Small molecule
PubChem CID 5284373
Cyclosporine
Neoral
- Mechanism of action
- Calcineurin inhibitor (immunosuppressant)
- In plain language
- Blocks a signal inside immune T cells that would normally tell them to multiply and attack, which is why it's used to stop the body from rejecting a transplanted organ or attacking its own tissue in autoimmune disease.
- How it works
- Cyclosporine is a calcineurin-inhibitor immunosuppressant. It diffuses into T lymphocytes and binds cyclophilin, a cytoplasmic immunophilin; the resulting cyclosporine-cyclophilin complex binds to and inhibits calcineurin, a calcium/calmodulin-dependent phosphatase. Under normal T-cell activation, calcineurin dephosphorylates the transcription factor NFAT, allowing it to translocate into the nucleus and drive transcription of interleukin-2 and other cytokine genes. By blocking calcineurin's phosphatase activity, cyclosporine keeps NFAT out of the nucleus, suppressing IL-2 transcription and the T-cell proliferation it drives, with T-helper cells as the main target.
- Therapeutic applications
- Per FDA-approved labeling, Neoral (cyclosporine capsules, modified) is indicated for the prophylaxis of organ rejection in kidney, liver, and heart allogeneic transplants, typically used with corticosteroids and, at times, azathioprine. It is also indicated for the treatment of patients with severe active rheumatoid arthritis who have not adequately responded to methotrexate, and for adult, nonimmunocompromised patients with severe, recalcitrant plaque psoriasis who have failed at least one systemic therapy or cannot tolerate other systemic options.
- Class
- Small molecule
- Therapeutic area
- Transplant Immunology
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