Kohira Naoki, West Joshua, Ito Akinobu, Ito-Horiyama Tsukasa, Nakamura Rio, Sato Takafumi, Rittenhouse Stephen, Tsuji Masakatsu, Yamano Yoshinori
Discovery Research Laboratory for Core Therapeutic Areas, Shionogi & Co., Ltd., Toyonaka, Osaka, Japan
GlaxoSmithKline, Collegeville, Pennsylvania, USA.
Antimicrob Agents Chemother. 2015 Nov 16;60(2):729-34. doi: 10.1128/AAC.01695-15. Print 2016 Feb.
S-649266 is a novel siderophore cephalosporin antibiotic with a catechol moiety on the 3-position side chain. Two sets of clinical isolate collections were used to evaluate the antimicrobial activity of S-649266 against Enterobacteriaceae. These sets included 617 global isolates collected between 2009 and 2011 and 233 β-lactamase-identified isolates, including 47 KPC-, 49 NDM-, 12 VIM-, and 8 IMP-producers. The MIC90 values of S-649266 against the first set of Escherichia coli, Klebsiella pneumoniae, Serratia marcescens, Citrobacter freundii, Enterobacter aerogenes, and Enterobacter cloacae isolates were all ≤1 μg/ml, and there were only 8 isolates (1.3%) among these 617 clinical isolates with MIC values of ≥8 μg/ml. In the second set, the MIC values of S-649266 were ≤4 μg/ml against 109 strains among 116 KPC-producing and class B (metallo) carbapenemase-producing strains. In addition, S-649266 showed MIC values of ≤2 μg/ml against each of the 13 strains that produced other types of carbapenemases such as SME, NMC, and OXA-48. The mechanisms of the decreased susceptibility of 7 class B carbapenemase-producing strains with MIC values of ≥16 μg/ml are uncertain. This is the first report to demonstrate that S-649266, a novel siderophore cephalosporin, has significant antimicrobial activity against Enterobacteriaceae, including strains that produce carbapenemases such as KPC and NDM-1.
S-649266是一种新型的铁载体头孢菌素抗生素,其3位侧链带有儿茶酚部分。使用两组临床分离株集合来评估S-649266对肠杆菌科细菌的抗菌活性。这些集合包括2009年至2011年收集的617株全球分离株以及233株经β-内酰胺酶鉴定的分离株,其中包括47株产KPC酶、49株产NDM酶、12株产VIM酶和8株产IMP酶的菌株。S-649266对第一组大肠杆菌、肺炎克雷伯菌、粘质沙雷氏菌、弗氏柠檬酸杆菌、产气肠杆菌和阴沟肠杆菌分离株的MIC90值均≤1μg/ml,在这617株临床分离株中,只有8株(1.3%)的MIC值≥8μg/ml。在第二组中,S-649266对116株产KPC酶和产B类(金属)碳青霉烯酶的菌株中的109株的MIC值≤4μg/ml。此外,S-649266对13株产其他类型碳青霉烯酶(如SME、NMC和OXA-48)的菌株的MIC值均≤2μg/ml。7株MIC值≥16μg/ml的产B类碳青霉烯酶菌株敏感性降低的机制尚不清楚。这是首次报道表明新型铁载体头孢菌素S-649266对肠杆菌科细菌具有显著的抗菌活性,包括产碳青霉烯酶(如KPC和NDM-1)的菌株。