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Antimicrobial Agents and Chemotherapy, March 1998, p. 555-563, Vol. 42, No. 3
0066-4804/98/$04.00+0
Copyright © 1998, American Society for Microbiology. All rights reserved.

In Vitro and In Vivo Antibacterial Activities of CS-834, a New Oral Carbapenem

Keizo Yamaguchi,* Haruki Domon, Shuichi Miyazaki, Kazuhiro Tateda, Akira Ohno, Kazuhiro Ishii, Tetsuya Matsumoto, and Nobuhiko Furuya

Department of Microbiology, Toho University School of Medicine, Omori-nishi, 5-21-16, Ota-ku, Tokyo 143, Japan

Received 29 September 1997/Returned for modification 5 November 1997/Accepted 18 December 1997

CS-834 is a prodrug of the carbapenem R-95867, developed by Sankyo Co., Ltd., Tokyo, Japan. To investigate the possibility that CS-834 may be the first carbapenem usable in an oral dosage form, its in vitro antibacterial activity (as R-95867) and in vivo antibacterial activity were compared with those of cefpodoxime proxetil, cefditoren pivoxil, cefdinir, ofloxacin, imipenem, and amoxicillin. R-95867 had high levels of activity against methicillin-susceptible staphylococci and streptococci, including penicillin-resistant Streptococcus pneumoniae, as well as Neisseria gonorrhoeae, Moraxella catarrhalis, the members of the family Enterobacteriaceae (with the exception of Serratia marcescens), Haemophilus influenzae, and Bordetella pertussis; for all these strains, the MICs at which 90% of tested strains are inhibited (MIC90s) were 1.0 µg/ml or less. Against methicillin-resistant staphylococci, enterococci, Serratia marcescens, Brukholderia cepacia, Stenotrophomonas maltophilia, and Acinetobacter calcoaceticus, R-95867 showed activity comparable to or slightly less than that of imipenem, with MIC90s ranging from 2 to >128 µg/ml. The in vivo efficacy of oral CS-834 against experimental mouse septicemia caused by gram-positive and gram-negative bacteria was better than that of comparative drugs. In murine respiratory infection models, the efficacy of CS-834 reflected not only its potent in vitro activity but also the high levels present in the lungs.

* Corresponding author. Mailing address: Department of Microbiology, Toho University School of Medicine, Omori-nishi, 5-21-16, Ota-ku, Tokyo 143, Japan. Phone: 81-3-3762-4151, ext. 2392. Fax: 81-3-5493-5415. E-mail: keizo{at}sirius.med.toho-u.ac.jp.

Antimicrobial Agents and Chemotherapy, March 1998, p. 555-563, Vol. 42, No. 3
0066-4804/98/$04.00+0
Copyright © 1998, American Society for Microbiology. All rights reserved.


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