In vitro antimicrobial activity and therapeutic efficacy in lower respiratory tract infections of CS-807

Akira Watanabe, Kohtaro Ohizumi, Masako Sasaki, Seiichi Aonuma, Kikuo Ohnuma, Reiko Ono, Yoshihiro Honda, Kiyoshi Konno

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    1 Citation (Scopus)


    CS-807, an ester derivative of R-3763, has been developed in Japan as a new cephem for oral use. We investigated the in vitro antimicrobial activity of R-3746, a sodium salt of R-3763, by broth dilution method using the Dynatech MIC 2000 system, and evaluated its therapeutic efficacy in lower respiratory tract infections. The minimum inhibitory concentrations (MIC's) of R-3746, cefaclor (CCL), cefixime (CFIX) and amoxicillin (AMPC) against 165 clinical isolates consisting of 20 strains each of S. aureus, B. catarrhalis, E. coli, K. pneumoniae, E. cloacae, S. marcescens and P. aeruginosa, and 25 of H. influenzae were determined. Results: we found that against S. aureus, R-3746 was more active than CFIX, and as active as CCL and AMPC. Against H. influenzae and B. catarrhalis, R-3746 was somewhat less active than CFIX, but much more so than CCL and AMPC. R-3746 was almost as active as CFIX against E. coli, K. pneumoniae, E. cloacae and S. marcescens. On the other hand, R-3746 was less active against P. aeruginosa, MIC's being above 100μg/ml against all the strains tested, except one. A daily dose of 200 or 400mg of CS-807 was administered orally to 9 patients: acute bronchitis 1, acute pneumonia 2, infected bronchiectasis 5, and infection in association with pulmonary emphysema 1. Clinical effects were excellent in 1 patient, good in 6, fair in 1 and poor in 1. Six strains of H. influenzae and one each of S. aureus and S. pneumoniae were identified as causative organisms. All were eradicated by CS-807. Neither adverse reactions nor abnormal laboratory data were observed. From the above results, we conclude that CS-807 is a most useful antibiotic for the oral treatment of lower respiratory tract infections.

    Original languageEnglish
    Pages (from-to)375-385
    Number of pages11
    Publication statusPublished - 1988 Jan 1

    ASJC Scopus subject areas

    • Pharmacology (medical)
    • Infectious Diseases
    • Pharmacology
    • Drug Discovery
    • Oncology


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