This study aimed to investigate the antitumor effect and chemosensitization of PI3K/mTOR inhibitor NVP-BEZ235 in NPC both in vivo and in vitro, which would gain more insight on the potential of using NVP-BEZ235 to treat NPC and overcome the resistance of CDDP therapy, especially in NPC harboring PIK3CA mutations. Here, PIK3CA is linked to nasopharyngeal carcinoma.