Chronic obstructive pulmonary disease (COPD) is a major cause of morbidity and mortality. Theoretically, an appropriate management of the disease should be aimed to prevent and reduce symptoms, to reduce the number and the severity of exacerbations, to improve exercise tolerance and lung function and to decrease the rate of mortality. However, the rapid progress in understanding the pathophysiologic aspects of COPD has been followed by very few advances in its management and currently there is no pharmacological treatment which is able to reduce the decline in lung function that occurs in these patients or to affect mortality. Effective symptomatic relief and improvement in exercise capacity can be obtained with inhaled bronchodilators and a new long-acting (> 24 h) inhaled anticholinergic, tiotropium bromide, is now available. New pharmacological approaches for COPD include the development of drugs which should be able to control the neutrophilic, steroid-insensitive inflammation, to reassess the protease/antiprotease balance and to reduce oxidative stress in the airways. While most of these drugs are still in preclinical evaluation, some recent phase II-III clinical trials have shown the beneficial effects of a new class of anti-inflammatory compounds, the phosphodiesterase-4 (PDE-4) inhibitors, in patients with COPD. Given the relevance of mucus hypersecretion in the pathophysiology of this disease, efforts have been made also to draw definitive conclusions on the effectiveness of the available mucoactive drugs and in the development of new mucoactive molecules. Further studies are required to understand the impact of each potential therapeutic strategy in the effective control of COPD.