Tetrandrine is a principle from a traditional Chinese medicine of the root of Stephania tetrandra S Moore approved by State Drugs Administration of China as a new drug for the treatment of silicosis. Except for its antiinflammatory, antifibrogenetic, immunomodulating effects and antioxidant effects, tetrandrine presents antiallergic effects, inhibitory effects on pulmonary vessels and airway smooth muscle contraction, and platelet aggregation via its nonspecific calcium channel antagonism that suggested its potential in the treatment of asthma, pulmonary hypertension and chronic obstructive pulmonary disease (COPD). In general, the clinical results to date with tetrandrine in asthma and pulmonary hypertension have been exciting. The last 10 years have witnessed great leaps forward in our understanding of the molecular biology and biochemistry of chronic inflammatory diseases as well as the treatment drugs, which may create opportunities for future therapeutic innovation, development of tetrandrine derivatives or new extracts from other Chinese medicine. The current article briefly reviews the basic and clinical pharmacology of tetrandrine as well as the in vitro and in vivo data supporting the view that tetrandrine is as a novel drug for the treatment of silicosis, asthma and pulmonary hypertension.