How are immunosuppressive drugs classified?

Updated: Jan 04, 2016
  • Author: Bethany Pellegrino, MD; Chief Editor: Mary C Mancini, MD, PhD, MMM  more...
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Answer

Answer

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)

Glucocorticoids

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

 

Leflunomide

FK778

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

 

Eculizumab

Protease inhibitor

 

Bortezomib

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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