Non-small-cell lung cancer (NSCLC) accounts for up to 85% of all cases of lung cancer, which is the most frequent cause of cancer-related deaths worldwide. The need for effective treatments against NSCLC is urgent, and one promising target is pyruvate kinase M2, which plays metabolic and nonmetabolic roles in the cell. This enzyme has been implicated in various cancers beyond NSCLC, including pancreatic, gastric and breast cancers.