Given its significant role in cancer metabolism, ASCT2 is considered a promising target for cancer therapy. Inhibitors of ASCT2 have been developed to block glutamine uptake, thereby starving cancer cells of a critical nutrient. These inhibitors have shown potential in preclinical studies, demonstrating reduced tumor growth and enhanced sensitivity to other therapies. However, clinical trials are necessary to validate the efficacy and safety of ASCT2 inhibitors in cancer patients.