PFK-158 is primarily investigated for its potential in cancer therapy. It functions as an inhibitor of 6-phosphofructo-2-kinase/fructose-2,6-biphosphatase 3 (PFKFB3), a key enzyme in cancer cell metabolism. By targeting PFKFB3, it disrupts the glycolytic pathway, which is crucial for the energy production and survival of cancer cells, particularly in hypoxic environments. This makes it a promising candidate for reducing tumor growth and enhancing the efficacy of other cancer treatments. Research is ongoing to explore its use in combination with chemotherapy or radiation therapy to improve outcomes in various cancer types.