Abstract: Except for the traditional radiotherapy sensitization agents such as nitro imidazoles and nitrobenzene, some chemotherapeutics also showed sensitization effect. Molecular targeted drug research is in the ascendant, respectively interacting with histone deacetylase, signal transducer and activator of transcription 3, poly(adenosine diphosphate-ribose)polymerase, prostaglandin H synthase-2, (hypoxia inducible factor-1, nuclear factor kappa-light-chain-enhancer of activated B cells, heat shock protein, ataxia-telangiectasia mutated gene and so on, through various ways such as interfering DNA repair, inhibiting tumor cell proliferation, promoting tumor cell apoptosis and inhibiting angiogenesis to improve the sensitivity of cancer cells to iron radiation.