Ezatiostat is primarily investigated for its potential in cancer therapy, particularly in hematological malignancies. It functions as a glutathione analog and inhibits glutathione S-transferase, an enzyme often overexpressed in tumor cells that contributes to drug resistance. By inhibiting this enzyme, ezatiostat can sensitize cancer cells to chemotherapy and promote apoptosis. It has shown promise in clinical trials for myelodysplastic syndromes (MDS) and acute myeloid leukemia (AML), where it helps restore normal hematopoiesis and reduce disease progression. Additionally, its ability to modulate oxidative stress pathways makes it a candidate for targeting the tumor microenvironment. Research continues to explore its role in combination therapies and its impact on immune response in cancer.