Mast cells play a central role in innate immunity and in orchestrating the asthmatic response. Current medication relies on beta-agonists to relieve bronchoconstriction and steroids to reduce inflammation. However, recently drugs such as leukotriene-receptor antagonists and anti-immunoglobulin E have come on to the market. In this paper, a number of potential targets for modifying mast cell activation in asthma are reviewed. Some are already under study, including clinical trials (eg, tryptase inhibitors); others are more speculative (eg, inhibitors of 3-hydroxy-3-methylglutaryl coenzyme A reductase activity). In each case, where data are available, the action of the agents on human lung mast cells is described.