In the Western world, an average of 250 mg per day of triterpenes (member of phytosterol family), largely derived from vegetable oils, cereals, fruits and vegetables is consumed by humans. During the last decade, there has been an unprecedented escalation of interest in triterpenes due to their cholesterol-lowering properties and evidence of this phenomenon include at least 25 clinical studies, 20 patents and at least 10 major commercially triterpene-based products currently being sold all around the world. Lupeol a triterpene (also known as Fagarsterol) found in white cabbage, green pepper, strawberry, olive, mangoes and grapes was reported to possess beneficial effects as a therapeutic and preventive agent for a range of disorders. Last 15 years have seen tremendous efforts by researchers worldwide to develop this wonderful molecule for its clinical use for the treatment of variety of disorders. These studies also provide insight into the mechanism of action of Lupeol and suggest that it is a multi-target agent with immense anti-inflammatory potential targeting key molecular pathways which involve nuclear factor kappa B (NFκB), cFLIP, Fas, Kras, phosphatidylinositol-3-kinase (PI3 K)/Akt and Wnt/β-catenin in a variety of cells. It is noteworthy that Lupeol at its effective therapeutic doses exhibit no toxicity to normal cells and tissues. This mini review provides detailed account of preclinical studies conducted to determine the utility of Lupeol as a therapeutic and chemopreventive agent for the treatment of inflammation and cancer.