RRx-001 is used in cancer therapy as a multifunctional agent that targets the tumor microenvironment. It acts as a radiosensitizer and chemosensitizer, making cancer cells more responsive to radiation and chemotherapy. The compound induces oxidative stress in tumor cells, leading to DNA damage and cell death. It also modulates the immune system by promoting the release of damage-associated molecular patterns (DAMPs), which can stimulate anti-tumor immune responses. RRx-001 is being investigated in clinical trials for various solid tumors and hematologic malignancies due to its ability to reverse resistance to standard treatments. Its small size and favorable safety profile allow for repeated dosing, enhancing its potential in combination therapies.