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Currently, kidney transplantation is the best treatment option for kidney failure for the majority of eligible patients. It is associated with a better quality of life and reduced mortality as compared to remaining on dialysis. Many of the improvements in kidney transplant outcomes observed in recent decades are due to more efficient immunosuppression strategies. Therefore, developing expertise in the management of immunosuppressive drugs is key to the success of kidney transplantation. In this review, we briefly addressed the historical aspects of