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Cyclosporin or tacrolimus
Cyclosporin and tacrolimus are calcineurin inhibitors that suppress T-cell activation by blocking the transcription of pro-inflammatory cytokines.
Cyclosporin and tacrolimus are calcineurin inhibitors that suppress T-cell activation by blocking the transcription of pro-inflammatory cytokines. Used for Organ transplant rejection prophylaxis (renal, cardiac, hepatic), Autoimmune diseases (atopic dermatitis, psoriasis, rheumatoid arthritis).
At a glance
| Generic name | Cyclosporin or tacrolimus |
|---|---|
| Sponsor | Wyeth is now a wholly owned subsidiary of Pfizer |
| Drug class | Calcineurin inhibitor |
| Target | Calcineurin (protein phosphatase 2B) |
| Modality | Small molecule |
| Therapeutic area | Immunology |
| Phase | Phase 3 |
Mechanism of action
Both drugs bind to immunophilins (cyclophilin for cyclosporin, FKBP for tacrolimus) and inhibit calcineurin phosphatase, preventing dephosphorylation and nuclear translocation of NFAT transcription factors. This blocks IL-2 and other cytokine production, suppressing T-cell proliferation and immune responses. Tacrolimus is typically more potent than cyclosporin on a molar basis.
Approved indications
- Organ transplant rejection prophylaxis (renal, cardiac, hepatic)
- Autoimmune diseases (atopic dermatitis, psoriasis, rheumatoid arthritis)
Common side effects
- Nephrotoxicity
- Hypertension
- Hyperglycemia
- Neurotoxicity (tremor, headache)
- Gingival hyperplasia
- Infections
- Hyperlipidemia
Key clinical trials
- 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)
- A Study on the Efficacy and Safety of JAK Inhibitors Versus Calcineurin Inhibitors as Initial Therapy for Interstitial Lung Disease Associated With Antisynthetase Syndrome (NA)
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:
- Cyclosporin or tacrolimus CI brief — competitive landscape report
- Cyclosporin or tacrolimus updates RSS · CI watch RSS
- Wyeth is now a wholly owned subsidiary of Pfizer portfolio CI