Risk Assessment is an important area in toxicology and the methodology for risk assessment has been developed. Mathematical models used for risk assessment include one-hit multi-hit, two-stage, probit logistic, multistage, and linearized multistage models. For the assessment of exposure dose, environmental monitoring has been applied, but it has limitation to accurately assess exposure level because the levels in the air, water, foods, and soil may vary depending on time of sampling. In addition, humans can be exposed to various sources of exposure and thus it will be impossible to estimate the total level of exposure in humans by environmental monitoring. To eliminate the limitation of environmental monitoring, a direct measurement of toxic materials or modified biomolecules (called biomarkers) associated with the exposure of toxic materials is needed. Here, scientific basis of biomarkers and future direction have been considered for the assessment of carcinogen exposure and cancer risk in humans.