Box Helen, Livermore Joanne, Johnson Adam, McEntee Laura, Felton Timothy W, Whalley Sarah, Goodwin Joanne, Hope William W
Antimicrobial Pharmacodynamics and Therapeutics, Department of Molecular and Clinical Pharmacology, Institute of Translational Medicine, University of Liverpool, Liverpool, United Kingdom.
Antimicrobial Pharmacodynamics and Therapeutics, Department of Molecular and Clinical Pharmacology, Institute of Translational Medicine, University of Liverpool, Liverpool, United Kingdom
Antimicrob Agents Chemother. 2015 Oct 26;60(1):278-87. doi: 10.1128/AAC.01364-15. Print 2016 Jan.
Isavuconazonium sulfate is a novel triazole prodrug that has been recently approved for the treatment of invasive aspergillosis by the FDA. The active moiety (isavuconazole) has a broad spectrum of activity against many pathogenic fungi. This study utilized a dynamic in vitro model of the human alveolus to describe the pharmacodynamics of isavuconazole against two wild-type and two previously defined azole-resistant isolates of Aspergillus fumigatus. A human-like concentration-time profile for isavuconazole was generated. MICs were determined using CLSI and EUCAST methodologies. Galactomannan was used as a measure of fungal burden. Target values for the area under the concentration-time curve (AUC)/MIC were calculated using a population pharmacokinetics-pharmacodynamics (PK-PD) mathematical model. Isolates with higher MICs required higher AUCs in order to achieve maximal suppression of galactomannan. The AUC/MIC targets necessary to achieve 90% probability of galactomannan suppression of <1 were 11.40 and 11.20 for EUCAST and CLSI, respectively.
硫酸艾沙康唑是一种新型三唑前体药物,最近已被美国食品药品监督管理局批准用于治疗侵袭性曲霉病。活性部分(艾沙康唑)对许多致病真菌具有广谱活性。本研究利用人肺泡的动态体外模型来描述艾沙康唑对两株野生型和两株先前定义的耐唑类烟曲霉分离株的药效学。生成了类似人体的艾沙康唑浓度-时间曲线。使用临床和实验室标准协会(CLSI)及欧洲抗菌药物敏感性试验委员会(EUCAST)方法测定最低抑菌浓度(MIC)。半乳甘露聚糖用作真菌负荷的指标。使用群体药代动力学-药效学(PK-PD)数学模型计算浓度-时间曲线下面积(AUC)/MIC的目标值。MIC较高的分离株需要更高的AUC才能实现对半乳甘露聚糖的最大抑制。对于EUCAST和CLSI,实现半乳甘露聚糖抑制率<1的概率为90%所需的AUC/MIC目标值分别为11.40和11.20。