Immunosuppressive drugs are used for the prevention or treatment of rejection after transplantation of solid organs, tissues and cells, as well as therapy of autoimmune and a variety of other diseases. Primary goals of immunosuppression are: (1) to effectively control immune responses against foreign antigens and (2) to minimise any undesired drug side effects and toxicities. The development of numerous substances, together with the understanding of their molecular action has paved the way to meet these goals, and to individualise immunosuppression. The objective of this inventory is to give a systematic overview on immunosuppressive agents currently in use or under evaluation for transplantation, as a guide for scientific research and clinical practice. Key Concepts: Immunosuppressive drugs are required for prophylaxis and therapy of rejection in solid organ transplantation. A broad spectrum of immunosuppressive drugs is available and new drugs are in the pipeline or under development. Some immunosuppressive drugs are critical dose drugs with a narrow therapeutic index and require therapeutic drug monitoring. Calcineurin inhibitors are commonly used as the basic immunosuppressives despite their nephrotoxic potential. Immunosuppressive drug combinations with different mode of actions are helpful to lower single drug dosages and avoid drug‐related adverse effects as well as to use synergistic or additive immunosuppressive effects. Many factors (e.g. age, gender, liver or renal dysfunction, genetic polymorphism, drug–drug interactions, etc.) can alter the pharmacokinetics of immunosuppressive drugs. Withdrawal of immunosuppressive medication in solid organ transplantation can cause graft failure.

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