Renal transplantation is the gold standard therapy for patients affected by end stage renal disease. It is a clinical condition characterized by severe biological/biochemical alterations that requires renal replacement therapy to ensure patients survival. In most cases, it is followed by a significant improvement of patients quality of life, reduction in medical expenses and prolongation of life. However, to reach these positive clinical effects, patients need to take several immunosuppressive medications (calcineurin inhibitors, mTOR inhibitors and antimetabolites) characterized by a narrow therapeutic index, that, in some cases, could cause important adverse effects. To avoid toxicities and adverse drug reactions, immunosuppressors should be correctly administered, according to the blood trough levels. Nevertheless, in most of the times, this methodology to adjust drug doses gives inadequate and non-reproducible results. Additionally, as largely described, inherited differences in drug metabolism and disposition and genetic variability in therapeutic targets (e.g. receptors) need to be taken into account because of their role in modulating drug effects and toxicities. Therefore, worldwide researchers are working together to identify biomarkers, useful to personalize therapy based on genetic characteristics of patients. In this context, we believe that the omics techniques could represent a future powerful instruments that, whether employed routinely, could help to reach this objective.