Antimicrobial activity of Ro 23-9424, a novel ester-linked codrug of fleroxacin and desacetylcefotaxime.

Antimicrobial Agents and Chemotherapy
R N JonesC Thornsberry

Abstract

Ro 23-9424 is a novel ester-linked codrug of fleroxacin (Ro 23-6240; AM-833) and the cefotaxime metabolite desacetylcefotaxime. Its potency was determined against over 1,000 organisms and found to be intermediate between those of the two components. More than 99% of members of the family Enterobacteriaceae were inhibited by greater than or equal micrograms of Ro 23-9424 per ml; its MIC for 50% of strains tested ranged from greater than or equal to 0.06 to 1 micrograms/ml. Staphylococci, streptococci, Branhamella catarrhalis, Corynebacterium jeikeium, Bacillus spp., Haemophilus influenzae, Listeria monocytogenes, and the pathogenic Neisseria spp., including oxacillin-resistant Staphylococcus aureus, beta-lactamase-producing strains, and penicillin-resistant pneumococci, were also inhibited by Ro 23-9424. Pseudomonas aeruginosa, Enterococcus spp., and Bacteroides fragilis group isolates were more refractory to Ro 23-9424 (the MIC for 90% of strains tested was less than or equal to 32 micrograms/ml). Overall, Ro 23-9424 inhibited 97% of the aerobic strains, compared with 90% for ceftazidime and 92% for cefoperazone. Ro 23-9424 was bactericidal, was relatively stable to inoculum effects on MICs at 10(7) CFU/ml, and was determined t...Continue Reading

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Citations

Oct 1, 1993·Journal of Clinical Pharmacology·S M QadriB A Cunha
Jun 1, 1990·European Journal of Clinical Microbiology & Infectious Diseases : Official Publication of the European Society of Clinical Microbiology·R N Jones
Jan 1, 1990·Pharmacology & Therapeutics·S Rádl
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Jan 1, 1994·Diagnostic Microbiology and Infectious Disease·R N Jones, M L Sanchez
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Oct 1, 1990·Antimicrobial Agents and Chemotherapy·J G ChristensonA Specian
Jul 5, 2005·Expert Opinion on Investigational Drugs·A Dalhoff
Jul 2, 2005·Expert Opinion on Investigational Drugs·A Bryskier
Nov 6, 2015·Molecular Biology and Evolution·Kathy K WangRoy Kishony
May 10, 2016·Expert Opinion on Drug Delivery·Ibrahim A AljuffaliJia-You Fang
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Jul 1, 2008·Expert Review of Clinical Pharmacology·Marion Skalweit Helfand
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