Cefuroxime axetil

Cefuroxime axetil is an orally effective broad-spectrum β-lactam antibiotic that targets bacterial penicillin-binding proteins (PBPs, such as PBP3 and PBP1). Cefuroxime axetil inhibits cell wall synthesis, leading to bacterial lysis and death, with a minimum inhibitory concentration (MIC) of 0.12-4 mg/L for non-typeable Haemophilus influenzae (NTHi). Cefuroxime axetil is hydrolyzed by esterase to the active ingredient Cefuroxime (HY-B1256A) after oral absorption. Topical administration of Cefuroxime via bioadhesive nanoparticles (BNPs) can prolong the drug's retention time in the middle ear (≥7 days). Cefuroxime axetil can be used in the study of otitis media (especially NTHi infection). Cefuroxime axetil can achieve precise antibacterial effects through oral or topical nano-delivery systems, reducing systemic exposure and the risk of antibiotic resistance^[1][2][3]. In Vitro:Kinase activity assay:
Cefuroxime axetil has a potent inhibitory effect on penicillin-binding proteins (PBPs) of Gram-positive bacteria (such as Streptococcus pneumoniae and Streptococcus pyogenes) and Gram-negative bacteria (such as Haemophilus influenzae and Moraxella catarrhalis). The MIC₉₀ for penicillin-sensitive Streptococcus pneumoniae is ≤0.25 mg/L, and the MIC₉₀ for β-lactamase-producing Haemophilus influenzae and Moraxella catarrhalis are 1-2 mg/L and 0.5 mg/L, respectively[1].
In vitro antibacterial tests:
Cefuroxime axetil has limited activity against penicillin-resistant Streptococcus pneumoniae (MIC₉₀=2-8 mg/L) and methicillin-susceptible Staphylococcus aureus (MIC₉₀=2-4 mg/L), with highly sensitive to Neisseria gonorrhoeae (MIC₉₀=0.06-0.125 mg/L)^[1].
In Vivo:Acute otitis media mouse model:
Cefuroxime axetil (30 mg/kg; oral gavage; twice daily; 5-10 days) significantly inhibits the bacterial load in the middle ear in the acute otitis media model induced by non-typical Haemophilus influenzae (NTHi) in C57BL/6J female mice (6-8 weeks old). The middle ear effusion disappeares after 7 days, and histopathology shows a significant reduction in inflammation. The blood concentration is below the detection limit without systemic toxicity^[1].
Community-acquired pneumonia (CAP) rat model:
Cefuroxime axetil (20 mg/kg/day; oral; twice daily; 7-14 days) shows comparable bacterial clearance to the control group in the adult rat CAP model compared with sequential treatment with intravenous cefuroxime (HY-B1256A) with good gastrointestinal tolerance^[1].