A fixed-dose inhaled corticosteroid/long-acting β2-agonist (ICS/LABA) combination of extrafine beclometasone dipropionate and formoterol fumarate (BDP/FF) has been recently approved for use in chronic obstructive pulmonary disease (COPD). Small airway inflammation and remodelling are cardinal features of COPD; therefore, the ability of this extrafine formulation to reach the small, as well as the large, airways is likely to be therapeutically important by enabling treatment of inflammatory processes in the whole bronchial tree. The clinical development of extrafine BDP/FF has demonstrated significant benefits over extrafine FF in terms of lung function improvement and reduction of the exacerbation rate, thus supporting the beneficial effect of an ICS combined to a LABA in COPD patients. Head-to-head comparison studies versus other ICS/LABA combinations have shown that the extrafine formulation enables the clinical benefits to be achieved with a lower dose of ICS. Extrafine BDP/FF showed lung function and dyspnoea improvements comparable to other ICS/LABAs, and a significantly faster onset of action was observed when compared with a salmeterol-containing fixed-dose combination. This review summarises the clinical evidence supporting the efficacy of extrafine BDP/FF in COPD and confirming that extrafine BDP/FF achieves the type of health benefit expected from such a targeted ICS/LABA combination in COPD.