替比培南（SPR859）对革兰氏阴性菌和革兰氏阳性菌青霉素结合蛋白的活性。
Activity of Tebipenem (SPR859) against Penicillin-Binding Proteins of Gram-Negative and Gram-Positive Bacteria.
机构信息
Centre d'Étude et de Valorisation de la Diversité Microbienne (CEVDM), Département de biologie, Faculté des sciences, Université de Sherbrooke, Sherbrooke, Quebec, Canada.
Spero Therapeutics, Inc., Cambridge, Massachusetts, USA.
出版信息
Antimicrob Agents Chemother. 2019 Mar 27;63(4). doi: 10.1128/AAC.02181-18. Print 2019 Apr.
Abstract
Tebipenem (SPR859) is the microbiologically active form of SPR994 (tebipenem-pivoxil), an orally available carbapenem with activity against extended-spectrum β-lactamase (ESBL)-producing Measurement of the relative binding of SPR859 to the bacterial cell targets revealed that it is a potent inhibitor of multiple penicillin-binding proteins (PBPs) but primarily a Gram-negative PBP 2 inhibitor, similar to other compounds in this class. These data support further clinical development of SPR994.
摘要
替比培南（SPR859）是微生物活性形式的 SPR994（替比培南匹伏酯），一种可口服的碳青霉烯类药物，对产超广谱β-内酰胺酶（ESBL）的药物具有活性。对 SPR859 与细菌细胞靶标相对结合的测量表明，它是多种青霉素结合蛋白（PBPs）的有效抑制剂，但主要是革兰氏阴性 PBP2 抑制剂，类似于该类中的其他化合物。这些数据支持 SPR994 的进一步临床开发。
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