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Antimicrobial Agents and Chemotherapy, August 2004, p. 2831-2837, Vol. 48, No. 8
0066-4804/04/$08.00+0     DOI: 10.1128/AAC.48.8.2831-2837.2004
Copyright © 2004, American Society for Microbiology. All Rights Reserved.

In Vitro Activities of ME1036 (CP5609), a Novel Parenteral Carbapenem, against Methicillin-Resistant Staphylococci

Mizuyo Kurazono,* Takashi Ida, Keiko Yamada, Yoko Hirai, Takahisa Maruyama, Eiki Shitara, and Minoru Yonezawa

Pharmaceutical Research Center, Meiji Seika Kaisha Ltd., 760 Morooka-cho, Kohoku-ku, Yokohama 222-8567, Japan

Received 27 November 2003/ Returned for modification 22 January 2004/ Accepted 26 April 2004

ME1036, formerly CP5609, is a novel parenteral carbapenem with a 7-acylated imidazo[5,1-b]thiazole-2-yl group directly attached to the carbapenem moiety of the C-2 position. The present study evaluated the in vitro activities of ME1036 against clinical isolates of gram-positive and gram-negative bacteria. ME1036 displayed broad activity against aerobic gram-positive and gram-negative bacteria. Unlike other marketed ß-lactam antibiotics, ME1036 maintained excellent activity against multiple-drug-resistant gram-positive bacteria, such as methicillin-resistant staphylococci and penicillin-resistant Streptococcus pneumoniae (PRSP). The MICs of this compound at which 90% of isolates were inhibited were 2 µg/ml for methicillin-resistant Staphylococcus aureus (MRSA), 2 µg/ml for methicillin-resistant coagulase-negative staphylococci, and 0.031 µg/ml for PRSP. In time-kill studies with six strains of MRSA, ME1036 at four times the MIC caused a time-dependent decrease in the numbers of viable MRSA cells. The activity of ME1036 against MRSA is related to its high affinity for penicillin-binding protein 2a, for which the 50% inhibitory concentration of ME1036 was approximately 300-fold lower than that of imipenem. In conclusion, ME1036 demonstrated a broad antibacterial spectrum and high levels of activity in vitro against staphylococci, including ß-lactam-resistant strains.

* Corresponding author. Mailing address: Pharmaceutical Research Center, Meiji Seika Kaisha Ltd., 760 Morooka-cho, Kohoku-ku, Yokohama 222-8567, Japan. Phone: 81-45-545-3178. Fax: 81-45-541-2359. E-mail: mizuyo_kurazono{at}meiji.co.jp.

Antimicrobial Agents and Chemotherapy, August 2004, p. 2831-2837, Vol. 48, No. 8
0066-4804/04/$08.00+0     DOI: 10.1128/AAC.48.8.2831-2837.2004
Copyright © 2004, American Society for Microbiology. All Rights Reserved.



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