Abstract: Chemotherapy is one of the main comprehensive treatments for lung cancer, especially for non-small cell lung cancer(NSC1C) Multi-drug resistance of lung cancer plays an important role in the failure of chemotherapy. Early detection of multi-drug resistance(MDR) is essential for choosing a suitable chemotherapy regimen for the patients of lung cancer. In recent years lots of literature reports that MDR of lung cancer is related to many kinds of multi-drug resistance protein(MRP) expression in lung cancer. Some lipophilic chemotherapy drugs and ⁹⁹Tc^m-methoxyisobutylisonitrile (⁹⁹Tc^m-MIBI) may be the same substrate for some MRP. These MHP can transport them out of the tumor cells, then the chemotherapy is invalid or non-radioactive concentration. The retention of ⁹⁹Tc^m-MIBI in tumor cells is correlated with the expression of MRP, thus the prediction of the MRP expression before chemotherapy or monitoring MRP expression changes in the process of chemotherapy by using the noninvasive ⁹⁹Tc^m-MIBI single photon emission computed tomography imaging is helpful to predict the MDR and chemotherapy efficacy of lung cancer.