Cytochrome P450s (CYPs) are one of the first steps in the metabolism of xenobiotics, such as polycyclic aromatic hydrocarbons ( PAHs ), which are bioactivated into carcinogens. As such, changes in CYP expression are potential biomarkers in human biomonitoring applications. For the proper biomonitoring of environmental toxicants, it is important to understand the biological relevance of each biomarker and the associations among the biomarkers for uses as exposure, effects, and susceptibility biomarkers. Here, we have reviewed various aspects of CYPs for biomonitoring environmental health in terms of the CYP substrates, such as PAHs , aromatic amines, benzene/toluene, and tobacco smoking-related nitrosamines. This review also includes association studies between CYP phenotypical alterations and other exposure, susceptibility, and effect biomarkers. The association studies were mainly performed in CYP gene-transfected cells and noninvasive human biospecies, such as urine and peripheral blood. In conclusion, we suggest that phenotypical alterations in CYPs with exposure to environmental toxicants are useful as susceptibility or effect biomarkers, particularly when the phenotype-related genotypes are unknown.