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Cyclosporine (CsA)
Cyclosporine inhibits calcineurin phosphatase, blocking T-cell activation and proliferation by preventing IL-2 transcription.
Cyclosporine inhibits calcineurin phosphatase, blocking T-cell activation and proliferation by preventing IL-2 transcription. Used for Organ transplant rejection prevention (renal, cardiac, hepatic), Autoimmune diseases (rheumatoid arthritis, psoriasis, nephrotic syndrome).
At a glance
| Generic name | Cyclosporine (CsA) |
|---|---|
| Also known as | Sandimmune® |
| Sponsor | Assistance Publique - Hôpitaux de Paris |
| Drug class | Calcineurin inhibitor |
| Target | Calcineurin (protein phosphatase 2B) |
| Modality | Small molecule |
| Therapeutic area | Immunology |
| Phase | Phase 3 |
Mechanism of action
Cyclosporine binds to cyclophilin, and this complex inhibits calcineurin (protein phosphatase 2B), which normally dephosphorylates NFAT transcription factors. By preventing NFAT nuclear translocation, cyclosporine suppresses the transcription of interleukin-2 and other cytokines essential for T-cell activation and clonal expansion. This potent immunosuppressive effect makes it valuable in transplantation and autoimmune diseases.
Approved indications
- Organ transplant rejection prevention (renal, cardiac, hepatic)
- Autoimmune diseases (rheumatoid arthritis, psoriasis, nephrotic syndrome)
Common side effects
- Nephrotoxicity
- Hypertension
- Tremor
- Gingival hyperplasia
- Hirsutism
- Infection
- Neurotoxicity (headache, confusion)
Key clinical trials
- Radiation- and Alkylator-free Bone Marrow Transplantation Regimen for Patients With Dyskeratosis Congenita (PHASE2)
- Campath/Fludarabine/Melphalan Transplant Conditioning for Non-Malignant Diseases (PHASE1, PHASE2)
- Rituximab Plus Cyclosporine in Idiopathic Membranous Nephropathy (PHASE2)
- Letermovir Prophylaxis in Children With EBV-Positive T/NK-Cell Lymphoproliferative Disease and Refractory/Relapsed EBV-Associated Hemophagocytic Lymphohistiocytosis (NA)
- A Study to Evaluate Axatilimab Versus Best Available Therapy in Participants With Chronic Graft Versus Host Disease After at Least 2 Prior Lines of Systemic Therapy (PHASE3)
- A Study to Evaluate Axatilimab Versus Best Available Therapy in Pediatric Participants With Chronic Graft-Versus-Host Disease After at Least 2 Prior Lines of Systemic Therapy (AGAVE-256) (PHASE2)
- Study on the Efficacy and Safety of the TmBU Conditioning Regimen in High-risk or Relapsed/Refractory Acute Leukemia (PHASE2)
- Effect of Anti-Psoriatic Biologics on Risk of Anogenital Warts (CONDYPSO)
Primary sources
Every claim on this page is sourced from regulatory or scientific primary sources. See our editorial policy for full methodology.
| Source | Used for |
|---|---|
| ClinicalTrials.gov | Trial enrolment, design, endpoints, results |