Lycopene (name derived from tomatoe (Solanum lycopersicum)), is a red carotenoid pigment that is found in tomatoes and other red fruits. This phytochemical is the most common carotenoid in the human body and is one of the most potent carotenoid antioxidants. Lycopene was shown to be orally bioavailable and non-toxic and is associated with decreased risk of chronic diseases such as cancer and cardiovascular diseases in numerous studies. Lycopene has multitargeted activities relevant to the treatment of cancer, including reducing DNA damage, inducing apoptosis, preventing oxidative stress, reducing the proliferation of cancerous cells, inhibiting metastasis, and arresting the cell cycle. Moreover, lycopene seems to improve gap-junctional communication, which induces the expression of oxidative defense proteins and phase II drug-metabolizing enzymes. The anti-proliferative effect of lycopene on tumor cells and its effect on the rate of apoptosis were shown to depend on its dosage and the type of the malignant cells. Some identified metabolites of lycopene might also act as chemoprevention agents. The molecular, structural, chemical and biological properties besides the anticarcinogenic action mechanisms of lycopene will be evaluated in this review.