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Susceptibility

In Vitro and In Vivo Properties of Ro 63-9141, a Novel Broad-Spectrum Cephalosporin with Activity against Methicillin-Resistant Staphylococci

Paul Hebeisen, Ingrid Heinze-Krauss, Peter Angehrn, Peter Hohl, Malcolm G. P. Page, Rudolf L. Then
Paul Hebeisen
Pharmaceutical Research, F. Hoffmann-La Roche Ltd., and
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Ingrid Heinze-Krauss
Basilea Pharmaceutica, CH-4070 Basel, Switzerland
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Peter Angehrn
Pharmaceutical Research, F. Hoffmann-La Roche Ltd., and
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Peter Hohl
Pharmaceutical Research, F. Hoffmann-La Roche Ltd., and
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Malcolm G. P. Page
Basilea Pharmaceutica, CH-4070 Basel, Switzerland
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Rudolf L. Then
Pharmaceutical Research, F. Hoffmann-La Roche Ltd., and
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DOI: 10.1128/AAC.45.3.825-836.2001
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ABSTRACT

Ro 63-9141 is a new member of the pyrrolidinone-3-ylidenemethyl cephem series of cephalosporins. Its antibacterial spectrum was evaluated against significant gram-positive and gram-negative pathogens in comparison with those of reference drugs, including cefotaxime, cefepime, meropenem, and ciprofloxacin. Ro 63-9141 showed high antibacterial in vitro activity against gram-positive bacteria except ampicillin-resistant enterococci, particularly vancomycin-resistant strains of Enterococcus faecium. Its MIC at which 90% of the isolates tested were inhibited (MIC90) for methicillin-resistant Staphylococcus aureus (MRSA) was 4 μg/ml. Ro 63-9141 was bactericidal against MRSA. Development of resistance to the new compound in MRSA was not observed. Ro 63-9141 was more potent than cefotaxime against penicillin-resistant Streptococcus pneumoniae(MIC90 = 2 μg/ml). It was active against ceftazidime-susceptible strains of Pseudomonas aeruginosaand against Enterobacteriaceae except Proteus vulgaris and some isolates producing extended-spectrum β-lactamases. The basis for the antibacterial spectrum of Ro 63-9141 lies in its affinity to essential penicillin-binding proteins, including PBP 2′ of MRSA, and its stability towards β-lactamases. The in vivo findings were in accordance with the in vitro susceptibilities of the pathogens. These data suggest the potential utility of Ro 63-9141 for the therapy of infections caused by susceptible pathogens, including MRSA. Since insufficient solubility of Ro 63-9141 itself precludes parenteral administration in humans, a water-soluble prodrug, Ro 65-5788, is considered for development.

  • Copyright © 2001 American Society for Microbiology
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In Vitro and In Vivo Properties of Ro 63-9141, a Novel Broad-Spectrum Cephalosporin with Activity against Methicillin-Resistant Staphylococci
Paul Hebeisen, Ingrid Heinze-Krauss, Peter Angehrn, Peter Hohl, Malcolm G. P. Page, Rudolf L. Then
Antimicrobial Agents and Chemotherapy Mar 2001, 45 (3) 825-836; DOI: 10.1128/AAC.45.3.825-836.2001

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In Vitro and In Vivo Properties of Ro 63-9141, a Novel Broad-Spectrum Cephalosporin with Activity against Methicillin-Resistant Staphylococci
Paul Hebeisen, Ingrid Heinze-Krauss, Peter Angehrn, Peter Hohl, Malcolm G. P. Page, Rudolf L. Then
Antimicrobial Agents and Chemotherapy Mar 2001, 45 (3) 825-836; DOI: 10.1128/AAC.45.3.825-836.2001
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KEYWORDS

Bacterial Proteins
cephalosporins
Hexosyltransferases
methicillin resistance
Peptidyl Transferases
Staphylococcus aureus

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