Objectives: The current article was designed to review the main clinical and pharmacological data on the currently approved immunosuppressants used for the prevention and treatment of kidney transplant rejection. Design: A narrative review manuscript Settings: A comprehensive search for the available literature on renal transplant pharmacotherapy on PubMed, Google, Medline Scopus and clinicalTrials.gov. Subjects: Key related articles published until May 2020 Intervention: Non-interventional Main outcome measures: The induction therapy should be started with high doses of immunosuppressants immediately after transplantation, followed by gradual dosage reduction in maintenance therapy. It commonly involves thymoglobulin or alemtuzumab. Basiliximab is also approved as an induction agent, especially in recipients with low risk of rejection. Results: Thymoglobulin is superior in patients on a steroid-free maintenance regimen. The maintenance therapy should be started early after transplantation or even before. It can be made up of different combinations of calcineurin inhibitors (CNIs) like cyclosporine A / tacrolimus, mycophenolate mofetil (MMF), mTOR inhibitors (sirolimus/everolimus) and corticosteroids. Tacrolimus is considered a first-line agent in maintenance therapy and it is associated with a better allograft function. MMF is a major drug in the current maintenance therapy in combination with CNIs, and a main part in CNI-free regimens. Corticosteroids are still a main component in immunosuppressive regimens, despite the current interest in avoiding them due to their various long-term side effects. The rates of transplant loss are still unacceptably high, mainly due to dose-limiting toxicities. Conclusion: New drugs are being developed to improve the efficacy and safety profile of maintenance therapy. Some of them showed promising results.