Radiation therapy is one of the most commonly used treatments for cancer. Radiation modifiers are agents that alter tumor or normal tissue response to radiation, such as radiation sensitizers and radiation protectors. Radiation sensitizers target aspects of tumor molecular biology or physiology to enhance tumor cell killing after irradiation. Radioprotectors prevent damage of normal tissues selectively. Radiation modifiers remain largely investigational at present, with the promise that molecular characterization of tumors may enhance the capacity for successful clinical development moving forward. A variety of radiation modifiers are described.