Cancer cells evade death by dysregulating the relevant apoptotic pathways, but they can be induced to die by both conventional chemotherapy and molecularly targeted agents; therefore, the development of drugs that selectively induce apoptosis in cancer cells is one of the most highly prioritised agendas in cancer treatment research. To completely eradicate cancer, it might be necessary to kill the cancer stem cells, which can self renew, proliferate and regenerate both primary and metastatic tumours. In this regard, there is encouraging evidence that apoptosis can be selectively induced in cancer stem cells and not in normal adult somatic stem cells. Finally, killing premalignant cells is a valid strategy for cancer chemoprevention and, indeed, it has been discovered that several cancer chemopreventive agents exert proapoptotic effects. Taken together, the concept of selectively inducing apoptosis in premalignant and malignant cells can have broad implications for cancer chemoprevention, treatment and perhaps even cure.