Formoterol is a selective long-acting beta2-adrenergic receptor agonist (LABA) that provides significant and sustained bronchodilatory effect for up to 12h following a single dose. The onset of effect is significantly faster with formoterol compared with an alternative LABA, salmeterol, although both have a similar duration of action. The overall efficacy of formoterol in improving lung function and controlling symptoms of chronic obstructive pulmonary disease (COPD) is comparable to that of salmeterol and potentially superior to that of ipratropium or theophylline. Formoterol provides additional benefit when administered in combination with other bronchodilators or inhaled corticosteroids. In clinical studies, formoterol was well tolerated and had an adverse-event profile similar to that of other beta2-adrenergic receptor agonists. Formoterol is a rapidly acting, well-tolerated, effective beta2-adrenergic receptor agonist that can be regularly used as a long-acting bronchodilator for patients with moderate to severe COPD, as per recommendations of the current treatment guidelines.