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Delafloxacin, a non-zwitterionic fluoroquinolone in Phase III of clinical development: evaluation of its pharmacology, pharmacokinetics, pharmacodynamics and clinical efficacy

机译:Delafloxacin,临床开发第III期的非两性离子氟喹诺酮:评估其药理学,药代动力学,药效学和临床疗效

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摘要

ABSTRACT  Delafloxacin is a fluoroquinolone lacking a basic substituent in position 7. It shows MICs remarkably low against Gram-positive organisms and anaerobes and similar to those of ciprofloxacin against Gram-negative bacteria. It remains active against most fluoroquinolone-resistant strains, except enterococci. Its potency is further increased in acidic environments (found in many infection sites). Delafloxacin is active on staphylococci growing intracellularly or in biofilms. It is currently evaluated as an intravenous and intravenous/oral stepdown therapy in Phase III trials for the treatment of complicated skin/skin structure infections. It was also granted as Qualified Infectious Disease Product for the treatment of acute bacterial skin and skin structure infections and community-acquired bacterial pneumonia, due to its high activity on pneumococci and atypical pathogens.
机译:摘要Delafloxacin是缺乏含有第7位的基本取代基的氟喹啉酮。它显示刺激性生物体和厌氧物显着低,并类似于对革兰氏阴性细菌的环氟苯胺苯丙甲嘧啶的麦克风。除了肠球菌外,它仍然是对大多数氟喹诺酮抗性菌株的活性。其效力在酸性环境中进一步增加(在许多感染部位发现)。 Delafloxacin在细胞内或生物膜生长的葡萄球菌上活跃。目前正在评估为治疗复杂的皮肤/皮肤结构感染的III期试验中的静脉内和静脉/口腔降压治疗。由于其对肺炎球菌和非典型病原体的高活性,还授予术语急性细菌皮肤和皮肤结构感染和社区收购的细菌肺炎的合格传染病产品。

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  • 作者

    Françoise Van Bambeke;

  • 作者单位
  • 年度 2015
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  • 原文格式 PDF
  • 正文语种 eng
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