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首页> 外文期刊>Drug Design, Development and Therapy >Review of nemonoxacin with special focus on clinical development
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Review of nemonoxacin with special focus on clinical development

机译：奈诺沙星的综述，特别关注临床发展

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Abstract: Nemonoxacin is a novel C-8-methoxy nonfluorinated quinolone with remarkably enhanced in vitro activity against a wide variety of clinically relevant pathogens, especially gram-positive bacteria, including multidrug-resistant Streptococcus pneumoniae and methicillin-resistant Staphylococcus aureus. It has a low propensity for selecting resistant pathogens than fluoroquinolones, since bacteria become resistant to nemonoxacin only when three different mutations occur in their quinolone resistance-determining regions. Nemonoxacin shows greater efficacy than most of the widely used fluoroquinolones in the murine model of systemic, pulmonary, or ascending urinary tract infection. Nemonoxacin has a sound PK profile in healthy volunteers. It rapidly reaches maximum concentration Cmax 1–2 hours after oral administration in the fasting state and has a relatively long elimination half-life of more than 10 hours, which is similar to fluoroquinolones. Approximately 60%–75% of the administered dose is excreted in unchanged form via kidneys over 24–72 hours. Phase II and III studies of oral nemonoxacin and Phase II studies of intravenous nemonoxacin have been completed in patients with community-acquired pneumonia (CAP), before which the Phase I studies of oral and intravenous nemonoxacin indicated sound tolerance and safety with healthy volunteers. The published results demonstrate that an oral dose of either 500 mg or 750 mg nemonoxacin once daily for 7 days is as effective and safe as levofloxacin 500 mg once daily for 7 days. Nemonoxacin is well-tolerated in patients with CAP. The most common adverse events of oral administration are observed in the gastrointestinal and nervous system, the incidence of which is similar to levofloxacin treatment. The Phase III studies of intravenous nemonoxacin for treating CAP and oral nemonoxacin for diabetic foot infection has been registered with promising outcomes to be expected.
机译：摘要：Nemonoxacin是一种新型的C-8-甲氧基非氟化喹诺酮，对多种临床相关病原体具有显着增强的体外活性，尤其是革兰氏阳性细菌，包括耐多药肺炎链球菌和耐甲氧西林金黄色葡萄球菌。它比氟喹诺酮类药物更容易选择耐药病原体，因为细菌只有在其喹诺酮耐药性决定区域发生三种不同的突变时才对奈莫沙星产生耐药性。在系统性，肺部或上行尿路感染的小鼠模型中，尼莫沙星比大多数广泛使用的氟喹诺酮类药物显示出更高的疗效。尼莫沙星在健康志愿者中具有良好的PK分布。在禁食状态下口服后1至2小时，它迅速达到最大浓度Cmax，消除半衰期相对较长，超过10小时，这与氟喹诺酮类药物相似。在24-72小时内，约60％-75％的给药剂量以不变的形式经肾脏排泄。社区获得性肺炎（CAP）患者已完成口服奈诺沙星的II期和III期研究以及静脉内奈沙星的II期研究，在此之前，口服奈诺沙星和静脉内奈沙星的I期研究表明健康志愿者具有良好的耐受性和安全性。已发表的结果表明，每天一次500毫克或750毫克奈诺沙星的口服剂量持续7天，与每天500毫克左氧氟沙星7天的口服剂量一样有效和安全。 CAP患者耐莫沙星的耐受性良好。在胃肠道和神经系统中观察到最常见的口服不良反应，其发生率与左氧氟沙星治疗相似。静脉注射奈诺沙星治疗CAP和口服奈诺沙星治疗糖尿病足感染的III期研究已经获得了预期的结果。

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