The goal of immunosuppression after heart transplantation is to prevent or treat allograft rejection while minimizing drug toxicities and adverse effects of immunodeficiency. Currently, Interleukin-2 receptor antagonists had become the most commonly used immune inducers in heart transplantation. The clinical results showed that tacrolimus-based regimens may be associated with lower rejection rates but not with superior survival than cyclosporine-based regimens, the recipients who had extensive metabolism genotype among yellow race taking cyclosporine is more likely to achieve the target plasma concentration with lower doses. Compared with azathioprine, mycophenolate mofetil had been shown to reduce the mortality, the incidence of heart allograft dysfunction, and associated with slower progression of cardiac allograft vasculopathy. Mammalian target of rapamycin (mTOR) inhibitors, Sirolimus and Everolimus, have been used in selected patients with renal insufficiency or cardiac allograft vasculopathy in an attempt to reverse or slow progression of these conditions. However, the high incidence of drug-related adverse effects may limit the widespread use of these agents in heart transplantation. For glucocorticoid, when to stop or reduce it is still a matter of controversy. The timing of corticosteroid withdrawal or reduction remain controversial.