Vaborbactam

一种β-内酰胺酶抑制剂（对A类和C类β-内酰胺酶的抑制常数Ki为29-110纳摩尔）；相较于一系列哺乳动物丝氨酸蛋白酶，对细菌β-内酰胺酶具有选择性（对哺乳动物丝氨酸蛋白酶的半数抑制浓度IC50≥1000微摩尔）；在浓度为0.02微克/毫升时，可增强比阿培南对表达KPC-2型酶的肺炎克雷伯菌的抗菌活性；增强碳青霉烯类抗生素对各种细菌临床分离株的抗菌活性（存在该化合物时，最低抑菌浓度MIC≤0.06-4微克/毫升，不存在该化合物时，最低抑菌浓度MIC为4-64微克/毫升）；在中性粒细胞减少的小鼠肺部感染模型中，与比阿培南或美罗培南按50毫克/千克的剂量联合使用时，可减少肺部的菌落形成单位（CFU）数量。A β-lactamase inhibitor (Kis = 29-110 nM for class A and class C enzymes); selective for bacterial β-lactamases over a panel of mammalian serine proteases (IC50s = ≥1,000 μM); potentiates the activity of biapenem against K. pneumonia expressing KPC-2 at 0.02 μg/ml; potentiates the activity of carbapenem antibiotics against clinical isolates of various bacteria (MICs = ≤0.06-4 and 4-64 μg/ml in the presence and absence of compound, respectively); reduces the number of CFUs in the lung in a neutropenic mouse lung infection model when used in combination with biapenem or meropenem at 50 mg/kg.