Molecular medicine has fully entered in to the oncology arena. The development of targeted therapies is one of the major ongoing efforts in cancer treatment. Targeted therapy refers to treatment strategies directed against molecular targets considered to be involved in neoplastic transformation. Such molecularly targeted agents (MTA) are currently under study in all treatment settings including that of chemoprevention, defined as the use of natural or synthetic agents to interrupt the carcinogenic process, to nip tumours in the bud. This review article aims to provide a general overview of the potential use of some of these MTA in the chemoprevention setting.