The present invention is related to a method and pharmaceutical composition for treating lung cancer. The pharmaceutical composition comprises an effective amount of 16-hydroxy-cleroda-3,13-dine-15,16-olide as active ingredient, and a pharmaceutically acceptable carrier. The present method and pharmaceutical composition provides good efficacy in treating lung cancer even for drug-resistance patient. The present invention also establishes an animal model bearing human lung cancer, which provides a better drug screening platform for the research.