Obstructive lung diseases, in particular asthma and chronic obstructive pulmonary disease, are a worldwide health problem that is increasing in incidence. While significant progress has been made in the control of symptoms, further advances must be made in modifying the clinical situation in terms of disease progression. Numerous pathogenetic studies have demonstrated that inflammatory responses play a crucial role in the development of chronic lung obstruction, while current molecular findings have provided a myriad of new and promising therapeutic targets. The aim of this article is to provide an overview of clinically and pharmacologically relevant targets for asthma and chronic obstructive pulmonary diseases, considering currently investigated therapeutic approaches.