Efficacy and safety of the long-acting β₂-agonist olodaterol over 4 weeks in japanese patients with chronic obstructive pulmonary disease

Background: Olodaterol is a novel long-acting β₂-agonist with proven $24-hour duration of action in preclinical and clinical studies. Objective: This randomized, double-blind, placebo-controlled, parallel-group study evaluated the dose response of once-daily (QD) olodaterol based on bronchodilator efficacy, safety, and pharmacokinetics over 4 weeks in Japanese patients with chronic obstructive pulmonary disease (COPD). Methods: All eligible patients were randomized to receive 2 μg, 5 μg, or 10 μg of olodaterol or placebo for 4 weeks via the Respimat® Soft Mist™ inhaler. The primary end point was the change from baseline in trough forced expiratory volume in 1 second (FEV₁) after 4 weeks of olodaterol treatment. Secondary end points included trough FEV₁ after 1 week and 2 weeks of treatment, FEV₁ area under the curve from 0 hour to 3 hours (AUC_0–3), peak FEV₁ from 0 hour to 3 hours (peak FEV1), and corresponding forced vital capacity (FVC) responses. Rescue medication use, COPD symptoms, physician global evaluation, pharmacokinetics, and safety were also assessed. Results: A total of 328 patients with COPD were randomized to receive treatment. All olodaterol doses assessed in the study showed statistically significant increases in trough FEV₁ compared to placebo at Day 29 (P,0.0001). Mean increases in peak FEV₁ and FEV₁ AUC_0–3 compared to placebo were also significant (P,0.0001). A clear dose–response relationship was observed across all treatment groups. FVC responses (trough and FVC AUC_0–3) supported FEV₁ outcomes. All doses of olodaterol were well tolerated, and no safety concerns were identified. Conclusion: QD olodaterol demonstrated 24-hour bronchodilator efficacy and was well tolerated in Japanese patients with COPD.