form used in commercial preparations typically carries the formula C29H35N6O10P3S3. Its unique chemical structure features a dihydrothiazine ring fused with a beta-lactam core, modified with a specific side chain that enables high-affinity binding to penicillin-binding protein 2a (PBP2a), a key enzyme responsible for beta-lactam resistance in MRSA. This mechanism distinguishes it from earlier generations of cephalosporins, which are ineffective against PBP2a-containing organisms.
The primary clinical indication for ceftaroline fosamil includes the treatment of acute bacterial skin and skin structure infections (ABSSSI) caused by susceptible strains of S. aureus, including MRSA, as well as community-acquired bacterial pneumonia (CABP). It demonstrates broad-spectrum activity against both Gram-positive bacteria, such as Streptococcus pneumoniae and Streptococcus pyogenes, and select Gram-negative organisms like Haemophilus influenzae and Klebsiella pneumoniae. However, it lacks activity against anaerobes and most Pseudomonas species. Approved by regulatory agencies globally, ceftaroline represents a critical therapeutic advance in managing severe infections where vancomycin resistance or intolerance is a concern. Common adverse effects include nausea, diarrhea, headache, and injection site reactions, with rare instances of hypersensitivity reported. Due to its stability in blood and ability to penetrate tissues effectively, it has become a cornerstone agent in hospital formularies for empiric therapy of serious skin and respiratory infections, offering a valuable alternative in the fight against escalating antimicrobial resistance.
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