We review fundamental processes, such as mutation, oxidative stress, and inflammation that are critical for carcinogenesis and provide specific molecular targets for new chemopreventive agents. New information from molecular biology studies has identified such targets, including regulatory molecules such as Nrf2 (nuclear factor erythroid 2-related factor 2), epidermal growth factor receptor kinases, phosphatidylinositol 3-kinase, components of the Janus kinase–signal transducers and activators of transcription (JAK–STAT) pathway, nuclear factor-κB, and cyclin D. The development of new drugs for the control of these targets that are both safe and effective will be important for the future of cancer chemoprevention.