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Cyclosporins/Tacrolimus
Cyclosporins and tacrolimus suppress the immune system by inhibiting calcineurin, a key enzyme required for T-cell activation and cytokine production.
Cyclosporins and tacrolimus suppress the immune system by inhibiting calcineurin, a key enzyme required for T-cell activation and cytokine production. Used for Prevention of organ rejection in transplant recipients (kidney, heart, liver, pancreas), Autoimmune diseases including atopic dermatitis, psoriasis, and rheumatoid arthritis, Graft-versus-host disease (GVHD) prophylaxis and treatment.
At a glance
| Generic name | Cyclosporins/Tacrolimus |
|---|---|
| Also known as | Gengraf (cyclosporin), Neoral (cyclosporin), Prograf (tacrolimus) |
| Sponsor | University of Minnesota |
| Drug class | Calcineurin inhibitor |
| Target | Calcineurin |
| Modality | Small molecule |
| Therapeutic area | Immunology |
| Phase | FDA-approved |
Mechanism of action
Both drugs bind to immunophilins (cyclophilin for cyclosporine, FKBP for tacrolimus) and form complexes that inhibit calcineurin phosphatase activity. This prevents dephosphorylation and nuclear translocation of NFAT (nuclear factor of activated T cells), blocking the transcription of IL-2 and other pro-inflammatory cytokines essential for T-cell proliferation and immune response.
Approved indications
- Prevention of organ rejection in transplant recipients (kidney, heart, liver, pancreas)
- Autoimmune diseases including atopic dermatitis, psoriasis, and rheumatoid arthritis
- Graft-versus-host disease (GVHD) prophylaxis and treatment
Common side effects
- Nephrotoxicity/renal dysfunction
- Hypertension
- Hyperglycemia/new-onset diabetes
- Neurotoxicity (tremor, headache, paresthesia)
- Infections
- Gingival hyperplasia (cyclosporine)
- Hirsutism (cyclosporine)
- Hyperkalemia
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)
- 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)
- Cord Blood Transplant in Children and Young Adults With Blood Cancers and Non-malignant Disorders (PHASE2)
- Graft Versus Host Disease-Reduction Strategies for Donor Blood Stem Cell Transplant Patients With Acute Leukemia or Myelodysplastic Syndrome (MDS) (PHASE2)
- Tocilizumab in Cardiac Transplantation (PHASE2)
- Extended vs Short-term Abatacept Dosing for Graft Versus Host Disease Prophylaxis (PHASE2)
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 |
Competitive intelligence
For the full competitive landscape — auto-detected comparators, recent regulatory actions across the set, upcoming PDUFA, patent timeline, sponsor landscape:
- Cyclosporins/Tacrolimus CI brief — competitive landscape report
- Cyclosporins/Tacrolimus updates RSS · CI watch RSS
- University of Minnesota portfolio CI