Cefditoren sodium

Cefditoren sodium (ME 1206) is a broad-spectrum, third-generation, oral cephalosporin antibacterial with enhanced stability against many common β lactamases. Cefditoren sodium has activity against Gram-negative organisms and Gram-positive organisms. Cefditoren sodium can be used in the research of infection diseases such as acute exacerbations of chronic bronchitis, community-acquired pneumonia (CAP), streptococcal pharyngitis/tonsillitis, or uncomplicated skin and skin structure infections[1][2].

Cefditoren (sodium) shows good activity against pneumoniae, S. pyogenes, Staphylococcus aureus, H. influenzae and H. parainfluenzae, M. catarrhalis[1]. Organism MIC50 (mg/L) MIC90 (mg/L) susceptible (%) Gram-positive organisms Streptococcus pneumoniae(untyped)a 0.015-0.25 0.12-1 PS ≤0.008-0.03 0.015-0.25 99-100 PI 0.06-0.5 0.25-0.5 94-100 PR 0.25-1 0.5-2 7-100 S. pyogenes ≤0.008-0.03 0.015-0.03 100 Staphylococcus aureus (MS) 0.12-0.5 0.5-1 50-100 Gram-negative organisms Haemophilus ≤0.008-≤0.03 0.015-0.13 influenzae (untyped)b β-Lactamase + ≤0.008-0.03 0.015-0.06 100 β-Lactamase - ≤0.008-0.03 0.015-0.06 100 H. parainfluenzaeb ≤0.03 0.06 Moraxella 0.03-0.5 0.25-1 96 catarrhalis (untyped)b β-Lactamase + ≤0.03-0.25 0.12-0.5 100 β-Lactamase - ≤0.008-0.03 0.015-0.06 100 a Including PS, PI and PR strains.b Including both β-lactamase-positive and -negative strains.MIC50/90=mean minimum inhibitory concentrations required to inhibit the growth of 50% or 90% of bacterial strains; MS=susceptible to meticillin; PI=intermediate susceptibility to penicillin; PR=resistant to penicillin; PS=susceptible to penicillin.

Pharmacokinetics in mice[1]: Cefditoren (mg/kg) C0 (&#181g/ml) t1/2 (h) AUClast (&#181g× h/ml) Tlast (h) 6.25 53.0 0.9 30.4 6 12.5 168.4 1.1 64.1 8 25 232.5 0.9 101.3 8 50 290.6 1.1 124.4 8

[1]. Wellington K, et al. Cefditoren pivoxil: a review of its use in the treatment of bacterial infections. Drugs. 2004;64(22):2597-618.
[2]. Cafini F, et al. Enhanced in vivo activity of cefditoren in pre-immunized mice against penicillin-resistant S. pneumoniae (serotypes 6B, 19F and 23F) in a sepsis model. PLoS One. 2010 Aug 10;5(8):e12041.