Comprehensive Monograph on Indacaterol (DB05039)

Executive Summary

Indacaterol is a small molecule pharmaceutical agent classified as a selective, ultra-long-acting beta-2 adrenergic agonist (ultra-LABA). Developed by Novartis, it is indicated for the long-term, once-daily maintenance bronchodilator treatment of airflow obstruction in patients with Chronic Obstructive Pulmonary Disease (COPD), including chronic bronchitis and emphysema.[1] Its mechanism of action involves high-efficacy agonism at the β2-adrenoceptors located on airway smooth muscle, which stimulates adenylyl cyclase, increases intracellular cyclic adenosine monophosphate (cAMP), and results in potent bronchodilation.[1]

Pharmacologically, Indacaterol is distinguished by a unique profile that combines a rapid onset of action, observed within five minutes of inhalation, with a sustained 24-hour duration of effect.[1] This dual characteristic, which permits effective once-daily dosing, is attributed to its high intrinsic agonist activity and its high affinity for lipid raft microdomains in the cell membrane, creating a local depot for sustained receptor activation.[1]

The clinical development program for Indacaterol has robustly demonstrated its efficacy in improving lung function, as measured by trough forced expiratory volume in one second (FEV1​), and enhancing patient-reported outcomes, including dyspnea and health-related quality of life, in individuals with moderate to severe COPD.[5] Head-to-head comparative trials and network meta-analyses have consistently shown Indacaterol to be superior to placebo and established twice-daily LABAs such as salmeterol and formoterol.[5]