Phytosterols are the phytoconstituents resembling cholesterol in structure with a slight difference in side chain configuration and function. As human body cannot synthesize phytosterols, they can be obtained from the diet. The most common phytosterols include stigmasterol, Campesterol and β-sitosterol. Phytosterols have many health beneficial effects including hypocholesterolemic effect, protection from cardio vascular disorders, anti-cancer, anti-inflammatory, immunomodulatory, antioxidant activity. The most important and studied effect of phytosterols is its antihyperlipidemic activity. Many preclinical and clinical studies have been performed in order to prove this activity. Now-a-days, many functional foods are being enriched with phytosterols for its cholesterol lowering abilities. Phytosterol supplementation is also combined with the therapy of statins as well as ezetimibe in order to enhance its effectiveness. Also, a self-GRAS (Generally Recognized As Safe) procedure has been followed for them, to which USFDA raised no objections. However, some side effects of phytosterols include decrease in absorption of certain amounts of fat soluble vitamins like tocopherols and carotenoids. But this effect can be minimised by adjusting the levels of these vitamins in diet. Phytosterolemia is a rare, genetic disease due to mutation in genes coding for ABCG5 and ABCG8 which results in excessive absorption and high plasma levels of phytosterols.