This study evaluated the effects of ZD1839, an orally active, selective epidermal growth factor receptor (EGFR)tyrosine kinase inhibitor, on nasopharyngeal carcinoma (NPC) both in vitro and in vivo. Influence of ZD1839alone or combined with cisplatin on the NPC cell line CNE2 was detected by MTT assay with flow cytometryassessment of cell cycle distribution and apoptosis rates. Nude mice NPC xenografts were also used to evaluatethe effects of ZD1839 alone or combined with cisplatin. The Student’s t test evaluated statistical significance.ZD1839 alone or combined with cisplatin inhibited CNE2 cell line proliferation. ZD1839 induced CNE2 cellcycle arrest in the G1 phase, and higher concentrations induced apoptosis. Xenograft tumors were significantlysmaller when treated with 200 mg/kg ZD1839, cisplatin, or cisplatin combined with 100 mg/kg ZD1839 thanuntreated controls. ZD1839 (200 mg/kg) alone showed good tumor inhibition effects, reduction of tumor weights,and smaller tumor volume without loss of body weight. ZD1839 (200 mg/kg) might provide a good and effectivetherapeutic reagent for NPC.