Laboratory and clinical evaluation of S-1108 for respiratory tract infections

Junko Miyamoto, Yuko Yoshitomi, Yasuhito Higashiyama, Haruko Matsuda, Kotaro Mitsutake, Yoshitsugu Miyazaki, Kenichi Tanaka, Masanori Iwamoto, Shigefumi Maesaki, Hironobu Koga, Shigeru Kohno, Kohei Hara, Chikako Mochida, Kazuyuki Sugawara, Mitsuo Kaku, Yasumasa Dotsu, Toshiaki Hayashi, Naomi Ito, Kazuo Sasayama

Research output: Contribution to journalArticlepeer-review

Abstract

A newly developed broad-spectrum cephem, S-1108, was evaluated in vitro and in vivo. The results were as follows. 1. Antimicrobial activity : Minimal inhibitory concentrations (MICs) against 3 standard strains and 298 clinical isolates, including 10 different species, were determined and compared with three other antibiotics, CFTM, CTM and CCL. S-1006, an active form of S-1108, showed excellent antimicrobial activity against both gram-positive and gram-negative bacteria, except E. cloacae and P. aeruginosa, and the MICs were the same or greater than those of the other three drugs. 2. S-1006 concentration in serum and sputum : Two patients with chronic bronchitis were given 200 mg of S-1108 orally, and its concentrations in serum and sputum were measured at intervals using HPLC or bioassay. The peak concentrations of S-1006 in serum were 2. 42μg/ml and 2.94μg/ml, while, the peak concentration in sputum was 0.07 μg/ml in the former patient, and the penetration ratio was 2.9%. 3. Clinical efficacy and adverse reactions : Eighteen patients with respiratory tract infections were treated with S-1108, and the overall efficacy ratio was 83.3% (excellent in 3 cases, good in 12, fair in 2 and poor in 1). Adverse reactions were cutaneous pruritus in one patient, anorexia in 1, nausea in 1 and diarrhea in 1. Elevation of CPK was observed in 1 case as an abnormal laboratory finding. All of the above were mild and improved repidly after completion of S-1108 treatment, indicating that S-1108 is a very safe agent.

Original languageEnglish
Pages (from-to)341-348
Number of pages8
JournalChemotherapy
Volume41
DOIs
Publication statusPublished - 1993
Externally publishedYes

ASJC Scopus subject areas

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

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