Basic and clinical studies on S-1108

Yoshiro Sawae, Kaoru Okada, Yukio Kumagai, Toshiyuki Ishimaru, Koji Takaki, Nobuyuki Shimono, Hiroyasu Misumi, Katsuhiko Eguchi, Satoshi Kuboi, Yoshiyuki Niho

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Abstract

We performed basic and clinical studies on S-1108, a new oral cephalosporin antibiotic, with the following results. 1) Antimicrobial activity The MICs of S-1006, the active substance of S-1108, were determined with an inoculum size of 106 cells/ml. The MIC90 of S-1006 was 0. 78μg/ml for Staphylococcus aureus, 100< for Enterococcus faecalis, 0.78 for Escherichia coli, 6.25 for Klebsiella pneumoniae, 25 for Enterobacter spp., 50 for Serratia marcescens and Citrobacter freundii, and 100 for Pseudomonas aeruginosa. Its activity against S. aureus was greater than that of the new oral cephems. On the other hand, its activity against gram-negative bacilli was the same as that of the new oral cephems and there were few strains highly-resistant to S-1006. 2) Clinical efficacy Four patients with pneumonia, 2 with acute bronchitis, 5 with chronic bronchitis, 2 with tonsillitis, and 1 with cystitis were treated with S-1108, The patients were treated with a daily dose of 150-600 mg for 2-40 days. The clinical response was excellent in 3, good in 5, fair in 3, poor in 1, and unknown in one patient. The efficacy rate was 69.3%. Adverse reactions were dysphoria (1 patient), and swelling of the vulva and nipple (1 patient), but there were no changes in the laboratory findings.

Original languageEnglish
Pages (from-to)326-333
Number of pages8
JournalChemotherapy
Volume41
DOIs
Publication statusPublished - Jan 1 1993

All Science Journal Classification (ASJC) codes

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

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    Sawae, Y., Okada, K., Kumagai, Y., Ishimaru, T., Takaki, K., Shimono, N., Misumi, H., Eguchi, K., Kuboi, S., & Niho, Y. (1993). Basic and clinical studies on S-1108. Chemotherapy, 41, 326-333. https://doi.org/10.11250/chemotherapy1953.41.Supplement1_326