Kanniess Frank, Boulet Louis-Philippe, Pierzchala Wladyslaw, Cameron Ray, Owen Roger, Higgins Mark
Pulmonary Research Institute, Hospital Grosshansdorf, Grosshansdorf, Germany.
J Asthma. 2008 Dec;45(10):887-92. doi: 10.1080/02770900802348321.
Indacaterol is a new once-daily inhaled beta(2)-agonist in clinical development for asthma as a component of a fixed-dose combination with an inhaled corticosteroid.
To investigate the efficacy and safety of indacaterol in patients with chronic persistent asthma.
A total of 115 patients were randomized in a double-blind, incomplete-block cross-over design to sequences of four 7-day treatment periods (separated by 7-day washouts) with indacaterol 100, 200, 300, 400, or 600 micro g or placebo, once daily, via single-dose dry-powder inhaler. After the fourth washout, patients received 1 day of open-label formoterol 12 mu g twice daily. Forced expiratory volume in 1 second (FEV(1)) was measured for 24 hours post-dose on days 1 and 7.
For standardized (with respect to time) FEV(1) area under the curve at 22 to 24 hours (AUC(22-24h)) on day 1, indacaterol doses >or=200 micro g were superior to placebo (p < 0.05) and similar or greater than formoterol 12 micro g twice daily. By day 7, mean differences from placebo in FEV(1) standardized AUC(22-24h) were 0.08, 0.16, 0.15, 0.11, and 0.16 L for indacaterol 100, 200, 300, 400, and 600 micro g, respectively (all p < 0.05 vs. placebo). Mean FEV(1) for indacaterol doses >or= 200 micro g on day 7 was higher than placebo (p < 0.05) pre-dose and at all post-dose time points. AEs were generally mild in severity; no serious AEs occurred. No clinically meaningful differences were observed between treatments in any safety assessments.
Once-daily indacaterol demonstrated sustained 24-hour bronchodilator efficacy, with similar efficacy on days 1 and 7, and was generally well tolerated.
茚达特罗是一种新型的每日一次吸入型β₂受体激动剂，目前正处于临床开发阶段，用于哮喘治疗，它是与吸入性糖皮质激素组成的固定剂量复方制剂的一部分。
研究茚达特罗在慢性持续性哮喘患者中的疗效和安全性。
总共115例患者采用双盲、不完全区组交叉设计，随机分为四个7天治疗期（间隔7天洗脱期）的序列组，分别使用100、200、300、400或600μg茚达特罗或安慰剂，通过单剂量干粉吸入器每日一次给药。在第四个洗脱期后，患者接受1天的开放标签福莫特罗治疗，剂量为12μg，每日两次。在第1天和第7天给药后24小时测量第1秒用力呼气容积（FEV₁）。
在第1天22至24小时标准化（相对于时间）的FEV₁曲线下面积（AUC₂₂ - ₂₄h）方面，茚达特罗剂量≥200μg优于安慰剂（p < 0.05），且与每日两次12μg福莫特罗相似或更高。到第7天，茚达特罗100、200、300、400和600μg在FEV₁标准化AUC₂₂ - ₂₄h方面与安慰剂的平均差异分别为0.08、0.16、0.15、0.11和0.16L（与安慰剂相比，均p < 0.05）。第7天茚达特罗剂量≥200μg时，FEV₁的平均值在给药前和所有给药后时间点均高于安慰剂（p < 0.05）。不良事件严重程度一般较轻；未发生严重不良事件。在任何安全性评估中，各治疗组之间均未观察到具有临床意义的差异。
每日一次的茚达特罗显示出持续24小时的支气管扩张疗效，在第1天和第7天疗效相似，且总体耐受性良好。
