Squamous cell carcinoma is the predominant type of oral malignancy and is a result of oral carcinogenesis. Oral carcinogenesis is a mutifactorial and complex process related to the sequential occurrence of alterations in genetic structures, promoting inhibitory or excitatory effects of the tumor oncogenes and gene suppressors, compromising the histophysiology of the division, differentiation and cell death; and therefore, methods to prevent, detect, or treat it in the best way is constantly being searched for. Biomarkers reveal the genetic and molecular changes related to early, intermediate and late endpoints in the process of oral carcinogenesis. Thereby, they are likely to not only refine our ability to predict the biologic course of oral cancer and distinguish individuals at high and/or low risk of oral cancer development; but, also they will also reveal the genetic and molecular changes related to various endpoints of oral carcinogenesis. Chemopreventives are chemicals of natural or synthetic origin, which reduce the incidence of fatal diseases such as cancer before clinical symptoms occur. Chemopreventives are agents whose curative capacity is defined with help of biomarkers, as the later determine the effectiveness and safety of chemopreventives.