University of Utah Health Sciences Center, 295 Chipeta Way, Clinical Pharmacology, Salt Lake City, UT 84108, USA.
Ther Adv Respir Dis. 2014 Feb;8(1):13-21. doi: 10.1177/1753465813508445. Epub 2013 Dec 10.
Inhaled therapies allow for the targeted delivery of antimicrobials directly into the lungs and have been widely used in the treatment of cystic fibrosis (CF) acute pulmonary exacerbations. Nebulized levofloxacin solution (MP-376) is a novel therapy that is currently being evaluated in phase I, II, and III clinical trials among patients with stable CF and recent isolation of Pseudomonas aeruginosa from sputum. Phase I studies have investigated the single and multiple-dose pharmacokinetics of MP-376 and shown that it is rapidly absorbed from the lungs and results in low systemic concentrations. A subsequent phase IB study found that MP-376 pharmacokinetics were comparable among adults and children 6-16 years of age. Further phase II studies reported that sputum P. aeruginosa density decreased in a dose-dependent manner among patients who were randomized to MP-376 when compared with patients who received placebo. Improvements in pulmonary function and a decrease in the need for other antipseudomonal antibiotics were also reported for patients who received inhaled levofloxacin. The most common adverse event was dysgeusia (abnormal taste sensation), which was reported by nearly half of the participants who received MP-376. No serious drug-related adverse events were reported. These findings are encouraging; however, data from the two ongoing phase III trials are needed to determine whether MP-376 demonstrates substantial evidence of safety and efficacy as a chronic CF maintenance therapy and therefore may be useful in routine clinical practice.
吸入疗法可将抗生素靶向递送至肺部,已广泛用于治疗囊性纤维化(CF)急性肺部加重。雾化左氧氟沙星溶液(MP-376)是一种新型疗法,目前正在 CF 稳定期且近期从痰中分离出铜绿假单胞菌的患者中进行 I、II 和 III 期临床试验评估。I 期研究调查了 MP-376 的单剂量和多剂量药代动力学,结果表明它可从肺部迅速吸收,导致全身浓度较低。随后的 Ib 期研究发现,MP-376 药代动力学在 6-16 岁的成年患者和儿童中相似。进一步的 II 期研究报告称,与接受安慰剂的患者相比,随机接受 MP-376 的患者痰液中铜绿假单胞菌密度呈剂量依赖性下降。接受吸入左氧氟沙星的患者的肺功能也有所改善,对其他抗假单胞菌抗生素的需求减少。接受 MP-376 治疗的患者最常见的不良事件是味觉障碍(异常味觉),近一半的患者报告了这种不良事件。未报告严重的药物相关不良事件。这些发现令人鼓舞;然而,需要来自两项正在进行的 III 期试验的数据来确定 MP-376 是否作为慢性 CF 维持治疗具有充分的安全性和疗效证据,因此可能在常规临床实践中有用。