Within the field of solid organ transplantation there is an unprecedented interest in therapeutic drug monitoring of immunosuppressive drugs. Ideally therapeutic drug monitoring should cost-effectively lead to improved efficacy of the drug and to a reduction in side effects. Therapeutic drug monitoring will be most effective if there is a large interpatient variability and a small intrapatient variability. Therapeutic drug monitoring in transplantation is largely based on correlations between drug concentrations and toxicity or between drug concentrations and efficacy. Pharmacodynamic monitoring of immunosuppressive drugs has not reached the stage of widespread clinical application. In part this is caused by the fact that most of the pharmacodynamic assays are time-consuming, costly and in some cases only give a result after several days of incubation. Another reason for the limited interest in pharmacodynamic monitoring is the lack of data showing improved outcome if dose adjustment is based on pharmacodynamics rather than pharmacokinetics. On the other hand, such data are also lacking for pharmacokinetic monitoring. Prospective investigations on the contribution of therapeutic drug monitoring may result in further improvement of the safety and efficacy of our immunosuppressive regimens and more refined methods for therapeutic drug monitoring. There is no contest between pharmacokinetic and pharmacodynamic monitoring. Most likely the results of both ways of monitoring will be complementary.