Chronic obstructive pulmonary disease (COPD) is a progressing lung disorder mainly caused by cigarette smoking. The central pathogeneses are inflammation, oxidative stress, apoptosis and excessive proteases which lead to matrix degradation and loss of lung cells. The inflammation is somehow perpetuated even after quit smoking and is generally refractory to glucocorticoid therapy. It is thus hoped to develop novel anti-inflammatory agents for prevention of disease progression. As molecular mechanisms of COPD are gradually clarified, numerous numbers of molecular targeted agents have been developed for therapeutics. In this section, novel agents for COPD targeted at signal transduction molecules, cytokines, chemokines and those receptors, adhesion molecules, oxidative stress and proteases are discussed.