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Journal of Antimicrobial Chemotherapy (2000) 46, 629-632
© 2000 The British Society for Antimicrobial Chemotherapy

Brief report

Efficacy of a novel tetracycline derivative, glycylcycline, against penicillin-resistant Streptococcus pneumoniae in a mouse model of pneumonia

Kenichiro Murakami, Kazuhiro Tateda*, Tetsuya Matsumoto, Shuichi Miyazaki and Keizo Yamaguchi

Department of Microbiology, Toho University School of Medicine, 5-21-16 Ohmori-nishi, Ohta-ku, Tokyo 143-8540, Japan

The MIC90 of glycylcycline (<=0.06 mg/L) against 55 strains of Streptococcus pneumoniae was 100-fold lower than that of minocycline or tetracycline. In a mouse model of penicillin-resistant S. pneumoniae (PRSP) pneumonia, glycylcycline (10 mg/kg) decreased bacterial counts in the lungs from 106 cfu to <102 cfu, whereas no apparent reduction of bacterial numbers was observed with minocycline or penicillin G. Pharmacokinetic studies showed that the half-life and area under the curve of glycylcycline were superior to those of minocycline and penicillin G in the lungs. These results show a preferential distribution of glycylcycline in the lungs and potent in vivo bactericidal activity in PRSP pneumonia.

*Corresponding author. Tel: +81-3-3762-4151; Fax: +81-3-5493-5415; E-mail: address:kazu{at}med.toho-u.ac.jp


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