Disclosed herein is a method for enhancing the susceptibility of a subject having epidermoid carcinoma toward a tyrosine kinase inhibitor. The method includes administering to the subject an effective amount of a targeted therapy sensitizer and an effective amount of gefitinib. According to various embodiments of the present disclosure, the targeted therapy sensitizer consists of rapamycin and a substituted quinoline, such as chloroquine. Also included herein is a pharmaceutical composition that includes an effective amount of gefitinib, an effective amount of a targeted therapy sensitizer for synergistically improving or enhancing the efficacy of the gefitinib for treating epidermoid carcinoma in a subject in need thereof, and a pharmaceutically acceptable excipient.
