Bronchial asthma as such exists because airway smooth muscle (ASM) contracts excessively in response to various stimuli. After several decades during which research was mainly focused on airway inflammation, increasing attention is now being paid to a possible abnormal behaviour of ASM. Thus, ASM is regarded as a major target for anti-asthma treatments. This review first describes the mechanisms of ASM contraction and airway hyperresponsiveness, through cellular, animal and human models. The developments of new drugs targeting extra and/or intracellular pathway of ASM contraction are discussed.