Chronic obstructive pulmonary disease (COPD) is a widespread disease. Nowadays therapy used for its treatment can improve the patient’s condition only for a short period of time and is not able to prevent its progression. In order to find new effective drugs, various links in the COPD pathogenesis are being intensively studied as targets for the effects. Those targets include disease-mediated proinflammatory mediators and ways of signaling into cells. Other approaches are related to the targeted effect on the mucus hypersecretion and pulmonary hypertension. Despite lacking of the desired effect of many drugs studied, others preparations administered to patients or used in experiments were able to improve the functional capacity of the lungs, to reduce the pulmonary hypertension or to increase the sensitivity to glucocorticoids, and to reduce the exacerbation frequency. The latter drugs include compounds that inhibit the CXCR2, the mitogen-activated protein kinase / Src kinase, the myristoilated alanine-rich C kinase substrate, selectins, etc. Some transcription activators are also very promising in this direction. Thus, use of agonists of the nuclear receptor g activated by the peroxysomal proliferator, of rosiglitazone and pioglitazone led to reducing of the exacerbations frequency in COPD patients. In this review, an attempt is made to summarize the results of numerous pharmaceutical approaches to the disease treatment in order to identify the most promising of them.