Studies on the various cholesterol-lowering agents is one of the important areas in clinical research. Identification and characterization of potential molecules from various sources have been carried out in the past and their relationship with the enzymes which are involved in the cholesterol cascade is gaining interest. In this review, we have highlighted various inhibitors involved in the cholesterol cascade as well as cholesterol-lowering agents, viz., tocotrienol, flavonoids, phytosterols, phytostanols, statins, DADS, and synthetic compounds. The mechanism of action and characterization of these hypocholesterolemic compounds are discussed in this communication. Major natural sources as well as synthetic and biological routes of synthesis of these compounds are reviewed in a concise manner. Especially, various HMG-CoA analogues including statins have been reviewed specifically. © Seenivasan et al.