Allogenic solid organ transplantation has become the routine procedure in patients with end stage organ disease. Although the transplanted organ compensates deficient body functions, its allogenic nature requires institution of immune tolerance, nowadays provided by immunosuppressive drug administration. Both the safety and efficacy of immunosuppressive treatment depend on many factors, and maintaining levels of immunosuppressants within therapeutic range is the essential target for success in graft function preservation. It is obvious that drug and metabolite concentrations depend on efficiency of individual patient metabolism. Recently, many studies were undertaken to investigate the relationship between genetic factors, drug pharmacokinetics and therapy outcome, and interindividual variability apparently can be explained, at least in part, by genetically determined polymorphisms of xenobiotic-metabolizing enzymes, transport proteins and also in some cases, drug targets. This review presents the recent state of knowledge in the field of pharmacogenetics related to solid organ transplantation.