Laboratory and clinical studies on TMS-19-Q

Munetaka Komori, Hlroko Nakazato, Masao Nagasawa, Hlronobu Koga, Koichi Watanabe, Yoshiaki Fukuda, Hiroshi Tomita, Naomi Ito, Katsuhiko Sawatari, Yoshiteru Shigeno, Yoji Suzuyama, Kinichi Izumikawa, Atsushi Saito, Kohei Hara, Kazuyuki Sugawara, Chikako Mochida, Mitsuo Kaku, Keizo Yamaguchi, Hiromaru Iwasaki, Tsuneo TsutsumiAkira Ikebe, Masamoto Nakano, Kazuhiro Okuno, Rokushi Oka, Tsunetoshi Koteda, Takashi Ishizaki, Toshiyuki Oye, Masao Sai, Haruji Ohmagari

Research output: Contribution to journalArticlepeer-review

3 Citations (Scopus)

Abstract

Laboratory and clinical studies on TMS-19-Q, a new macrolide antibiotic, were carried out and the results were as follows 1) Antimicrobial activity The minimal inhibitory concentrations (MICs) of TMS-19-Q against 50 clinical isolates of Mycoplasma pneumoniae (M. pneumoniae) ranged from 0.0035 to 0. 06 μg/ml. The peak MIC of TMS-19-Q was 0. 015 μg/ml, which was superior to those of josamycin (JM) and oleandomycin (OL). The growth inhibitory effect of TMS-19-Q against M. pneumoniae in test tube revealed bactericidal activity in the concentration of 0.5 and 1.0 μg/ml. In the treatment of hamster experimentally infected with M. pneumoniae the viable organisms in the lungs decreased to 102cells/ml on the 3rd day. On the 10 th day of drug treatment, 80% (8 out of 10) of the hamsters receiving TMS-19-Q showed no viable M. pneumoniae cells upon the culture of their lungs. The antimicrobial activity of TMS-19-Q against 50 strains of Legionella pneumophila was almost same as that of erythromycin (EM). The MICs of TMS-19-Q against 155 clinical isolates (Streptococcus pneumoniae 47, Streptococcus pyogenes 54, Streptococcus faecalis 27 and Staphylococcus epidermidis 27) were compared with those of JM and EM. The antibacterial activity of TMS-19-Q was superior to that of JM and was almost equal to that of EM. 2) Absorption and excretion in humans The average peak plasma level of TMS-19-Q in six healthy adult volunteers after single oral dosage of 600 mg with TMS-19-Q·O tablet was 0. 5 μg/ml; while same dosage of TMS-19-Q with GC tablet to same volunteers yielded an average peak plasma level of 1.8 μg/ml. When TMS-19-Q·GC tablet (600mg) was given to four patients with chronic respiratory tract infections, the peak sputum level was 0. 38 μg/ml and the urinary excretion rate was about 3% on average. 3) Clinical evaluation and adverse reaction Twenty-nine patients with respiratory tract infections were treated with TMS-19-Q·GC tablet at daily dose of 600mg for 4 to 19 days. In clinical response of 29 patients, excellent was 10, good was 15, fair was 2, poor was 2. Over all efficacy rate was 86. 2%. Neither side effects nor changes in laboratory data attributable to the drug were observed in these patients.

Original languageEnglish
Pages (from-to)346-357
Number of pages12
JournalChemotherapy
Volume32
DOIs
Publication statusPublished - 1984 Jan

ASJC Scopus subject areas

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

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