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Antimicrobial Agents and Chemotherapy, January 2004, p. 53-62, Vol. 48, No. 1
0066-4804/04/$08.00+0     DOI: 10.1128/AAC.48.1.53-62.2004
Copyright © 2004, American Society for Microbiology. All Rights Reserved.

In Vitro Activities of the Novel Cephalosporin LB 11058 against Multidrug-Resistant Staphylococci and Streptococci

The JONES Group/JMI Laboratories, North Liberty, Iowa,¹ Universidade Federal de São Paulo, São Paulo, Brazil,² Tufts University School of Medicine, Boston, Massachusetts³

Received 5 June 2003/ Returned for modification 7 August 2003/ Accepted 3 October 2003

LB 11058 is a novel parenteral cephalosporin with a C-3 pyrimidinyl-substituted vinyl sulfide group and a C-7 2-amino-5-chloro-1,3-thiazole group. This study evaluated the in vitro activity and spectrum of LB 11058 against 1,245 recent clinical isolates, including a subset of gram-positive strains with specific resistant phenotypes. LB 11058 was very active against Streptococcus pneumoniae. The novel cephalosporin was 8- to 16-fold more potent than ceftriaxone, cefepime, or amoxicillin-clavulanate against both penicillin-intermediate and -resistant S. pneumoniae. LB 11058 was also very active against both ß-hemolytic streptococci (MIC at which 90% of isolates were inhibited [MIC₉₀], 0.008 µg/ml) and viridans group streptococci (MIC₉₀, 0.03 to 0.5 µg/ml), including penicillin-resistant strains. Among oxacillin-susceptible Staphylococcus aureus, LB 11058 MIC results varied from 0.06 to 0.25 µg/ml (MIC₅₀, 0.12 µg/ml), while among oxacillin-resistant strains LB 11058 MICs varied from 0.25 to 1 µg/ml (MIC₅₀, 1 µg/ml). Coagulase-negative staphylococci showed an LB 11058 susceptibility pattern similar to that of S. aureus, with all isolates being inhibited at 1 µg/ml. LB 11058 also showed reasonable in vitro activity against Enterococcus faecalis, including vancomycin-resistant strains (MIC₅₀, 1 µg/ml), and Bacillus spp. (MIC₅₀, 0.25 µg/ml); however, it was less active against Enterococcus faecium (MIC₅₀, >64 µg/ml) and Corynebacterium spp. (MIC₅₀, 32 µg/ml). Against gram-negative pathogens, LB 11058 showed activity against Haemophilus influenzae (MIC₉₀, 0.25 to 0.5 µg/ml) and Moraxella catarrhalis (MIC₉₀, 0.25 µg/ml), with MICs not influenced by ß-lactamase production. In conclusion, LB 11058 demonstrated a broad antibacterial spectrum and was highly active against gram-positive bacteria, particularly against multidrug-resistant staphylococci and streptococci.

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