Acetylcholine is the predominant parasympathetic neurotransmitter in the airways, and plays a key role in the pathophysiology of chronic obstructive pulmonary disease (COPD). Muscarinic receptors are found in smooth muscle cells and submucosal glands. Binding of acetylcholine to muscarinic receptors could trigger bronchoconstriction. Muscarinic antagonists prevent acetylcholine from binding to its receptors and produce bronchodilation. Revefenacin is the first once-daily dosed nebulized long-acting muscarinic antagonist indicated for the maintenance treatment of patients with COPD. Areas covered: In this paper, the chemical properties, mechanism of action, pharmacokinetics, clinical efficacy and safety of Revefenacin was introduced, and the evolution of muscarinic antagonists is also briefly described. Expert commentary: Revefenacin is a new M3 muscarinic receptor antagonist, which could prevent acetylcholine from binding with the muscarinic receptor, making bronchodilation and relieving COPD symptoms. Revefenacin has a rapid onset of action, and the curative effect is to maintain a long time. Clinical trials showed that Revefenacin could significantly increase forced expiratory volume in 1 s (FEV1) in patients with COPD and improve their quality of life. The recommended dose of Revefenacin inhalation solution is 175 μg once daily. Adverse reactions were mild and the drug was well tolerated.
Keywords: Chronic obstructive pulmonary disease; forced expiratory volume in 1 s; long-acting muscarinic antagonists; muscarinic receptor; revefenacin.