The Role of Revefenacin in Chronic Obstructive Pulmonary Disease

Muhammad Haisum Maqsood, Kinza Rubab, Muhammad Arqam Maqsood, Muhammad Haisum Maqsood, Kinza Rubab, Muhammad Arqam Maqsood

Abstract

Chronic obstructive pulmonary disease (COPD) is a chronic inflammatory lung disease characterized by progressive and persistent airflow limitation that is not fully reversible. Revefenacin is an investigational long-acting muscarinic antagonist (LAMA), in late-stage development as a nebulized inhalation solution, which has been designed to produce long-acting bronchodilation, consistent with once-daily dosing, and with a high degree of lung-selectivity. It is more selective for muscarinic type 3 (M3) than muscarinic type 2 (M2) or muscarinic type 1 (M1) receptors. Its dissociation half-life for M3 is 82 minutes and 6.9 minutes for M1, respectively. The bronchoprotective effect is seen as early as five-minute post-dose and is sustained for up to 24 hours. The estimated 24-hour potency (expressed as the concentration of dosing solution) is 45.0 mg/ml. Once-daily dose of revefenacin provided long-term improvement in trough forced expiratory volume in one second (FEV1). It improved day 28 trough FEV1 over placebo significantly (p < 0.001). M3: M2 receptor half-life is 12 compared to the other antagonists that have M3: M2 receptor half-life around 6.0. A 24-hour serial spirometry, on day 84, showed that revefenacin 88 or 175 µg was associated with significant (p <0.01) improvements in trough FEV1 at all time points compared with placebo. Revefenacin is generally well-tolerated and unlike the other anti-muscarinics, it has no systemic anti-cholinergic adverse effects.

Keywords: chronic obstructive pulmonary disease; copd; revefenacin.

Conflict of interest statement

The authors have declared that no competing interests exist.

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