How are immunosuppressive drugs classified?

Updated: Mar 01, 2021
  • Author: Bethany Pellegrino, MD; Chief Editor: Mary C Mancini, MD, PhD, MMM  more...
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Immunosuppressive drugs can be classified as induction therapies, maintenance therapies and antirejection therapies. Maintenance immunosuppressive therapies include small molecule drugs (calcineurin inhibitors and antiproliferatives), fusion proteins and glucorticorticoids. There is also special agents include intravenous immunoglobulin, rituximab, leflunomide, eculizimab and bortezomib. Induction immunosuppressive agents consist of depleting and non-depleting protein drugs (polyclonal and monoclonal antibodies).

Table. Classification of Immunosuppressive Therapies Used in Organ Transplantation (Open Table in a new window)


Small-molecule drugs


Immunophilin-binding drugs


Calcineurin inhibitors


Cyclophilin-binding drugs: cyclosporine

FKB12-binding drugs: tacrolimus, modified release tacrolimus

Target-of-rapamycin inhibitors: sirolimus, everolimus


Inhibitors of nucleotide synthesis


Purine synthesis (IMDH) inhibitors


Mycophenolate mofetil

Enteric-coated mycophenolic acid (EC-MFS)

Mizoribine (MZR)


Pyrimidine synthesis (DHODH) inhibitors




Antimetabolites: azathioprine (Aza)

Sphingosine-1-phosphate-receptor antagonists: FTY720

Protein drugs


Depleting antibodies (against T cells, B cells, or both)


Polyclonal antibody: horse or rabbit antithymocyte globulin

Mouse monoclonal anti-CD3 antibody (muromonab-CD3)

Humanized monoclonal anti CD-52 antibody (alemtuzumab)

B-cell-depleting monoclonal anti-CD-20 antibody (rituximab)

Nondepleting antibodies and fusion proteins


Humanized or chimeric monoclonal anti-CD25 antibody (basiliximab)

Fusion protein with natural binding properties: CTLA4-Ig (Belatacept)

Intravenous gammaglobulin

C5 inhibitor



Protease inhibitor



A study by Molnar et al compared the clinical efficacy and bioequivalence of generic immunosuppressive drugs in patients with solid organ transplant. The study did not find high quality data showing bioequivalence and clinical efficacy of generic immunosuppressive drugs. [1, 2]

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