Tetrandrine is known to exert antitumor effect, however, little is known about its effect on nasopharyngeal carcinoma cells. In this study, we tested tetrandrine-induced apoptosis and radiosensitivity in nasopharyngeal carcinoma cell line CNE and investigated the possible mechanisms. Using flow cytometry and DNA electrophoresis, we found that tetrandrine could induce cell apoptosis. Further, it was shown that the level of Bcl-2 mRNA decreased and Bax mRNA increased after addition of tetrandrine by using reverse transcription-polymerase chain reaction. X-ray-induced G2 arrest was abrogated by treatment with tetrandrine, as detected by flow cytometry and mitotic index. The accumulation of cyclinB1 protein and the suppression of Cdc2 tyrosine-15 and Cdc25C serine-216 phosphorylation were detected in irradiated cells treated with tetrandrine using Western blot analysis. Taken together, these results show that tetrandrine can induce apoptosis and abrogate radiation-induced G2 arrest in CNE cells.