Thiopurine methyltransferase (TPMT) is the enzyme responsible for the S-methylation of thiopurine drugs. The enzyme, present in human red blood cells (RBC), is known to exhibit genetic polymorphism and interethnic differences in its activity have been demonstrated. We have studied the role of TPMT polymorphism in Koreans and compared enzyme activity between this and other ethnic groups. In a population of 360 unrelated healthy Korean subjects TPMT activity showed a large interindividual variation ranging from 3.2 to 22.9 nmol ml-1 packed RBC h-1 with a median value of 12.0 and mode of 11.0 nmol ml-1 packed RBC h-1. The enzyme activity was higher in male subjects than that in female (median values; 12.2 vs 11.2, 95% confidence interval of the difference; -2.1, 4.0 nmol ml-1 packed RBC h-1). All subjects had detectable TPMT activity, but contrary to previous reports in other ethnic groups, this was distributed unimodally. The median RBC TPMT activity was very similar to values found in Caucasian populations, higher than in Floridian blacks and lower than that of a Norwegian Saami population.