Ceftolozane sulfate

Ceftolozane sulfate（CAS号936111-69-2）是Ceftolozane 的硫酸盐形式。Ceftolozane（头孢洛扎）为时间依赖性氧亚氨基头孢菌素类抗菌药，核心生物学功能为抑制细菌青霉素结合蛋白（PBP3 为主要靶点），并高亲和力结合铜绿假单胞菌 PBP1b、PBP1c 以阻断细胞壁合成发挥杀菌作用，对染色体 AmpC β- 内酰胺酶高度稳定。

关键活性数据：对铜绿假单胞菌 MIC₅₀/MIC₉₀为 0.5/2 mg/L，多重耐药 / 广泛耐药铜绿假单胞菌 MIC₉₀为 8/16 mg/L，对非产碳青霉烯酶肠杆菌科 MIC₅₀/MIC₉₀为 0.25/0.5-4 mg/L，产 ESBL 肺炎克雷伯菌 MIC₉₀升至 16-32 mg/L，对产碳青霉烯酶菌株无抗菌活性（MIC>64 mg/L）。

动物实验常用于疾病模型治疗，常见应用模型包括中性粒细胞减少小鼠大腿铜绿假单胞菌 / 肠杆菌科感染模型，用于评估杀菌效力与 PK/PD 靶标。

常用应用与浓度：细胞培养为体外药敏实验（阳离子调节 MH 肉汤），测试浓度范围 0.03-32 mg/L；动物实验以人体等效剂量给药，杀菌靶标为游离药物浓度超过 MIC 的时间占给药间隔 30%-50%；临床用于复杂腹腔 / 尿路感染时为 1g 每 8 小时静脉输注，用于医院获得性 / 呼吸机相关性肺炎、铜绿假单胞菌菌血症（高肾清除患者）时为 2g 每 8 小时延长输注，有效治疗浓度要求为游离药物浓度超过 MIC 的时间占给药间隔 40%-50% 以上。

参考文献：

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