PFK-158 is primarily investigated for its potential in cancer therapy due to its ability to inhibit glycolysis, a key energy-producing pathway in many tumor cells. By targeting the glycolytic enzyme PFKFB3, it disrupts the metabolic activity of rapidly dividing cancer cells, leading to reduced tumor growth and increased cell death. It has shown promise in preclinical models for cancers that rely heavily on glucose metabolism, including leukemia, breast cancer, and colorectal cancer. Additionally, PFK-158 may enhance the effectiveness of other anticancer treatments such as chemotherapy and radiation by weakening tumor cell resilience. Its role in modulating immune cell metabolism also opens avenues for use in combination with immunotherapies. Research is ongoing to evaluate its efficacy and safety in clinical settings.