Combination of agents that increase the amount of reactive oxygen species with agents that are activated, enhanced, or induced by oxygen species for the treatment of cancer and pre-cancerous disease. Pharmaceutical compositions comprising a therapeutic agent or drug that generate or produce reactive oxygen species (ROS) in a disease microenvironment, and at least one drug or agent that is activated, enhanced, or induced by ROS for the treatment of mammalian cancer, dysplastic disorders, neoplastic, or hyperproliferative disorders and methods of using thereof for the treatment of mammalian cancer dysplastic disorders, neoplastic, or hyperproliferative disorders.