Indacaterol is a potent, orally administered ultra-long-acting β2 adrenergic receptor (ADRB2) agonist, widely recognized for its therapeutic potential in respiratory and cardiovascular conditions. By selectively activating ADRB2, indacaterol not only enhances bronchodilation but also exhibits a unique mechanism of action by inhibiting NF-κB activity in a β-arrestin2-dependent manner. This dual functionality helps mitigate lung inflammation, prevent further pulmonary damage, and improve lung function in patients with chronic obstructive pulmonary disease (COPD). Beyond its respiratory applications, indacaterol has also emerged as a valuable tool in cardiovascular disease research, offering insights into its broader therapeutic effects. Its multifaceted pharmacological profile positions indacaterol as a promising candidate for addressing complex disease mechanisms and advancing treatment strategies in both respiratory and cardiovascular fields.