Astaxanthin, a red-orange liposoluble carotenoid, has been the centre of considerable attention in recent years for its numerous biological activities, notably its potent antioxidant activity. It is reported that astaxanthin elicits these biological activities via a number of cellular pathways. The Nrf2/Keap1 pathway is a major regulator of the antioxidant defence system of cells; it modulates the expression of a plethora of genes related to redox homeostasis as well as cellular detoxification. The pathway has received lots of attention as a prospective therapeutic target for diseases related to oxidative stress and inflammation. Several reports have shown that the pathway is inducible by many natural compounds. This present work reviews the Nrf2/Keap1 pathway, its regulation and involvement in diseases, provides a brief overview of naturally occurring compounds as activators of the pathway as well as discusses the effect of astaxanthin on the pathway.