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Antimicrobial Agents and Chemotherapy, October 2005, p. 4185-4196, Vol. 49, No. 10
0066-4804/05/$08.00+0     doi:10.1128/AAC.49.10.4185-4196.2005
Copyright © 2005, American Society for Microbiology. All Rights Reserved.

In Vitro and In Vivo Antibacterial Activities of SM-216601, a New Broad-Spectrum Parenteral Carbapenem

Yutaka Ueda,* Katsunori Kanazawa, Ken Eguchi, Koji Takemoto, Yoshiro Eriguchi, and Makoto Sunagawa

Sumitomo Pharmaceuticals Research Division, 3-1-98 Kasugade-naka, Konohana, Osaka 554-0022, Japan

Received 15 April 2005/ Returned for modification 24 May 2005/ Accepted 22 July 2005

SM-216601 is a novel parenteral 1ß-methylcarbapenem. In agar dilution susceptibility testing, the MIC of SM-216601 for 90% of the methicillin-resistant Staphylococcus aureus (MRSA) strains tested (MIC90) was 2 µg/ml, which was comparable to those of vancomycin and linezolid. SM-216601 was also very potent against Enterococcus faecium, including vancomycin-resistant strains (MIC90 = 8 µg/ml). SM-216601 exhibited potent activity against penicillin-resistant Streptococcus pneumoniae, ampicillin-resistant Haemophilus influenzae, Moraxella catarrhalis, Escherichia coli, Klebsiella pneumoniae, and Proteus mirabilis, with MIC90s of less than 0.5 µg/ml, and intermediate activity against Citrobacter freundii, Enterobacter cloacae, Serratia marcescens, and Pseudomonas aeruginosa. The therapeutic efficacy of SM-216601 against experimentally induced infections in mice caused by S. aureus, E. faecium, E. coli, and P. aeruginosa reflected its in vitro activity and plasma level. Thus, SM-216601 is a promising candidate for nosocomial bacterial infections caused by a wide range of gram-positive and gram-negative bacteria, including multiresistant pathogens.

* Corresponding author. Mailing address: Discovery Research Laboratories II, Sumitomo Pharmaceuticals Research Division, 3-1-98 Kasugade-naka, Konohana, Osaka 554-0022, Japan. Phone: 81-6-8466-5271. Fax: 81-6-6466-5491. E-mail: yutakau{at}sumitomopharm.co.jp.

Antimicrobial Agents and Chemotherapy, October 2005, p. 4185-4196, Vol. 49, No. 10
0066-4804/05/$08.00+0     doi:10.1128/AAC.49.10.4185-4196.2005
Copyright © 2005, American Society for Microbiology. All Rights Reserved.



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