Drug intelligence / Profile preview

azathioprine + cyclosporine + prednisolone

Development stage
Unknown
Lead developer
GSK
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Oral, Intravenous
01

Overview

This is a combination therapy consisting of three immunosuppressive agents—azathioprine, cyclosporine, and prednisolone. The regimen is used primarily for the prevention of organ transplant rejection (notably renal transplantation) and for the management of autoimmune diseases such as membranous lupus nephritis and steroid-refractory ulcerative colitis.

  • Azathioprine is a prodrug that converts to 6-mercaptopurine in the body, inhibiting purine synthesis and thus suppressing lymphocyte proliferation.
  • Cyclosporine inhibits calcineurin, thereby blocking T-cell activation by preventing interleukin-2 transcription.
  • Prednisolone is a synthetic glucocorticoid that modulates gene expression to broadly suppress inflammation and immune responses.

The combination provides synergistic immunosuppression by targeting different pathways in immune cell activation and proliferation. This triple therapy has been shown to reduce rates of organ rejection after transplantation, induce remission or prevent relapse in autoimmune nephritis, and manage severe cases of inflammatory bowel disease when other treatments fail.

Other names
Triple immunosuppressive therapyTriple therapy
02

Targets

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