Revefenacin, a once-daily, long-acting muscarinic antagonist, or nebulized maintenance therapy in patients with chronic obstructive pulmonary disease

AMERICAN JOURNAL OF HEALTH-SYSTEM PHARMACY(2021)

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摘要
Purpose. This article reviews the efficacy and safety of revefenacin, the first once-daily, long-acting muscarinic antagonist, when delivered via a standard jet nebulizer in patients with chronic obstructive pulmonary disease (COPD). Summary. Revefenacin 175 mu g is indicated for the maintenance treatment of patients with moderate to very severe COPD. Preclinical studies showed that revefenacin is a potent and selective antagonist with similar affinity for the different subtypes of muscarinic receptors (M-1-M-6). Furthermore, prevention of methacholine- and acetylcholine-induced bronchoconstrictive effects was dose dependent and lasted longer than 24 hours, demonstrating a long duration of action. In phase 2 and 3 trials, treatment with revefenacin was demonstrated to result in statistical improvements in pulmonary function (>= 100 mL, P < 0.05) vs placebo, including among patients with markers of more severe disease and those who received concomitant long-acting beta-agonists or long-acting beta-agonists together with inhaled corticosteroids. Revefenacin was also demonstrated to have efficacy similar to that of tiotropium. The clinical trial findings indicated no significant difference between revefenacin and tiotropium with regard to rates of adverse events. Overall, revefenacin was well tolerated, with COPD worsening/exacerbation, dyspnea, headache, and cough among the most common adverse events noted in the clinical trials. Conclusions. Revefenacin treatment delivered via nebulization led to improvements in lung function in patients with COPD. It was also generally well tolerated, with no major safety concerns. Revefenacin provides a viable treatment option for patients with COPD and may be a suitable alternative for those with conditions that may impair proper use of traditional handheld inhalers.
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关键词
anticholinergics, bronchodilators, chronic obstructive pulmonary disease, drug administration, drug development and approval, revefenacin
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