Center for Genomics and Personalized Medicine Research and Translational Medicine Institute, Wake Forest University Health Sciences, Winston-Salem, NC 27157, USA.
Int J Chron Obstruct Pulmon Dis. 2011;6:431-8. doi: 10.2147/COPD.S21073. Epub 2011 Aug 18.
Indacaterol is an inhaled, once-daily long-acting β(2)-agonist bronchodilator for regular use in patients with chronic obstructive pulmonary disease (COPD). As indacaterol is the first once-daily β(2)-agonist to be developed, it is relevant to evaluate its bronchodilator efficacy, safety, and tolerability.
Data were pooled from three randomized, double-blind, clinical studies in patients with moderate-to-severe COPD treated with indacaterol 150 μg qd (n = 627) or placebo (n = 1021). Bronchodilator efficacy was assessed as trough (24-hour post-dose) forced expiratory volume in 1 second (FEV(1)) after 12 weeks (primary endpoint in individual studies) and FEV(1) measured serially post-dose. Rescue use of albuterol was monitored.
At week 12, indacaterol increased trough FEV(1) by 160 mL compared with placebo (P < 0.001), exceeding the 120 mL level prespecified as clinically important. FEV(1) during the first 12-hour post-dose at week 12 averaged 210 mL higher with indacaterol than with placebo (P < 0.001). Patients receiving indacaterol recorded 53% of days without use of rescue albuterol, compared with 38% of days in the placebo group (P < 0.001). Adverse events (mostly mild or moderate) were reported for 52% and 46% of patients receiving indacaterol and placebo, respectively, and serious adverse events for 4% and 5%. Worsening of COPD was the most frequent adverse event (10% indacaterol; 15% placebo). Indacaterol had little effect on pulse or blood pressure or measures of systemic β(2)-adrenoceptor activity (blood glucose, serum potassium, and corrected QT interval).
Indacaterol was an effective bronchodilator and was well tolerated, with a good safety profile over 12 weeks of treatment. It should prove a useful treatment for patients with moderate-to-severe COPD.
茚达特罗是一种吸入性、每日一次的长效β2-激动剂支气管扩张剂，用于慢性阻塞性肺疾病（COPD）患者的常规治疗。茚达特罗是首个每日一次的β2-激动剂，因此对其支气管扩张疗效、安全性和耐受性进行评估很有意义。
对接受茚达特罗 150μg qd（n=627）或安慰剂（n=1021）治疗的中重度 COPD 患者的三项随机、双盲临床试验数据进行了汇总。12 周时的谷值（24 小时后给药）用力呼气量第一秒（FEV1）（各研究的主要终点）和给药后连续测量的 FEV1评估支气管扩张疗效。监测沙丁胺醇的急救使用情况。
第 12 周时，与安慰剂相比，茚达特罗使谷值 FEV1增加 160mL（P＜0.001），超过了预设的 120mL 临床重要性水平。第 12 周时，给药后 12 小时的 FEV1平均增加 210mL，与安慰剂相比（P＜0.001）。接受茚达特罗治疗的患者中有 53%的天数无需使用沙丁胺醇急救，而安慰剂组为 38%（P＜0.001）。分别有 52%和 46%的患者报告了茚达特罗和安慰剂的不良事件（主要为轻度或中度），分别有 4%和 5%的患者报告了严重不良事件。COPD 恶化是最常见的不良事件（10%茚达特罗；15%安慰剂）。茚达特罗对脉搏或血压或全身β2-肾上腺素能受体活性的测量值（血糖、血清钾和校正 QT 间期）几乎没有影响。
茚达特罗是一种有效的支气管扩张剂，耐受性良好，在 12 周的治疗期间具有良好的安全性。它应该是治疗中重度 COPD 患者的一种有效治疗方法。
