In Vivo Pharmacokinetic/Pharmacodynamic Targets of Levonadifloxacin against Staphylococcus aureus in a Neutropenic Murine Lung Infection Model

Bhagwat Sachin S.; Periasamy Hariharan; Takalkar Swapna S.; Chavan Rajesh; Tayde Pavan; Kulkarni Amol; Satav Jaikumar; Zope Vineet; Patel Mahesh

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In Vivo Pharmacokinetic/Pharmacodynamic Targets of Levonadifloxacin against Staphylococcus aureus in a Neutropenic Murine Lung Infection Model

机译：在中性细胞鼠肺部感染模型中，左旋甲基甲嘧辛对左旋甲酰金黄色葡萄球菌的体内药代动力学/药效学靶

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Levonadifloxacin is a novel benzoquinolizine subclass of fluoroquinolone, active against quinolone-resistant Staphylococcus aureus. A phase 3 trial for levonadifloxacin and its oral prodrug was recently completed. The present study identified area under the concentration-time curve for the free, unbound fraction of a drug divided by the MIC (fAUC/MIC) as an efficacy determinant for levonadifloxacin in a neutropenic murine lung infection model. Mean plasma fAUC/MIC requirement for static and 1 log(10) kill effects against 9 S. aureus were 8.1 +/- 6.0 and 25.8 +/- 12.3, respectively. These targets were employed in the selection of phase 3 doses.

机译：Levonadifloxacin是一种新型氟喹诺酮的苯并喹啉亚类，对抗喹诺酮抗性金黄色葡萄球菌。最近完成了左旋甲基甲酰辛及其口腔前药的第3期试验。本研究鉴定了浓度 - 时间曲线下的区域，用于自由，未结合的药物除以麦克风（Fauc / MIC）作为中性细胞鼠肺部感染模型中Levonadifloxacin的疗效决定蛋白。平均静态血浆Fauc / MIC要求静态和1个log（10）杀伤9s的杀伤作用分别为8.1 +/- 6.0和25.8 +/- 12.3。这些靶标在选择3剂量中使用。

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来源
《Antimicrobial agents and chemotherapy.》 |2019年第8期|共1页
作者
Bhagwat Sachin S.; Periasamy Hariharan; Takalkar Swapna S.; Chavan Rajesh; Tayde Pavan; Kulkarni Amol; Satav Jaikumar; Zope Vineet; Patel Mahesh;
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作者单位

Wockhardt Res Ctr Aurangabad Maharashtra India;

Wockhardt Res Ctr Aurangabad Maharashtra India;

Wockhardt Res Ctr Aurangabad Maharashtra India;

Wockhardt Res Ctr Aurangabad Maharashtra India;

Wockhardt Res Ctr Aurangabad Maharashtra India;

Wockhardt Res Ctr Aurangabad Maharashtra India;

Wockhardt Res Ctr Aurangabad Maharashtra India;

Wockhardt Res Ctr Aurangabad Maharashtra India;

Wockhardt Res Ctr Aurangabad Maharashtra India;

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原文格式 PDF
正文语种 eng
中图分类治疗学;
关键词
ABSSSIs; MRSA; levonadifloxacin;

机译：asbsss;mrsa;pervaginalfloxacin;

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1. In Vivo Pharmacokinetic/Pharmacodynamic Targets of Levonadifloxacin against Staphylococcus aureus in a Neutropenic Murine Lung Infection Model [J] . Bhagwat Sachin S., Periasamy Hariharan, Takalkar Swapna S., Antimicrobial agents and chemotherapy. . 2019,第8期

机译：在中性细胞鼠肺部感染模型中，左旋甲基甲嘧辛对左旋甲酰金黄色葡萄球菌的体内药代动力学/药效学靶
2. Pharmacodynamics of a new cephalosporin, PPI-0903 (TAK-599), active against methicillin-resistant Staphylococcus aureus in murine thigh and lung infection models: identification of an in vivo pharmacokinetic-pharmacodynamic target. [J] . Andes D, Craig WA Antimicrobial agents and chemotherapy. . 2006,第4期

机译：一种新的头孢菌素PPI-0903（TAK-599）的药效学在鼠大腿和肺部感染模型中对耐甲氧西林的金黄色葡萄球菌有活性：体内药代动力学药效学靶标的鉴定。
3. In Vivo Pharmacodynamic Target Assessment of Delafloxacin against Staphylococcus aureus, Streptococcus pneumoniae, and Klebsiella pneumoniae in a Murine Lung Infection Model [J] . Lepak Alexander J., Andes David R. Antimicrobial agents and chemotherapy. . 2016,第8期

机译：在小鼠肺炎金黄色葡萄球菌，链球菌肺炎氏菌，肺炎链球菌和克雷斯氏菌在鼠肺部感染模型中的体内药效靶标评估
4. Multimodality Imaging Mass Spectrometry for CoMultimodality Imaging Mass Spectrometry for CoMultimodality Co-localization of Trace Metals and Proteins localization of Trace Metals and Proteins in Murine Tissue Abscesses Elicited by in Murine Tissue Abscesses Elicited by Staphylococcus aureusStaphylococcus aureusStaphylococcus aureus Infection [C] . Jessica L. Moore, Yaofang Zhang, Thomas E. Kehl-fie, American Society for Mass Spectrometry Conference on Mass Spectrometry and Allied Topics . 2013

机译：多态成像对痕量金属和蛋白质群和蛋白质分析痕量金属和蛋白质中的痕量金属和蛋白质中鼠组织脓肿中的血管组织脓肿脓肿的蛋白质和蛋白质的核心化的群体成像质谱法。葡萄球菌感染术引出的鼠组织脓肿
5. Murine models of Staphylococcus aureus biofilm infections and therapeutic protein a vaccination. [D] . Walton, Kelly D. 2013

机译：金黄色葡萄球菌生物膜感染和治疗性蛋白疫苗的小鼠模型。
6. In Vivo Pharmacokinetic/Pharmacodynamic Targets of Levonadifloxacin against Staphylococcus aureus in a Neutropenic Murine Lung Infection Model [O] . Sachin S. Bhagwat, Hariharan Periasamy, Swapna S. Takalkar, 2019

机译：在中性粒细胞减少症的小鼠肺部感染模型中Levonadifloxacin对抗金黄色葡萄球菌的体内药代动力学/药效学目标。
7. Pharmacodynamics of a New Cephalosporin, PPI-0903 (TAK-599), Active against Methicillin-Resistant Staphylococcus aureus in Murine Thigh and Lung Infection Models: Identification of an In Vivo Pharmacokinetic-Pharmacodynamic Target [O] . Andes, D., Craig, W. A. 2014

机译：一种新的头孢菌素，PPI-0903（TAK-599），在鼠大腿和肺部感染模型中对耐甲氧西林金黄色葡萄球菌有活性的药效学：体内药代动力学药效学靶标的鉴定

In Vivo Pharmacokinetic/Pharmacodynamic Targets of Levonadifloxacin against Staphylococcus aureus in a Neutropenic Murine Lung Infection Model

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