The efficacy and safety of the novel long-acting β2 agonist vilanterol in patients with COPD: a randomized placebo-controlled trial

Chest. 2012 Jul;142(1):119-127. doi: 10.1378/chest.11-2231.


Background: Vilanterol (GW642444M) (VI) is a novel, inhaled, long-acting β(2) agonist with inherent 24-h activity under development as a once-daily combination therapy with an inhaled corticosteroid for COPD and asthma. This study assessed the dose response, efficacy, and safety of VI at doses of 3 to 50 μg in patients with moderate to severe COPD.

Methods: Six hundred two patients (intent-to-treat) were randomized (double-blind) to VI 3, 6.25, 12.5, 25, or 50 μg or placebo once daily for 28 days. The primary end point was change from baseline in trough FEV1 at the end of the 28-day treatment period. Secondary end points included 0- to 24-h weighted mean FEV(1) on days 1 and 28 and time to increases of ≥ 100 mL or ≥ 12% from baseline FEV(1) on day 1. Safety assessments included adverse events, vital signs, ECG assessment, and clinical laboratory tests.

Results: VI once daily for 28 days significantly improved trough FEV(1) in a dose-dependent manner vs placebo. Clinically relevant treatment differences of ≥ 130 mL in trough and 0- to 24-h weighted mean FEV(1) were observed with VI 25- and 50-μg doses vs placebo. All doses of VI were associated with a low incidence of treatment-related adverse events/serious adverse events, with no suggestion of effects on BP, pulse rate, QT intervals corrected for heart rate calculated by Fridericia formula, or blood glucose and potassium levels.

Conclusions: VI 25 and 50 μg once daily provided both statistically and clinically relevant 24-h improvements in lung function in patients with COPD compared with placebo. All doses of VI had a safety and tolerability profile similar to placebo.

Publication types

  • Multicenter Study
  • Randomized Controlled Trial
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Administration, Inhalation
  • Adrenal Cortex Hormones / therapeutic use
  • Adrenergic beta-2 Receptor Agonists / adverse effects*
  • Adrenergic beta-2 Receptor Agonists / therapeutic use*
  • Adult
  • Aged
  • Aged, 80 and over
  • Benzyl Alcohols / adverse effects*
  • Benzyl Alcohols / therapeutic use*
  • Chlorobenzenes / adverse effects*
  • Chlorobenzenes / therapeutic use*
  • Dose-Response Relationship, Drug
  • Double-Blind Method
  • Drug Therapy, Combination
  • Electrocardiography
  • Female
  • Forced Expiratory Volume
  • Humans
  • Male
  • Middle Aged
  • Outcome Assessment, Health Care
  • Pulmonary Disease, Chronic Obstructive / drug therapy*
  • Severity of Illness Index
  • Treatment Outcome


  • Adrenal Cortex Hormones
  • Adrenergic beta-2 Receptor Agonists
  • Benzyl Alcohols
  • Chlorobenzenes
  • vilanterol