Affiliation:
1. Department of Pathology, Hershey Medical Center, Hershey, Pennsylvania 17033
2. Basilea Pharmaceutica AG, Basel, Switzerland
Abstract
ABSTRACT
Ceftobiprole (formerly BAL9141), the active component of the prodrug BAL5788 (ceftobiprole medocaril), is a novel cephalosporin with expanded activity against gram-positive bacteria. Among 152
Staphylococcus aureus
isolates, including 5 vancomycin-intermediate and 2 vancomycin-resistant strains, MIC
50
and MIC
90
values for ceftobiprole were each 0.5 μg/ml against methicillin-susceptible strains and 2 μg/ml against methicillin-resistant strains. Against 151 coagulase-negative staphylococci (including 4 vancomycin-intermediate strains), MIC
50
and MIC
90
values were, respectively, 0.125 μg/ml and 1 μg/ml against methicillin-susceptible and 1 μg/ml and 2 μg/ml against methicillin-resistant strains. Teicoplanin was less active than vancomycin against coagulase-negative strains. Linezolid, quinupristin-dalfopristin, and daptomycin were active against all strains, whereas increased MICs for amoxicillin-clavulanate, cefazolin, minocycline, gentamicin, trimethoprim-sulfamethoxazole, levofloxacin, rifampin, mupirocin, fusidic acid, and fosfomycin were sometimes observed. At 2× MIC, ceftobiprole was bactericidal against 11 of 12 test strains by 24 h. Prolonged serial passage in the presence of subinhibitory concentrations of ceftobiprole failed to select for clones with MICs >4 times those of the parents; the maximum MIC achieved for ceftobiprole after 50 passages (in 1 of 10 strains) was 8 μg/ml. Single-passage selections showed very low frequencies of resistance to ceftobiprole irrespective of genotype or phenotype; the maximal ceftobiprole MIC of recovered clones was 8 μg/ml.
Publisher
American Society for Microbiology
Subject
Infectious Diseases,Pharmacology (medical),Pharmacology
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