Current immunosuppressive regimens typically consist of two phases: induction phase (medications given at the time of the initial transplant) and maintenance therapy. Induction medications are given to decrease the occurrence of early acute rejection, avoid or minimise corticosteroids, and potentially induce long-term favourable immunoregulatory effects. As tolerance remains an elusive goal, life-long maintenance immunosuppression is required after all solid-organ transplantations. The various agents used in these two phases of immunosuppression are reviewed in this article. The similarities and differences between the agents within each class, with respect to efficacy and tolerability, are discussed.