Triphala, made of the three dry medicinal fruits Amalaki (Emblica officinalis), Haritaki (Terminalia chebula) and Bibhitaki (Terminalia belerica) is one of the most important tridoshic rasayana drugs in Ayurveda. It is widely used to rejuvenate or attain the complete potential of an individual in order to prevent diseases and degenerative changes that lead to disease. Studies in the past ten years have shown that Triphala possesses anticancer, radioprotective, antimutagenic and chemopreventive effects. The present review appraises the various mechanistic activities of Triphala to support the above observations, its role as a prophylactic medication and significance in the prevention of radiation toxicity and carcinogenesis. Emerging data suggests that the possible mechanisms include induction of selective apoptosis in the neoplastic cells, quenching of free radicals, enhancement of cellular detoxification mechanisms, repair of damaged non-proliferating cells, immunostimulation, induction of cell proliferation and self-renewal of damaged proliferating tissues, and replenishment by eliminating damaged or mutated cells with fresh cells. This review summarizes results related to the potential use of Triphala as anticancer, radioprotective, cancer chemopreventive agent, their mechanisms of action and recent developments that may hold future promise.