The purpose of this study, therefore, was to mechanistically identify the mode of action of 21α-MMD on human NSCLC cells and further relate its regulatory mechanism on cell growth and survival-related signals such as the PI3K/AKT/AMPK and MAPKs with P-gp/MDR1-associated MDR occurrence in a lung cancer phenotype. Here, ABCB1 is linked to lung cancer.