Previous studies reported that polychlorinated dibenzo-p-dioxins and dibenzofurans (PCDD/Fs) induced hepatic cytochrome P-4501A1 (CYP1A1). The aim of this study was to examine the interactive influence of CYP1A1 genotypes and PCDD/Fs exposure on liver function profile. PCDD/Fs levels and liver function parameters were determined in serum and correlated with genetic polymorphism of CYP1A1/Msp 1 in 225 human volunteers who had no or minimal occupational exposure to PCDD/F. The results showed that the highest glutamate pyruvate transaminase (GPT) activity levels were found in subjects with homozygous variant CYP1A1/Msp 1, followed by heterozygous variant, and finally homozygous wild type for those individuals whose serum PCDD/Fs levels were higher than 17.4 pg WHO-TEQ/g lipid. Data suggest that GPT activity levels may be modified by interaction of CYP1A1/Msp 1 genotype with dioxin after adjustment for age, alcohol consumption, and history of liver illness. Further studies are needed to characterize the variation in other related genes to verify whether a correlation exists between serum PCDD/Fs levels and adverse health effects.