Biological monitoring, analyses of internal dose for exposure to toxicants, has been thought as one of the belt approaches for risk assessment. As the amount detected in human samples is generally very low, typically in the parts-per-bilion (ppb) or parts-per-trillion (ppt) range, analytic technologies such at HPLC, GC/MS, LC/MS, and LC/MS/MS have been continuously developed. In addition, route specific and sensitive exposure biomarkers have been developed for proper biological monitoring. PBPK modeling, particularly reverse dosimetry, has been emphasized as an useful method via interpretation of biological monitoring results for regulation of toxicants. Thus, this review is focused on the use of PBPK dosimetry models for toxicology research and risk assessment in Korea.