Laboratory and clinical studies on MT-141 a new cephamycin antibiotic

Yoshiteru Shigeno, Hiroko Nakazato, Hideaki Shigeno, Hironobu Koga, Masao Nagasawa, Kenji Mori, Yoshiaki Fukuda, Hiroshi Tomita, Koichi Watanabe, Hikaru Tanaka, Toshiaki Hayashi, Kiyo Fujita, Yoji Suzuyama, Atsushi Saito, Kohei Hara, Masumi Matsuse, Mitsuo Kaku, Kazuyuki Sugawara, Chikako Mochida, Keizo YamaguchiHiroyuki Okada, Hirosuke Ohta, Toshiro Oda, Isao Nakamura, Nobuharu Ohe, Kenji Kawano, Mikio Oka, Yukinobu Mishima

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Abstract

Laboratory and clinical studies on MT-141, a newly developed cephamycin antibiotic, were carried out with the following results. 1) Antibacterial activity : The in vitro antibacterial activity of MT-141 was tested by microbroth dilution method. The minimum inhibitory concentrations (MICs) against total 372 strains consisting of 30 standard strains and 240 clinical isolates including S. aureus 30, S.faecalis 30, E.coli 30, K. aerogenes 30, E. cloacae 29, P.mirabilis 30, P. vulgaris 30, S.marcescens 30, P. aeruginosa 30, A. anitratus 30, H. influenzae 43 were compared with those of cefazolin (CEZ), cefmetazole (CMZ) and cefo-perazone (CPZ). Antibacterial activities of MT-141 against S. aureus and S.faecalis were less potent than those of CEZ, CMZ and CPZ. On the other hand, it was strongest among antibiotics tested against E. coli, K. aerogenes, P. mirabilis, P.vulgaris and A. anitratus. CPZ was most active against H. influenzae, E. cloacae, S. marcescens, P. aeruginosa, and MT-141 followed. 2) Serum and sputum levels in chronic bronchitis : Four patients with chronic bronchitis were subjected to this study. After a dose of 1 gr. of MT-141 was given to them by intravenous drip infusion for 1 hour, their levels in sera and sputa were measured by bioassay method. As the results, peak serum levels were obtained at the end of DIV showing values of 89.5 to 100. 8 μg/ml, and serum levels after 6 hours showed values of 12. 8 to 34. 9 μg/ml. On the other hand, concentrations in sputa reached their peaks at 1 to 2 hours after administration in two cases with purulent sputum and theirit values were 0.38 and 0. 48 μg/ml. But in one case with muco-purulent sputum the value was under the limit of measurement, and in one case with bloody sputum the value was 23. 0 μg/ml. 3) Clinical effect and adverse reactions : Twenty three patients with respiratory infections (pneumonia 16, chronic bronchitis 4, bronchiectasis 3) were treated with 1 to 2 gr. of MT-141 daily for 5 to 34 days by intravenous drip infusion. Eighteen of 23 patients responded satisfactorily to the treatment and the efficacy rate was 78.3% (excellent 4, good 14, fair 3, poor 2). Subjective and objective symptoms, hematological and biochemical data and renal functions were checked up before and after administration of MT-141. Five cases in total showed the following adverse reactions : slight elevations of S-GOT in 2, that of BUN in 1, transient eosinophilia in 1 and anemia in 1. These abnormal values returned to normal after discontinuation of the drug.

Original languageEnglish
Pages (from-to)290-302
Number of pages13
JournalChemotherapy
Volume32
DOIs
Publication statusPublished - 1984 Jan

ASJC Scopus subject areas

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

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  • Cite this

    Shigeno, Y., Nakazato, H., Shigeno, H., Koga, H., Nagasawa, M., Mori, K., Fukuda, Y., Tomita, H., Watanabe, K., Tanaka, H., Hayashi, T., Fujita, K., Suzuyama, Y., Saito, A., Hara, K., Matsuse, M., Kaku, M., Sugawara, K., Mochida, C., ... Mishima, Y. (1984). Laboratory and clinical studies on MT-141 a new cephamycin antibiotic. Chemotherapy, 32, 290-302. https://doi.org/10.11250/chemotherapy1953.32.Supplement5_290